Patent Publication Number: US-2020283439-A1

Title: Tricyclic quinoline and quinoxaline derivatives

Description:
CROSS-REFERENCE TO RELATED APPLICATIONS 
     This is a non-provisional of U.S. Patent Application No. 61/701,514, filed on Sep. 14, 2012, U.S. Patent Application No. 61/701,531, filed on Sep. 14, 2012, U.S. Patent Application No. 61/793,033, filed on Mar. 15, 2013, and claims priority to Chinese Patent Application No. CN 201310410951.1, filed on Sep. 11, 2013, the contents of all of which are fully incorporated herein by reference. 
    
    
     FIELD OF THE INVENTION 
     The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT 2C  receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT 2C  receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C  receptor, and processes for preparing such compounds and compositions. 
     BACKGROUND OF THE INVENTION 
     Diseases, disorders and conditions where 5-HT 2C  modulation is desired are for example depression, anxiety, schizophrenia, bipolar disorder, obsessive compulsive disorder, migraine, pain, epilepsy, substance abuse, eating disorders, obesity, diabetes, erectile dysfunction and others. 
     Serotonin (5-hydroxytryptamine, 5-HT), a monoamine neurotransmitter and local hormone, is formed by the hydroxylation and decarboxylation of tryptophan. The greatest concentration is found in the enterochromaffin cells of the gastrointestinal tract, the remainder being predominantly present in platelets and in the Central Nervous System (CNS). 5-HT is implicated in a vast array of physiological and pathophysiological pathways. In the periphery, it contracts a number of smooth muscles and induces endothelium-dependent vasodilation. In the CNS, it is believed to be involved in a wide range of functions, including the control of appetite, mood, anxiety, hallucinations, sleep, vomiting and pain perception. 
     Neurons that secrete 5-HT are termed serotonergic. The function of 5-HT is exerted upon its interaction with specific (serotonergic) neurons. Seven types of 5-HT receptors have been identified: 5-HT 1  (with subtypes 5-HT 1A , 5-HT 1B , 5-HT 1D , 5-HT 1E  and 5-HT 1F ), 5-HT 2  (with subtypes 5-HT 2A , 5-HT 2B  and 5-HT 2 c), 5-HT 3 , 5-HT 4 , 5-HT 5  (with subtypes 5-HT 5A  and 5-HT 5B ), 5-HT 6  and 5-HT 7 . Most of these receptors are coupled to G-proteins that affect the activities of adenylate cyclase or phospholipase Cγ. 
     Alterations in the activity of multiple neurotransmitter receptor systems (dopamine, serotonin, glutamate, GABA, acetylcholine) have been implicated in the manifestation of the symptoms of schizophrenia. The most widely accepted “Dopamine Hypothesis of Schizophrenia” in its simplest form states that the positive symptoms of this pathology relate to a functional hyperactivity of the mesolimbic dopaminergic system, while the negative and cognitive aspects can be traced to a functional hypoactivity of the mesocortical dopaminergic projections. Atypical antipsychotics block the mesolimbic dopaminergic neurotransmission, thereby controlling positive symptoms, with little or no effect on the nigrostriatal system, leading to less induction of extrapyramidal side effects (EPS). 
     Primary negative and cognitive symptoms of schizophrenia reflect a dysfunction of the frontal cortex (“hypofrontality”), which is thought to be induced by a decreased tone in the mesocortical dopaminergic projection field [Davis K L, Kahn R S, Ko G and Davidson M (1991). Dopamine in schizophrenia: a review and re-conceptualization.  Am J Psychiatry  148: 1474-86. Weinberger D R and Berman K F (1996). Prefrontal function in schizophrenia: confounds and controversies.  Philos Trans R Soc Lond B Biol Sci  351: 1495-503]. Agents that selectively enhance dopamine levels in the cortex have the potential to address the negative symptoms of this disorder. Atypical antipsychotics lack robust efficacy against negative and cognitive components of the schizophrenic syndrome. 
     The schizophrenic symptomatology is further complicated by the occurrence of drug-induced so-called secondary negative symptoms and cognitive impairment, which are difficult to distinguish from primary negative and cognitive symptoms [Remington G and Kapur S (2000). Atypical antipsychotics: are some more atypical than others? Psychopharmacol  148: 3-15]. The occurrence of secondary negative symptoms not only limits therapeutic efficacy but also, together with these side effects, negatively affects patient compliance. 
     It may thus be hypothesized that a novel mechanistic approach that blocks dopaminergic neurotransmission in the limbic system but does not affect the striatal and pituitary projection fields, and stimulates frontocortical projection fields, would provide an efficacious treatment for all parts of the schizophrenic pathology, including its positive, negative and cognitive symptoms. Moreover, a selective compound that is substantially free of the ancillary pharmacology that characterizes current agents would be expected to avoid a variety of off-target side effects that plague current treatments such as extrapyramidal side effects (EPS) and weight gain. 
     The 5-HT 2C  receptor, previously named 5-HT1C, is a G-protein-coupled receptor, which couples to multiple cellular effector systems including the phospholipase C, A and D pathways. It is found primarily in the brain and its distribution is particularly high in the plexus choroideus, where it is assumed to control cerebrospinal fluid production [Kaufman M J, Hirata F (1996) Cyclic GMP inhibits phosphoinositide turnover in choroid plexus: evidence for interactions between second messengers concurrently triggered by 5-HT 2C  receptors.  Neurosci Lett  206:153-156]. Very high levels were also found in the retrosplenial, piriform and entorhinal cortex, anterior olfactory nucleus, lateral septal nucleus, subthalamic nucleus, amygdala, subiculum and ventral part of CA3, lateral habenula, substantia nigra pars  compacta , several brainstem nuclei and the whole grey matter of the spinal cord [Pompeiano M, Palacios J M, Mengod G (1994). Distribution of the serotonin 5-HT2 receptor family mRNAs: comparison between 5-HT 2A  and 5-HT 2C  receptors.  Brain Res Mol Brain Res  23:163-178]. A comparison of the distribution of 5-HT 2C  mRNA with that of 5-HT 2 c protein in monkey and human brains has revealed both pre- and postsynaptic localization [Lopez-Gimenez J F, Mengod G, Palacios J M, Vilaro M T (2001) Regional distribution and cellular localization of 5-HT 2C  receptor mRNA in monkey brain: comparison with [ 3 H]mesulergine binding sites and choline acetyltransferase mRNA.  Synapse  42:12-26]. 
     It is anticipated that modulation of the 5-HT 2C  receptor will improve disorders such as depression, anxiety, schizophrenia, cognitive deficits of schizophrenia, obsessive compulsive disorder, bipolar disorder, migraine, epilepsy, substance abuse, eating disorders, obesity, diabetes, sexual dysfunction/erectile dysfunction, sleep disorders, psoriasis, Parkinson&#39;s disease, pain conditions and disorders, and spinal cord injury, smoking cessation, ocular hypertension and Alzheimer&#39;s disease. Modulators of the 5-HT 2C  receptor are also shown to be useful in the modulation of bladder function, including the prevention or treatment of urinary incontinence. 
     There is an ongoing need for providing compounds having high affinity and selectivity for the 5-HT 2c  receptor. In particular the compounds should have low affinity to adrenergic receptors, such as the al-adrenergic receptor, histamine receptors, such as the H 1 -receptor, and dopaminergic receptors, such as the D 2 -receptor, in order to avoid or reduce side effects associated with modulation of these receptors, such as postural hypotension, reflex tachycardia, potentiation of the antihypertensive effect of prazosin, terazosin, doxazosin and labetalol or dizziness associated with the blockade of the α 1 -adrenergic receptor, weight gain, sedation, drowsiness or potentiation of central depressant drugs associated with the blockade of the H 1 -receptor, or extrapyramidal movement disorder, such as dystonia, parkinsonism, akathisia, tardive dyskinesia or rabbit syndrome, or endocrine effects, such as prolactin elevation (galactorrhea, gynecomastia, mentstrual changes, sexual dysfunction in males), associated with the blockade of the D 2 -receptor. 
     The present invention provides compounds which have an affinity for the 5-HT 2C , thus allowing the treatment of disorders related to or affected by the 5-HT 2C  receptor. 
     SUMMARY OF THE INVENTION 
     The invention is directed to tricyclic quinoline and quinoxaline derivatives, compositions comprising such compounds, their use as modulators, especially agonists or partial agonists, of the 5-HT 2C  receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT 2C  receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT 2C  receptor, and processes for preparing such compounds and compositions. 
     In one aspect, the present invention relates to compounds of the formula (I): 
     
       
         
         
             
             
         
       
     
     wherein
     G is (CR 3a R 3b ) n ;   X is NR 6  or CR 7 R 8 ;   R 1  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —C(═O)R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 2  is independently selected from the group consisting of cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 3a  and R 3b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 4a  and R 4b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl,
       —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or   R 4a  and R 4b  form together a group ═O or ═S;   
       R 5a  and R 5b , independently of each other, are selected from the group consisting of hydrogen, deuterium, halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; where R 5a  and R 5b  are not simultaneously hydroxy; or
       R 5a  and R 5b , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring (i.e. a spiro ring), where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       R 6  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, fluorinated C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 6 -alkoxy, fluorinated, C 1 -C 6 -alkoxy, —C(═O)R 10 , —SO 2 R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   R 7  and R 8 , independently of each other, are selected from the group consisting of deuterium, halogen, cyano, nitro, hydroxyl, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; where R 7  and R 8  are not simultaneously hydroxyl; and where R 7  is not hydroxyl if R 8  is C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, phenoxy or benzyloxy; or
       R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring (i.e. a spiro ring), where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   each R 9  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkenyl, fluorinated C 3 -C 8 -cycloalkenyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or   two radicals R 9  bound on neighbouring carbon atoms, together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       each R 10  is independently selected from the group consisting of hydrogen, cyano, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —NR 12a R 12b , —CH 2 NR 12a R 12b , phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the five last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 11  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —COOH, —NR 12a R 12b , —CH 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy and fluorinated C 1 -C 6 -alkylcarbonyloxy;
       or two radicals R 11 , together with the atom(s) they are bound to, form a saturated, partially unsaturated or maximally unsaturated 3-, 4-, 5-, 6- or 7-membered carbocyclic or heterocyclic ring, where the heterocyclic ring contains 1, 2 or 3 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members;   
       R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, phenyl and benzyl, where the phenyl moieties in the two last-mentioned radicals may carry 1, 2 or 3 substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy; or,
       if R 12a  and R 12b  are bound to the same nitrogen atom, together with this nitrogen atom may form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy;   
       a is 0, 1 or 2;   b is 0, 1, 2 or 3; and   n is 1 or 2;   and the N-oxides, tautomeric forms, stereoisomers and pharmaceutically acceptable salts thereof, and the compound of the general formula I, wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope.   

     In another aspect, the invention relates to compounds of formula I as defined above, wherein
     G is (CR 3a R 3b ) n ;   X is NR 6  or CR 7 R 8 ;   R 1  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —C(═O)R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 2  is independently selected from the group consisting of cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 2a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 3a  and R 3b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 4a  and R 4b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl,
       —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or   R 4a  and R 4b  form together a group ═O or ═S;   
       R 5a  and R 5b , independently of each other, are selected from the group consisting of hydrogen, deuterium, halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       R 5a  and R 5b , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       R 6  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, fluorinated C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —C(═O)R 10 , —SO 2 R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   R 7  and R 8 , independently of each other, are selected from the group consisting of deuterium, halogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       each R 9  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkenyl, fluorinated C 3 -C 8 -cycloalkenyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       two radicals R 9  bound on neighbouring carbon atoms, together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       each R 10  is independently selected from the group consisting of hydrogen, cyano, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —NR 12a R 12b , —CH 2 NR 12a R 12b , phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the five last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 11  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —COOH, —NR 12a R 12b , —CH 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy and fluorinated C 1 -C 6 -alkylcarbonyloxy;   R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, phenyl and benzyl, where the phenyl moieties in the two last-mentioned radicals may carry 1, 2 or 3 substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy; or,
       if R 12a  and R 12b  are bound to the same nitrogen atom, together with this nitrogen atom may form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy;   
       a is 0, 1 or 2;   b is 0, 1, 2 or 3; and   n is 1 or 2;   and the N-oxides, tautomeric forms, stereoisomers and pharmaceutically acceptable salts thereof, and the compound of the general formula I, wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope.   

     Preferably, R 5a  and R 5b  are not simultaneously hydroxyl. 
     In another aspect, the invention relates to compounds of formula I 
     
       
         
         
             
             
         
       
     
     wherein
     G is (CR 3a R 3b ) n ;   X is NR 6  or CR 7 R 8 ;   R 1  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —C(═O)R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 2  is independently selected from the group consisting of cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 3a  and R 3b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ;   
       R 4a  and R 4b , independently of each other, are selected from the group consisting of hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl,
       —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or R 4a  and R 4b  form together a group ═O or ═S;   
       R 5a  and R 5b , independently of each other, are selected from the group consisting of hydrogen, deuterium, halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       R 5a  and R 5b , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       R 6  is selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —C(═O)R 10 , —SO 2 R 10 , phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 ;   R 7  and R 8 , independently of each other, are selected from the group consisting of deuterium, halogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       each R 9  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkenyl, fluorinated C 3 -C 8 -cycloalkenyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b , —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or
       two radicals R 9  bound on neighbouring carbon atoms, together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;   
       each R 10  is independently selected from the group consisting of hydrogen, cyano, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —NR 12a R 12b , —CH 2 NR 12a R 12b , phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the five last-mentioned radicals may be substituted with one or more substituents R 11 ;   each R 11  is independently selected from the group consisting of halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —COOH, —NR 12a R 12b , —CH 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy and fluorinated C 1 -C 6 -alkylcarbonyloxy;   R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from the group consisting of hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, phenyl and benzyl, where the phenyl moieties in the two last-mentioned radicals may carry 1, 2 or 3 substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy; or,
       if R 12a  and R 12b  are bound to the same nitrogen atom, together with this nitrogen atom may form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy;   
       a is 0, 1 or 2;   b is 0, 1, 2 or 3; and   n is 1 or 2;
 
and the N-oxides, tautomeric forms, stereoisomers and pharmaceutically acceptable salts thereof, and the compound of the general formula I, wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope.
   

     Preferably, R 5a  and R 5b  are not simultaneously hydroxyl. 
     In another aspect, the invention relates to a pharmaceutical composition comprising a therapeutically effective amount of at least one compound of formula I or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof, or comprising at least one compound as defined above or below wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope, preferably wherein at least one hydrogen atom has been replaced by a deuterium atom, in combination with at least one pharmaceutically acceptable carrier and/or auxiliary substance. 
     In yet another aspect, the invention relates to a compound of formula I or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for use as a medicament. 
     In yet another aspect, the invention relates to a compound of formula I or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the treatment of disorders which responds to the modulation of the 5-HT 2c  receptor. 
     In yet another aspect, the invention relates to the use of a compound of formula I or of an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of disorders which respond to the modulation of the 5-HT 2c  receptor. 
     In yet another aspect, the invention relates to the use of a compound of formula I or of an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of disorders selected from the group consisting of damage of the central nervous system, disorders of the central nervous system, eating disorders, ocular hypertension, cardiovascular disorders, gastrointestinal disorders and diabetes, and especially from the group consisting of bipolar disorder, depression, atypical depression, mood episodes, adjustment disorders, anxiety, panic disorders, post-traumatic syndrome, psychoses, schizophrenia, cognitive deficits of schizophrenia, memory loss, dementia of aging, Alzheimer&#39;s disease, behavioral disorders associated with dementia, social phobia, mental disorders in childhood, attention deficit hyperactivity disorder, organic mental disorders, autism, mutism, disruptive behavior disorder, impulse control disorder, borderline personality disorder, obsessive compulsive disorder, migraine and other conditions associated with cephalic pain or other pain, raised intracranial pressure, seizure disorders, epilepsy, substance use disorders, alcohol abuse, cocaine abuse, tobacco abuse, smoking cessation, sexual dysfunction/erectile dysfunction in males, sexual dysfunction in females, premenstrual syndrome, late luteal phase syndrome, chronic fatigue syndrome, sleep disorders, sleep apnoea, chronic fatigue syndrome, psoriasis, Parkinson&#39;s disease, spinal cord injury, trauma, stroke, pain, bladder dysfunction/urinary incontinence, encephalitis, meningitis, eating disorders, obesity, bulimia, weight loss, anorexia nervosa, ocular hypertension, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, diabetes mellitus, type I diabetes, type II diabetes, type III diabetes, diabetes secondary to pancreatic diseases, diabetes related to steroid use, diabetes complications, hyperglycemia and insulin resistance. 
     In yet another aspect, the invention relates to a method for treating disorders which respond to the modulation of the 5-HT 2c  receptor, which method comprises administering to a subject in need thereof at least one compound of formula I or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. 
     In yet another aspect, the invention relates to a method for treating disorders selected from the group consisting of damage of the central nervous system, disorders of the central nervous system, eating disorders, ocular hypertension, cardiovascular disorders, gastrointestinal disorders and diabetes, and especially from the group consisting of bipolar disorder, depression, atypical depression, mood episodes, adjustment disorders, anxiety, panic disorders, post-traumatic syndrome, psychoses, schizophrenia, cognitive deficits of schizophrenia, memory loss, dementia of aging, Alzheimer&#39;s disease, behavioral disorders associated with dementia, social phobia, mental disorders in childhood, attention deficit hyperactivity disorder, organic mental disorders, autism, mutism, disruptive behavior disorder, impulse control disorder, borderline personality disorder, obsessive compulsive disorder, migraine and other conditions associated with cephalic pain or other pain, raised intracranial pressure, seizure disorders, epilepsy, substance use disorders, alcohol abuse, cocaine abuse, tobacco abuse, smoking cessation, sexual dysfunction/erectile dysfunction in males, sexual dysfunction in females, premenstrual syndrome, late luteal phase syndrome, chronic fatigue syndrome, sleep disorders, sleep apnoea, chronic fatigue syndrome, psoriasis, Parkinson&#39;s disease, spinal cord injury, trauma, stroke, pain, bladder dysfunction/urinary incontinence, encephalitis, meningitis, eating disorders, obesity, bulimia, weight loss, anorexia nervosa, ocular hypertension, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, diabetes mellitus, type I diabetes, type II diabetes, type III diabetes, diabetes secondary to pancreatic diseases, diabetes related to steroid use, diabetes complications, hyperglycemia and insulin resistance, which method comprises administering to a subject in need thereof at least one compound of formula I or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. 
    
    
     DETAILED DESCRIPTION 
     The compounds of the formula I may exist in different spatial arrangements. For example, if the compounds possess one or more centers of asymmetry, polysubstituted rings or double bonds, or as different tautomers, the present invention contemplates the possible use of enantiomeric mixtures, in particular racemates, diastereomeric mixtures and tautomeric mixtures, such as the respective essentially pure enantiomers, diastereomers and tautomers of the compounds of formula I and/or their salts. 
     It is likewise possible to use physiologically tolerated salts of the compounds of the formula I, especially acid addition salts with physiologically tolerated acids. Examples of suitable physiologically tolerated organic and inorganic acids are hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, acetic acid, trifluoroacetic acid, C 1 -C 4 -alkylsulfonic acids, such as methanesulfonic acid, aromatic sulfonic acids, such as benzenesulfonic acid and toluenesulfonic acid, oxalic acid, maleic acid, fumaric acid, lactic acid, tartaric acid, adipic acid and benzoic acid. Other utilizable acids are described in Fortschritte der Arzneimittelforschung [Advances in drug research], Volume 10, pages 224 et seq., Birkhäuser Verlag, Basel and Stuttgart, 1966. 
     The compounds of formula I may also be present in the form of tautomers. In one aspect, tautomery may be present in compounds I wherein R 4a  and R 4b  form together a group ═O and R 5a  or R 5b  is H. For example, the compounds of formula I may have the following tautomeric formulae: 
     
       
         
         
             
             
         
       
     
     In another aspect, tautomery may be present in compounds I containing rings which have one or more C═O groups as ring members which are neighboured to a CH 2  group. 
     The organic moieties mentioned in the above definitions of the variables are, like the term halogen, collective terms for individual listings of the individual group members. The prefix C n -C m  indicates in each case the possible number of carbon atoms in the group. 
     The term “halogen” denotes in each case fluorine, bromine, chlorine or iodine. In one aspect, the halogen may be fluorine, chlorine or bromine. 
     The term “alkyl” as used herein and in the alkyl moieties of alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylcarbonyl, alkoxycarbonyl and the like refers to saturated straight-chain or branched hydrocarbon radicals having 1 to 2 (“C 1 -C 2 -alkyl”), 1 to 3 (“C 1 -C 3 -alkyl”), 1 to 4 (“C 1 -C 4 -alkyl”) or 1 to 6 (“C 1 -C 6 -alkyl”) carbon atoms. C 1 -C 2 -Alkyl is methyl or ethyl. C 1 -C 3 -Alkyl is additionally propyl and isopropyl. C 1 -C 4 -Alkyl is additionally butyl, 1-methylpropyl (sec-butyl), 2-methylpropyl (isobutyl) or 1,1-dimethylethyl (tert-butyl). C 1 -C 6 -Alkyl is additionally also, for example, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, 1-ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl, or 1-ethyl-2-methylpropyl. 
     The term “fluorinated alkyl” as used herein refers to straight-chain or branched alkyl groups having 1 to 2 (“fluorinated C 1 -C 2 -alkyl”), 1 to 3 (“fluorinated C 1 -C 3 -alkyl”), 1 to 4 (“fluorinated C 1 -C 4 -alkyl”) or 1 to 6 (“fluorinated C 1 -C 6 -alkyl”) carbon atoms (as mentioned above), where some or all of the hydrogen atoms in these groups are replaced by fluorine atoms. Fluorinated C 1 -C 2 -alkyl is an alkyl group having 1 or 2 carbon atoms (as mentioned above), where at least one of the hydrogen atoms, e.g. 1, 2, 3, 4 or 5 hydrogen atoms in these groups are replaced by fluorine atoms, such as difluoromethyl, trifluoromethyl, 1-fluoroethyl, (R)-1-fluoroethyl, (S)-1-fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, or pentafluoroethyl. Fluorinated C 1 -C 4 -alkyl is a straight-chain or branched alkyl group having 1 to 4 carbon atoms (as mentioned above), where at least one of the hydrogen atoms, e.g. 1, 2, 3, 4 or 5 hydrogen atoms in these groups are replaced by fluorine atoms. Examples are, apart those listed above for C 1 -C 2 -fluoroalkyl, 1-fluoropropyl, (R)-1-fluoropropyl, (S)-1-fluoropropyl, 2-fluoropropyl, (R)-2-fluoropropyl, (S)-2-fluoropropyl, 3-fluoropropyl, 1,1-difluoropropyl, 2,2-difluoropropyl, 1,2-difluoropropyl, 2,3-difluoropropyl, 1,3-difluoropropyl, 3,3-difluoropropyl, 1,1,2-trifluoropropyl, 1,2,2-trifluoropropyl, 1,2,3-trifluoropropyl, 2,2,3-trifluoropropyl, 3,3,3-trifluoropropyl, 1,1,1-trifluoroprop-2-yl, 2-fluoro-1-methylethyl, (R)-2-fluoro-1-methylethyl, (S)-2-fluoro-1-methylethyl, 2,2-difluoro-1-methylethyl, (R)-2,2-difluoro-1-methylethyl, (S)-2,2-difluoro-1-methylethyl, 1,2-difluoro-1-methylethyl, (R)-1,2-difluoro-1-methylethyl, (S)-1,2-difluoro-1-methylethyl, 2,2,2-trifluoro-1-methylethyl, (R)-2,2,2-trifluoro-1-methylethyl, (S)-2,2,2-trifluoro-1-methylethyl, 2-fluoro-1-(fluoromethyl)ethyl, 1-(difluoromethyl)-2,2-difluoroethyl, 1-(trifluoromethyl)-2,2,2-trifluoroethyl, 1-(trifluoromethyl)-1,2,2,2-tetrafluoroethyl, 1-fluorobutyl, (R)-1-fluorobutyl, (S)-1-fluorobutyl, 2-fluorobutyl, (R)-2-fluorobutyl, (S)-2-fluorobutyl, 3-fluorobutyl, (R)-3-fluorobutyl, (S)-3-fluorobutyl, 4-fluorobutyl, 1,1-difluorobutyl, 2,2-difluorobutyl, 3,3-difluorobutyl, 4,4-difluorobutyl, 4,4,4-trifluorobutyl and the like. Fluorinated C 1 -C 6 -alkyl is a straight-chain or branched alkyl group having 1 to 6 carbon atoms (as mentioned above), where at least one of the hydrogen atoms, e.g. 1, 2, 3, 4 or 5 hydrogen atoms in these groups are replaced by fluorine atoms. Additionally examples include for C 1 -C 4 -fluoroalkyl, 1-fluoropentyl, (R)-1-fluoropentyl, (S)-1-fluoropentyl, 2-fluoropentyl, (R)-2-fluoropentyl, (S)-2-fluoropentyl, 3-fluoropentyl, (R)-3-fluoropentyl, (S)-3-fluoropentyl, 4-fluoropentyl, (R)-4-fluoropentyl, (S)-4-fluoropentyl, 5-fluoropentyl, (R)-5-fluoropentyl, (S)-5-fluoropentyl, 1-fluorohexyl, (R)-1-fluorohexyl, (S)-1-fluorohexyl, 2-fluorohexyl, (R)-2-fluorohexyl, (S)-2-fluorohexyl, 3-fluorohexyl, (R)-3-fluorohexyl, (S)-3-fluorohexyl, 4-fluorohexyl, (R)-4-fluorohexyl, (S)-4-fluorohexyl, 5-fluorohexyl, (R)-5-fluorohexyl, (S)-5-fluorohexyl, 6-fluorohexyl, (R)-6-fluorohexyl, (S)-6-fluorohexyl, and the like. 
     The term “alkenyl” as used herein refers to monounsaturated straight-chain or branched hydrocarbon radicals having 2 to 3 (“C 2 -C 3 -alkenyl”), 2 to 4 (“C 2 -C 4 -alkenyl”) or 2 to 6 (“C 2 -C 6 -alkenyl”) carbon atoms and a double bond in any position, such as C 2 -C 3 -alkenyl, such as ethenyl, 1-propenyl, 2-propenyl or 1-methylethenyl; C 2 -C 4 -alkenyl, such as ethenyl, 1-propenyl, 2-propenyl, 1-methylethenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-methyl-1-propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl or 2-methyl-2-propenyl; and C 2 -C 6 -alkenyl, such as ethenyl, 1-propenyl, 2-propenyl, 1-methylethenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-methyl-1-propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-methyl-1-butenyl, 2-methyl-1-butenyl, 3-methyl-1-butenyl, 1-methyl-2-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1,1-dimethyl-2-propenyl, 1,2-dimethyl-1-propenyl, 1,2-dimethyl-2-propenyl, 1-ethyl-1-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-1-pentenyl, 2-methyl-1-pentenyl, 3-methyl-1-pentenyl, 4-methyl-1-pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-1-butenyl, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-1-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl, 2,2-dimethyl-3-butenyl, 2,3-dimethyl-1-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl, 3,3-dimethyl-2-butenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1-ethyl-1-methyl-2-propenyl, 1-ethyl-2-methyl-1-propenyl, 1-ethyl-2-methyl-2-propenyl and the like. 
     The term “fluorinated alkenyl” as used herein refers to unsaturated straight-chain or branched hydrocarbon radicals having 2 to 3 (“fluorinated C 2 -C 3 -alkenyl”), 2 to 4 (“fluorinated C 2 -C 4 -alkenyl”) or 2 to 6 (“fluorinated C 2 -C 6 -alkenyl”) carbon atoms and a double bond in any position (as mentioned above), where some or all of the hydrogen atoms in these groups are replaced by fluorine atoms, such as, fluorovinyl, fluoroallyl and the like. 
     The term “alkynyl” as used herein refers to straight-chain or branched hydrocarbon groups having 2 to 3 (“C 2 -C 3 -alkynyl”), 2 to 4 (“C 2 -C 4 -alkynyl”) or 2 to 6 (“C 2 -C 6 -alkynyl”) carbon atoms and one or two triple bonds in any position, such as C 2 -C 3 -alkynyl, such as ethynyl, 1-propynyl or 2-propynyl; C 2 -C 4 -alkynyl, such as ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl and the like, and C 2 -C 6 -alkynyl, such as ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-methyl-2-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 3-methyl-1-butynyl, 1,1-dimethyl-2-propynyl, 1-ethyl-2-propynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-1-pentynyl, 3-methyl-4-pentynyl, 4-methyl-1-pentynyl, 4-methyl-2-pentynyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl, 1-ethyl-1-methyl-2-propynyl and the like. 
     The term “fluorinated alkynyl” as used herein refers to unsaturated straight-chain or branched hydrocarbon radicals having 2 to 3 (“fluorinated C 2 -C 3 -alkynyl”), 3 to 4 (“fluorinated C 3 -C 4 -alkynyl”) or 2 to 6 (“fluorinated C 2 -C 6 -alkynyl”) carbon atoms and one or two triple bonds in any position (as mentioned above), where some or all of the hydrogen atoms in these groups are replaced by fluorine atoms. 
     The term “cycloalkyl” as used herein refers to mono- or bicyclic saturated hydrocarbon radicals having 3 to 8 (“C 3 -C 8 -cycloalkyl”), in particular 3 to 6 carbon atoms (“C 3 -C 6 -cycloalkyl”) or 3 to 5 carbon atoms (“C 3 -C 8 -cycloalkyl”) or 3 or 4 carbon atoms (“C 3 -C 4 -cycloalkyl”). In one aspect, C 3 -C 4 -cycloalkyl, C 3 -C 8 -cycloalkyl and C 3 -C 6 -cycloalkyl are monocyclic. Examples for C 3 -C 4 -cycloalkyl are cyclopropyl and cyclobutyl. Examples of monocyclic radicals having 3 to 5 carbon atoms are cyclopropyl, cyclobutyl and cyclopentyl. Examples of monocyclic radicals having 3 to 6 carbon atoms are cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. Examples of monocyclic radicals having 3 to 8 carbon atoms are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl. Examples of bicyclic radicals having 7 or 8 carbon atoms comprise bicyclo[2.2.1]heptyl, bicyclo[3.1.1]heptyl, bicyclo[2.2.2]octyl and bicyclo[3.2.1]octyl. In one aspect, the term cycloalkyl denotes a monocyclic saturated hydrocarbon radical. 
     The term “fluorinated cycloalkyl” as used herein refers to mono- or bicyclic saturated hydrocarbon groups having 3 to 8 (“C 3 -C 8 -halocycloalkyl”) or preferably 3 to 6 (“C 3 -C 6 -halocycloalkyl”) or 3 to 5 (“C 3 -C 8 -halocycloalkyl”) carbon ring members (as mentioned above) in which some or all of the hydrogen atoms are replaced by fluorine atoms. Examples include 1-fluorocyclopropyl, 2-fluorocyclopropyl, (S)- and (R)-2,2-difluorocyclopropyl, 1,2-difluorocyclopropyl, 2,3-difluorocyclopropyl, pentafluorocyclopropyl, 1-fluorocyclobutyl, 2-fluorocyclobutyl, 3-fluorocyclobutyl, 2,2-difluorocyclobutyl, 3,3-difluorocyclobutyl, 1,2-difluorocyclobutyl, 1,3-difluorocyclobutyl, 2,3-difluorocyclobutyl, 2,4-difluorocyclobutyl, 1,2,2-trifluorocyclobutyl, 1-fluorocycloheptyl, 2-fluorocycloheptyl, 3-fluorocycloheptyl, 4-fluorocycloheptyl, 1,2-difluorocycloheptyl, 1,3-difluorocycloheptyl, 1,4-difluorocycloheptyl, 2,2-difluorocycloheptyl, 2,3-difluorocycloheptyl, 2,4-difluorocycloheptyl, 2,5-difluorocycloheptyl, 2,6-difluorocycloheptyl, 2,7-difluorocycloheptyl, 3,3-difluorocycloheptyl, 3,4-difluorocycloheptyl, 3,5-difluorocycloheptyl, 3,6-difluorocycloheptyl, 4,4-difluorocycloheptyl, 4,5-difluorocycloheptyl, and the like. 
     The term “cycloalkenyl” as used herein refers to monocyclic partially unsaturated, non-aromatic hydrocarbon radicals having 3 to 8 (“C 3 -C 8 -cycloalkenyl”), in particular 5 to 7 carbon atoms (“C 5 -C 7 -cycloalkenyl”) or 5 or 6 carbon atoms (“C 5 -C 6 -cycloalkenyl”) and one or more non-cumulative, preferably one, C—C double bonds in the ring. Examples for C 5 -C 6 -cycloalkenyl are cyclopent-1-en-1-yl, cyclopent-1-en-3-yl, cyclopent-1-en-4-yl, cyclopenta-1,3-dien-1-yl, cyclopenta-1,3-dien-2-yl, cyclopenta-1,3-dien-5-yl, cyclohex-1-en-1-yl, cyclohex-1-en-3-yl, cyclohex-1-en-4-yl, cyclohexa-1,3-dien-1-yl, cyclohexa-1,3-dien-2-yl, cyclohexa-1,3-dien-5-yl, cyclohexa-1,4-dien-1-yl and cyclohexa-1,4-dien-3-yl. Examples of C 5 -C 7 -cycloalkenyl are, apart those mentioned above, include for C 5 -C 6 -cycloalkenyl, cyclohept-1-en-1-yl, cyclohept-1-en-3-yl, cyclohept-1-en-4-yl, cyclohept-1-en-5-yl, cyclohepta-1,3-dien-1-yl, cyclohepta-1,3-dien-2-yl, cyclohepta-1,3-dien-5-yl, cyclohepta-1,3-dien-6-yl, cyclohepta-1,4-dien-1-yl, cyclohepta-1,4-dien-2-yl, cyclohepta-1,4-dien-3-yl and cyclohepta-1,4-dien-6-yl. Examples of C 3 -C 8 -cycloalkenyl are, apart those mentioned above for C 5 -C 6 -cycloalkenyl, cycloprop-1-en-1-yl, cycloprop-1-en-3-yl, cyclobut-1-en-1-yl, cyclobut-1-en-3-yl, cyclooct-1-en-1-yl, cyclooct-1-en-3-yl, cyclooct-1-en-4-yl, cyclooct-1-en-5-yl, cycloocta-1,3-dien-1-yl, cycloocta-1,3-dien-2-yl, cycloocta-1,3-dien-5-yl, cycloocta-1,3-dien-6-yl, cycloocta-1,4-dien-1-yl, cycloocta-1,4-dien-2-yl, cycloocta-1,4-dien-3-yl, cycloocta-1,4-dien-6-yl, cycloocta-1,4-dien-7-yl, cycloocta-1,5-dien-1-yl, and cycloocta-1,5-dien-3-yl. 
     The term “fluorinated cycloalkenyl” as used herein refers to monocyclic partially unsaturated, non-aromatic hydrocarbon radicals having 3 to 8 (“fluorinated C 3 -C 8 -cycloalkenyl”), in particular 5 to 7 carbon atoms (“fluorinated C 5 -C 7 -cycloalkenyl”) or 5 or 6 carbon atoms (“fluorinated C 5 -C 6 -cycloalkenyl”) and one or more non-cumulative, preferably one, C—C double bonds in the ring and in which some or all of the hydrogen atoms are replaced by fluorine atoms. 
     The term “cycloalkyl-C 1 -C 4 -alkyl” refers to a C 3 -C 8 -cycloalkyl group (“C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl”), preferably a C 3 -C 6 -cycloalkyl group (“C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl”) as defined above which is bound to the remainder of the molecule via a C 1 -C 4 -alkyl group, as defined above. The term “cycloalkyl-C 1 -C 2 -alkyl” refers to a C 3 -C 8 -cycloalkyl group (“C 3 -C 8 -cycloalkyl-C 1 -C 2 -alkyl”), preferably a C 3 -C 6 -cycloalkyl group (“C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl”) as defined above which is bound to the remainder of the molecule via a C 1 -C 2 -alkyl group, as defined above. Examples for C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl are cyclopropylmethyl, cyclopropylethyl, cyclobutylmethyl, cyclobutylethyl, cyclopentylmethyl, cyclopentylethyl, cyclohexylmethyl and cyclohexylethyl. Examples for C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, apart those mentioned for C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, are cyclopropylpropyl, cyclopropylbutyl, cyclobutylpropyl, cyclobutylbutyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexylpropyl and cyclohexylbutyl. Examples for C 3 -C 8 -cycloalkyl-C 1 -C 2 -alkyl, apart those mentioned for C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, are cycloheptylmethyl, cycloheptylethyl, cyclooctylmethyl and cyclooctylethyl. Examples for C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, apart those mentioned for C 3 -C 8 -cycloalkyl-C 1 -C 2 -alkyl, are cycloheptylpropyl, cycloheptylbutyl, cyclooctylpropyland cyclooctylbutyl. 
     The term “fluorinated cycloalkyl-C 1 -C 4 -alkyl” refers to a fluorinated C 3 -C 8 -cycloalkyl group (“fluorinated C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl”), preferably a fluorinated C 3 -C 6 -cycloalkyl group (“fluorinated C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl”) as defined above which is bound to the remainder of the molecule via a C 1 -C 4 -alkyl group, as defined above. The term “fluorinated cycloalkyl-C 1 -C 2 -alkyl” refers to a fluorinated C 3 -C 8 -cycloalkyl group (“fluorinated C 3 -C 8 -cycloalkyl-C 1 -C 2 -alkyl”), preferably a fluorinated C 3 -C 6 -cycloalkyl group (“fluorinated C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl”) as defined above which is bound to the remainder of the molecule via a C 1 -C 2 -alkyl group, as defined above. 
     The term “C 1 -C 2 -alkoxy” is a C 1 -C 2 -alkyl group, as defined above, attached via an oxygen atom. The term “C 1 -C 3 -alkoxy” is a C 1 -C 3 -alkyl group, as defined above, attached via an oxygen atom. The term “C 1 -C 4 -alkoxy” is a C 1 -C 4 -alkyl group, as defined above, attached via an oxygen atom. The term “C 1 -C 6 -alkoxy” is a C 1 -C 6 -alkyl group, as defined above, attached via an oxygen atom. C 1 -C 2 -Alkoxy is methoxy or ethoxy. C 1 -C 3 -Alkoxy is additionally, for example, n-propoxy and 1-methylethoxy (isopropoxy). C 1 -C 4 -Alkoxy is additionally, for example, butoxy, 1-methylpropoxy (sec-butoxy), 2-methylpropoxy (isobutoxy) or 1,1-dimethylethoxy (tert-butoxy). C 1 -C 6 -Alkoxy is additionally, for example, pentoxy, 1-methylbutoxy, 2-methylbutoxy, 3-methylbutoxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, 2,2-dimethylpropoxy, 1-ethylpropoxy, hexoxy, 1-methylpentoxy, 2-methylpentoxy, 3-methylpentoxy, 4-methylpentoxy, 1,1-dimethylbutoxy, 1,2-dimethylbutoxy, 1,3-dimethylbutoxy, 2,2-dimethylbutoxy, 2,3-dimethylbutoxy, 3,3-dimethylbutoxy, 1-ethylbutoxy, 2-ethylbutoxy, 1,1,2-trimethylpropoxy, 1,2,2-trimethylpropoxy, 1-ethyl-1-methylpropoxy or 1-ethyl-2-methylpropoxy. C 1 -C 8 -Alkoxy is additionally, for example, heptyloxy, octyloxy, 2-ethylhexyloxy and positional isomers thereof. 
     The term “fluorinated C 1 -C 2 -alkoxy” is a fluorinated C 1 -C 2 -alkyl group, as defined above, attached via an oxygen atom. The term “fluorinated C 1 -C 3 -alkoxy” is a fluorinated C 1 -C 3 -alkyl group, as defined above, attached via an oxygen atom. The term “fluorinated C 1 -C 6 -haloalkoxy” is a fluorinated C 1 -C 6 -alkyl group, as defined above, attached via an oxygen atom. Fluorinated C 1 -C 2 -alkoxy is, for example, OCH 2 F, OCHF 2 , OCF 3 , 1-fluoroethoxy, (R)-1-fluoroethoxy, (S)-1-fluoroethoxy, 2-fluoroethoxy, 1,1-difluoroethoxy, 1,2-difluoroethoxy, 2,2-difluoroethoxy, 1,1,2-trifluoroethoxy, 1,2,2-trifluoroethoxy, 2,2,2-trifluoroethoxy, 1,1,2,2-tetrafluoroethoxy or OC 2 F 5 . Fluorinated C 1 -C 3 -alkoxy is additionally, for example, 1-fluoropropoxy, (R)-1-fluoropropoxy, (S)-1-fluoropropoxy, 2-fluoropropoxy, (R)-2-fluoropropoxy, (S)-2-fluoropropoxy, 3-fluoropropoxy, 1,1-difluoropropoxy, 2,2-difluoropropoxy, 2,3-difluoropropoxy, 3,3-difluoropropoxy, 3,3,3-trifluoropropoxy, (R)-2-fluoro-1-methylethoxy, (S)-2-fluoro-1-methylethoxy, (R)-2,2-difluoro-1-methylethoxy, (S)-2,2-difluoro-1-methylethoxy, (R)-1,2-difluoro-1-methylethoxy, (S)-1,2-difluoro-1-methylethoxy, (R)-2,2,2-trifluoro-1-methylethoxy, (S)-2,2,2-trifluoro-1-methylethoxy, 2-fluoro-1-(fluoromethyl)ethoxy, 1-(difluoromethyl)-2,2-difluoroethoxy, OCH 2 —C 2 F 5 , OCF 2 —C 2 F 5  or 1-(CH 2 F)-2-fluoroethoxy. Fluorinated C 1 -C 4 -alkoxy is additionally, for example, 1-fluorobutoxy, (R)-1-fluorobutoxy, (S)-1-fluorobutoxy, 2-fluorobutoxy, 3-fluorobutoxy, 4-fluorobutoxy, 1,1-difluorobutoxy, 2,2-difluorobutoxy, 3,3-difluorobutoxy, 4,4-difluorobutoxy, 4,4,4-trifluorobutoxy or nonafluorobutoxy. Fluorinated C 1 -C 6 -alkoxy is additionally, for example, 5-fluoropentoxy, undecafluoropentoxy, 6-fluorohexoxy or tridecafluorohexoxy. 
     The term “C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl” as used herein, refers to a straight-chain or branched alkyl group having 1 to 4 carbon atoms, as defined above, where one hydrogen atom is replaced by a C 1 -C 4 -alkoxy group, as defined above. The term “C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl” as used herein, refers to a straight-chain or branched alkyl group having 1 to 4 carbon atoms, as defined above, where one hydrogen atom is replaced by a C 1 -C 6 -alkoxy group, as defined above. Examples are methoxymethyl, ethoxymethyl, propoxymethyl, isopropoxymethyl, n-butoxymethyl, sec-butoxymethyl, isobutoxymethyl, tert-butoxymethyl, 1-methoxyethyl, 1-ethoxyethyl, 1-propoxyethyl, 1-isopropoxyethyl, 1-n-butoxyethyl, 1-sec-butoxyethyl, 1-isobutoxyethyl, 1-tert-butoxyethyl, 2-methoxyethyl, 2-ethoxyethyl, 2-propoxyethyl, 2-isopropoxyethyl, 2-n-butoxyethyl, 2-sec-butoxyethyl, 2-isobutoxyethyl, 2-tert-butoxyethyl, 1-methoxypropyl, 1-ethoxypropyl, 1-propoxypropyl, 1-isopropoxypropyl, 1-n-butoxypropyl, 1-sec-butoxypropyl, 1-isobutoxypropyl, 1-tert-butoxypropyl, 2-methoxypropyl, 2-ethoxypropyl, 2-propoxypropyl, 2-isopropoxypropyl, 2-n-butoxypropyl, 2-sec-butoxypropyl, 2-isobutoxypropyl, 2-tert-butoxypropyl, 3-methoxypropyl, 3-ethoxypropyl, 3-propoxypropyl, 3-isopropoxypropyl, 3-n-butoxypropyl, 3-sec-butoxypropyl, 3-isobutoxypropyl, 3-tert-butoxypropyl and the like. 
     The term “hydroxy-C 1 -C 4 -alkyl” as used herein, refers to a straight-chain or branched alkyl group having 1 to 4 carbon atoms, as defined above, where one hydrogen atom is replaced by a hydroxy group. The term “hydroxy-C 1 -C 6 -alkyl” as used herein, refers to a straight-chain or branched alkyl group having 1 to 6 carbon atoms, as defined above, where one hydrogen atom is replaced by a hydroxy group. Examples for hydroxy-C 1 -C 4 -alkyl include hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1-hydroxypropyl, 2-hydroxypropyl, 3-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl, 4-hydroxybutyl, 1-hydroxybut-2-yl, 2-hydroxybut-2-yl, 3-hydroxybut-2-yl, 4-hydroxybut-2-yl, hydroxy-tert-butyl and the like. Examples for hydroxy-C 1 -C 6 -alkyl are, apart those mentioned for hydroxy-C 1 -C 4 -alkyl, include, 1-hydroxypentyl, 2-hydroxypentyl, 3-hydroxypentyl, 4-hydroxypentyl, 5-hydroxypentyl, 1-hydroxyhexyl, 2-hydroxyhexyl, 3-hydroxyhexyl, 4-hydroxyhexyl, 5-hydroxyhexyl, 6-hydroxyhexyl and the like. 
     The term “hydroxy-C 1 -C 4 -alkoxy” as used herein, refers to a C 1 -C 4 -alkoxy group, as defined above, where one hydrogen atom is replaced by a hydroxy group. The term “hydroxy-C 1 -C 6 -alkoxy” as used herein, refers to a C 1 -C 6 -alkoxy group, as defined above, where one hydrogen atom is replaced by a hydroxy group. Examples for hydroxy-C 1 -C 4 -alkoxy include hydroxymethoxy, 1-hydroxyethoxy, 2-hydroxyethoxy, 1-hydroxypropoxy, 2-hydroxypropoxy, 3-hydroxypropoxy, 1-hydroxy-2-propoxy, 2-hydroxy-2-propoxy, 1-hydroxybutoxy, 2-hydroxybutoxy, 3-hydroxybutoxy, 4-hydroxybutoxy, 1-hydroxy-2-butoxy, 2-hydroxy-2-butoxy, 3-hydroxy-2-butoxy, 4-hydroxy-2-butoxy, hydroxy-tert-butoxy and the like. Examples for hydroxy-C 1 -C 6 -alkoxy include, apart those mentioned for hydroxy-C 1 -C 4 -alkoxy, 1-hydroxypentoxy, 2-hydroxypentoxy, 3-hydroxypentoxy, 4-hydroxypentoxy, 5-hydroxypentoxy, 1-hydroxyhexoxy, 2-hydroxyhexoxy, 3-hydroxyhexoxy, 4-hydroxyhexoxy, 5-hydroxyhexoxy, 6-hydroxyhexoxy and the like. 
     The term “C 1 -C 4 -alkoxy-C 1 -C 4 -alkoxy” as used herein, refers to a C 1 -C 4 -alkoxy group, as defined above, where one hydrogen atom is replaced by a C 1 -C 4 -alkoxy group, as defined above. The term “C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy” as used herein, refers to a C 1 -C 4 -alkoxy group, as defined above, where one hydrogen atom is replaced by a C 1 -C 4 -alkoxy group, as defined above. Examples are methoxymethoxy, ethoxymethoxy, propoxymethoxy, isopropoxymethoxy, butoxymethoxy, sec-butoxymethoxy, isobutoxymethoxy, tert-butoxymethoxy, 1-methoxyethoxy, 1-ethoxyethoxy, 1-propoxyethoxy, 1-isopropoxyethoxy, 1-butoxyethoxy, 1-sec-butoxyethoxy, 1-isobutoxyethoxy, 1-tert-butoxyethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, 2-propoxyethoxy, 2-isopropoxyethoxy, 2-butoxyethoxy, 2-sec-butoxyethoxy, 2-isobutoxyethoxy, 2-tert-butoxyethoxy, 1-methoxypropoxy, 1-ethoxypropoxy, 1-propoxypropoxy, 1-isopropoxypropoxy, 1-butoxypropoxy, 1-sec-butoxypropoxy, 1-isobutoxypropoxy, 1-tert-butoxypropoxy, 2-methoxypropoxy, 2-ethoxypropoxy, 2-propoxypropoxy, 2-isopropoxypropoxy, 2-butoxypropoxy, 2-sec-butoxypropoxy, 2-isobutoxypropoxy, 2-tert-butoxypropoxy, 3-methoxypropoxy, 3-ethoxypropoxy, 3-propoxypropoxy, 3-isopropoxypropoxy, 3-butoxypropoxy, 3-sec-butoxypropoxy, 3-isobutoxypropoxy, 3-tert-butoxypropoxy and the like. 
     The term “C 1 -C 2 -alkylthio” is a C 1 -C 2 -alkyl group, as defined above, attached via a sulfur atom. The term “C 1 -C 3 -alkylthio” refers to a C 1 -C 3 -alkyl group, as defined above, attached via a sulfur atom. The term “C 1 -C 4 -alkylthio” is a C 1 -C 4 -alkyl group, as defined above, attached via a sulfur atom. The term “C 1 -C 6 -alkylthio” refers to a C 1 -C 6 -alkyl group, as defined above, attached via a sulfur atom. The term “C 1 -C 10 -alkylthio” refers to a C 1 -C 10 -alkyl group, as defined above, attached via a sulfur atom. C 1 -C 2 -Alkylthio is methylthio or ethylthio. C 1 -C 3 -Alkylthio is additionally, for example, n-propylthio or 1-methylethylthio (isopropylthio). C 1 -C 4 -Alkylthio is additionally, for example, butylthio, 1-methylpropylthio (sec-butylthio), 2-methylpropylthio (isobutylthio) or 1,1-dimethylethylthio (tert-butylthio). C 1 -C 6 -Alkylthio is additionally, for example, pentylthio, 1-methylbutylthio, 2-methylbutylthio, 3-methylbutylthio, 1,1-dimethylpropylthio, 1,2-dimethylpropylthio, 2,2-dimethylpropylthio, 1-ethylpropylthio, hexylthio, 1-methylpentylthio, 2-methylpentylthio, 3-methylpentylthio, 4-methylpentylthio, 1,1-dimethylbutylthio, 1,2-dimethylbutylthio, 1,3-dimethylbutylthio, 2,2-dimethylbutylthio, 2,3-dimethylbutylthio, 3,3-dimethylbutylthio, 1-ethylbutylthio, 2-ethylbutylthio, 1,1,2-trimethylpropylthio, 1,2,2-trimethylpropylthio, 1-ethyl-1-methylpropylthio or 1-ethyl-2-methylpropylthio. 
     The term “fluorinated C 1 -C 2 -alkylthio” refers to a fluorinated C 1 -C 2 -alkyl group, as defined above, attached via a sulfur atom. The term “fluorinated C 1 -C 3 -alkylthio” refers to a fluorinated C 1 -C 3 -alkyl group, as defined above, attached via a sulfur atom. The term “fluorinated C 1 -C 4 -alkylthio” refers to a fluorinated C 1 -C 4 -alkyl group, as defined above, attached via a sulfur atom. The term “fluorinated C 1 -C 6 -alkylthio” refers to a fluorinated C 1 -C 6 -alkyl group, as defined above, attached via a sulfur atom. Fluorinated C 1 -C 2 -alkylthio refers to, for example, SCH 2 F, SCHF 2 , SCF 3 , 2-fluoroethylthio, 2,2-difluoroethylthio, 2,2,2-trifluoroethylthio, or SC 2 F 5 . Fluorinated C 1 -C 3 -alkylthio may additionally, for example, include 2-fluoropropylthio, 3-fluoropropylthio, 2,2-difluoropropylthio, 2,3-difluoropropylthio, 3,3,3-trifluoropropylthio, SCH 2 —C 2 F 5 , SCF 2 —C 2 F 5  or 1-(CH 2 F)-2-fluoroethylthio. Fluorinated C 1 -C 4 -alkylthio may additionally, for example, include 4-fluorobutylthio or nonafluorobutylthio. Fluorinated C 1 -C 6 -alkylthio is additionally, for example, 5-fluoropentylthio, undecafluoropentylthio, 6-fluorohexylthio or dodecafluorohexylthio. 
     The term “C 1 -C 2 -alkylsulfinyl” refers to a C 1 -C 2 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. The term “C 1 -C 4 -alkylsulfinyl” is a C 1 -C 4 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. The term “C 1 -C 6 -alkylsulfinyl” is a C 1 -C 6 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. C 1 -C 2 -Alkylsulfinyl is methylsulfinyl or ethylsulfinyl. C 1 -C 4 -Alkylsulfinyl is additionally, for example, n-propylsulfinyl, 1-methylethylsulfinyl (isopropylsulfinyl), butylsulfinyl, 1-methylpropylsulfinyl (sec-butylsulfinyl), 2-methylpropylsulfinyl (isobutylsulfinyl) or 1,1-dimethylethylsulfinyl (tert-butylsulfinyl). C 1 -C 6 -Alkylsulfinyl is additionally, for example, pentylsulfinyl, 1-methylbutylsulfinyl, 2-methylbutylsulfinyl, 3-methylbutylsulfinyl, 1,1-dimethylpropylsulfinyl, 1,2-dimethylpropylsulfinyl, 2,2-dimethylpropylsulfinyl, 1-ethylpropylsulfinyl, hexylsulfinyl, 1-methylpentylsulfinyl, 2-methylpentylsulfinyl, 3-methylpentylsulfinyl, 4-methylpentylsulfinyl, 1,1-dimethylbutylsulfinyl, 1,2-dimethylbutylsulfinyl, 1,3-dimethylbutylsulfinyl, 2,2-dimethylbutylsulfinyl, 2,3-dimethylbutylsulfinyl, 3,3-dimethylbutylsulfinyl, 1-ethylbutylsulfinyl, 2-ethylbutylsulfinyl, 1,1,2-trimethylpropylsulfinyl, 1,2,2-trimethylpropylsulfinyl, 1-ethyl-1-methylpropylsulfinyl or 1-ethyl-2-methylpropylsulfinyl. 
     The term “fluorinated C 1 -C 2 -alkylsulfinyl” refers to a fluorinated C 1 -C 2 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. The term “fluorinated C 1 -C 3 -alkylsulfinyl” refers to a fluorinated C 1 -C 3 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. The term “fluorinated C 1 -C 4 -alkylsulfinyl” refers to a fluorinated C 1 -C 4 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. The term “fluorinated C 1 -C 6 -alkylsulfinyl” refers to a fluorinated C 1 -C 6 -alkyl group, as defined above, attached via a sulfinyl [S(O)] group. Fluorinated C 1 -C 2 -alkylsulfinyl is, for example, S(O)CH 2 F, S(O)CHF 2 , S(O)CF 3 , 2-fluoroethylsulfinyl, 2,2-difluoroethylsulfinyl, 2,2,2-trifluoroethylsulfinyl, or S(O)C 2 F 5 . Fluorinated C 1 -C 3 -alkylsulfinyl may additionally, for example, include 2-fluoropropylsulfinyl, 3-fluoropropylsulfinyl, 2,2-difluoropropylsulfinyl, 2,3-difluoropropylsulfinyl, 3,3,3-trifluoropropylsulfinyl, S(O)CH 2 —C 2 F 5 , S(O)CF 2 —C 2 F 5  or 1-(CH 2 F)-2-fluoroethylsulfinyl. Fluorinated C 1 -C 4 -alkylsulfinyl may additionally, for example, include 4-fluorobutylsulfinyl or nonafluorobutylsulfinyl. Fluorinated C 1 -C 6 -alkylsulfinyl may additionally, for example, include 5-fluoropentylsulfinyl, undecafluoropentylsulfinyl, 6-fluorohexylsulfinyl or dodecafluorohexylsulfinyl. 
     The term “C 1 -C 2 -alkylsulfonyl” refers to a C 1 -C 2 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. The term “C 1 -C 4 -alkylsulfonyl” refers to a C 1 -C 4 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. The term “C 1 -C 6 -alkylsulfonyl” is a C 1 -C 6 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. C 1 -C 2 -Alkylsulfonyl refers to a methylsulfonyl or ethylsulfonyl. C 1 -C 4 -Alkylsulfonyl is additionally, for example, n-propylsulfonyl, 1-methylethylsulfonyl (isopropylsulfonyl), butylsulfonyl, 1-methylpropylsulfonyl (sec-butylsulfonyl), 2-methylpropylsulfonyl (isobutylsulfonyl) or 1,1-dimethylethylsulfonyl (tert-butylsulfonyl). C 1 -C 6 -Alkylsulfonyl is additionally, for example, pentylsulfonyl, 1-methylbutylsulfonyl, 2-methylbutylsulfonyl, 3-methylbutylsulfonyl, 1,1-dimethylpropylsulfonyl, 1,2-dimethylpropylsulfonyl, 2,2-dimethylpropylsulfonyl, 1-ethylpropylsulfonyl, hexylsulfonyl, 1-methylpentylsulfonyl, 2-methylpentylsulfonyl, 3-methylpentylsulfonyl, 4-methylpentylsulfonyl, 1,1-dimethylbutylsulfonyl, 1,2-dimethylbutylsulfonyl, 1,3-dimethylbutylsulfonyl, 2,2-dimethylbutylsulfonyl, 2,3-dimethylbutylsulfonyl, 3,3-dimethylbutylsulfonyl, 1-ethylbutylsulfonyl, 2-ethylbutylsulfonyl, 1,1,2-trimethylpropylsulfonyl, 1,2,2-trimethylpropylsulfonyl, 1-ethyl-1-methylpropylsulfonyl or 1-ethyl-2-methylpropylsulfonyl. 
     The term “fluorinated C 1 -C 2 -alkylsulfonyl” refers to a fluorinated C 1 -C 2 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. The term “fluorinated C 1 -C 3 -alkylsulfonyl” refers to a fluorinated C 1 -C 3 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. The term “fluorinated C 1 -C 4 -alkylsulfonyl” refers to a fluorinated C 1 -C 4 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. The term “fluorinated C 1 -C 6 -alkylsulfonyl” refers to a fluorinated C 1 -C 6 -alkyl group, as defined above, attached via a sulfonyl [S(O) 2 ] group. Fluorinated C 1 -C 2 -alkylsulfonyl is, for example, S(O) 2 CH 2 F, S(O) 2 CHF 2 , S(O) 2 CF 3 , 2-fluoroethylsulfonyl, 2,2-difluoroethylsulfonyl, 2,2,2-trifluoroethylsulfonyl, or S(O) 2 C 2 F 5 . Fluorinated C 1 -C 3 -alkylsulfonyl is additionally, for example, 2-fluoropropylsulfonyl, 3-fluoropropylsulfonyl, 2,2-difluoropropylsulfonyl, 2,3-difluoropropylsulfonyl, 3,3,3-trifluoropropylsulfonyl, S(O) 2 CH 2 —C 2 F5, S(O) 2 CF 2 —C 2 F 5  or 1-(CH 2 F)-2-fluoroethylsulfonyl. Fluorinated C 1 -C 4 -alkylsulfonyl is additionally, for example, 4-fluorobutylsulfonyl or nonafluorobutylsulfonyl. Fluorinated C 1 -C 6 -alkylsulfonyl is additionally, for example, 5-fluoropentylsulfonyl, undecafluoropentylsulfonyl, 6-fluorohexylsulfonyl or dodecafluorohexylsulfonyl. 
     C 1 -C 4 -Alkylcarbonyl refers to a straight-chain or branched alkyl group having from 1 to 4 carbon atoms), which is bound to the remainder of the molecule via a carbonyl group (CO), such as in acetyl, propionyl, isopropylcarbonyl, butylcarbonyl, sec-butylcarbonyl, isobutylcarbonyl, and tert-butylcarbonyl. C 1 -C 6 -Alkylcarbonyl is a straight-chain or branched alkyl group having from 1 to 6 carbon atoms, which is bound to the remainder of the molecule via a carbonyl group (CO). Examples include, apart those listed above for C 1 -C 4 -alkylcarbonylpentylcarbonyl, hexylcarbonyl and the constitutional isomers thereof. 
     Fluorinated C 1 -C 4 -alkylcarbonyl refers to a straight-chain or branched fluorinated alkyl group having from 1 to 4 carbon atoms as defined above, which is bound to the remainder of the molecule via a carbonyl group (CO). Fluorinated C 1 -C 6 -alkylcarbonyl is a straight-chain or branched fluorinated alkyl group having from 1 to 6 carbon atoms as defined above, which is bound to the remainder of the molecule via a carbonyl group (CO). Examples include trifluoromethylcarbonyl, 2,2,2-trifluoroethylcarbonyl and the like. 
     C 3 -C 6 -cycloalkylcarbonyl relates to a C 3 -C 6 -cycloalkyl group as defined above which is bound to the remainder of the molecule via a carbonyl group (CO), such as in cyclopropylcarbonyl, cyclobutylcarbonyl, cyclopentylcarbonyl and cyclohexylcarbonyl. 
     C 1 -C 6 -Alkoxycarbonyl refers to a straight-chain or branched alkoxy group having from 1 to 6, especially 1 to 4 carbon atoms (═C 1 -C 4 -alkoxycarbonyl), in particular 1 to 3 carbon atoms (═C 1 -C 3 -alkoxycarbonyl), which is bound to the remainder of the molecule via a carbonyl group (CO), such as in methoxycarbonyl, ethoxycarbonyl, propyloxycarbonyl, and isopropyloxycarbonyl. 
     Fluorinated C 1 -C 6 -alkoxycarbonyl refers to a straight-chain or branched fluorinated alkoxy group having from 1 to 6, especially 1 to 4 carbon atoms (=fluorinated C 1 -C 4 -alkoxycarbonyl), in particular 1 to 3 carbon atoms (=fluorinated C 1 -C 3 -alkoxycarbonyl) as defined above, which is bound to the remainder of the molecule via a carbonyl group (CO). Examples include trifluoromethoxycarbonyl, 2,2,2-trifluoroethoxycarbonyl and the like. 
     C 1 -C 4 -Alkylcarbonyloxy refers to a straight-chain or branched alkyl group having from 1 to 4 carbon atoms, which is bound to the remainder of the molecule via a carbonyloxy group [C(O)—O—], such as in acet(yl)oxy, propionyloxy, isopropylcarbonyloxy, butylcarbonyloxy, sec-butylcarbonyloxy, isobutylcarbonyloxy, and tert-butylcarbonyloxy. C 1 -C 6 -Alkylcarbonyloxy is a straight-chain or branched alkyl group having from 1 to 6 carbon atoms, which is bound to the remainder of the molecule via a carbonyloxy group [C(O—O—]. Examples include, apart those listed above for C 1 -C 4 -alkylcarbonyloxy, pentylcarbonyloxy, hexylcarbonyloxy and the constitutional isomers thereof. 
     Fluorinated C 1 -C 4 -alkylcarbonyloxy refers to a straight-chain or branched fluorinated alkyl group having from 1 to 4 carbon atoms as defined above, which is bound to the remainder of the molecule via a carbonyloxy group [C(O)—O—]. Fluorinated C 1 -C 6 -alkylcarbonyloxy is a straight-chain or branched fluorinated alkyl group having from 1 to 6 carbon atoms as defined above, which is bound to the remainder of the molecule via a carbonyloxy group [C(O)—O—]. Examples include trifluoromethylcarbonyloxy, 2,2,2-trifluoroethylcarbonyloxy and the like. 
     Phenyl-C 1 -C 2 -alkyl is a phenyl group bound to the remainder of the molecule via a C 1 -C 2 -alkyl group. Examples are benzyl, 1-phenylethyl and 2-phenylethyl (phenethyl). 
     The term “3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members” denotes a 3-, 4-, 5-, 6-, 7- or 8-membered, preferably a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximum unsaturated heteromonocyclic ring containing 1, 2, 3 or 4 (preferably 1, 2 or 3) heteroatoms or heteroatom groups selected from N, O, S, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members. 
     Unsaturated rings contain at least one C—C and/or C—N and/or N—N double bond(s). Maximally unsaturated rings contain as many conjugated C—C and/or C—N and/or N—N double bonds as allowed by the ring size. Maximally unsaturated 5- or 6-membered heterocyclic rings are aromatic. 7- and 8-membered rings cannot be aromatic. They are homoaromatic (7-membered ring, 3 double bonds) or have 4 double bonds (8-membered ring). Partially unsaturated rings contain less than the maximum number of C—C and/or C—N and/or N—N double bond(s) allowed by the ring size. The heterocyclic ring may be attached to the remainder of the molecule via a carbon ring member or via a nitrogen ring member. As a matter of course, the heterocyclic ring contains at least one carbon ring atom. If the ring contains more than one O ring atom, these are not adjacent. 
     Examples of a 3-, 4-, 5-, 6- or 7-membered saturated heterocyclic ring include: Oxiranyl, thiiranyl, aziridinyl, oxetanyl, thietanyl, azetidinyl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydrofuran-2-on-3-yl, tetrahydrofuran-2-on-4-yl, tetrahydrofuran-2-on-5-yl, tetrahydrofuran-2-thion-3-yl, tetrahydrofuran-2-thion-4-yl, tetrahydrofuran-2-thion-5-yl, tetrahydrothien-2-yl, tetrahydrothien-3-yl, tetrahydrothien-2-on-3-yl, tetrahydrothien-2-on-4-yl, tetrahydrothien-2-on-5-yl, tetrahydrothien-2-thion-3-yl, tetrahydrothien-2-thion-4-yl, tetrahydrothien-2-thion-5-yl, pyrrolidin-1-yl, pyrrolidine-2-on-1-yl, pyrrolidine-2,5-dion-1-yl, pyrrolidine-2-thion-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, pyrrolidine-2-on-3-yl, pyrrolidine-2-on-4-yl, pyrrolidine-2-on-5-yl, pyrrolidine-2,5-dion-3-yl, pyrrolidine-2-thion-3-yl, pyrrolidine-2-thion-4-yl, pyrrolidine-2-thion-5-yl, pyrazolidin-1-yl, pyrazolidin-3-yl, pyrazolidin-4-yl, pyrazolidin-5-yl, imidazolidin-1-yl, imidazolidin-2-on-1-yl, imidazolidin-2-thion-1-yl, imidazolidin-2-yl, imidazolidin-4-yl, imidazolidin-2-on-4-yl, imidazolidin-2-thion-4-yl, oxazolidin-2-yl, oxazolidin-3-yl, oxazolidin-4-yl, oxazolidin-5-yl, isoxazolidin-2-yl, isoxazolidin-3-yl, isoxazolidin-4-yl, isoxazolidin-5-yl, thiazolidin-2-yl, thiazolidin-3-yl, thiazolidin-4-yl, thiazolidin-5-yl, isothiazolidin-2-yl, isothiazolidin-3-yl, isothiazolidin-4-yl, isothiazolidin-5-yl, 1,2,4-oxadiazolidin-3-yl, 1,2,4-oxadiazolidin-5-yl, 1,2,4-thiadiazolidin-3-yl, 1,2,4-thiadiazolidin-5-yl, 1,2,4-triazolidin-3-yl, 1,3,4-oxadiazolidin-2-yl, 1,3,4-thiadiazolidin-2-yl, 1,3,4-triazolidin-1-yl, 1,3,4-triazolidin-2-yl, 2-tetrahydropyranyl, 4-tetrahydropyranyl, 1,3-dioxan-5-yl, 1,4-dioxan-2-yl, piperidin-1-yl, piperidin-2-on-1-yl, piperidin-2,5-dion-1-yl, piperidine-2-thion-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-2-on-3-yl, piperidin-2,5-dion-3-yl, piperidin-2-thion-3-yl, piperidin-4-yl, hexahydropyridazin-3-yl, hexahydropyridazin-4-yl, hexahydropyrimidin-2-yl, hexahydropyrimidin-4-yl, hexahydropyrimidin-5-yl, piperazin-1-yl, piperazin-2-yl, 1,3,5-hexahydrotriazin-1-yl, 1,3,5-hexahydrotriazin-2-yl and 1,2,4-hexahydrotriazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, thiomorpholin-2-yl, thiomorpholin-3-yl, thiomorpholin-4-yl, 1-oxothiomorpholin-2-yl, 1-oxothiomorpholin-3-yl, 1-oxothiomorpholin-4-yl, 1,1-dioxothiomorpholin-2-yl, 1,1-dioxothiomorpholin-3-yl, 1,1-dioxothiomorpholin-4-yl, azepan-1-, -2-, -3- or -4-yl, oxepan-2-, -3-, -4- or -5-yl, hexahydro-1,3-diazepinyl, hexahydro-1,4-diazepinyl, hexahydro-1,3-oxazepinyl, hexahydro-1,4-oxazepinyl, hexahydro-1,3-dioxepinyl, hexahydro-1,4-dioxepinyl and the like. 
     Examples of a 3-, 4-, 5-, 6-, 7- or 8-membered saturated heterocyclic ring further include oxocane, thiocane, azocane, [1,3]diazocane, [1,4]diazocane, [1,5]diazocane, [1,5]oxazocane and the like. 
     Examples of a 3-, 4-, 5-, 6- or 7-membered partially unsaturated heterocyclic ring include: 2,3-dihydrofur-2-yl, 2,3-dihydrofur-3-yl, 2,4-dihydrofur-2-yl, 2,4-dihydrofur-3-yl, 2,3-dihydrothien-2-yl, 2,3-dihydrothien-3-yl, 2,4-dihydrothien-2-yl, 2,4-dihydrothien-3-yl, 2-pyrrolin-2-yl, 2-pyrrolin-3-yl, 3-pyrrolin-2-yl, 3-pyrrolin-3-yl, 2-isoxazolin-3-yl, 3-isoxazolin-3-yl, 4-isoxazolin-3-yl, 2-isoxazolin-4-yl, 3-isoxazolin-4-yl, 4-isoxazolin-4-yl, 2-isoxazolin-5-yl, 3-isoxazolin-5-yl, 4-isoxazolin-5-yl, 2-isothiazolin-3-yl, 3-isothiazolin-3-yl, 4-isothiazolin-3-yl, 2-isothiazolin-4-yl, 3-isothiazolin-4-yl, 4-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-5-yl, 4-isothiazolin-5-yl, 2,3-dihydropyrazol-1-yl, 2,3-dihydropyrazol-2-yl, 2,3-dihydropyrazol-3-yl, 2,3-dihydropyrazol-4-yl, 2,3-dihydropyrazol-5-yl, 3,4-dihydropyrazol-1-yl, 3,4-dihydropyrazol-3-yl, 3,4-dihydropyrazol-4-yl, 3,4-dihydropyrazol-5-yl, 4,5-dihydropyrazol-1-yl, 4,5-dihydropyrazol-3-yl, 4,5-dihydropyrazol-4-yl, 4,5-dihydropyrazol-5-yl, 2,3-dihydrooxazol-2-yl, 2,3-dihydrooxazol-3-yl, 2,3-dihydrooxazol-4-yl, 2,3-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4-dihydrooxazol-3-yl, 3,4-dihydrooxazol-4-yl, 3,4-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4-dihydrooxazol-3-yl, 3,4-dihydrooxazol-4-yl, 2-, 3-, 4-, 5- or 6-di- or tetrahydropyridinyl, 3-di- or tetrahydropyridazinyl, 4-di- or tetrahydropyridazinyl, 2-di- or tetrahydropyrimidinyl, 4-di- or tetrahydropyrimidinyl, 5-di- or tetrahydropyrimidinyl, di- or tetrahydropyrazinyl, 1,3,5-di- or tetrahydrotriazin-2-yl, 1,2,4-di- or tetrahydrotriazin-3-yl, 2,3,4,5-tetrahydro[1H]azepin-1-, -2-, -3-, -4-, -5-, -6- or -7-yl, 3,4,5,6-tetrahydro[2H]azepin-2-, -3-, -4-, -5-, -6- or -7-yl, 2,3,4,7-tetrahydro[1H]azepin-1-, -2-, -3-, -4-, -5-, -6- or -7-yl, 2,3,6,7-tetrahydro[1H]azepin-1-, -2-, -3-, -4-, -5-, -6- or -7-yl, tetrahydrooxepinyl, such as 2,3,4,5-tetrahydro[1H]oxepin-2-, -3-, -4-, -5-, -6- or -7-yl, 2,3,4,7-tetrahydro[1H]oxepin-2-, -3-, -4-, -5-, -6- or -7-yl, 2,3,6,7-tetrahydro[1H]oxepin-2-, -3-, -4-, -5-, -6- or -7-yl, tetrahydro-1,3-diazepinyl, tetrahydro-1,4-diazepinyl, tetrahydro-1,3-oxazepinyl, tetrahydro-1,4-oxazepinyl, tetrahydro-1,3-dioxepinyl and tetrahydro-1,4-dioxepinyl. 
     Examples of a 3-, 4-, 5-, 6-, 7- or 8-membered partially unsaturated heterocyclic ring further include 1,2,3,4,5,6-hexahydroazocine, 2,3,4,5,6,7-hexahydroazocine, 1,2,3,4,5,8-hexahydroazocine, 1,2,3,4,7,8-hexahydroazocine, 1,2,3,4,5,6-hexahydro-[1,5]diazocine,1,2,3,4,7,8-hexahydro-[1,5]diazocine and the like. 
     Examples of a 3-, 4-, 5-, 6- or 7-membered maximally unsaturated (including aromatic) heterocyclic ring include 5- or 6-membered heteroaromatic rings, such as 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 1-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl, 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 1-imidazolyl, 2-imidazolyl, 4-imidazolyl, 1,3,4-triazol-1-yl, 1,3,4-triazol-2-yl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 1-oxopyridin-2-yl, 1-oxopyridin-3-yl, 1-oxopyridin-4-yl, 3-pyridazinyl, 4-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl and 2-pyrazinyl, and also homoaromatic radicals, such as 1H-azepine, 1H-[1,3]-diazepine and 1H-[1,4]-diazepine. 
     Examples of a 3-, 4-, 5-, 6-, 7- or 8-membered maximally unsaturated heterocyclic ring further include [1,3]diazocine, [1,5]diazocine and [1,5]diazocine. 
     A 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members is either saturated, partially unsaturated and carbocyclic (if it contains only C═O and/or C═S as heteroatom group and no further heteroatoms or heteroatom groups) or saturated, partially unsaturated or maximally unsaturated heterocyclic. Examples are, in addition to the heterocyclic rings mentioned above, carbocyclic rings, such as cyclopropanonyl, cyclobutanonyl, cyclopentanonyl, cyclohexanonyl, cyclohexandionyl, cycloheptanonyl, cyclooctanonyl, cyclopropanthionyl, cyclobutanthionyl, cyclopentanthionyl, cyclohexanthionyl, cyclohexandithionyl, cycloheptanthionyl, cyclooctanthionyl, cyclopropenonyl, cyclopentenonyl, cyclohexenonyl and the like. 
     The remarks made above and in the following with respect to preferred aspects of the invention, e.g. to preferred meanings of the variables R 1 , R 2 , R 3a , R 3b , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , a, b and n of compounds I, to preferred compounds I and to preferred embodiments of the method or the use according to the invention, apply in each case on their own or in particular to combinations thereof. 
     In a preferred embodiment, R 1  is selected from hydrogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, —C(═O)R 10 , phenyl and benzyl, where the phenyl moiety in the two last-mentioned radicals may carry 1, 2 or 3 radicals R 11 , where R 10  and R 11  have one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     In the above group —C(═O)R 10  as a meaning for R 1 , R 10  is preferably selected from C 1 -C 4 -alkyl and C 1 -C 4 -alkoxy and more preferably from C 1 -C 2 -alkyl and tert-butoxy. 
     More preferably, R 1  is selected from hydrogen and C 1 -C 6 -alkyl, in particular from hydrogen and methyl, and is specifically hydrogen. 
     In a preferred embodiment, R 2  is selected from cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, more preferably from C 1 -C 6 -alkyl, in particular from methyl, ethyl, propyl and isopropyl, more particularly from methyl and ethyl, and is specifically methyl. 
     In a preferred embodiment, R 3a  and R 3b , independently of each other, are selected from hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy. More preferably, R 3a  is selected from hydrogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, and R 3b  is hydrogen. Even more preferably, R 3a  is selected from hydrogen and methyl and R 3b  is hydrogen. In particular, both R 3a  and R 3b  are hydrogen. 
     In a preferred embodiment, R 4a  and R 4b , independently of each other, are selected from hydrogen, C 1 -C 6 -alkyl and fluorinated C 1 -C 6 -alkyl or form together a group ═O. 
     More preferably, they are hydrogen or form together a group ═O. In another embodiment, one of R 4a  and R 4b  is hydrogen and the other is methyl; especially if X is CR 7 R 8 . In particular, both R 4a  and R 4b  are hydrogen. 
     In a preferred embodiment,
     R 5a  is selected from hydrogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy; and in case that X is CR 7 R 8  is further selected from halogen; or   R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; and   R 5b  is selected from hydrogen and deuterium and is preferably hydrogen; where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.   

     More preferably,
     R 5a  is selected from hydrogen, C 1 -C 6 -alkyl and fluorinated C 1 -C 6 -alkyl; and in case that
       X is CR 7 R 8  is further selected from halogen; and is preferably selected from hydrogen and methyl, or   R 5a  and R 6  form together a group (CH 2 ) r , where r is 2, 3, 4 or 5, preferably 2, 3 or 4; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3, 4 or 5, preferably 2, 3 or 4; and   
       R 5b  is selected from hydrogen and deuterium and is preferably hydrogen.   

     In an alternative more preferred embodiment,
     R 5a  is selected from hydrogen, C 1 -C 6 -alkyl and fluorinated C 1 -C 6 -alkyl; and in case that
       X is CR 7 R 8  is further selected from halogen; and is preferably selected from hydrogen and methyl, or   R 5a  and R 6  form together a group (CH 2 ) r , where r is 2, 3, 4 or 5, where two hydrogen atoms bound to adjacent CH 2  groups may be replaced by two radicals   R 11 , where the two radicals R 11  form together a group (CH 2 ) t , where t is 1, 2, 3, 4 or 5, preferably 1, 2 or 3; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3, 4 or 5, preferably 2, 3 or 4; and   
       R 5b  is selected from hydrogen and deuterium and is preferably hydrogen.   

     In particular,
     R 5a  is hydrogen; and in case that X is CR 7 R 8 , is selected from hydrogen and methyl and is in particular hydrogen; or
       R 5a  and R 6  form together a group (CH 2 ) r , where r is 3, 4 or 5, where two hydrogen atoms bound to adjacent CH 2  groups may be replaced by two radicals R 11 , where the two radicals R 11  form together a group (CH 2 ) t , where t is 1, 2, 3, 4 or 5, preferably 1, 2 or 3 and specifically 1; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3 or 4, in particular 3; and   
       R 5b  is hydrogen.   

     In an alternatively preferred embodiment, R 5a  and R 5b , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; and form in particular a 5- or 6-membered saturated or partially unsaturated carbocyclic ring, and where the ring may be substituted with one or more substituents R 11 . 
     In one embodiment, X is NR 6 , where R 6  has one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     Preferably, R 6  is selected from the group consisting of hydrogen, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, —C(═O)R 10 , —SO 2 R 10 , phenyl and benzyl, where the phenyl moiety in the two last-mentioned radicals may carry 1, 2 or 3 radicals R 11 ; or
     R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;
 
where R 10  and R 11  have one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     In the above group —C(═O)R 10 , R 6 , R 10  is preferably selected from C 1 -C 4 -alkyl and C 1 -C 4 -alkoxy and more preferably from C 1 -C 2 -alkyl and tert-butoxy. 
     In the above group —SO 2 R 10 , R 6 , R 10  is preferably selected from C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl and phenyl, where phenyl may be substituted with 1, 2, 3, 4 or 5, preferably 1, 2 or 3, in particular 1, radicals R 11 , where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     In one more preferred embodiment, R 6  is —SO 2 R 10 , where R 10  has one of the general meanings given above or is preferably selected from C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl and phenyl, where phenyl may be substituted with 1, 2, 3, 4 or 5, preferably 1, 2 or 3, in particular 1, radicals R 11 , where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     In another preferred embodiment, R 6  is selected from hydrogen, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, fluorinated C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, fluorinated C 1 -C 4 -alkoxy, —C(═O)R 10 , where R 10  is selected from C 1 -C 6 -alkyl and C 3 -C 6 -cycloalkyl; phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 . 
     In another preferred embodiment, R 6  is selected from C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, fluorinated C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, phenyl, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 . 
     In a more preferred embodiment, R 6  is phenyl-C 1 -C 2 -alkyl, and in particular benzyl. 
     In another more preferred embodiment, R 6  is selected from C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl and fluorinated C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, and in particular from C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-methyl and fluorinated C 3 -C 6 -cycloalkyl-methyl. 
     In another more preferred embodiment, R 6  is a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  and optionally also 1 or 2 C═O and/or C═S groups as ring members, where the cyclic moieties in the three last-mentioned radicals may be substituted with one or more substituents R 11 . Even more preferably, R 6  is a 3-, 4- or 5-membered saturated heterocyclic ring containing 1 or 2 heteroatoms independently selected from N, O and S, where the heterocyclic ring may be substituted with one or two substituents selected from halogen and C 1 -C 4 -alkyl, and is in particular oxetanyl which may carry one or two substituents selected from halogen and C 1 -C 4 -alkyl and especially from F. 
     In another more preferred embodiment, R 6  is selected from hydrogen, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 -cycloalkylcarbonyl, C 1 -C 4 -alkoxy, fluorinated C 1 -C 4 -alkoxy, phenyl-C 1 -C 2 -alkyl and a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1 or 2 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  as ring members; and is in particular selected from C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, and a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1 or 2 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  as ring members, where the saturated heterocyclic ring preferably contains 1 heteroatom selected from O and S as ring member. Specifically, R 6  is selected from C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl and oxetanyl and very specifically from ethyl, n-propyl, cyclopropyl, cyclobutyl and 3-oxetanyl. 
     In another more preferred embodiment, R 5a  and R 6 , together with the atoms they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; 
     where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     In particular, R 5a  and R 6  form together a group (CH 2 ) r , where r is 2, 3, 4 or 5, preferably 2, 3 or 4 or, in particular, 3, 4 or 5. Alternatively, R 5a  and R 6  form together a group (CH 2 ) r , where r is 2, 3, 4 or 5 and in particular 3, 4 or 5, where two hydrogen atoms bound to adjacent CH 2  groups may be replaced by two radicals R 11 , where the two radicals R 11  form together a group (CH 2 ) t , where t is 1, 2, 3, 4 or 5, in particular 1, 2 or 3 and specifically 1. 
     In an alternative embodiment, X is CR 7 R 8 , where R 7  and R 8  have one of the general meanings given above, or, in particular, one of the preferred meanings given below. 
     In case that R 7  and R 8 , together with the carbon atom they are bound to, form a ring, this ring is spiro-bound to the carbon atom carrying R 7  and R 8 . 
     Preferably,
     R 7  and R 8 , independently of each other, are selected from the group consisting of halogen, cyano, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, fluorinated C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 6 -hydroxyalkoxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylthio, fluorinated C 1 -C 6 -alkylthio, C 1 -C 6 -alkylsulfinyl, fluorinated C 1 -C 6 -alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 -alkylsulfonyl, —NR 12a R 12b , —CH 2 NR 12a R 12b ,
       —NR 12a C(O)R 10 , —C(═O)R 10 , SO 2 NR 12a R 12b , C 1 -C 6 -alkylcarbonyloxy, fluorinated C 1 -C 6 -alkylcarbonyloxy, phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, phenylsulfonyl, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the six last-mentioned radicals may be substituted with one or more substituents R 11 ; or   
       R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;
 
in which case R 8  has one of the above meanings or is deuterium;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     More preferably,
     R 7  and R 8 , independently of each other, are selected from halogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, phenyl, phenyl-C 1 -C 2 -alkyl, benzyloxy and a 3-, 4-, 5- or 6-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the four last-mentioned radicals may be substituted with one or more substituents R 11 ; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7 , together with the carbon atoms they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents R 11 ;
 
in which case R 8  has one of the above meanings or is deuterium; and
   R 5b  is selected from hydrogen and deuterium and is preferably hydrogen;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     Even more preferably,
     R 7  and R 8 , independently of each other, are selected from halogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl and phenyl, or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5  and R 7  form together a group (CH 2 ) s , where s is 2, 3, 4 or 5, preferably 2, 3 or 4; in which case R 8  has one of the above meanings or is deuterium; and   R 5b  is selected from hydrogen and deuterium and is preferably hydrogen;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     In particular,
     R 8  is selected from halogen, cyano, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl and phenyl; and   R 7  is selected from C 1 -C 6 -alkyl and fluorinated C 1 -C 6 -alkyl, preferably from methyl and CF 3  and is in particular methyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3, 4 or 5, preferably 2, 3 or 4;
 
in which case R 8  has one of the above meanings or is deuterium; and
   R 5b  is selected from hydrogen and deuterium and is preferably hydrogen;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     In an alternative particular embodiment,
     R 7  is C 1 -C 6 -alkyl and is in particular methyl;   R 8  is selected from hydroxyl, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy and phenyl and in particular from C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, fluorinated C 1 -C 4 -alkoxy and phenyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3 or 4 and where R 8  is methyl; and   R 5b  is hydrogen.   

     Specifically,
     R 8  is selected from C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl and phenyl and specifically from methyl, CF 3  and phenyl; and   R 7  is methyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5- or 6-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 3 or 4, specifically 3;
 
in which case R 8  is selected from methyl and deuterium; and
   R 5b  is selected from hydrogen and deuterium and is specifically hydrogen;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     In an alternative specific embodiment,
     R 7  is methyl;   R 8  is selected from hydroxyl, methyl, ethyl, CF 3 , methoxy and phenyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5- or 6-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 2, 3 or 4 and in particular and where R 8  is methyl; and   R 5b  is hydrogen.   

     Very specifically,
     R 8  is selected from methyl, CF 3  and phenyl; and   R 7  is methyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 4, 5- or 6-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or form a 3-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ; or   R 5a  and R 7  form together a group (CH 2 ) s , where s is 3 or 4, specifically 3;
 
in which case R 8  is selected from methyl and deuterium and in particular methyl; and
   R 5b  is selected from hydrogen and deuterium and is specifically hydrogen;
 
where R 11  has one of the general meanings given above, or, in particular, one of the preferred meanings given below.
   

     In one particular embodiment, the ring formed by R 7  and R 8  together with the carbon atom they are bound to is a carbocyclic ring, preferably a saturated or partially unsaturated carbocyclic ring, in particular a saturated carbocyclic ring. 
     If R 7  and R 8 , together with the carbon atom they are bound to, form a carbocyclic ring, this is particularly preferably a 4- or 5-membered saturated carbocyclic ring (i.e. 
     R 7  and R 8  form together a group —(CH 2 ) 3 - or —(CH 2 ) 4 -) and in particular a 4-membered saturated carbocyclic ring (i.e. R 7  and R 8  form together a group —(CH 2 ) 3 -), where the ring may be substituted with one or more substituents R 11 . Specifically, the ring is not substituted. Alternatively, the carbocyclic ring is 3-membered (i.e. R 7  and R 8  form together a group —(CH 2 ) 2 —)—), where the ring may be substituted with one or more substituents R 11 . Specifically, the ring is not substituted. 
     In an alternative particular embodiment, the ring formed by R 7  and R 8  together with the carbon atom they are bound to is a heterocyclic ring containing 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from O, S, N, SO and SO 2  as ring members, preferably containing 1 or 2 heteroatoms or heteroatom-containing groups selected from O, S, N, SO and SO 2  as ring members. Preferably, the heterocyclic ring is 3-, 4-, 5- or 6-membered and saturated and may carry one or more substituents R 11 . In particular, the heterocyclic ring is oxetanyl which may carry one or more substituents R 11 . 
     Specifically, R 7  and R 8 , together with the carbon atom they are bound to, form a 3- or 4-membered saturated carbocyclic ring (i.e. R 7  and R 8  form together a group —(CH 2 ) 2 — or —(CH 2 ) 3 —) and in particular a 4-membered saturated carbocyclic ring (i.e. R 7  and R 8  form together a group —(CH 2 ) 3 —); the ring not being substituted. 
     In a preferred embodiment, each R 9  is independently selected from halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy and a 3-, 4-, 5- or 6-membered saturated heterocyclic ring containing 1 or 2 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO and SO 2  as ring members, where the heterocyclic ring may be substituted with one or more substituents R 11 . The heterocyclic ring is specifically oxetanyl. 
     More preferably, each R 9  is independently selected from halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, even more preferably from halogen, cyano, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy and fluorinated C 1 -C 4 -alkoxy, and is in particular selected from halogen, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl and C 1 -C 6 -alkoxy, more particularly from halogen, C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy, and is specifically halogen, especially F or Cl, and more specifically F. 
     In case that X is NR 6 , in alternatively more preferred embodiment, each R 9  is independently selected from halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, fluorinated C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, even more preferably from halogen, C 1 -C 6 -alkyl and C 3 -C 6 -cycloalkyl, and in particular from halogen and C 1 -C 6 -alkyl. 
     In a preferred embodiment, R 10  is selected from hydrogen, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 3 -C 8 -cycloalkyl, fluorinated C 3 -C 8 -cycloalkyl, C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, —NR 12a R 12b , —CH 2 NR 12a R 12b , phenyl, phenyl-C 1 -C 2 -alkyl, phenoxy, benzyloxy and a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring containing 1, 2, 3 or 4 heteroatoms or heteroatom groups independently selected from N, O, S, NO, SO, SO 2 , C═O and C═S as ring members, where the cyclic moieties in the five last-mentioned radicals may be substituted with one or more substituents R 11 , where R 11 , R 12a  and R 12b  have one of the general meanings given above, or, in particular, one of the preferred meanings given below. More preferably, R 10  is selected from hydrogen, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, and even more preferably from C 1 -C 4 -alkyl and C 1 -C 4 -alkoxy. In particular, R 10  is selected from C 1 -C 2 -alkyl and tert-butoxy. 
     In a preferred embodiment, each R 11  is independently selected from halogen, cyano, nitro, hydroxy, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy, and is in particular halogen or C 1 -C 4 -alkyl. Alternatively, two radicals R 11  bound on adjacent ring atoms form together a group (CH 2 ) t , where t is 1, 2, 3, 4 or 5 and in particular 1, 2 or 3. 
     In a preferred embodiment, R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from hydrogen, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkylcarbonyl, fluorinated C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, phenyl and benzyl, where the phenyl moieties in the two last-mentioned radicals may carry 1, 2 or 3 substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy; or, 
     if R 12a  and R 12b  are bound to the same nitrogen atom, together with this nitrogen atom may form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the ring may further contain 1 or 2 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2 , C═O and C═S as ring members, and where the ring may be substituted with one or more substituents selected from halogen, cyano nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy and fluorinated C 1 -C 6 -alkoxy. 
     More preferably, R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from hydrogen, C 1 -C 6 -alkyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl and benzyl, where the phenyl moiety in the last-mentioned radical may carry 1, 2 or 3 substituents selected from halogen, cyano nitro, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy and fluorinated C 1 -C 4 -alkoxy; or, if R 12a  and R 12b  are bound to the same nitrogen atom, together with this nitrogen atom may form a 5- or 6-membered saturated or aromatic heterocyclic ring, where the ring may further contain 1 or 2 heteroatoms or heteroatom-containing groups selected from O, S, N, SO, SO 2  and C═O as ring members, and where the ring may be substituted with 1 or 2 substituents selected from halogen, cyano nitro, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy and fluorinated C 1 -C 4 -alkoxy. 
     In particular, R 12a  and R 12b , independently of each other and independently of each occurrence, are selected from hydrogen and C 1 -C 6 -alkyl. 
     In a preferred embodiment, a is 0 or 1 and in particular 0. 
     In a particular embodiment, a is 1 and R 2  is bound in 3-position to the nitrogen ring atom carrying R 1  (this is for the example the position of R 2b  in below formula I.2). 
     In a preferred embodiment, b is 0, 1 or 2 and in particular 0 or 1. 
     In a preferred embodiment, n is 1. 
     In a particular embodiment, the compound of formula I is a compound of formula I.1 
     
       
         
         
             
             
         
       
     
     wherein X, R 5a , R 5b , R 9  and b have one of the above general, or, in particular, one of the above preferred meanings. 
     In a specific embodiment, the compound of formula I is a compound of formula I.1.1 
     
       
         
         
             
             
         
       
     
     wherein
     R 9a  is selected from H, halogen, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl and fluorinated C 3 -C 6 -cycloalkyl, especially from H or F; and   R 5a , R 5b , R 6 , R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In another specific embodiment, the compound of formula I is a compound of formula I.1.2 
     
       
         
         
             
             
         
       
     
     wherein
     R 7  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl;   R 8  is selected from C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, fluorinated C 1 -C 4 -alkoxy and phenyl; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7-membered, in particular a 3- or 4-membered saturated or partially unsaturated ring, especially a saturated carbocyclic ring, where the ring may be substituted with one or more substituents R 11 , and form especially a 3- or 4-membered saturated carbocyclic ring;   R 9a  is H, Cl, F or methyl, especially H, Cl or F; and   R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In an alternative embodiment, in compounds I.1.2,
     R 7  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl, preferably from methyl and CF 3 , and is in particular methyl;   R 8  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl, and preferably from methyl and CF 3 ; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 , and form preferably a 5- or 6-membered saturated or partially unsaturated ring;   R 9a  is H or F; and   R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In another specific embodiment, the compound of formula I is a compound of formula I.1.3 
     
       
         
         
             
             
         
       
     
     wherein R 8  is selected from deuterium, F, Cl, CN and CH 3 , in particular from deuterium, F, Cl and CN. 
     Among these, preference is given to the trans compounds, i.e. of formula I.1.3-trans: 
     
       
         
         
             
             
         
       
     
     wherein R 8  is selected from deuterium, F, Cl, CN and CH 3 , in particular from deuterium, F, Cl and CN. 
     In another particular embodiment, the compound of formula I is a compound of formula I.2 
     
       
         
         
             
             
         
       
     
     wherein X, R 5a , R 5b , R 9  and b have one of the above general, or, in particular, one of the above preferred meanings. 
     In another particular embodiment, the compound of formula I is a compound of formula I.2.1 
     
       
         
         
             
             
         
       
     
     wherein
     R 2a , R 2b  and R 3a , independently of each other, are selected from hydrogen and methyl; and where in particular at most one of R 2a , R 2b  and R 3a  is methyl;   R 9a  is selected from H, halogen, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 3 -C 6 -cycloalkyl and fluorinated C 3 -C 6 -cycloalkyl; and   R 5a , R 5b , R 6 , R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In particular, in compounds I.2.1,
     R 9a  is H or F; and   R 5a , R 5b , R 6 , R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In particular, in compounds 1.2.1, R 2b  is methyl and R 2a  and R 3a  are hydrogen. 
     In another particular embodiment, the compound of formula I is a compound of formula I.2.2 
     
       
         
         
             
             
         
       
     
     wherein
     R 2a , R 2b , R 3a  and R 5a , independently of each other, are selected from hydrogen, methyl and ethyl, in particular from hydrogen and methyl;   R 7  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl, in particular from methyl and CF 3 , and is especially methyl;   R 8  is selected from C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, fluorinated C 1 -C 4 -alkoxy and phenyl; and in particular from methyl and CF 3 ; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7-membered, in particular a 3- or 4-membered saturated or partially unsaturated, especially a saturated carbocyclic ring, ring, where the ring may be substituted with one or more substituents R 11 , and form especially a 3- or 4-membered saturated carbocyclic ring;   R 9a  is H, Cl, F or methyl, especially H, Cl or F; and   R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In particular, in compound 1.2.2,
     R 2a , R 2b , R 3a  and R 5a , independently of each other, are selected from hydrogen and methyl;   R 7  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl, preferably from methyl and CF 3 , and is in particular methyl;   R 8  is selected from C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl, and preferably from methyl and CF 3 ; or   R 7  and R 8 , together with the carbon atom they are bound to, form a 3-, 4-, 5-, 6- or 7-membered saturated or partially unsaturated ring, where the ring may be substituted with one or more substituents R 11 ;   R 9a  is H or F; and   R 9  and b have one of the above general, or, in particular, one of the above preferred meanings.   

     In particular, in compound 1.2.2, R 2b  is methyl and R 2a , R 3a  and R 5a  are hydrogen. In the above formulae I.1.1, I.1.2, I.2.1 and I.2.2, (b-1) is preferably 0. 
     Preferably, in the above formulae I.1.2, I.2.1 and I.2.2, R 2a , R 2b , R 3a  and R 5a  are selected from hydrogen and methyl, with the proviso that at most two, preferably at most one, of the substituents R 2a , R 2b , R 3a  and R 5a  are methyl. In particular, R 2b  is hydrogen and R 2a , R 3a  and R 5a  are selected from hydrogen and methyl, with the proviso that at most two, preferably at most one, of the substituents R 2a , R 3a  and R 5a  are methyl. However, more particularly, R 2b  is hydrogen or methyl, especially methyl, and R 2a , R 3a  and R 5a  are hydrogen (if the latter does not form a ring together with R 6  or R 7  and the atoms they are bond to). 
     Preferably, in the above formulae I.2, I.2.1 and I.2.2, R 7  and R 8 , together with the carbon atom they are bound to, form a 3, 4-, 5- or 6-membered saturated or partially unsaturated carbocyclic ring, preferably a 3, 4- or 5-membered saturated carbocyclic ring, in particular a 4-membered saturated carbocyclic ring, where the ring may be substituted with one or more substituents R 11 . 
     Examples of preferred compounds are compounds of the following formulae I.a to I.ii, where the variables have one of the general or preferred meanings given above. 
     Examples of preferred compounds are the individual compounds compiled in the tables 1 to 36 below. Moreover, the meanings mentioned below for the individual variables in the tables are per se, independently of the combination in which they are mentioned, a particularly preferred embodiment of the substituents in question. 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
     Table 1 
     Compounds of the formula I.a in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 2 
     Compounds of the formula I.b in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 3 
     Compounds of the formula I.c in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 4 
     Compounds of the formula I.d in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 5 
     Compounds of the formula I.e in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 6 
     Compounds of the formula I.f in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 7 
     Compounds of the formula I.g in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 8 
     Compounds of the formula I.h in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 9 
     Compounds of the formula I.i in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 10 
     Compounds of the formula I.j in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 11 
     Compounds of the formula I.k in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 12 
     Compounds of the formula I.1 in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 13 
     Compounds of the formula I.m in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 14 
     Compounds of the formula I.n in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 15 
     Compounds of the formula I.o in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 16 
     Compounds of the formula I.p in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 17 
     Compounds of the formula I.q in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 18 
     Compounds of the formula I.r in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 19 
     Compounds of the formula I.s in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 20 
     Compounds of the formula I.t in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 21 
     Compounds of the formula I.u in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 22 
     Compounds of the formula I.v in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 23 
     Compounds of the formula I.w in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 24 
     Compounds of the formula I.x in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 25 
     Compounds of the formula I.y in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 26 
     Compounds of the formula I.z in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 27 
     Compounds of the formula I.zz in which the combination of R 5a , R 5b , R 7 , R 8  and R 9a  for a compound corresponds in each case to one row of Table B. 
     Table 28 
     Compounds of the formula I.aa in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 29 
     Compounds of the formula I.bb in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 30 
     Compounds of the formula I.cc in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 31 
     Compounds of the formula I.dd in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 32 
     Compounds of the formula I.ee in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 33 
     Compounds of the formula I.ff in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 34 
     Compounds of the formula I.gg in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 35 
     Compounds of the formula I.hh in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     Table 36 
     Compounds of the formula I.ii in which the combination of R 5a , R 5b , R 6  and R 9a  for a compound corresponds in each case to one row of Table A. 
     
       
         
           
               
               
               
               
               
             
               
                 TABLE A 
               
               
                   
               
               
                 No. 
                 R 9a   
                 R 5b   
                 R 5a   
                 R 6   
               
               
                   
               
             
            
               
                 A-1 
                 H 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-2 
                 F 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-3 
                 Cl 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-4 
                 Br 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-5 
                 CH 3   
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-6 
                 CF 3   
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-7 
                 OCH 3   
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-8 
                 OCF 3   
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-9 
                 cyclopropyl 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-10 
                 cyclobutyl 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-11 
                 cyclopentyl 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-12 
                 cyclohexyl 
                 H 
                 H 
                 —SO 2 —CH 3   
               
               
                 A-13 
                 H 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-14 
                 F 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-15 
                 Cl 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-16 
                 Br 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-17 
                 CH 3   
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-18 
                 CF 3   
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-19 
                 OCH 3   
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-20 
                 OCF 3   
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-21 
                 cyclopropyl 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-22 
                 cyclobutyl 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-23 
                 cyclopentyl 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-24 
                 cyclohexyl 
                 CH 3   
                 H 
                 —SO 2 —CH 3   
               
               
                 A-25 
                 H 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-26 
                 F 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-27 
                 Cl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-28 
                 Br 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-29 
                 CH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-30 
                 CF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-31 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-32 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-33 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-34 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-35 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-36 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 3   
               
               
                 A-37 
                 H 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-38 
                 F 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-39 
                 Cl 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-40 
                 Br 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-41 
                 CH 3   
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-42 
                 CF 3   
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-43 
                 OCH 3   
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-44 
                 OCF 3   
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-45 
                 cyclopropyl 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-46 
                 cyclobutyl 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-47 
                 cyclopentyl 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-48 
                 cyclohexyl 
                 H 
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-49 
                 H 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-50 
                 F 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-51 
                 Cl 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-52 
                 Br 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-53 
                 CH 3   
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-54 
                 CF 3   
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-55 
                 OCH 3   
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-56 
                 OCF 3   
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-57 
                 cyclopropyl 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-58 
                 cyclobutyl 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-59 
                 cyclopentyl 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-60 
                 cyclohexyl 
                 CH 3   
                 H 
                 —SO 2 —CH 2 CH 3   
               
               
                 A-61 
                 H 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-62 
                 F 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-63 
                 Cl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-64 
                 Br 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-65 
                 CH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-66 
                 CF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-67 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-68 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-69 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-70 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-71 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-72 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CH 2 CH 3   
               
               
                 A-73 
                 H 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-74 
                 F 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-75 
                 Cl 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-76 
                 Br 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-77 
                 CH 3   
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-78 
                 CF 3   
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-79 
                 OCH 3   
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-80 
                 OCF 3   
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-81 
                 cyclopropyl 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-82 
                 cyclobutyl 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-83 
                 cyclopentyl 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-84 
                 cyclohexyl 
                 H 
                 H 
                 —SO 2 —CF 3   
               
               
                 A-85 
                 H 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-86 
                 F 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-87 
                 Cl 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-88 
                 Br 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-89 
                 CH 3   
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-90 
                 CF 3   
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-91 
                 OCH 3   
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-92 
                 OCF 3   
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-93 
                 cyclopropyl 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-94 
                 cyclobutyl 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-95 
                 cyclopentyl 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-96 
                 cyclohexyl 
                 CH 3   
                 H 
                 —SO 2 —CF 3   
               
               
                 A-97 
                 H 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-98 
                 F 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-99 
                 Cl 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-100 
                 Br 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-101 
                 CH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-102 
                 CF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-103 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-104 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-105 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-106 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-107 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-108 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —SO 2 —CF 3   
               
               
                 A-109 
                 H 
                 H 
                 H 
                 —SO 2 —C 6 H 5 * 
               
               
                 A-110 
                 F 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-111 
                 Cl 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-112 
                 Br 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-113 
                 CH 3   
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-114 
                 CF 3   
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-115 
                 OCH 3   
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-116 
                 OCF 3   
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-117 
                 cyclopropyl 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-118 
                 cyclobutyl 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-119 
                 cyclopentyl 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-120 
                 cyclohexyl 
                 H 
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-121 
                 H 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-122 
                 F 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-123 
                 Cl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-124 
                 Br 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-125 
                 CH 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-126 
                 CF 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-127 
                 OCH 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-128 
                 OCF 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-129 
                 cyclopropyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-130 
                 cyclobutyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-131 
                 cyclopentyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-132 
                 cyclohexyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 5   
               
               
                 A-133 
                 H 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-134 
                 F 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-135 
                 Cl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-136 
                 Br 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-137 
                 CH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-138 
                 CF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-139 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-140 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-141 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-142 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-143 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-144 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 5   
               
               
                 A-145 
                 H 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3 ** 
               
               
                 A-146 
                 F 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-147 
                 Cl 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-148 
                 Br 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-149 
                 CH 3   
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-150 
                 CF 3   
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-151 
                 OCH 3   
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-152 
                 OCF 3   
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-153 
                 cyclopropyl 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-154 
                 cyclobutyl 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-155 
                 cyclopentyl 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-156 
                 cyclohexyl 
                 H 
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-157 
                 H 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-158 
                 F 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-159 
                 Cl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-160 
                 Br 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-161 
                 CH 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-162 
                 CF 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-163 
                 OCH 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-164 
                 OCF 3   
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-165 
                 cyclopropyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-166 
                 cyclobutyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-167 
                 cyclopentyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-168 
                 cyclohexyl 
                 CH 3   
                 H 
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-169 
                 H 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-170 
                 F 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-171 
                 Cl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-172 
                 Br 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-173 
                 CH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-174 
                 CF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-175 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-176 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-177 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-178 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-179 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-180 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —SO 2 —C 6 H 4 CH 3   
               
               
                 A-181 
                 H 
                 H 
                 H 
                 benzyl 
               
               
                 A-182 
                 F 
                 H 
                 H 
                 benzyl 
               
               
                 A-183 
                 Cl 
                 H 
                 H 
                 benzyl 
               
               
                 A-184 
                 Br 
                 H 
                 H 
                 benzyl 
               
               
                 A-185 
                 CH 3   
                 H 
                 H 
                 benzyl 
               
               
                 A-186 
                 CF 3   
                 H 
                 H 
                 benzyl 
               
               
                 A-187 
                 OCH 3   
                 H 
                 H 
                 benzyl 
               
               
                 A-188 
                 OCF 3   
                 H 
                 H 
                 benzyl 
               
               
                 A-189 
                 cyclopropyl 
                 H 
                 H 
                 benzyl 
               
               
                 A-190 
                 cyclobutyl 
                 H 
                 H 
                 benzyl 
               
               
                 A-191 
                 cyclopentyl 
                 H 
                 H 
                 benzyl 
               
               
                 A-192 
                 cyclohexyl 
                 H 
                 H 
                 benzyl 
               
               
                 A-193 
                 H 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-194 
                 F 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-195 
                 Cl 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-196 
                 Br 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-197 
                 CH 3   
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-198 
                 CF 3   
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-199 
                 OCH 3   
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-200 
                 OCF 3   
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-201 
                 cyclopropyl 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-202 
                 cyclobutyl 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-203 
                 cyclopentyl 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-204 
                 cyclohexyl 
                 CH 3   
                 H 
                 benzyl 
               
               
                 A-205 
                 H 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-206 
                 F 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-207 
                 Cl 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-208 
                 Br 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-209 
                 CH 3   
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-210 
                 CF 3   
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-211 
                 OCH 3   
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-212 
                 OCF 3   
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-213 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-214 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-215 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-216 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 benzyl 
               
               
                 A-217 
                 H 
                 H 
                 H 
                 H 
               
               
                 A-218 
                 F 
                 H 
                 H 
                 H 
               
               
                 A-219 
                 Cl 
                 H 
                 H 
                 H 
               
               
                 A-220 
                 Br 
                 H 
                 H 
                 H 
               
               
                 A-221 
                 CH 3   
                 H 
                 H 
                 H 
               
               
                 A-222 
                 CF 3   
                 H 
                 H 
                 H 
               
               
                 A-223 
                 OCH 3   
                 H 
                 H 
                 H 
               
               
                 A-224 
                 OCF 3   
                 H 
                 H 
                 H 
               
               
                 A-225 
                 cyclopropyl 
                 H 
                 H 
                 H 
               
               
                 A-226 
                 cyclobutyl 
                 H 
                 H 
                 H 
               
               
                 A-227 
                 cyclopentyl 
                 H 
                 H 
                 H 
               
               
                 A-228 
                 cyclohexyl 
                 H 
                 H 
                 H 
               
               
                 A-229 
                 H 
                 CH 3   
                 H 
                 H 
               
               
                 A-230 
                 F 
                 CH 3   
                 H 
                 H 
               
               
                 A-231 
                 Cl 
                 CH 3   
                 H 
                 H 
               
               
                 A-232 
                 Br 
                 CH 3   
                 H 
                 H 
               
               
                 A-233 
                 CH 3   
                 CH 3   
                 H 
                 H 
               
               
                 A-234 
                 CF 3   
                 CH 3   
                 H 
                 H 
               
               
                 A-235 
                 OCH 3   
                 CH 3   
                 H 
                 H 
               
               
                 A-236 
                 OCF 3   
                 CH 3   
                 H 
                 H 
               
               
                 A-237 
                 cyclopropyl 
                 CH 3   
                 H 
                 H 
               
               
                 A-238 
                 cyclobutyl 
                 CH 3   
                 H 
                 H 
               
               
                 A-239 
                 cyclopentyl 
                 CH 3   
                 H 
                 H 
               
               
                 A-240 
                 cyclohexyl 
                 CH 3   
                 H 
                 H 
               
               
                 A-241 
                 H 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-242 
                 F 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-243 
                 Cl 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-244 
                 Br 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-245 
                 CH 3   
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-246 
                 CF 3   
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-247 
                 OCH 3   
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-248 
                 OCF 3   
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-249 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-250 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-251 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-252 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 H 
               
               
                 A-253 
                 H 
                 H 
                 H 
                 CH 3   
               
               
                 A-254 
                 F 
                 H 
                 H 
                 CH 3   
               
               
                 A-255 
                 Cl 
                 H 
                 H 
                 CH 3   
               
               
                 A-256 
                 Br 
                 H 
                 H 
                 CH 3   
               
               
                 A-257 
                 CH 3   
                 H 
                 H 
                 CH 3   
               
               
                 A-258 
                 CF 3   
                 H 
                 H 
                 CH 3   
               
               
                 A-259 
                 OCH 3   
                 H 
                 H 
                 CH 3   
               
               
                 A-260 
                 OCF 3   
                 H 
                 H 
                 CH 3   
               
               
                 A-261 
                 cyclopropyl 
                 H 
                 H 
                 CH 3   
               
               
                 A-262 
                 cyclobutyl 
                 H 
                 H 
                 CH 3   
               
               
                 A-263 
                 cyclopentyl 
                 H 
                 H 
                 CH 3   
               
               
                 A-264 
                 cyclohexyl 
                 H 
                 H 
                 CH 3   
               
               
                 A-265 
                 H 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-266 
                 F 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-267 
                 Cl 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-268 
                 Br 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-269 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-270 
                 CF 3   
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-271 
                 OCH 3   
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-272 
                 OCF 3   
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-273 
                 cyclopropyl 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-274 
                 cyclobutyl 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-275 
                 cyclopentyl 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-276 
                 cyclohexyl 
                 CH 3   
                 H 
                 CH 3   
               
               
                 A-277 
                 H 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-278 
                 F 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-279 
                 Cl 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-280 
                 Br 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-281 
                 CH 3   
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-282 
                 CF 3   
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-283 
                 OCH 3   
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-284 
                 OCF 3   
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-285 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-286 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-287 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-288 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 CH 3   
               
               
                 A-289 
                 H 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-290 
                 F 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-291 
                 Cl 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-292 
                 Br 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-293 
                 CH 3   
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-294 
                 CF 3   
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-295 
                 OCH 3   
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-296 
                 OCF 3   
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-297 
                 cyclopropyl 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-298 
                 cyclobutyl 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-299 
                 cyclopentyl 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-300 
                 cyclohexyl 
                 H 
                 H 
                 C 2 H 5   
               
               
                 A-301 
                 H 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-302 
                 F 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-303 
                 Cl 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-304 
                 Br 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-305 
                 CH 3   
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-306 
                 CF 3   
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-307 
                 OCH 3   
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-308 
                 OCF 3   
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-309 
                 cyclopropyl 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-310 
                 cyclobutyl 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-311 
                 cyclopentyl 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-312 
                 cyclohexyl 
                 CH 3   
                 H 
                 C 2 H 5   
               
               
                 A-313 
                 H 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-314 
                 F 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-315 
                 Cl 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-316 
                 Br 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-317 
                 CH 3   
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-318 
                 CF 3   
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-319 
                 OCH 3   
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-320 
                 OCF 3   
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-321 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-322 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-323 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-324 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 C 2 H 5   
               
               
                 A-325 
                 H 
                 H 
                 H 
                 n-propyl 
               
               
                 A-326 
                 F 
                 H 
                 H 
                 n-propyl 
               
               
                 A-327 
                 Cl 
                 H 
                 H 
                 n-propyl 
               
               
                 A-328 
                 Br 
                 H 
                 H 
                 n-propyl 
               
               
                 A-329 
                 CH 3   
                 H 
                 H 
                 n-propyl 
               
               
                 A-330 
                 CF 3   
                 H 
                 H 
                 n-propyl 
               
               
                 A-331 
                 OCH 3   
                 H 
                 H 
                 n-propyl 
               
               
                 A-332 
                 OCF 3   
                 H 
                 H 
                 n-propyl 
               
               
                 A-333 
                 cyclopropyl 
                 H 
                 H 
                 n-propyl 
               
               
                 A-334 
                 cyclobutyl 
                 H 
                 H 
                 n-propyl 
               
               
                 A-335 
                 cyclopentyl 
                 H 
                 H 
                 n-propyl 
               
               
                 A-336 
                 cyclohexyl 
                 H 
                 H 
                 n-propyl 
               
               
                 A-337 
                 H 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-338 
                 F 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-339 
                 Cl 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-340 
                 Br 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-341 
                 CH 3   
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-342 
                 CF 3   
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-343 
                 OCH 3   
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-344 
                 OCF 3   
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-345 
                 cyclopropyl 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-346 
                 cyclobutyl 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-347 
                 cyclopentyl 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-348 
                 cyclohexyl 
                 CH 3   
                 H 
                 n-propyl 
               
               
                 A-349 
                 H 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-350 
                 F 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-351 
                 Cl 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-352 
                 Br 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-353 
                 CH 3   
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-354 
                 CF 3   
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-355 
                 OCH 3   
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-356 
                 OCF 3   
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-357 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-358 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-359 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-360 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 n-propyl 
               
               
                 A-361 
                 H 
                 H 
                 H 
                 isopropyl 
               
               
                 A-362 
                 F 
                 H 
                 H 
                 isopropyl 
               
               
                 A-363 
                 Cl 
                 H 
                 H 
                 isopropyl 
               
               
                 A-364 
                 Br 
                 H 
                 H 
                 isopropyl 
               
               
                 A-365 
                 CH 3   
                 H 
                 H 
                 isopropyl 
               
               
                 A-366 
                 CF 3   
                 H 
                 H 
                 isopropyl 
               
               
                 A-367 
                 OCH 3   
                 H 
                 H 
                 isopropyl 
               
               
                 A-368 
                 OCF 3   
                 H 
                 H 
                 isopropyl 
               
               
                 A-369 
                 cyclopropyl 
                 H 
                 H 
                 isopropyl 
               
               
                 A-370 
                 cyclobutyl 
                 H 
                 H 
                 isopropyl 
               
               
                 A-371 
                 cyclopentyl 
                 H 
                 H 
                 isopropyl 
               
               
                 A-372 
                 cyclohexyl 
                 H 
                 H 
                 isopropyl 
               
               
                 A-373 
                 H 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-374 
                 F 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-375 
                 Cl 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-376 
                 Br 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-377 
                 CH 3   
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-378 
                 CF 3   
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-379 
                 OCH 3   
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-380 
                 OCF 3   
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-381 
                 cyclopropyl 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-382 
                 cyclobutyl 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-383 
                 cyclopentyl 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-384 
                 cyclohexyl 
                 CH 3   
                 H 
                 isopropyl 
               
               
                 A-385 
                 H 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-386 
                 F 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-387 
                 Cl 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-388 
                 Br 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-389 
                 CH 3   
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-390 
                 CF 3   
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-391 
                 OCH 3   
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-392 
                 OCF 3   
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-393 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-394 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-395 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-396 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 isopropyl 
               
               
                 A-397 
                 H 
                 H 
                 H 
                 n-butyl 
               
               
                 A-398 
                 F 
                 H 
                 H 
                 n-butyl 
               
               
                 A-399 
                 Cl 
                 H 
                 H 
                 n-butyl 
               
               
                 A-400 
                 Br 
                 H 
                 H 
                 n-butyl 
               
               
                 A-401 
                 CH 3   
                 H 
                 H 
                 n-butyl 
               
               
                 A-402 
                 CF 3   
                 H 
                 H 
                 n-butyl 
               
               
                 A-403 
                 OCH 3   
                 H 
                 H 
                 n-butyl 
               
               
                 A-404 
                 OCF 3   
                 H 
                 H 
                 n-butyl 
               
               
                 A-405 
                 cyclopropyl 
                 H 
                 H 
                 n-butyl 
               
               
                 A-406 
                 cyclobutyl 
                 H 
                 H 
                 n-butyl 
               
               
                 A-407 
                 cyclopentyl 
                 H 
                 H 
                 n-butyl 
               
               
                 A-408 
                 cyclohexyl 
                 H 
                 H 
                 n-butyl 
               
               
                 A-409 
                 H 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-410 
                 F 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-411 
                 Cl 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-412 
                 Br 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-413 
                 CH 3   
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-414 
                 CF 3   
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-415 
                 OCH 3   
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-416 
                 OCF 3   
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-417 
                 cyclopropyl 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-418 
                 cyclobutyl 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-419 
                 cyclopentyl 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-420 
                 cyclohexyl 
                 CH 3   
                 H 
                 n-butyl 
               
               
                 A-421 
                 H 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-422 
                 F 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-423 
                 Cl 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-424 
                 Br 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-425 
                 CH 3   
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-426 
                 CF 3   
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-427 
                 OCH 3   
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-428 
                 OCF 3   
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-429 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-430 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-431 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-432 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 n-butyl 
               
               
                 A-433 
                 H 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-434 
                 F 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-435 
                 Cl 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-436 
                 Br 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-437 
                 CH 3   
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-438 
                 CF 3   
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-439 
                 OCH 3   
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-440 
                 OCF 3   
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-441 
                 cyclopropyl 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-442 
                 cyclobutyl 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-443 
                 cyclopentyl 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-444 
                 cyclohexyl 
                 H 
                 H 
                 cyclopropyl 
               
               
                 A-445 
                 H 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-446 
                 F 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-447 
                 Cl 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-448 
                 Br 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-449 
                 CH 3   
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-450 
                 CF 3   
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-451 
                 OCH 3   
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-452 
                 OCF 3   
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-453 
                 cyclopropyl 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-454 
                 cyclobutyl 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-455 
                 cyclopentyl 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-456 
                 cyclohexyl 
                 CH 3   
                 H 
                 cyclopropyl 
               
               
                 A-457 
                 H 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-458 
                 F 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-459 
                 Cl 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-460 
                 Br 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-461 
                 CH 3   
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-462 
                 CF 3   
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-463 
                 OCH 3   
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-464 
                 OCF 3   
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-465 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-466 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-467 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-468 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 cyclopropyl 
               
               
                 A-469 
                 H 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-470 
                 F 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-471 
                 Cl 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-472 
                 Br 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-473 
                 CH 3   
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-474 
                 CF 3   
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-475 
                 OCH 3   
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-476 
                 OCF 3   
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-477 
                 cyclopropyl 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-478 
                 cyclobutyl 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-479 
                 cyclopentyl 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-480 
                 cyclohexyl 
                 H 
                 H 
                 cyclobutyl 
               
               
                 A-481 
                 H 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-482 
                 F 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-483 
                 Cl 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-484 
                 Br 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-485 
                 CH 3   
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-486 
                 CF 3   
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-487 
                 OCH 3   
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-488 
                 OCF 3   
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-489 
                 cyclopropyl 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-490 
                 cyclobutyl 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-491 
                 cyclopentyl 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-492 
                 cyclohexyl 
                 CH 3   
                 H 
                 cyclobutyl 
               
               
                 A-493 
                 H 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-494 
                 F 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-495 
                 Cl 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-496 
                 Br 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-497 
                 CH 3   
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-498 
                 CF 3   
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-499 
                 OCH 3   
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-500 
                 OCF 3   
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-501 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-502 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-503 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-504 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 cyclobutyl 
               
               
                 A-505 
                 H 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-506 
                 F 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-507 
                 Cl 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-508 
                 Br 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-509 
                 CH 3   
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-510 
                 CF 3   
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-511 
                 OCH 3   
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-512 
                 OCF 3   
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-513 
                 cyclopropyl 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-514 
                 cyclobutyl 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-515 
                 cyclopentyl 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-516 
                 cyclohexyl 
                 H 
                 H 
                 cyclopentyl 
               
               
                 A-517 
                 H 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-518 
                 F 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-519 
                 Cl 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-520 
                 Br 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-521 
                 CH 3   
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-522 
                 CF 3   
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-523 
                 OCH 3   
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-524 
                 OCF 3   
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-525 
                 cyclopropyl 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-526 
                 cyclobutyl 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-527 
                 cyclopentyl 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-528 
                 cyclohexyl 
                 CH 3   
                 H 
                 cyclopentyl 
               
               
                 A-529 
                 H 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-530 
                 F 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-531 
                 Cl 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-532 
                 Br 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-533 
                 CH 3   
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-534 
                 CF 3   
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-535 
                 OCH 3   
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-536 
                 OCF 3   
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-537 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-538 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-539 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-540 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 cyclopentyl 
               
               
                 A-541 
                 H 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-542 
                 F 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-543 
                 Cl 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-544 
                 Br 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-545 
                 CH 3   
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-546 
                 CF 3   
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-547 
                 OCH 3   
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-548 
                 OCF 3   
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-549 
                 cyclopropyl 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-550 
                 cyclobutyl 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-551 
                 cyclopentyl 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-552 
                 cyclohexyl 
                 H 
                 H 
                 cyclohexyl 
               
               
                 A-553 
                 H 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-554 
                 F 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-555 
                 Cl 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-556 
                 Br 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-557 
                 CH 3   
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-558 
                 CF 3   
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-559 
                 OCH 3   
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-560 
                 OCF 3   
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-561 
                 cyclopropyl 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-562 
                 cyclobutyl 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-563 
                 cyclopentyl 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-564 
                 cyclohexyl 
                 CH 3   
                 H 
                 cyclohexyl 
               
               
                 A-565 
                 H 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-566 
                 F 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-567 
                 Cl 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-568 
                 Br 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-569 
                 CH 3   
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-570 
                 CF 3   
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-571 
                 OCH 3   
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-572 
                 OCF 3   
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-573 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-574 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-575 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-576 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 cyclohexyl 
               
               
                 A-577 
                 H 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-578 
                 F 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-579 
                 Cl 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-580 
                 Br 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-581 
                 CH 3   
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-582 
                 CF 3   
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-583 
                 OCH 3   
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-584 
                 OCF 3   
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-585 
                 cyclopropyl 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-586 
                 cyclobutyl 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-587 
                 cyclopentyl 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-588 
                 cyclohexyl 
                 H 
                 H 
                 oxetan-3-yl 
               
               
                 A-589 
                 H 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-590 
                 F 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-591 
                 Cl 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-592 
                 Br 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-593 
                 CH 3   
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-594 
                 CF 3   
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-595 
                 OCH 3   
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-596 
                 OCF 3   
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-597 
                 cyclopropyl 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-598 
                 cyclobutyl 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-599 
                 cyclopentyl 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-600 
                 cyclohexyl 
                 CH 3   
                 H 
                 oxetan-3-yl 
               
               
                 A-601 
                 H 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-602 
                 F 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-603 
                 Cl 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-604 
                 Br 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-605 
                 CH 3   
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-606 
                 CF 3   
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-607 
                 OCH 3   
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-608 
                 OCF 3   
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-609 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-610 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-611 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-612 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 oxetan-3-yl 
               
               
                 A-613 
                 H 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-614 
                 F 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-615 
                 Cl 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-616 
                 Br 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-617 
                 CH 3   
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-618 
                 CF 3   
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-619 
                 OCH 3   
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-620 
                 OCF 3   
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-621 
                 cyclopropyl 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-622 
                 cyclobutyl 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-623 
                 cyclopentyl 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-624 
                 cyclohexyl 
                 H 
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-625 
                 H 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-626 
                 F 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-627 
                 Cl 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-628 
                 Br 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-629 
                 CH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-630 
                 CF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-631 
                 OCH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-632 
                 OCF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-633 
                 cyclopropyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-634 
                 cyclobutyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-635 
                 cyclopentyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-636 
                 cyclohexyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopropyl 
               
               
                 A-637 
                 H 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-638 
                 F 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-639 
                 Cl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-640 
                 Br 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-641 
                 CH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-642 
                 CF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-643 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-644 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-645 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-646 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-647 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-648 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopropyl 
               
               
                 A-649 
                 H 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-650 
                 F 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-651 
                 Cl 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-652 
                 Br 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-653 
                 CH 3   
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-654 
                 CF 3   
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-655 
                 OCH 3   
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-656 
                 OCF 3   
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-657 
                 cyclopropyl 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-658 
                 cyclobutyl 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-659 
                 cyclopentyl 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-660 
                 cyclohexyl 
                 H 
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-661 
                 H 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-662 
                 F 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-663 
                 Cl 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-664 
                 Br 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-665 
                 CH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-666 
                 CF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-667 
                 OCH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-668 
                 OCF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-669 
                 cyclopropyl 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-670 
                 cyclobutyl 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-671 
                 cyclopentyl 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-672 
                 cyclohexyl 
                 CH 3   
                 H 
                 —CH 2 -cyclobutyl 
               
               
                 A-673 
                 H 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-674 
                 F 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-675 
                 Cl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-676 
                 Br 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-677 
                 CH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-678 
                 CF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-679 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-680 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-681 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-682 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-683 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-684 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclobutyl 
               
               
                 A-685 
                 H 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-686 
                 F 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-687 
                 Cl 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-688 
                 Br 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-689 
                 CH 3   
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-690 
                 CF 3   
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-691 
                 OCH 3   
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-692 
                 OCF 3   
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-693 
                 cyclopropyl 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-694 
                 cyclobutyl 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-695 
                 cyclopentyl 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-696 
                 cyclohexyl 
                 H 
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-697 
                 H 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-698 
                 F 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-699 
                 Cl 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-700 
                 Br 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-701 
                 CH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-702 
                 CF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-703 
                 OCH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-704 
                 OCF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-705 
                 cyclopropyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-706 
                 cyclobutyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-707 
                 cyclopentyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-708 
                 cyclohexyl 
                 CH 3   
                 H 
                 —CH 2 -cyclopentyl 
               
               
                 A-709 
                 H 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-710 
                 F 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-711 
                 Cl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-712 
                 Br 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-713 
                 CH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-714 
                 CF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-715 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-716 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-717 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-718 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-719 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-720 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclopentyl 
               
               
                 A-721 
                 H 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-722 
                 F 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-723 
                 Cl 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-724 
                 Br 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-725 
                 CH 3   
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-726 
                 CF 3   
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-727 
                 OCH 3   
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-728 
                 OCF 3   
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-729 
                 cyclopropyl 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-730 
                 cyclobutyl 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-731 
                 cyclopentyl 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-732 
                 cyclohexyl 
                 H 
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-733 
                 H 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-734 
                 F 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-735 
                 Cl 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-736 
                 Br 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-737 
                 CH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-738 
                 CF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-739 
                 OCH 3   
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-740 
                 OCF 3   
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-741 
                 cyclopropyl 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-742 
                 cyclobutyl 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-743 
                 cyclopentyl 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-744 
                 cyclohexyl 
                 CH 3   
                 H 
                 —CH 2 -cyclohexyl 
               
               
                 A-745 
                 H 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-746 
                 F 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-747 
                 Cl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-748 
                 Br 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-749 
                 CH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-750 
                 CF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-751 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-752 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-753 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-754 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-755 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-756 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —CH 2 -cyclohexyl 
               
               
                 A-757 
                 H 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-758 
                 F 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-759 
                 Cl 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-760 
                 Br 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-761 
                 CH 3   
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-762 
                 CF 3   
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-763 
                 OCH 3   
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-764 
                 OCF 3   
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-765 
                 cyclopropyl 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-766 
                 cyclobutyl 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-767 
                 cyclopentyl 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-768 
                 cyclohexyl 
                 H 
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-769 
                 H 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-770 
                 F 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-771 
                 Cl 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-772 
                 Br 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-773 
                 CH 3   
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-774 
                 CF 3   
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-775 
                 OCH 3   
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-776 
                 OCF 3   
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-777 
                 cyclopropyl 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-778 
                 cyclobutyl 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-779 
                 cyclopentyl 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-780 
                 cyclohexyl 
                 CH 3   
                 H 
                 —C(O)-cyclopropyl 
               
               
                 A-781 
                 H 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-782 
                 F 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-783 
                 Cl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-784 
                 Br 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-785 
                 CH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-786 
                 CF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-787 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-788 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-789 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-790 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-791 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-792 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopropyl 
               
               
                 A-793 
                 H 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-794 
                 F 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-795 
                 Cl 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-796 
                 Br 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-797 
                 CH 3   
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-798 
                 CF 3   
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-799 
                 OCH 3   
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-800 
                 OCF 3   
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-801 
                 cyclopropyl 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-802 
                 cyclobutyl 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-803 
                 cyclopentyl 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-804 
                 cyclohexyl 
                 H 
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-805 
                 H 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-806 
                 F 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-807 
                 Cl 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-808 
                 Br 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-809 
                 CH 3   
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-810 
                 CF 3   
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-811 
                 OCH 3   
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-812 
                 OCF 3   
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-813 
                 cyclopropyl 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-814 
                 cyclobutyl 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-815 
                 cyclopentyl 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-816 
                 cyclohexyl 
                 CH 3   
                 H 
                 —C(O)-cyclobutyl 
               
               
                 A-817 
                 H 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-818 
                 F 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-819 
                 Cl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-820 
                 Br 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-821 
                 CH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-822 
                 CF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-823 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-824 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-825 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-826 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-827 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-828 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclobutyl 
               
               
                 A-829 
                 H 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-830 
                 F 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-831 
                 Cl 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-832 
                 Br 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-833 
                 CH 3   
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-834 
                 CF 3   
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-835 
                 OCH 3   
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-836 
                 OCF 3   
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-837 
                 cyclopropyl 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-838 
                 cyclobutyl 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-839 
                 cyclopentyl 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-840 
                 cyclohexyl 
                 H 
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-841 
                 H 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-842 
                 F 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-843 
                 Cl 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-844 
                 Br 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-845 
                 CH 3   
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-846 
                 CF 3   
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-847 
                 OCH 3   
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-848 
                 OCF 3   
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-849 
                 cyclopropyl 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-850 
                 cyclobutyl 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-851 
                 cyclopentyl 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-852 
                 cyclohexyl 
                 CH 3   
                 H 
                 —C(O)-cyclopentyl 
               
               
                 A-853 
                 H 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-854 
                 F 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-855 
                 Cl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-856 
                 Br 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-857 
                 CH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-858 
                 CF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-859 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-860 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-861 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-862 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-863 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-864 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclopentyl 
               
               
                 A-865 
                 H 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-866 
                 F 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-867 
                 Cl 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-868 
                 Br 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-869 
                 CH 3   
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-870 
                 CF 3   
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-871 
                 OCH 3   
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-872 
                 OCF 3   
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-873 
                 cyclopropyl 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-874 
                 cyclobutyl 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-875 
                 cyclopentyl 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-876 
                 cyclohexyl 
                 H 
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-877 
                 H 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-878 
                 F 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-879 
                 Cl 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-880 
                 Br 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-881 
                 CH 3   
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-882 
                 CF 3   
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-883 
                 OCH 3   
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-884 
                 OCF 3   
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-885 
                 cyclopropyl 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-886 
                 cyclobutyl 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-887 
                 cyclopentyl 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-888 
                 cyclohexyl 
                 CH 3   
                 H 
                 —C(O)-cyclohexyl 
               
               
                 A-889 
                 H 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-890 
                 F 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-891 
                 Cl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-892 
                 Br 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-893 
                 CH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-894 
                 CF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-895 
                 OCH 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-896 
                 OCF 3   
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-897 
                 cyclopropyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-898 
                 cyclobutyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-899 
                 cyclopentyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
               
                 A-900 
                 cyclohexyl 
                 CH 3   
                 CH 3   
                 —C(O)-cyclohexyl 
               
            
           
           
               
               
               
               
            
               
                 A-901 
                 H 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-902 
                 F 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-903 
                 Cl 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-904 
                 Br 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-905 
                 CH 3   
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-906 
                 CF 3   
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-907 
                 OCH 3   
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-908 
                 OCF 3   
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-909 
                 cyclopropyl 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-910 
                 cyclobutyl 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-911 
                 cyclopentyl 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-912 
                 cyclohexyl 
                 H 
                 —(CH 2 ) 3 — 
               
               
                 A-913 
                 H 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-914 
                 F 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-915 
                 Cl 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-916 
                 Br 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-917 
                 CH 3   
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-918 
                 CF 3   
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-919 
                 OCH 3   
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-920 
                 OCF 3   
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-921 
                 cyclopropyl 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-922 
                 cyclobutyl 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-923 
                 cyclopentyl 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-924 
                 cyclohexyl 
                 CH 3   
                 —(CH 2 ) 3 — 
               
               
                 A-925 
                 H 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-926 
                 F 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-927 
                 Cl 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-928 
                 Br 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-929 
                 CH 3   
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-930 
                 CF 3   
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-931 
                 OCH 3   
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-932 
                 OCF 3   
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-933 
                 cyclopropyl 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-934 
                 cyclobutyl 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-935 
                 cyclopentyl 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-936 
                 cyclohexyl 
                 D 
                 —(CH 2 ) 3 — 
               
               
                 A-937 
                 H 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-938 
                 F 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-939 
                 Cl 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-940 
                 Br 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-941 
                 CH 3   
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-942 
                 CF 3   
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-943 
                 OCH 3   
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-944 
                 OCF 3   
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-945 
                 cyclopropyl 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-946 
                 cyclobutyl 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-947 
                 cyclopentyl 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-948 
                 cyclohexyl 
                 H 
                 —(CH 2 ) 4 — 
               
               
                 A-949 
                 H 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-950 
                 F 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-951 
                 Cl 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-952 
                 Br 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-953 
                 CH 3   
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-954 
                 CF 3   
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-955 
                 OCH 3   
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-956 
                 OCF 3   
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-957 
                 cyclopropyl 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-958 
                 cyclobutyl 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-959 
                 cyclopentyl 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-960 
                 cyclohexyl 
                 CH 3   
                 —(CH 2 ) 4 — 
               
               
                 A-961 
                 H 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-962 
                 F 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-963 
                 Cl 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-964 
                 Br 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-965 
                 CH 3   
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-966 
                 CF 3   
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-967 
                 OCH 3   
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-968 
                 OCF 3   
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-969 
                 cyclopropyl 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-970 
                 cyclobutyl 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-971 
                 cyclopentyl 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-972 
                 cyclohexyl 
                 D 
                 —(CH 2 ) 4 — 
               
               
                 A-973 
                 H 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-974 
                 F 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-975 
                 Cl 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-976 
                 Br 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-977 
                 CH 3   
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-978 
                 CF 3   
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-979 
                 OCH 3   
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-980 
                 OCF 3   
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-981 
                 cyclopropyl 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-982 
                 cyclobutyl 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-983 
                 cyclopentyl 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-984 
                 cyclohexyl 
                 H 
                 —(CH 2 ) 5 — 
               
               
                 A-985 
                 H 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-986 
                 F 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-987 
                 Cl 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-988 
                 Br 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-989 
                 CH 3   
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-990 
                 CF 3   
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-991 
                 OCH 3   
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-992 
                 OCF 3   
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-993 
                 cyclopropyl 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-994 
                 cyclobutyl 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-995 
                 cyclopentyl 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-996 
                 cyclohexyl 
                 CH 3   
                 —(CH 2 ) 5 — 
               
               
                 A-997 
                 H 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-998 
                 F 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-999 
                 Cl 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1000 
                 Br 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1001 
                 CH 3   
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1002 
                 CF 3   
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1003 
                 OCH 3   
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1004 
                 OCF 3   
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1005 
                 cyclopropyl 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1006 
                 cyclobutyl 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1007 
                 cyclopentyl 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1008 
                 cyclohexyl 
                 D 
                 —(CH 2 ) 5 — 
               
               
                 A-1009 
                 F 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)—*** 
               
               
                 A-1010 
                 Cl 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1011 
                 Br 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1012 
                 CH 3   
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1013 
                 CF 3   
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1014 
                 OCH 3   
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1015 
                 OCF 3   
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1016 
                 cyclopropyl 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1017 
                 cyclobutyl 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1018 
                 cyclopentyl 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1019 
                 cyclohexyl 
                 H 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1020 
                 H 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1021 
                 F 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1022 
                 Cl 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1023 
                 Br 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1024 
                 CH 3   
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1025 
                 CF 3   
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1026 
                 OCH 3   
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1027 
                 OCF 3   
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1028 
                 cyclopropyl 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1029 
                 cyclobutyl 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1030 
                 cyclopentyl 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1031 
                 cyclohexyl 
                 CH 3   
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1032 
                 H 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1033 
                 F 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1034 
                 Cl 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1035 
                 Br 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1036 
                 CH 3   
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1037 
                 CF 3   
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1038 
                 OCH 3   
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1039 
                 OCF 3   
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1040 
                 cyclopropyl 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1041 
                 cyclobutyl 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1042 
                 cyclopentyl 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                 A-1043 
                 cyclohexyl 
                 D 
                 —(CH 2 —CH-(μ-CH 2 )—CH)— 
               
               
                   
               
               
                 *C 6 H 5  = phenyl 
               
               
                 **C 6 H 4 CH 3  = 4-methylphenyl (p-tolyl) 
               
               
                 ***—(CH 2 —CH-(μ-CH 2 )—CH)— =  
               
               
                                   
(# = attachment point to the atoms carrying R 6  (left #) and R 5a  (right #)) 
               
            
           
         
       
     
                                         TABLE B               No.   R 9a     R 5b     R 5a     R 7     R 8                    B-1   H   H   H   CH 3     CH 3         B-2   F   H   H   CH 3     CH 3         B-3   Cl   H   H   CH 3     CH 3         B-4   Br   H   H   CH 3     CH 3         B-5   CH 3     H   H   CH 3     CH 3         B-6   CF 3     H   H   CH 3     CH 3         B-7   OCH 3     H   H   CH 3     CH 3         B-8   OCF 3     H   H   CH 3     CH 3         B-9   H   F   H   CH 3     CH 3         B-10   F   F   H   CH 3     CH 3         B-11   Cl   F   H   CH 3     CH 3         B-12   Br   F   H   CH 3     CH 3         B-13   CH 3     F   H   CH 3     CH 3         B-14   CF 3     F   H   CH 3     CH 3         B-15   OCH 3     F   H   CH 3     CH 3         B-16   OCF 3     F   H   CH 3     CH 3         B-17   H   Cl   H   CH 3     CH 3         B-18   F   Cl   H   CH 3     CH 3         B-19   Cl   Cl   H   CH 3     CH 3         B-20   Br   Cl   H   CH 3     CH 3         B-21   CH 3     Cl   H   CH 3     CH 3         B-22   CF 3     Cl   H   CH 3     CH 3         B-23   OCH 3     Cl   H   CH 3     CH 3         B-24   OCF 3     Cl   H   CH 3     CH 3         B-25   H   CH 3     H   CH 3     CH 3         B-26   F   CH 3     H   CH 3     CH 3         B-27   Cl   CH 3     H   CH 3     CH 3         B-28   Br   CH 3     H   CH 3     CH 3         B-29   CH 3     CH 3     H   CH 3     CH 3         B-30   CF 3     CH 3     H   CH 3     CH 3         B-31   OCH 3     CH 3     H   CH 3     CH 3         B-32   OCF 3     CH 3     H   CH 3     CH 3         B-33   H   CH 3     CH 3     CH 3     CH 3         B-34   F   CH 3     CH 3     CH 3     CH 3         B-35   Cl   CH 3     CH 3     CH 3     CH 3         B-36   Br   CH 3     CH 3     CH 3     CH 3         B-37   CH 3     CH 3     CH 3     CH 3     CH 3         B-38   CF 3     CH 3     CH 3     CH 3     CH 3         B-39   OCH 3     CH 3     CH 3     CH 3     CH 3         B-40   OCF 3     CH 3     CH 3     CH 3     CH 3         B-41   H   H   H   CH 3     CH 2 CH 3         B-42   F   H   H   CH 3     CH 2 CH 3         B-43   Cl   H   H   CH 3     CH 2 CH 3         B-44   Br   H   H   CH 3     CH 2 CH 3         B-45   CH 3     H   H   CH 3     CH 2 CH 3         B-46   CF 3     H   H   CH 3     CH 2 CH 3         B-47   OCH 3     H   H   CH 3     CH 2 CH 3         B-48   OCF 3     H   H   CH 3     CH 2 CH 3         B-49   H   F   H   CH 3     CH 2 CH 3         B-50   F   F   H   CH 3     CH 2 CH 3         B-51   Cl   F   H   CH 3     CH 2 CH 3         B-52   Br   F   H   CH 3     CH 2 CH 3         B-53   CH 3     F   H   CH 3     CH 2 CH 3         B-54   CF 3     F   H   CH 3     CH 2 CH 3         B-55   OCH 3     F   H   CH 3     CH 2 CH 3         B-56   OCF 3     F   H   CH 3     CH 2 CH 3         B-57   H   Cl   H   CH 3     CH 2 CH 3         B-58   F   Cl   H   CH 3     CH 2 CH 3         B-59   Cl   Cl   H   CH 3     CH 2 CH 3         B-60   Br   Cl   H   CH 3     CH 2 CH 3         B-61   CH 3     Cl   H   CH 3     CH 2 CH 3         B-62   CF 3     Cl   H   CH 3     CH 2 CH 3         B-63   OCH 3     Cl   H   CH 3     CH 2 CH 3         B-64   OCF 3     Cl   H   CH 3     CH 2 CH 3         B-65   H   CH 3     H   CH 3     CH 2 CH 3         B-66   F   CH 3     H   CH 3     CH 2 CH 3         B-67   Cl   CH 3     H   CH 3     CH 2 CH 3         B-68   Br   CH 3     H   CH 3     CH 2 CH 3         B-69   CH 3     CH 3     H   CH 3     CH 2 CH 3         B-70   CF 3     CH 3     H   CH 3     CH 2 CH 3         B-71   OCH 3     CH 3     H   CH 3     CH 2 CH 3         B-72   OCF 3     CH 3     H   CH 3     CH 2 CH 3         B-73   H   CH 3     CH 3     CH 3     CH 2 CH 3         B-74   F   CH 3     CH 3     CH 3     CH 2 CH 3         B-75   Cl   CH 3     CH 3     CH 3     CH 2 CH 3         B-76   Br   CH 3     CH 3     CH 3     CH 2 CH 3         B-77   CH 3     CH 3     CH 3     CH 3     CH 2 CH 3         B-78   CF 3     CH 3     CH 3     CH 3     CH 2 CH 3         B-79   OCH 3     CH 3     CH 3     CH 3     CH 2 CH 3         B-80   OCF 3     CH 3     CH 3     CH 3     CH 2 CH 3         B-81   H   H   H   CH 3     CF 3         B-82   F   H   H   CH 3     CF 3         B-83   Cl   H   H   CH 3     CF 3         B-84   Br   H   H   CH 3     CF 3         B-85   CH 3     H   H   CH 3     CF 3         B-86   CF 3     H   H   CH 3     CF 3         B-87   OCH 3     H   H   CH 3     CF 3         B-88   OCF 3     H   H   CH 3     CF 3         B-89   H   F   H   CH 3     CF 3         B-90   F   F   H   CH 3     CF 3         B-91   Cl   F   H   CH 3     CF 3         B-92   Br   F   H   CH 3     CF 3         B-93   CH 3     F   H   CH 3     CF 3         B-94   CF 3     F   H   CH 3     CF 3         B-95   OCH 3     F   H   CH 3     CF 3         B-96   OCF 3     F   H   CH 3     CF 3         B-97   H   Cl   H   CH 3     CF 3         B-98   F   Cl   H   CH 3     CF 3         B-99   Cl   Cl   H   CH 3     CF 3         B-100   Br   Cl   H   CH 3     CF 3         B-101   CH 3     Cl   H   CH 3     CF 3         B-102   CF 3     Cl   H   CH 3     CF 3         B-103   OCH 3     Cl   H   CH 3     CF 3         B-104   OCF 3     Cl   H   CH 3     CF 3         B-105   H   CH 3     H   CH 3     CF 3         B-106   F   CH 3     H   CH 3     CF 3         B-107   Cl   CH 3     H   CH 3     CF 3         B-108   Br   CH 3     H   CH 3     CF 3         B-109   CH 3     CH 3     H   CH 3     CF 3         B-110   CF 3     CH 3     H   CH 3     CF 3         B-111   OCH 3     CH 3     H   CH 3     CF 3         B-112   OCF 3     CH 3     H   CH 3     CF 3         B-113   H   CH 3     CH 3     CH 3     CF 3         B-114   F   CH 3     CH 3     CH 3     CF 3         B-115   Cl   CH 3     CH 3     CH 3     CF 3         B-116   Br   CH 3     CH 3     CH 3     CF 3         B-117   CH 3     CH 3     CH 3     CH 3     CF 3         B-118   CF 3     CH 3     CH 3     CH 3     CF 3         B-119   OCH 3     CH 3     CH 3     CH 3     CF 3         B-120   OCF 3     CH 3     CH 3     CH 3     CF 3         B-121   H   H   H   CF 3     CF 3         B-122   F   H   H   CF 3     CF 3         B-123   Cl   H   H   CF 3     CF 3         B-124   Br   H   H   CF 3     CF 3         B-125   CH 3     H   H   CF 3     CF 3         B-126   CF 3     H   H   CF 3     CF 3         B-127   OCH 3     H   H   CF 3     CF 3         B-128   OCF 3     H   H   CF 3     CF 3         B-129   H   F   H   CF 3     CF 3         B-130   F   F   H   CF 3     CF 3         B-131   Cl   F   H   CF 3     CF 3         B-132   Br   F   H   CF 3     CF 3         B-133   CH 3     F   H   CF 3     CF 3         B-134   CF 3     F   H   CF 3     CF 3         B-135   OCH 3     F   H   CF 3     CF 3         B-136   OCF 3     F   H   CF 3     CF 3         B-137   H   Cl   H   CF 3     CF 3         B-138   F   Cl   H   CF 3     CF 3         B-139   Cl   Cl   H   CF 3     CF 3         B-140   Br   Cl   H   CF 3     CF 3         B-141   CH 3     Cl   H   CF 3     CF 3         B-142   CF 3     Cl   H   CF 3     CF 3         B-143   OCH 3     Cl   H   CF 3     CF 3         B-144   OCF 3     Cl   H   CF 3     CF 3         B-145   H   CH 3     H   CF 3     CF 3         B-146   F   CH 3     H   CF 3     CF 3         B-147   Cl   CH 3     H   CF 3     CF 3         B-148   Br   CH 3     H   CF 3     CF 3         B-149   CH 3     CH 3     H   CF 3     CF 3         B-150   CF 3     CH 3     H   CF 3     CF 3         B-151   OCH 3     CH 3     H   CF 3     CF 3         B-152   OCF 3     CH 3     H   CF 3     CF 3         B-153   H   CH 3     CH 3     CF 3     CF 3         B-154   F   CH 3     CH 3     CF 3     CF 3         B-155   Cl   CH 3     CH 3     CF 3     CF 3         B-156   Br   CH 3     CH 3     CF 3     CF 3         B-157   CH 3     CH 3     CH 3     CF 3     CF 3         B-158   CF 3     CH 3     CH 3     CF 3     CF 3         B-159   OCH 3     CH 3     CH 3     CF 3     CF 3         B-160   OCF 3     CH 3     CH 3     CF 3     CF 3         B-161   H   H   H   CH 3     C 6 H 5 *       B-162   F   H   H   CH 3     C 6 H 5         B-163   Cl   H   H   CH 3     C 6 H 5         B-164   Br   H   H   CH 3     C 6 H 5         B-165   CH 3     H   H   CH 3     C 6 H 5         B-166   CF 3     H   H   CH 3     C 6 H 5         B-167   OCH 3     H   H   CH 3     C 6 H 5         B-168   OCF 3     H   H   CH 3     C 6 H 5         B-169   H   F   H   CH 3     C 6 H 5         B-170   F   F   H   CH 3     C 6 H 5         B-171   Cl   F   H   CH 3     C 6 H 5         B-172   Br   F   H   CH 3     C 6 H 5         B-173   CH 3     F   H   CH 3     C 6 H 5         B-174   CF 3     F   H   CH 3     C 6 H 5         B-175   OCH 3     F   H   CH 3     C 6 H 5         B-176   OCF 3     F   H   CH 3     C 6 H 5         B-177   H   Cl   H   CH 3     C 6 H 5         B-178   F   Cl   H   CH 3     C 6 H 5         B-179   Cl   Cl   H   CH 3     C 6 H 5         B-180   Br   Cl   H   CH 3     C 6 H 5         B-181   CH 3     Cl   H   CH 3     C 6 H 5         B-182   CF 3     Cl   H   CH 3     C 6 H 5         B-183   OCH 3     Cl   H   CH 3     C 6 H 5         B-184   OCF 3     Cl   H   CH 3     C 6 H 5         B-185   H   CH 3     H   CH 3     C 6 H 5         B-186   F   CH 3     H   CH 3     C 6 H 5         B-187   Cl   CH 3     H   CH 3     C 6 H 5         B-188   Br   CH 3     H   CH 3     C 6 H 5         B-189   CH 3     CH 3     H   CH 3     C 6 H 5         B-190   CF 3     CH 3     H   CH 3     C 6 H 5         B-191   OCH 3     CH 3     H   CH 3     C 6 H 5         B-192   OCF 3     CH 3     H   CH 3     C 6 H 5         B-193   H   CH 3     CH 3     CH 3     C 6 H 5         B-194   F   CH 3     CH 3     CH 3     C 6 H 5         B-195   Cl   CH 3     CH 3     CH 3     C 6 H 5         B-196   Br   CH 3     CH 3     CH 3     C 6 H 5         B-197   CH 3     CH 3     CH 3     CH 3     C 6 H 5         B-198   CF 3     CH 3     CH 3     CH 3     C 6 H 5         B-199   OCH 3     CH 3     CH 3     CH 3     C 6 H 5         B-200   OCF 3     CH 3     CH 3     CH 3     C 6 H 5         B-201   H   H   H   CH 3     OCH 3         B-202   F   H   H   CH 3     OCH 3         B-203   Cl   H   H   CH 3     OCH 3         B-204   Br   H   H   CH 3     OCH 3         B-205   CH 3     H   H   CH 3     OCH 3         B-206   CF 3     H   H   CH 3     OCH 3         B-207   OCH 3     H   H   CH 3     OCH 3         B-208   OCF 3     H   H   CH 3     OCH 3         B-209   H   F   H   CH 3     OCH 3         B-210   F   F   H   CH 3     OCH 3         B-211   Cl   F   H   CH 3     OCH 3         B-212   Br   F   H   CH 3     OCH 3         B-213   CH 3     F   H   CH 3     OCH 3         B-214   CF 3     F   H   CH 3     OCH 3         B-215   OCH 3     F   H   CH 3     OCH 3         B-216   OCF 3     F   H   CH 3     OCH 3         B-217   H   Cl   H   CH 3     OCH 3         B-218   F   Cl   H   CH 3     OCH 3         B-219   Cl   Cl   H   CH 3     OCH 3         B-220   Br   Cl   H   CH 3     OCH 3         B-221   CH 3     Cl   H   CH 3     OCH 3         B-222   CF 3     Cl   H   CH 3     OCH 3         B-223   OCH 3     Cl   H   CH 3     OCH 3         B-224   OCF 3     Cl   H   CH 3     OCH 3         B-225   H   CH 3     H   CH 3     OCH 3         B-226   F   CH 3     H   CH 3     OCH 3         B-227   Cl   CH 3     H   CH 3     OCH 3         B-228   Br   CH 3     H   CH 3     OCH 3         B-229   CH 3     CH 3     H   CH 3     OCH 3         B-230   CF 3     CH 3     H   CH 3     OCH 3         B-231   OCH 3     CH 3     H   CH 3     OCH 3         B-232   OCH 3     CH 3     H   CH 3     OCH 3         B-233   H   CH 3     CH 3     CH 3     OCH 3         B-234   F   CH 3     CH 3     CH 3     OCH 3         B-235   Cl   CH 3     CH 3     CH 3     OCH 3         B-236   Br   CH 3     CH 3     CH 3     OCH 3         B-237   CH 3     CH 3     CH 3     CH 3     OCH 3         B-238   CF 3     CH 3     CH 3     CH 3     OCH 3         B-239   OCH 3     CH 3     CH 3     CH 3     OCH 3         B-240   OCF 3     CH 3     CH 3     CH 3     OCH 3         B-241   H   H   H   CH 3     OH       B-242   Fv   H   H   CH 3     OH       B-243   Cl   H   H   CH 3     OH       B-244   Br   H   H   CH 3     OH       B-245   CH 3     H   H   CH 3     OH       B-246   CF 3     H   H   CH 3     OH       B-247   OCH 3     H   H   CH 3     OH       B-248   OCF 3     H   H   CH 3     OH       B-249   H   F   H   CH 3     OH       B-250   F   F   H   CH 3     OH       B-251   Cl   F   H   CH 3     OH       B-252   Br   F   H   CH 3     OH       B-253   CH 3     F   H   CH 3     OH       B-254   CF 3     F   H   CH 3     OH       B-255   OCH 3     F   H   CH 3     OH       B-256   OCF 3     F   H   CH 3     OH       B-257   H   Cl   H   CH 3     OH       B-258   F   Cl   H   CH 3     OH       B-259   Cl   Cl   H   CH 3     OH       B-260   Br   Cl   H   CH 3     OH       B-261   CH 3     Cl   H   CH 3     OH       B-262   CF 3     Cl   H   CH 3     OH       B-263   OCH 3     Cl   H   CH 3     OH       B-264   OCF 3     Cl   H   CH 3     OH       B-265   H   CH 3     H   CH 3     OH       B-266   F   CH 3     H   CH 3     OH       B-267   Cl   CH 3     H   CH 3     OH       B-268   Br   CH 3     H   CH 3     OH       B-269   CH 3     CH 3     H   CH 3     OH       B-270   CF 3     CH 3     H   CH 3     OH       B-271   OCH 3     CH 3     H   CH 3     OH       B-272   OCF 3     CH 3     H   CH 3     OH       B-273   H   CH 3     CH 3     CH 3     OH       B-274   F   CH 3     CH 3     CH 3     OH       B-275   Cl   CH 3     CH 3     CH 3     OH       B-276   Br   CH 3     CH 3     CH 3     OH       B-277   CH 3     CH 3     CH 3     CH 3     OH       B-278   CF 3     CH 3     CH 3     CH 3     OH       B-279   OCH 3     CH 3     CH 3     CH 3     OH       B-280   OCF 3     CH 3     CH 3     CH 3     OH                                 B-281   H   H   H   —(CH 2 ) 2 —       B-282   F   H   H   —(CH 2 ) 2 —       B-283   Cl   H   H   —(CH 2 ) 2 —       B-284   Br   H   H   —(CH 2 ) 2 —       B-285   CH 3     H   H   —(CH 2 ) 2 —       B-286   CF 3     H   H   —(CH 2 ) 2 —       B-287   OCH 3     H   H   —(CH 2 ) 2 —       B-288   OCF 3     H   H   —(CH 2 ) 2 —       B-289   H   F   H   —(CH 2 ) 2 —       B-290   F   F   H   —(CH 2 ) 2 —       B-291   Cl   F   H   —(CH 2 ) 2 —       B-292   Br   F   H   —(CH 2 ) 2 —       B-293   CH 3     F   H   —(CH 2 ) 2 —       B-294   CF 3     F   H   —(CH 2 ) 2 —       B-295   OCH 3     F   H   —(CH 2 ) 2 —       B-296   OCF 3     F   H   —(CH 2 ) 2 —       B-297   H   Cl   H   —(CH 2 ) 2 —       B-298   F   Cl   H   —(CH 2 ) 2 —       B-299   Cl   Cl   H   —(CH 2 ) 2 —       B-300   Br   Cl   H   —(CH 2 ) 2 —       B-301   CH 3     Cl   H   —(CH 2 ) 2 —       B-302   CF 3     Cl   H   —(CH 2 ) 2 —       B-303   OCH 3     Cl   H   —(CH 2 ) 2 —       B-304   OCF 3     Cl   H   —(CH 2 ) 2 —       B-305   H   CH 3     H   —(CH 2 ) 2 —       B-306   F   CH 3     H   —(CH 2 ) 2 —       B-307   Cl   CH 3     H   —(CH 2 ) 2 —       B-308   Br   CH 3     H   —(CH 2 ) 2 —       B-309   CH 3     CH 3     H   —(CH 2 ) 2 —       B-310   CF 3     CH 3     H   —(CH 2 ) 2 —       B-311   OCH 3     CH 3     H   —(CH 2 ) 2 —       B-312   OCF 3     CH 3     H   —(CH 2 ) 2 —       B-313   H   CH 3     CH 3     —(CH 2 ) 2 —       B-314   F   CH 3     CH 3     —(CH 2 ) 2 —       B-315   Cl   CH 3     CH 3     —(CH 2 ) 2 —       B-316   Br   CH 3     CH 3     —(CH 2 ) 2 —       B-317   CH 3     CH 3     CH 3     —(CH 2 ) 2 —       B-318   CF 3     CH 3     CH 3     —(CH 2 ) 2 —       B-319   OCH 3     CH 3     CH 3     —(CH 2 ) 2 —       B-320   OCF 3     CH 3     CH 3     —(CH 2 ) 2 —       B-321   H   H   H   —(CH 2 ) 3 —       B-322   F   H   H   —(CH 2 ) 3 —       B-323   Cl   H   H   —(CH 2 ) 3 —       B-324   Br   H   H   —(CH 2 ) 3 —       B-325   CH 3     H   H   —(CH 2 ) 3 —       B-326   CF 3     H   H   —(CH 2 ) 3 —       B-327   OCH 3     H   H   —(CH 2 ) 3 —       B-328   OCF 3     H   H   —(CH 2 ) 3 —       B-329   H   F   H   —(CH 2 ) 3 —       B-330   F   F   H   —(CH 2 ) 3 —       B-331   Cl   F   H   —(CH 2 ) 3 —       B-332   Br   F   H   —(CH 2 ) 3 —       B-333   CH 3     F   H   —(CH 2 ) 3 —       B-334   CF 3     F   H   —(CH 2 ) 3 —       B-335   OCH 3     F   H   —(CH 2 ) 3 —       B-336   OCF 3     F   H   —(CH 2 ) 3 —       B-337   H   Cl   H   —(CH 2 ) 3 —       B-338   F   Cl   H   —(CH 2 ) 3 —       B-339   Cl   Cl   H   —(CH 2 ) 3 —       B-340   Br   Cl   H   —(CH 2 ) 3 —       B-341   CH 3     Cl   H   —(CH 2 ) 3 —       B-342   CF 3     Cl   H   —(CH 2 ) 3 —       B-343   OCH 3     Cl   H   —(CH 2 ) 3 —       B-344   OCF 3     Cl   H   —(CH 2 ) 3 —       B-345   H   CH 3     H   —(CH 2 ) 3 —       B-346   F   CH 3     H   —(CH 2 ) 3 —       B-347   Cl   CH 3     H   —(CH 2 ) 3 —       B-348   Br   CH 3     H   —(CH 2 ) 3 —       B-349   CH 3     CH 3     H   —(CH 2 ) 3 —       B-350   CF 3     CH 3     H   —(CH 2 ) 3 —       B-351   OCH 3     CH 3     H   —(CH 2 ) 3 —       B-352   OCF 3     CH 3     H   —(CH 2 ) 3 —       B-353   H   CH 3     CH 3     —(CH 2 ) 3 —       B-354   F   CH 3     CH 3     —(CH 2 ) 3 —       B-355   Cl   CH 3     CH 3     —(CH 2 ) 3 —       B-356   Br   CH 3     CH 3     —(CH 2 ) 3 —       B-357   CH 3     CH 3     CH 3     —(CH 2 ) 3 —       B-358   CF 3     CH 3     CH 3     —(CH 2 ) 3 —       B-359   OCH 3     CH 3     CH 3     —(CH 2 ) 3 —       B-360   OCF 3     CH 3     CH 3     —(CH 2 ) 3 —       B-361   H   H   H   —(CH 2 ) 4 —       B-362   F   H   H   —(CH 2 ) 4 —       B-363   Cl   H   H   —(CH 2 ) 4 —       B-364   Br   H   H   —(CH 2 ) 4 —       B-365   CH 3     H   H   —(CH 2 ) 4 —       B-366   CF 3     H   H   —(CH 2 ) 4 —       B-367   OCH 3     H   H   —(CH 2 ) 4 —       B-368   OCF 3     H   H   —(CH 2 ) 4 —       B-369   H   F   H   —(CH 2 ) 4 —       B-370   F   F   H   —(CH 2 ) 4 —       B-371   Cl   F   H   —(CH 2 ) 4 —       B-372   Br   F   H   —(CH 2 ) 4 —       B-373   CH 3     F   H   —(CH 2 ) 4 —       B-374   CF 3     F   H   —(CH 2 ) 4 —       B-375   OCH 3     F   H   —(CH 2 ) 4 —       B-376   OCF 3     F   H   —(CH 2 ) 4 —       B-377   H   Cl   H   —(CH 2 ) 4 —       B-378   F   Cl   H   —(CH 2 ) 4 —       B-379   Cl   Cl   H   —(CH 2 ) 4 —       B-380   Br   Cl   H   —(CH 2 ) 4 —       B-381   CH 3     Cl   H   —(CH 2 ) 4 —       B-382   CF 3     Cl   H   —(CH 2 ) 4 —       B-383   OCH 3     Cl   H   —(CH 2 ) 4 —       B-384   OCF 3     Cl   H   —(CH 2 ) 4 —       B-385   H   CH 3     H   —(CH 2 ) 4 —       B-386   F   CH 3     H   —(CH 2 ) 4 —       B-387   Cl   CH 3     H   —(CH 2 ) 4 —       B-388   Br   CH 3     H   —(CH 2 ) 4 —       B-389   CH 3     CH 3     H   —(CH 2 ) 4 —       B-390   CF 3     CH 3     H   —(CH 2 ) 4 —       B-391   OCH 3     CH 3     H   —(CH 2 ) 4 —       B-392   OCF 3     CH 3     H   —(CH 2 ) 4 —       B-393   H   CH 3     CH 3     —(CH 2 ) 4 —       B-394   F   CH 3     CH 3     —(CH 2 ) 4 —       B-395   Cl   CH 3     CH 3     —(CH 2 ) 4 —       B-396   Br   CH 3     CH 3     —(CH 2 ) 4 —       B-397   CH 3     CH 3     CH 3     —(CH 2 ) 4 —       B-398   CF 3     CH 3     CH 3     —(CH 2 ) 4 —       B-399   OCH 3     CH 3     CH 3     —(CH 2 ) 4 —       B-400   OCF 3     CH 3     CH 3     —(CH 2 ) 4 —       B-401   H   H   H   —(CH 2 ) 5 —       B-402   F   H   H   —(CH 2 ) 5 —       B-403   Cl   H   H   —(CH 2 ) 5 —       B-404   Br   H   H   —(CH 2 ) 5 —       B-405   CH 3     H   H   —(CH 2 ) 5 —       B-406   CF 3     H   H   —(CH 2 ) 5 —       B-407   OCH 3     H   H   —(CH 2 ) 5 —       B-408   OCF 3     H   H   —(CH 2 ) 5 —       B-409   H   F   H   —(CH 2 ) 5 —       B-410   F   F   H   —(CH 2 ) 5 —       B-411   Cl   F   H   —(CH 2 ) 5 —       B-412   Br   F   H   —(CH 2 ) 5 —       B-413   CH 3     F   H   —(CH 2 ) 5 —       B-414   CF 3     F   H   —(CH 2 ) 5 —       B-415   OCH 3     F   H   —(CH 2 ) 5 —       B-416   OCF 3     F   H   —(CH 2 ) 5 —       B-417   H   Cl   H   —(CH 2 ) 5 —       B-418   F   Cl   H   —(CH 2 ) 5 —       B-419   Cl   Cl   H   —(CH 2 ) 5 —       B-420   Br   Cl   H   —(CH 2 ) 5 —       B-421   CH 3     Cl   H   —(CH 2 ) 5 —       B-422   CF 3     Cl   H   —(CH 2 ) 5 —       B-423   OCH 3     Cl   H   —(CH 2 ) 5 —       B-424   OCF 3     Cl   H   —(CH 2 ) 5 —       B-425   H   CH 3     H   —(CH 2 ) 5 —       B-426   F   CH 3     H   —(CH 2 ) 5 —       B-427   Cl   CH 3     H   —(CH 2 ) 5 —       B-428   Br   CH 3     H   —(CH 2 ) 5 —       B-429   CH 3     CH 3     H   —(CH 2 ) 5 —       B-430   CF 3     CH 3     H   —(CH 2 ) 5 —       B-431   OCH 3     CH 3     H   —(CH 2 ) 5 —       B-432   OCF 3     CH 3     H   —(CH 2 ) 5 —       B-433   H   CH 3     CH 3     —(CH 2 ) 5 —       B-434   F   CH 3     CH 3     —(CH 2 ) 5 —       B-435   Cl   CH 3     CH 3     —(CH 2 ) 5 —       B-436   Br   CH 3     CH 3     —(CH 2 ) 5 —       B-437   CH 3     CH 3     CH 3     —(CH 2 ) 5 —       B-438   CF 3     CH 3     CH 3     —(CH 2 ) 5 —       B-439   OCH 3     CH 3     CH 3     —(CH 2 ) 5 —       B-440   OCF 3     CH 3     CH 3     —(CH 2 ) 5 —       B-441   H   H   H   —(CH 2 ) 6 —       B-442   F   H   H   —(CH 2 ) 6 —       B-443   Cl   H   H   —(CH 2 ) 6 —       B-444   Br   H   H   —(CH 2 ) 6 —       B-445   CH 3     H   H   —(CH 2 ) 6 —       B-446   CF 3     H   H   —(CH 2 ) 6 —       B-447   OCH 3     H   H   —(CH 2 ) 6 —       B-448   OCF 3     H   H   —(CH 2 ) 6 —       B-449   H   F   H   —(CH 2 ) 6 —       B-450   F   F   H   —(CH 2 ) 6 —       B-451   Cl   F   H   —(CH 2 ) 6 —       B-452   Br   F   H   —(CH 2 ) 6 —       B-453   CH 3     F   H   —(CH 2 ) 6 —       B-454   CF 3     F   H   —(CH 2 ) 6 —       B-455   OCH 3     F   H   —(CH 2 ) 6 —       B-456   OCF 3     F   H   —(CH 2 ) 6 —       B-457   H   Cl   H   —(CH 2 ) 6 —       B-458   F   Cl   H   —(CH 2 ) 6 —       B-459   Cl   Cl   H   —(CH 2 ) 6 —       B-460   Br   Cl   H   —(CH 2 ) 6 —       B-461   CH 3     Cl   H   —(CH 2 ) 6 —       B-462   CF 3     Cl   H   —(CH 2 ) 6 —       B-463   OCH 3     Cl   H   —(CH 2 ) 6 —       B-464   OCF 3     Cl   H   —(CH 2 ) 6 —       B-465   H   CH 3     H   —(CH 2 ) 6 —       B-466   F   CH 3     H   —(CH 2 ) 6 —       B-467   Cl   CH 3     H   —(CH 2 ) 6 —       B-468   Br   CH 3     H   —(CH 2 ) 6 —       B-469   CH 3     CH 3     H   —(CH 2 ) 6 —       B-470   CF 3     CH 3     H   —(CH 2 ) 6 —       B-471   OCH 3     CH 3     H   —(CH 2 ) 6 —       B-472   OCF 3     CH 3     H   —(CH 2 ) 6 —       B-473   H   CH 3     CH 3     —(CH 2 ) 6 —       B-474   F   CH 3     CH 3     —(CH 2 ) 6 —       B-475   Cl   CH 3     CH 3     —(CH 2 ) 6 —       B-476   Br   CH 3     CH 3     —(CH 2 ) 6 —       B-477   CH 3     CH 3     CH 3     —(CH 2 ) 6 —       B-478   CF 3     CH 3     CH 3     —(CH 2 ) 6 —       B-479   OCH 3     CH 3     CH 3     —(CH 2 ) 6 —       B-480   OCF 3     CH 3     CH 3     —(CH 2 ) 6 —       B-481   H   H   H   —CH═CH—CH 2 —CH 2 —       B-482   F   H   H   —CH═CH—CH 2 —CH 2 —       B-483   Cl   H   H   —CH═CH—CH 2 —CH 2 —       B-484   Br   H   H   —CH═CH—CH 2 —CH 2 —       B-485   CH 3     H   H   —CH═CH—CH 2 —CH 2 —       B-486   CF 3     H   H   —CH═CH—CH 2 —CH 2 —       B-487   OCH 3     H   H   —CH═CH—CH 2 —CH 2 —       B-488   OCF 3     H   H   —CH═CH—CH 2 —CH 2 —       B-489   H   F   H   —CH═CH—CH 2 —CH 2 —       B-490   F   F   H   —CH═CH—CH 2 —CH 2 —       B-491   Cl   F   H   —CH═CH—CH 2 —CH 2 —       B-492   Br   F   H   —CH═CH—CH 2 —CH 2 —       B-493   CH 3     F   H   —CH═CH—CH 2 —CH 2 —       B-494   CF 3     F   H   —CH═CH—CH 2 —CH 2 —       B-495   OCH 3     F   H   —CH═CH—CH 2 —CH 2 —       B-496   OCF 3     F   H   —CH═CH—CH 2 —CH 2 —       B-497   H   Cl   H   —CH═CH—CH 2 —CH 2 —       B-498   F   Cl   H   —CH═CH—CH 2 —CH 2 —       B-499   Cl   Cl   H   —CH═CH—CH 2 —CH 2 —       B-500   Br   Cl   H   —CH═CH—CH 2 —CH 2 —       B-501   CH 3     Cl   H   —CH═CH—CH 2 —CH 2 —       B-502   CF 3     Cl   H   —CH═CH—CH 2 —CH 2 —       B-503   OCH 3     Cl   H   —CH═CH—CH 2 —CH 2 —       B-504   OCF 3     Cl   H   —CH═CH—CH 2 —CH 2 —       B-505   H   CH 3     H   —CH═CH—CH 2 —CH 2 —       B-506   F   CH 3     H   —CH═CH—CH 2 —CH 2 —       B-507   Cl   CH 3     H   —CH═CH—CH 2 —CH 2 —       B-508   Br   CH 3     H   —CH═CH—CH 2 —CH 2 —       B-509   CH 3     CH 3     H   —CH═CH—CH 2 —CH 2 —       B-510   CF 3     CH 3     H   —CH═CH—CH 2 —CH 2 —       B-511   OCH 3     CH 3     H   —CH═CH—CH 2 —CH 2 —       B-512   OCF 3     CH 3     H   —CH═CH—CH 2 —CH 2 —       B-513   H   CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-514   F   CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-515   Cl   CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-516   Br   CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-517   CH 3     CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-518   CF 3     CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-519   OCH 3     CH 3     CH 3     —CH═CH—CH 2 —CH 2 —       B-520   OCF 3     CH 3     CH 3     —CH═CH—CH 2 —CH 2 —                                 B-521   H   H   —(CH 2 ) 3 —   CH 3         B-522   F   H   —(CH 2 ) 3 —   CH 3         B-523   Cl   H   —(CH 2 ) 3 —   CH 3         B-524   Br   H   —(CH 2 ) 3 —   CH 3         B-525   CH 3     H   —(CH 2 ) 3 —   CH 3         B-526   CF 3     H   —(CH 2 ) 3 —   CH 3         B-527   OCH 3     H   —(CH 2 ) 3 —   CH 3         B-528   OCF 3     H   —(CH 2 ) 3 —   CH 3         B-529   H   D   —(CH 2 ) 3 —   CH 3         B-530   F   D   —(CH 2 ) 3 —   CH 3         B-531   Cl   D   —(CH 2 ) 3 —   CH 3         B-532   Br   D   —(CH 2 ) 3 —   CH 3         B-533   CH 3     D   —(CH 2 ) 3 —   CH 3         B-534   CF 3     D   —(CH 2 ) 3 —   CH 3         B-535   OCH 3     D   —(CH 2 ) 3 —   CH 3         B-536   OCF 3     D   —(CH 2 ) 3 —   CH 3         B-537   H   H   —(CH 2 ) 3 —   D       B-538   F   H   —(CH 2 ) 3 —   D       B-539   Cl   H   —(CH 2 ) 3 —   D       B-540   Br   H   —(CH 2 ) 3 —   D       B-541   CH 3     H   —(CH 2 ) 3 —   D       B-542   CF 3     H   —(CH 2 ) 3 —   D       B-543   OCH 3     H   —(CH 2 ) 3 —   D       B-544   OCF 3     H   —(CH 2 ) 3 —   D       B-545   H   D   —(CH 2 ) 3 —   D       B-546   F   D   —(CH 2 ) 3 —   D       B-547   Cl   D   —(CH 2 ) 3 —   D       B-548   Br   D   —(CH 2 ) 3 —   D       B-549   CH 3     D   —(CH 2 ) 3 —   D       B-550   CF 3     D   —(CH 2 ) 3 —   D       B-551   OCH 3     D   —(CH 2 ) 3 —   D       B-552   OCF 3     D   —(CH 2 ) 3 —   D       B-553   H   H   —(CH 2 ) 4 —   CH 3         B-554   F   H   —(CH 2 ) 4 —   CH 3         B-555   Cl   H   —(CH 2 ) 4 —   CH 3         B-556   Br   H   —(CH 2 ) 4 —   CH 3         B-557   CH 3     H   —(CH 2 ) 4 —   CH 3         B-558   CF 3     H   —(CH 2 ) 4 —   CH 3         B-559   OCH 3     H   —(CH 2 ) 4 —   CH 3         B-560   OCF 3     H   —(CH 2 ) 4 —   CH 3         B-561   H   D   —(CH 2 ) 4 —   CH 3         B-562   F   D   —(CH 2 ) 4 —   CH 3         B-563   Cl   D   —(CH 2 ) 4 —   CH 3         B-564   Br   D   —(CH 2 ) 4 —   CH 3         B-565   CH 3     D   —(CH 2 ) 4 —   CH 3         B-566   CF 3     D   —(CH 2 ) 4 —   CH 3         B-567   OCH 3     D   —(CH 2 ) 4 —   CH 3         B-568   OCF 3     D   —(CH 2 ) 4 —   CH 3         B-569   H   H   —(CH 2 ) 4 —   D       B-570   F   H   —(CH 2 ) 4 —   D       B-571   Cl   H   —(CH 2 ) 4 —   D       B-572   Br   H   —(CH 2 ) 4 —   D       B-573   CH 3     H   —(CH 2 ) 4 —   D       B-574   CF 3     H   —(CH 2 ) 4 —   D       B-575   OCH 3     H   —(CH 2 ) 4 —   D       B-576   OCF 3     H   —(CH 2 ) 4 —   D       B-577   H   D   —(CH 2 ) 4 —   D       B-578   F   D   —(CH 2 ) 4 —   D       B-579   Cl   D   —(CH 2 ) 4 —   D       B-580   Br   D   —(CH 2 ) 4 —   D       B-581   CH 3     D   —(CH 2 ) 4 —   D       B-582   CF 3     D   —(CH 2 ) 4 —   D       B-583   OCH 3     D   —(CH 2 ) 4 —   D       B-584   OCF 3     D   —(CH 2 ) 4 —   D               *C 6 H 5  = phenyl            
In a specific embodiment, the invention relates to compounds I selected from the compounds of the examples, either in form of free bases or of any pharmaceutically acceptable salt thereof or a steroisomer thereof.
 
     The compounds of the present invention can be prepared by using routine techniques familiar to a skilled person. In particular, the compounds of the formula I can be prepared according to the following schemes, wherein the variables, if not stated otherwise, are as defined above. 
     Compounds of formula I wherein X is CR 7 R 8  and R 5b  is H (=compounds I′) can be synthesized as described in scheme 1 below. The protected tetrahydrobenzodiazepine or tetrahydroquinoxaline 1, wherein Z is a hydrogen or a halogen atom, such as Cl, Br or I and PG is a common protective group, such as a carbamate, especially boc, is acylated with the acrylic acid derivative 2, wherein LG is an appropriate leaving group, such as Cl or an anhydride or a chloroformate, in the presence of a base, such as triethylamine or Hünig&#39;s base, in an organic solvent, such as ether or methylene chloride. Reaction of 3 with a Lewis acid or a Brönstedt acid HA or irradiation with a suitable wavelength commonly derived from a mercury lamp in an adequate solvent, such as acetone or toluene, in a common photoreactor yields cyclization to 4. Reduction of the carbonyl group with common reduction agents like borohydrides such as sodium borohydride or borane-tetrahydrofurane-complex yields 5, which is deprotected using suitable reagents such as strong bases or acids to I′, wherein R 4a  and R 4b  and R 5b  are H. Compounds I wherein R 4a  and R 4b  form together ═O can be obtained by skipping the reduction step to 5 and deprotecting 4. 
     
       
         
         
             
             
         
       
     
     If desired, substituents R 1  different from hydrogen can be introduced for example via alkylation under typical conditions such as stirring in an appropriate solvent in the presence of an alkylhalide and a base or via other common substitution reactions. 
     Compounds I wherein R 5b  is different from H can be prepared, for example, by reacting compound 4 with a compound LG-R 5b  in the presence of a base, wherein LG is an appropriate leaving group, such as Cl or Br. 
     Compounds I wherein R 5b  is different from H and R 8  is CH 3  (=compounds I″) can be prepared, for example, as out lined in scheme 2 below. Acylation of 1 with the allylic acid derivative 6, wherein LG is an appropriate leaving group, such as Cl or an anhydride or a chloroformate, in the presence of a base, such as triethylamine or Hünig&#39;s base, in an organic solvent, such as ether or methylene chloride, yields 7, which is reacted in a Heck-type reaction, e.g. employing palladium acetate in the presence of a base, such as potassium carbonate, to yield the cyclization product 8. Reduction of the carbonyl group with common reduction agents like borohydrides such as sodium borohydride or borane-tetrahydrofurane-complex yields 9, which is deprotected using suitable reagents such as strong bases or acids to I″, wherein R 4a  and R 4b  are H. Compounds I wherein R 4a  and R 4b  form together ═O can be obtained by skipping the reduction step to 9 and deprotecting 8. If desired, substituents R 1  different from hydrogen can be introduced for example via alkylation under typical conditions such as stirring in an appropriate solvent in the presence of an alkylhalide and a base or via other common substitution reactions. 
     
       
         
         
             
             
         
       
     
     Compounds I wherein X is NR 6  (=compounds I′″) can be prepared as outlined in scheme 3 below. Acylation of 1 with the β-amino acid derivative 10, wherein PG′ is a protection group different from PG and LG is an appropriate leaving group, such as Cl or an anhydride or a chloroformate, in the presence of a base, such as triethylamine or Hünig&#39;s base, in an organic solvent, such as ether or methylene chloride, yields 11. This is first selectively deprotected at the amino group NR 6 PG′. The partially deprotected compound is then reacted in a cyclization reaction to 12 under Buchwald-Hartwig reaction conditions such as the use of a Pd catalyst, e.g. tetrakis(triphenylphosphine) palladium in the presence of as base, such as sodium tert-butylate and potassium carbonate. Reduction of the carbonyl group of 12 with common reduction agents like borohydrides such as sodium borohydride or borane-tetrahydrofurane-complex yields 13, which is deprotected using suitable reagents such as strong bases or acids to I′″, wherein R 4a  and R 4b  are H. Compounds I wherein R 4a  and R 4b  form together ═O can be obtained by skipping the reduction step to 13 and deprotecting 12. If desired, substituents R 1  different from hydrogen can be introduced for example via alkylation under typical conditions such as stirring in an appropriate solvent in the presence of an alkylhalide and a base or via other common substitution reactions. 
     
       
         
         
             
             
         
       
     
     Alternatively to the method depicted in scheme 1, compounds I wherein X is CR 7 R 8  and R 5b  is H (=compounds I′) can be synthesized as described in scheme 4 below. Readily available anilines 14 are derivatized with carbonyl moieties 15 by acylation procedures employing appropriate leaving groups LG, such as chlorides or anhydrides, in the presence of a base such as triethylamine or Hünig&#39;s base, in an organic solvent, such as diethyl ether or methylene chloride to yield 16. Cyclization products 17 are received by irradiation with a suitable wavelength commonly derived from a mercury lamp in an adequate solvent such as acetone or toluene in a common photoreactor known to those skilled in the art. Reduction with common reduction agents like borohydrides such as sodium borohydride or borane-tetrahydrofurane-complex yield suitable intermediates 18 that are alkylated with alkylamides 19 employing suitable leaving groups LG such as chlorides or bromides. After reduction to the corresponding amines 20 cyclization is performed in a suitable solvent like acetonitrile or methanol at room temperature or higher temperature by addition of an acid and substituted ketones or aldehydes to obtain compounds I′. 
     
       
         
         
             
             
         
       
       
         
         
             
             
         
       
     
     Alternatively to the method depicted in scheme 3, compounds I wherein X is NR 6  (=compounds I′″) can be prepared as outlined in scheme 5 below. 
     Readily available starting materials 22 are alkylated with alkylamides 19 employing suitable leaving groups LG such as chlorides or bromides to give 23. After reduction to the corresponding amines 24 cyclization is performed in a suitable solvent like acetonitrile or methanol at room temperature or higher temperature by addition of an acid and substituted ketones or aldehydes 21 to obtain compounds I′″. 
     
       
         
         
             
             
         
       
     
     Compounds I wherein R 4a  and R 4b  are not H or do not form together a group ═O can be prepared by standard derivatization methods of compounds wherein R 4a  and R 4b  form together a group ═O. For instance, compounds wherein R 4a  and R 4b  form together a group ═S may be prepared by reaction with a sulfurization agent, such as Lawesson&#39;s reagent or P 2 S 5 . Alkyl and related groups as radicals R 4a  and R 4b  may be introduced via Grignard reduction. Amino and related groups may be introduced via reductive amination. Hydroxyl group R 4a  or R 4b  may be introduced by reducing the carbonyl group. This may be alkylated to yield alkoxy and related groups R 4a  and R 4b  or substituted by diverse groups. 
     If not otherwise indicated, the above-described reactions are generally carried out in a solvent at temperatures between room temperature and the boiling temperature of the solvent employed. Alternatively, the activation energy which is required for the reaction can be introduced into the reaction mixture using microwaves, something which has proved to be of value, in particular, in the case of the reactions catalyzed by transition metals (with regard to reactions using microwaves, see Tetrahedron 2001, 57, p. 9199 ff. p. 9225 ff. and also, in a general manner, “Microwaves in Organic Synthesis”, Andre Loupy (Ed.), Wiley-VCH 2002. 
     The acid addition salts of compounds I are prepared in a customary manner by mixing the free base with a corresponding acid, where appropriate in solution in an organic solvent, for example a lower alcohol, such as methanol, ethanol or propanol, an ether, such as methyl tert-butyl ether or diisopropyl ether, a ketone, such as acetone or methyl ethyl ketone, or an ester, such as ethyl acetate. 
     Routine experimentations, including appropriate manipulation of the reaction conditions, reagents and sequence of the synthetic route, protection of any chemical functionality that may not be compatible with the reaction conditions, and deprotection at a suitable point in the reaction sequence of the preparation methods are within routine techniques. 
     Suitable protecting groups and the methods for protecting and deprotecting different substituents using such suitable protecting groups are well known to those skilled in the art; examples of which may be found in T. Greene and P. Wuts, Protective Groups in Organic Synthesis (3 rd  ed.), John Wiley &amp; Sons, NY (1999), which is herein incorporated by reference in its entirety. Synthesis of the compounds of the invention may be accomplished by methods analogous to those described in the synthetic schemes described hereinabove and in specific examples. 
     Starting materials, if not commercially available, may be prepared by procedures selected from standard organic chemical techniques, techniques that are analogous to the synthesis of known, structurally similar compounds, or techniques that are analogous to the above described schemes or the procedures described in the synthetic examples section. 
     When an optically active form of a compound of the invention is required, it may be obtained by carrying out one of the procedures described herein using an optically active starting material (prepared, for example, by asymmetric induction of a suitable reaction step), or by resolution of a mixture of the stereoisomers of the compound or intermediates using a standard procedure (such as chromatographic separation, recrystallization or enzymatic resolution). 
     Similarly, when a pure geometric isomer of a compound of the invention is required, it may be obtained by carrying out one of the above procedures using a pure geometric isomer as a starting material, or by resolution of a mixture of the geometric isomers of the compound or intermediates using a standard procedure such as chromatographic separation. 
     Moreover, the present invention relates to compounds of formula I as defined above, wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope (e.g., hydrogen by deuterium,  12 C by  13 C,  14 N by  15 N,  16 O by  18 O) and preferably wherein at least one hydrogen atom has been replaced by a deuterium atom. 
     Additionally, the compounds according to the invention include more of the respective isotope than occurs naturally occurs and which is present in compounds I. 
     Stable isotopes (e.g., deuterium,  13 C,  15 N,  18 O) are nonradioactive isotopes which contain one additional neutron than the normally abundant isotope of the respective atom. Deuterated compounds have been used in pharmaceutical research to investigate the in vivo metabolic fate of the compounds by evaluation of the mechanism of action and metabolic pathway of the non deuterated parent compound (Blake et al.  J. Pharm. Sci.  64, 3, 367-391 (1975)). Such metabolic studies are important in the design of safe, effective therapeutic drugs, either because the in vivo active compound administered to the patient or because the metabolites produced from the parent compound prove to be toxic or carcinogenic (Foster et al., Advances in Drug Research Vol. 14, pp. 2-36, Academic press, London, 1985; Kato et al., J.  Labelled Comp. Radiopharmaceut.,  36(10):927-932 (1995); Kushner et al.,  Can. J. Physiol. Pharmacol.,  77, 79-88 (1999)). 
     Incorporation of a heavy atom, particularly substitution of deuterium for hydrogen, can give rise to an isotope effect that could alter the pharmacokinetics of the drug. 
     Stable isotope labeling of a drug can alter its physico-chemical properties such as pK a  and lipid solubility. These changes may influence the fate of the drug at different steps along its passage through the body. Absorption, distribution, metabolism or excretion can be changed. Absorption and distribution are processes that depend primarily on the molecular size and the lipophilicity of the substance. These effects and alterations can affect the pharmacodynamic response of the drug molecule if the isotopic substitution affects a region involved in a ligand-receptor interaction. 
     Drug metabolism can give rise to large isotopic effect if the breaking of a chemical bond to a deuterium atom is the rate limiting step in the process. While some of the physical properties of a stable isotope-labeled molecule are different from those of the unlabeled one, the chemical and biological properties are the same, with one important exception: because of the increased mass of the heavy isotope, any bond involving the heavy isotope and another atom will be stronger than the same bond between the light isotope and that atom. In any reaction in which the breaking of this bond is the rate limiting step, the reaction will proceed slower for the molecule with the heavy isotope due to “kinetic isotope effect”. A reaction involving breaking a C--D bond can be up to 700 percent slower than a similar reaction involving breaking a C—H bond. If the C--D bond is not involved in any of the steps leading to the metabolite, there may not be any effect to alter the behavior of the drug. If a deuterium is placed at a site involved in the metabolism of a drug, an isotope effect will be observed only if breaking of the C--D bond is the rate limiting step. There is evidence to suggest that whenever cleavage of an aliphatic C—H bond occurs, usually by oxidation catalyzed by a mixed-function oxidase, replacement of the hydrogen by deuterium will lead to observable isotope effect. It is also important to understand that the incorporation of deuterium at the site of metabolism slows its rate to the point where another metabolite produced by attack at a carbon atom not substituted by deuterium becomes the major pathway a process called “metabolic switching”. 
     Deuterium tracers, such as deuterium-labeled drugs and doses, in some cases repeatedly, of thousands of milligrams of deuterated water, are also used in healthy humans of all ages, including neonates and pregnant women, without reported incident (e.g. Pons G and Rey E, Pediatrics 1999 104: 633; Coward W A et al., Lancet 1979 7: 13; Schwarcz H P, Control. Clin. Trials 1984 5(4 Suppl): 573; Rodewald L E et al., J. Pediatr. 1989 114: 885; Butte N F et al. Br. J. Nutr. 1991 65: 3; MacLennan A H et al. Am. J. Obstet Gynecol. 1981 139: 948). Thus, it is clear that any deuterium released, for instance, during the metabolism of compounds of this invention poses no health risk. 
     The weight percentage of hydrogen in a mammal (approximately 9%) and natural abundance of deuterium (approximately 0.015%) indicates that a 70 kg human normally contains nearly a gram of deuterium. Furthermore, replacement of up to about 15% of normal hydrogen with deuterium has been effected and maintained for a period of days to weeks in mammals, including rodents and dogs, with minimal observed adverse effects (Czajka D M and Finkel A J, Ann. N.Y. Acad. Sci. 1960 84: 770; Thomson J F, Ann. New York Acad. Sci 1960 84: 736; Czakja D M et al., Am. J. Physiol. 1961 201: 357). Higher deuterium concentrations, usually in excess of 20%, can be toxic in animals. However, acute replacement of as high as 15%-23% of the hydrogen in humans&#39; fluids with deuterium was found not to cause toxicity (Blagojevic N et al. in “Dosimetry &amp; Treatment Planning for Neutron Capture Therapy”, Zamenhof R, Solares G and Harling O Eds. 1994. Advanced Medical Publishing, Madison Wis. pp. 125-134; Diabetes Metab. 23: 251 (1997)). 
     Increasing the amount of deuterium present in a compound above its natural abundance is called enrichment or deuterium-enrichment. Examples of the amount of enrichment include from about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37, 42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96, to about 100 mol %. 
     The hydrogens present on a particular organic compound have different capacities for exchange with deuterium. Certain hydrogen atoms are easily exchangeable under physiological conditions and, if replaced by deuterium atoms, it is expected that they will readily exchange for protons after administration to a patient. Certain hydrogen atoms may be exchanged for deuterium atoms by the action of a deuteric acid such as D 2 SO 4 /D 2 O. Alternatively, deuterium atoms may be incorporated in various combinations during the synthesis of compounds of the invention. Certain hydrogen atoms are not easily exchangeable for deuterium atoms. However, deuterium atoms at the remaining positions may be incorporated by the use of deuterated starting materials or intermediates during the construction of compounds of the invention. 
     Deuterated and deuterium-enriched compounds of the invention can be prepared by using known methods described in the literature. Such methods can be carried out utilizing corresponding deuterated and optionally, other isotope-containing reagents and/or intermediates to synthesize the compounds delineated herein, or invoking standard synthetic protocols known in the art for introducing isotopic atoms to a chemical structure. Relevant procedures and intermediates are disclosed, for instance in Lizondo, J et al.,  Drugs Fut,  21(11), 1116 (1996); Brickner, S J et al.,  J Med Chem,  39(3), 673 (1996); Mallesham, B et al.,  Org Lett,  5(7), 963 (2003); PCT publications WO1997010223, WO2005099353, WO1995007271, WO2006008754; U.S. Pat. Nos. 7,538,189; 7,534,814; 7,531,685; 7,528,131; 7,521,421; 7,514,068; 7,511,013; and US Patent Application Publication Nos. 20090137457; 20090131485; 20090131363; 20090118238; 20090111840; 20090105338; 20090105307; 20090105147; 20090093422; 20090088416; 20090082471, the methods are hereby incorporated by reference. 
     The present invention further relates to a pharmaceutical composition comprising a therapeutically effective amount of at least one compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof, or comprising at least one compound as defined in any of the preceding claims wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope, preferably wherein at least one hydrogen atom has been replaced by a deuterium atom, in combination with at least one pharmaceutically acceptable carrier and/or auxiliary substance. 
     The present invention further relates to a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for use as a medicament. 
     The present invention also relates to a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the treatment of disorders which respond to the modulation of the 5-HT 2C  receptor. 
     The present invention also relates to the use of a compound I as defined above or of an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of disorders which respond to the modulation of the 5-HT 2C  receptor, and to a method for treating disorders which respond to the modulation of the 5-HT 2C  receptor, which method comprises administering to a subject in need thereof at least one compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. 
     The compounds of the present invention are modulators of the 5-HT 2C  receptor. Specifically, the compounds of formula I are agonists or partial agonists of the 5-HT 2 c receptor. Thus, in a specific embodiment, the invention relates to a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the treatment of disorders which respond to 5-HT 2c  receptor agonists, further to the use of a compound I as defined above or of an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of disorders which respond to 5-HT 2c  receptor agonists, and to a method for treating disorders which respond to 5-HT 2c  receptor agonists, which method comprises administering to a subject in need thereof at least one compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. 
     Within the meaning of the invention, the term “disorder” denotes disturbances and/or anomalies which are as a rule regarded as being pathological conditions or functions and which can manifest themselves in the form of particular signs, symptoms and/or malfunctions. While the treatment according to the invention can be directed toward individual disorders, i.e. anomalies or pathological conditions, it is also possible for several anomalies, which may be causatively linked to each other, to be combined into patterns, i.e. syndromes, which can be treated in accordance with the invention. 
     In one aspect of the invention, the diseases to be treated are disorders are damage of the central nervous system, disorders of the central nervous system, eating disorders, ocular hypertension, cardiovascular disorders, gastrointestinal disorders and diabetes. 
     Disorders or diseases of the central nervous system are understood as meaning disorders which affect the spinal cord and, in particular, the brain. These are, for example, cognitive dysfunction, attention deficit disorder/hyperactivity syndrome and cognitive deficits related with schizophrenia, attention deficit/hyperactivity syndrome, personality disorders, affective disorders, motion or motor disorders, pain, migraine, sleep disorders (including disturbances of the Circadian rhythm), feeding disorders, diseases associated with neurodegeneration, addiction diseases, obesity or psoriasis. 
     Examples of cognitive dysfunction are deficits in memory, cognition, and learning, Alzheimer&#39;s disease, age-related cognitive decline, and mild cognitive impairment, or any combinations thereof. Examples of personality disorders are schizophrenia and cognitive deficits related to schizophrenia. Examples of affective disorders are depression, anxiety, bipolar disorder and obsessive compulsive disorders, or any combination thereof. Examples of motion or motor disorders are Parkinson&#39;s disease and epilepsy. Examples of feeding disorders are obesity, bulimia, weight loss and anorexia, especially anorexia nervosa. Examples of diseases associated with neurodegeneration are stroke, spinal or head trauma, and head injuries, such as hydrocephalus. 
     Pain condition includes nociceptive pain, neuropathic pain or a combination thereof. Such pain conditions or disorders can include, but are not limited to, post-operative pain, osteoarthritis pain, pain due to inflammation, rheumatoid arthritis pain, musculoskeletal pain, burn pain (including sunburn), ocular pain, the pain associated with dental conditions (such as dental caries and gingivitis), post-partum pain, bone fracture, herpes, HIV, traumatic nerve injury, stroke, post-ischemia, fibromyalgia, reflex sympathetic dystrophy, complex regional pain syndrome, spinal cord injury, sciatica, phantom limb pain, diabetic neuropathy, hyperalgesia and cancer. 
     In certain other embodiments, the disease condition is bladder dysfunction, including urinary incontinence. 
     Diabetes includes diabetes insipidus, diabetes mellitus, type I diabetes, type II diabetes, type III diabetes, diabetes secondary to pancreatic diseases, diabetes related to steroid use, diabetes complications, hyperglycemia and insulin resistance. 
     The addiction diseases include psychiatric disorders and behavioral disturbances which are caused by the abuse of psychotropic substances, such as pharmaceuticals or narcotics, and also other addiction diseases, such as addiction to gaming (impulse control disorders not elsewhere classified). Examples of addictive substances are: opioids (e.g. morphine, heroin and codeine), cocaine; nicotine; alcohol; substances which interact with the GABA chloride channel complex, sedatives, hypnotics and tranquilizers, for example benzodiazepines; LSD; cannabinoids; psychomotor stimulants, such as 3,4-methylenedioxy-N-methylamphetamine (ecstasy); amphetamine and amphetamine-like substances such as methylphenidate, other stimulants including caffeine and nicotine. Addictive substances which come particularly into consideration are opioids, cocaine, amphetamine or amphetamine-like substances, nicotine and alcohol. Especially, addiction disorders include alcohol abuse, cocaine abuse, tobacco abuse and smoking cessation. 
     With regard to the treatment of addiction diseases, particular preference is given to those compounds according to the invention of the formula (I) which themselves do not possess any psychotropic effect. This can also be observed in a test using rats, which, after having been administered compounds which can be used in accordance with the invention, reduce their self administration of psychotropic substances, for example cocaine. 
     Examples of gastrointestinal disorders are irritable bowel syndrome. 
     Preferably, the disorders are selected from the group consisting of bipolar disorder, depression, atypical depression, mood episodes, adjustment disorders, anxiety, panic disorders, post-traumatic syndrome, psychoses, schizophrenia, cognitive deficits of schizophrenia, memory loss, dementia of aging, Alzheimer&#39;s disease, behavioral disorders associated with dementia, social phobia, mental disorders in childhood, attention deficit hyperactivity disorder, organic mental disorders, autism, mutism, disruptive behavior disorder, impulse control disorder, borderline personality disorder, obsessive compulsive disorder, migraine and other conditions associated with cephalic pain or other pain, raised intracranial pressure, seizure disorders, epilepsy, substance use disorders, alcohol abuse, cocaine abuse, tobacco abuse, smoking cessation, sexual dysfunction/erectile dysfunction in males, sexual dysfunction in females, premenstrual syndrome, late luteal phase syndrome, chronic fatigue syndrome, sleep disorders, sleep apnoea, chronic fatigue syndrome, psoriasis, Parkinson&#39;s disease, spinal cord injury, trauma, stroke, pain, bladder dysfunction/urinary incontinence, encephalitis, meningitis, eating disorders, obesity, bulimia, weight loss, anorexia nervosa, ocular hypertension, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, diabetes mellitus, type I diabetes, type II diabetes, type III diabetes, diabetes secondary to pancreatic diseases, diabetes related to steroid use, diabetes complications, hyperglycemia and insulin resistance, and are specifically schizophrenia, depression, bipolar disorders, obesity or substance use disorders. 
     The compounds of the invention may be used for a preventive treatment (prophylaxis), in particular as relapse prophylaxis or phase prophylaxis, but are preferably used for a treatment in its proper sense, i.e. for the treatment of acute or chronic signs, symptoms and/or malfunctions. The treatment can be orientated symptomatically, for example as the suppression of symptoms. It can be effected over a short period, be orientated over the medium term or can be a long-term treatment, for example within the context of a maintenance therapy. 
     In another embodiment, the present invention relates to the use of a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for preparing a medicament for preventing (the development of) a disease condition as described above and to a method for preventing (the development of) a disease condition as described above comprises administering to the subject in need of treatment thereof (e.g., a mammal, such as a human) a therapeutically effective amount of a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. As used herein, the term “prevent” a disease condition by administration of any of the compounds described herein means that the detectable physical characteristics or symptoms of the disease or condition do not develop following the administration of the compound described herein. Alternatively, the method comprises administering to the subject a therapeutically effective amount of a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof, in combination with a therapeutically effective amount of at least one cognitive enhancing drug. 
     In yet another embodiment, the present invention relates to the use a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof for preparing a medicament for preventing the progression (e.g., worsening) of a disease condition and to a method for preventing the progression (e.g., worsening) of a disease condition, which method comprises administering to the subject in need of treatment thereof (e.g., a mammal, such as a human) a therapeutically effective amount of a compound I as defined above or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof. 
     There are several lines of evidence suggesting that 5-HT 2C  agonists or partial agonists would have therapeutic use in a variety of diseases, disorders and conditions. 
     Knockout mice models lacking the 5-HT 2C  receptor exhibit hyperphagia, obesity and are more prone to seizures and sudden death [Tecott L H, Sun L M, Akana S F, Strack A M, Lowenstein D H, Dallman M F, Julius D (1995) Eating disorder and epilepsy in mice lacking 5-HT 2C  serotonin receptors.  Nature  374:542-546]. They also exhibit compulsive-like behavior [Chou-Green J M, Holscher T D, Dallman M F, Akana S F (2003). Compulsive behavior in the 5-HT 2C  receptor knockout mouse.  Phys. Behav.  78:641-649], hyperresponsiveness to repeated stress [Chou-Green J M, Holscher T D, Dallman M F, Akana S F (2003). Repeated stress in young and old 5-HT 2C  receptor knockout mouse.  Phys. Behav.  79:217-226], wakefulness [Frank M G, Stryker M P, Tecott L H (2002). Sleep and sleep homeostasis in mice lacking the 5-HT 2C  receptor.  Neuropsychopharmacology  27:869-873], hyperactivity and drug dependence [Rocha B A, Goulding E H, O&#39;Dell L E, Mead A N, Coufal N G, Parsons L H, Tecott L H (2002). Enhanced locomotor, reinforcing and neurochemical effects of cocaine in serotonin 5-hydroxytryptamine 2C receptor mutant mice.  J. Neurosci.  22:10039-10045]. 
     5-HT 2C  is unique among other G-protein-coupled receptors (GPCRs) in that its pre-mRNA is a substrate for base modification via hydrolytic deamination of adenosines to yield inosines. Five adenosines, located within a sequence encoding the putative second intracellular domain can be converted to inosines. This editing can alter the coding potential of the triplet codons and allows for the generation of multiple different receptor isoforms. The edited receptor isoforms were shown to have reduced ability to interact with G-proteins in the absence of agonist stimulation [Werry, T D, Loiacono R, Sexton P A, Christopoulos A (2008). RNA editing of the serotonin 5-HT 2C  receptor and its effects on cell signaling, pharmacology and brain function.  Pharmac. Therap.  119:7-23]. 
     Edited 5-HT 2C  isoforms with reduced function are significantly expressed in the brains of depressed suicide victims [Schmauss C (2003) Serotonin 2C receptors: suicide, serotonin, and runaway RNA editing.  Neuroscientist  9:237-242. Iwamoto K, Kato T (2003). RNA editing of serotonin 2C receptor in human postmortem brains of major mental disorders.  Neurosci. Lett.  346:169-172] and in the learned helplessness rats (a well established animal model of depression) [Iwamotoa K, Nakatanib N, Bundoa M, Yoshikawab T, Katoa T (2005). Altered RNA editing of serotonin 2C receptor in a rat model of depression.  Neurosci. Res.  53: 69-76] suggesting a link between 5-HT 2C  function and depression. There are also implications of edited 5-HT 2C  isoforms and spatial memory [Du Y, Stasko M, Costa A C, Davissone M T, Gardiner K J (2007). Editing of the serotonin 2C receptor pre-mRNA Effects of the Morris Water Maze.  Gene  391:186-197]. In addition, fully edited isoforms of the human 5-HT 2C  receptor display a striking reduction in sensitivity to lysergic acid diethylamide (LSD) and to atypical antipsychotic drugs clozapine and loxapine, suggesting a possible role of the receptor in the etiology and pharmacology of schizophrenia [Niswender C M, Herrick-Davis K., Dilley G E, Meltzer H Y, Overholser J C, Stockmeier C A, Emeson R B, Sanders-Bush E (2001). RNA Editing of the Human Serotonin 5-HT 2C  Receptor: Alterations in Suicide and Implications for Serotonergic  Pharmacotherapy. Neuropsychopharm.  24:478-491]. 
     Recently, the availability of potent and selective 5-HT 2C  receptor agonists made it possible to directly investigate the effects of 5-HT 2C  agonists and their therapeutic potential. Thus recent studies demonstrated that selective 5-HT 2C  agonists resulted in decreased food intake and body weight gain in normal and obese rats [Smith B M, et al. (2008). Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT 2C  receptor agonist for the treatment of obesity.  J Med Chem  51:305-313. Thomsen W J, Grottick A J, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W, Al-Shama H, Smith B, Chalmers D, Behan D (2008) Lorcaserin, A Novel Selective Human 5-HT 2C  Agonist: In Vitro and In Vivo Pharmacological Characterization.  J Pharmacol Exp Ther.  325:577-587. Rosenzweig-Lipson S, Zhang J, Mazandarani H, Harrison B L, Sabb A, Sabalski J, Stack G, Welmaker G, Barrett J E, Dunlop J (2006) Antiobesity-like effects of the 5-HT 2C  receptor agonist WAY-161503 . Brain Res.  1073-1074:240-251. Dunlop J, Sabb A L, Mazandarani H, Zhang J, Kalgaonker S, Shukhina E, Sukoff S, Vogel R L, Stack G, Schechter L, Harrison B L, Rosenzweig-Lipson S (2005). WAY-163909 [97bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor—selective agonist with anorectic activity.  J Pharmacol Exp Ther.  313:862-869.]. 
     Furthermore, selective 5-HT 2C  receptor agonists produce antidepressant effects in animal models of depression comparable to those of SSRIs but with a much faster onset of action and a therapeutic window that avoids antidepressant-induced sexual dysfunction. These agonists were also effective in animal models of compulsive behavior such as scheduled induced polydipsia and they also exhibited decreased hyperactivity and aggression in rodents [Rosenzweig-Lipson S, Sabb A, Stack G, Mitchell P, Lucki I, Malberg J E, Grauer S, Brennan J, Cryan J F, Sukoff Rizzo S J, Dunlop J, Barrett J E, Marquis K L (2007) Antidepressant-like effects of the novel, selective, 5-HT 2C  receptor agonist WAY-163909 in rodents.  Psychopharmacology  (Berlin) 192:159-170. Rosenzweig-Lipson S, Dunlop J, Marquis K L (2007) 5-HT 2C  receptor agonists as an innovative approach for psychiatric disorders.  Drug news Perspect,  20: 565-571. Cryan, J F, Lucki I (2000). Antidepressant-like behavioral effects mediated by 5-Hydroxytryptamine 2C receptors.  J. Pharm. Exp. Ther.  295:1120-1126.]. 
     Acute or chronic administration of 5-HT 2C  agonists decreases the firing rate of ventral tegmental area dopamine neurons but not that of substantia nigra. In addition 5-HT 2C  agonists reduce dopamine levels in the nucleus accumbens but not in the striatum (the region of the brain mostly associated with extrapyramidal side effects) [Di Matteo, V., Di Giovanni, G., Di Mascio, M., &amp; Esposito, E. (1999). SB 242084, a selective serotonin 2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system.  Neuropharmacology  38, 1195-1205. Di Giovanni, G., Di Matteo, V., Di Mascio, M., &amp; Esposito, E. (2000). Preferential modulation of mesolimbic vs. nigrostriatal dopaminergic function by serotonin 2C/2B receptor agonists: a combined in vivo electrophysiological and microdialysis study.  Synapse  35, 53-61. Marquis K L, Sabb A L, Logue S F, Brennan J A, Piesla M J, Comery T A, Grauer S M, Ashby C R, Jr., Nguyen H Q, Dawson L A, Barrett J E, Stack G, Meltzer H Y, Harrison B L, Rosenzweig-Lipson S (2007) WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A novel 5-hydroxytryptamine 2C receptor-selective agonist with preclinical antipsychotic-like activity.  J Pharmacol Exp Ther  320:486-496.]. Therefore it is expected that 5-HT 2C  receptor agonists will selectively decrease mesolimibic dopamine levels without affecting the nigrostriatal pathway thus avoiding the EPS side effects of typical antipsychotics. Several 5-HT 2C  receptor agonists have shown antipsychotic activity in animal models of schizophrenia without EPS based on the lack of effect in catalepsy [Marquis K L, Sabb A L, Logue S F, Brennan J A, Piesla M J, Comery T A, Grauer S M, Ashby C R, Jr., Nguyen H Q, Dawson L A, Barrett J E, Stack G, Meltzer H Y, Harrison B L, Rosenzweig-Lipson S (2007) WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A novel 5-hydroxytryptamine 2C receptor-selective agonist with preclinical antipsychotic-like activity.  J Pharmacol Exp Ther  320:486-496. Siuciak J A, Chapin D S, McCarthy S A, Guanowsky V, Brown J, Chiang P, Marala R, Patterson T, Seymour P A, Swick A, Iredale P A (2007) CP-809,101, a selective 5-HT 2C  agonist, shows activity in animal models of antipsychotic activity.  Neuropharmacology  52:279-290]. The antipsychotic activity of 5-HT 2C  receptor agonists without EPS coupled with their beneficial effects in mood disorders and cognition and their antiobesity like effects render 5-HT 2C  receptor agonists as unique agents to treat schizophrenia [Rosenzweig-Lipson S, Dunlop J, Marquis K L (2007) 5-HT 2C  receptor agonists as an innovative approach for psychiatric disorders.  Drug news Perspect,  20: 565-571. Dunlop J, Marquis K L, Lim H K, Leung L, Kao J, Cheesman C, Rosenzweig-Lipson S (2006). Pharmacological profile of the 5-HT 2C  receptor agonist WAY-163909; therapeutic potential in multiple indications.  CNS Dug Rev.  12:167-177.]. 
     In addition 5-HT 2C  modulation has been implicated in epilepsy [Isaac M (2005). Serotonergic 5-HT 2C  receptors as a potential therapeutic target for the antiepileptic drugs.  Curr. Topics fed. Chem.  5:59:67], psoriasis [Thorslund K, Nordlind K (2007). Serotonergic drugs-a possible role in the treatment of psoriasis?  Drug News Perspect  20:521-525], Parkinson&#39;s disease and related motor disorders [Esposito E, Di Matteo V, Pierucci M, Benigno A, Di Giavanni, G (2007). Role of central 5-HT 2C  receptor in the control of basal ganglia functions.  The Basal Ganglia Pathophysiology: Recent Advances  97-127], behavioral deficits [Barr A M, Lahmann-Masten V, Paulus M, Gainetdinov R P, Caron M G, Geyer M A (2004). The selective serotonin-2A receptor antagonist M100907 reverses behavioral deficits in dopamine transporter knockout mice.  Neuropsychopharmacology  29:221-228], anxiety [Dekeyne A, Mannoury la Cour C, Gobert A, Brocco M, Lejuene F, Serres F, Sharp T, Daszuta A, Soumier A, Papp M, Rivet J M, Flik G, Crerners T I, Muller O, Lavielle G, Millan M J (2208). S32006, a novel 5-HT 2C  receptor antagonists displaying broad-based antidepressant and anxiolytic properties in rodent models.  Psychopharmacology  199:549-568. Nunes-de-Souza V, Nunes-de-Souza R L, Rodgers R J, Canto-de-Souza A (2008). 5-HT2 receptor activation in the midbrain periaqueductal grey (PAG) reduces anxiety-like behavior in mice.  Behav. Brain Res.  187:72-79.], migraine [Leone M, Rigamonti A, D&#39;Amico D, Grazzi L, Usai S, Bussone G (2001). The serotonergic system in migraine.  Journal of Headache and Pain  2( Suppl.  1):S43-S46], Alzheimer&#39;s disease [Arjona A A, Pooler A M, Lee R K, Wurtman R J (2002). Effect of a 5-HT 2C  serotonin agonist, dexnorfenfluramine, on amyloid precursor protein metabolism in guinea pigs.  Brain Res.  951:135-140], pain and spinal cord injury [Nakae A, Nakai K, Tanaka T, Hagihira S, Shibata M, Ueda K, Masimo T (2008). The role of RNA editing of the serotonin 2C receptor in a rat model of oro-facial neuropathic pain.  The European Journal of Neuroscience  27:2373-2379. Nakae A, Nakai K, Tanaka T, Takashina M, Hagihira S, Shibata M, Ueda K, Mashimo T (2008). Serotonin 2C receptor mRNA editing in neuropathic pain model.  Neurosci. Res.  60:228-231. Kao T, Shumsky J S, Jacob-Vadakot S, Timothy H B, Murray M, Moxon, K A (2006). Role of the 5-HT 2C  receptor in improving weight-supported stepping in adult rats spinalized as neonates.  Brain Res.  1112:159-168.], sexual dysfunction [Motofei I G (2008). A dual physiological character for sexual function: the role of serotonergic receptors.  BJU International  101:531-534. Shimada I, Maeno K, Kondoh Y, Kaku H, Sugasawa K, Kimura Y, Hatanaka K; Naitou Y, Wanibuchi F, Sakamoto S; Tsukamoto S (2008). Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT 2 c receptor agonists.  Bioorg. Med. Chem.  16:3309-3320.], smoking cessation [Fletcher P J, Le A D, Higgins G A (2008). Serotonin receptors as potential targets for modulation of nicotine use and dependence.  Progress Brain Res.  172:361-83], substance dependence [Bubar M J, Cunningham K A (2008). Prospects for serotonin 5-HT2R pharmacotherapy in psychostimulant abuse.  Progress Brain Res.  172:319-46], and ocular hypertension [Sharif N A, McLaughlin M A, Kelly C R (2006). AL-34662: a potent, selective, and efficacious ocular hypotensive serotonin-2 receptor agonist.  J Ocul Pharmacol Ther.  23:1-13]. 
     Further, 5HT modulation can be useful in the treatment of pain, both neuropathic and nociceptive pain, see for example U.S. Patent application publication US2007/0225277. Obata, Hideaki; Ito, Naomi; Sasaki, Masayuki; Saito, Shigeru; Goto, Fumio. Possible involvement of spinal noradrenergic mechanisms in the antiallodynic effect of intrathecally administered 5-HT2C receptor agonists in the rats with peripheral nerve injury.  European Journal of Pharmacology  (2007), 567(1-2), 89-94. Serotonin2C receptor mRNA editing in neuropathic pain model. Nakae, Aya; Nakai, Kunihiro; Tanaka, Tatsuya; Takashina, Masaki; Hagihira, Satoshi; Shibata, Masahiko; Ueda, Koichi; Mashimo, Takashi. Department of Anesthesiology &amp; Intensive Care Medicine, Graduate School of Medicine, Osaka University,  Neuroscience Research  (Amsterdam, Netherlands) (2008), 60(2), 228-231. Antiallodynic effects of intrathecally administered 5-HT2C receptor agonists in rats with nerve injury. Obata, Hideaki; Saito, Shigeru; Sakurazawa, Shinobu; Sasaki, Masayuki; Usui, Tadashi; Goto, Fumio. Department of Anesthesiology, Gunma University Graduate School of Medicine, Maebashi, Gunma,  Japan. Pain  (2004), 108(1-2), 163-169. Influence of 5,7-dihydroxytryptamine (5,7-DHT) on the antinociceptive effect of serotonin (5-HT) 5-HT2C receptor agonist in male and female rats. Brus, Ryszard; Kasperska, Alicja; Oswiecimska, Joanna; Szkilnik, Ryszard. Department of Pharmacology, Silesian Medical University, Zabrze, Pol.  Medical Science Monitor  (1997), 3(5), 654-656. 
     Modulation of 5HT2 receptors may be beneficial in the treatment of conditions related to bladder function, in particular, urinary incontinence. [Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence. Brennan, Paul E.; Whitlock, Gavin A.; Ho, Danny K. H.; Conlon, Kelly; McMurray, Gordon.  Bioorganic  &amp;  Medicinal Chemistry Letters  (2009), 19(17), 4999-5003. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anesthetized female rat. Mbaki, Y.; Ramage, A. G. Department of Pharmacology, University College London, London, UK.  British Journal of Pharmacology  (2008), 155(3), 343-356.] In particular, compounds with agonist activity at 5-HT 2C  have been shown to be useful in treating urinary incontinence, see for example U.S. Patent application publications US2008/0146583 and US 2007/0225274. 
     In the use and the method of the invention, an effective quantity of one or more compounds, as a rule formulated in accordance with pharmaceutical and veterinary practice, is administered to the individual to be treated, preferably a mammal, in particular a human being, productive animal or domestic animal. Whether such a treatment is indicated, and in which form it is to take place, depends on the individual case and is subject to medical assessment (diagnosis) which takes into consideration signs, symptoms and/or malfunctions which are present, the risks of developing particular signs, symptoms and/or malfunctions, and other factors. 
     Actual dosage levels of active ingredients in the pharmaceutical compositions of the present invention can be varied so as to obtain an amount of the active compound(s) that is effective to achieve the desired therapeutic response for a particular subject (e.g., a mammal, preferably, a human (patient)), compositions and mode of administration. The selected dosage level will depend upon the activity of the particular compound, the route of administration, the severity of the condition being treated and the condition and prior medical history of the patient being treated. However, it is within the skill of the art to start doses of the compound at levels lower than required to achieve the desired therapeutic effect and to gradually increase the dosage until the desired effect is achieved. 
     Compounds of the present invention can also be administered to a subject as a pharmaceutical composition comprising the compounds of interest in combination with at least one pharmaceutically acceptable carriers. The phrase “therapeutically effective amount” of the compound of the present invention means a sufficient amount of the compound to treat disorders, at a reasonable benefit/risk ratio applicable to any medical treatment. It will be understood, however, that the total daily usage of the compounds and compositions of the present invention will be decided by the attending physician within the scope of sound medical judgment. The specific therapeutically effective dose level for any particular patient will depend upon a variety of factors including the disorder being treated and the severity of the disorder; activity of the specific compound employed; the specific composition employed; the age, body weight, general health, sex and diet of the patient; the time of administration, route of administration, and rate of excretion of the specific compound employed; the duration of the treatment; drugs used in combination or coincidental with the specific compound employed; and like factors well-known in the medical arts. For example, it is well within the skill of the art to start doses of the compound at levels lower than required to achieve the desired therapeutic effect and to gradually increase the dosage until the desired effect is achieved. 
     The total daily dose of the compounds of this invention administered to a subject (namely, a mammal, such as a human) ranges from about 0.01 mg/kg body weight to about 100 mg/kg body weight. More preferable doses can be in the range of from about 0.01 mg/kg body weight to about 30 mg/kg body weight. If desired, the effective daily dose can be divided into multiple doses for purposes of administration. Consequently, single dose compositions may contain such amounts or submultiples thereof to make up the daily dose. 
     In one aspect, the present invention provides pharmaceutical compositions. The pharmaceutical compositions of the present invention comprise the compounds of the present invention or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt or solvate thereof. The pharmaceutical compositions of the present invention comprise compounds of the present invention that can be formulated together with at least one non-toxic pharmaceutically acceptable carrier. 
     In yet another embodiment, the present invention provides a pharmaceutical composition comprising compounds of the present invention or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, alone or in combination with one or more compounds that are not the compounds of the present invention. Examples of one or more compounds that can be combined with the compounds of the present invention in pharmaceutical compositions, include, but are not limited to, one or more cognitive enhancing drugs. 
     The pharmaceutical compositions of this present invention can be administered to a subject (e.g., a mammal, such as a human) orally, rectally, parenterally, intracisternally, intravaginally, intraperitoneally, topically (as by powders, ointments or drops), bucally or as an oral or nasal spray. The term “parenterally” as used herein, refers to modes of administration which include intravenous, intramuscular, intraperitoneal, intrasternal, subcutaneous and intraarticular injection and infusion. 
     The term “pharmaceutically acceptable carrier” as used herein, means a non-toxic, inert solid, semi-solid or liquid filler, diluent, encapsulating material or formulation auxiliary of any type. Some examples of materials which can serve as pharmaceutically acceptable carriers are sugars such as, but not limited to, lactose, glucose and sucrose; starches such as, but not limited to, corn starch and potato starch; cellulose and its derivatives such as, but not limited to, sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; powdered tragacanth; malt; gelatin; talc; excipients such as, but not limited to, cocoa butter and suppository waxes; oils such as, but not limited to, peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil and soybean oil; glycols; such a propylene glycol; esters such as, but not limited to, ethyl oleate and ethyl laurate; agar; buffering agents such as, but not limited to, magnesium hydroxide and aluminum hydroxide; alginic acid; pyrogen-free water; isotonic saline; Ringer&#39;s solution; ethyl alcohol, and phosphate buffer solutions, as well as other non-toxic compatible lubricants such as, but not limited to, sodium lauryl sulfate and magnesium stearate, as well as coloring agents, releasing agents, coating agents, sweetening, flavoring and perfuming agents, preservatives and antioxidants can also be present in the composition, according to the judgment of the formulator. 
     Pharmaceutical compositions of the present invention for parenteral injection comprise pharmaceutically acceptable sterile aqueous or nonaqueous solutions, dispersions, suspensions or emulsions as well as sterile powders for reconstitution into sterile injectable solutions or dispersions just prior to use. Examples of suitable aqueous and nonaqueous carriers, diluents, solvents or vehicles include water, ethanol, polyols (such as glycerol, propylene glycol, polyethylene glycol and the like), vegetable oils (such as olive oil), injectable organic esters (such as ethyl oleate) and suitable mixtures thereof. Proper fluidity can be maintained, for example, by the use of coating materials such as lecithin, by the maintenance of the required particle size in the case of dispersions and by the use of surfactants. 
     These compositions may also contain adjuvants such as preservatives, wetting agents, emulsifying agents and dispersing agents. Prevention of the action of microorganisms can be ensured by the inclusion of various antibacterial and antifungal agents, for example, paraben, chlorobutanol, phenol sorbic acid and the like. It may also be desirable to include isotonic agents such as sugars, sodium chloride and the like. 
     Prolonged absorption of the injectable pharmaceutical form can be brought about by the inclusion of agents which delay absorption such as aluminum monostearate and gelatin. 
     In some cases, in order to prolong the effect of the drug, it is desirable to slow the absorption of the drug from subcutaneous or intramuscular injection. This can be accomplished by the use of a liquid suspension of crystalline or amorphous material with poor water solubility. The rate of absorption of the drug then depends upon its rate of dissolution which, in turn, may depend upon crystal size and crystalline form. Alternatively, delayed absorption of a parenterally administered drug form is accomplished by dissolving or suspending the drug in an oil vehicle. 
     Injectable depot forms are made by forming microencapsule matrices of the drug in biodegradable polymers such as polylactide-polyglycolide. Depending upon the ratio of drug to polymer and the nature of the particular polymer employed, the rate of drug release can be controlled. Examples of other biodegradable polymers include poly(orthoesters) and poly(anhydrides). Depot injectable formulations are also prepared by entrapping the drug in liposomes or microemulsions which are compatible with body tissues. 
     The injectable formulations can be sterilized, for example, by filtration through a bacterial-retaining filter or by incorporating sterilizing agents in the form of sterile solid compositions which can be dissolved or dispersed in sterile water or other sterile injectable medium just prior to use. 
     Solid dosage forms for oral administration include capsules, tablets, pills, powders and granules. In such solid dosage forms, the active compound may be mixed with at least one inert, pharmaceutically acceptable excipient or carrier, such as sodium citrate or dicalcium phosphate and/or a) fillers or extenders such as starches, lactose, sucrose, glucose, mannitol and silicic acid; b) binders such as carboxymethylcellulose, alginates, gelatin, polyvinylpyrrolidone, sucrose and acacia; c) humectants such as glycerol; d) disintegrating agents such as agar-agar, calcium carbonate, potato or tapioca starch, alginic acid, certain silicates and sodium carbonate; e) solution retarding agents such as paraffin; f) absorption accelerators such as quaternary ammonium compounds; g) wetting agents such as cetyl alcohol and glycerol monostearate; h) absorbents such as kaolin and bentonite clay and i) lubricants such as talc, calcium stearate, magnesium stearate, solid polyethylene glycols, sodium lauryl sulfate and mixtures thereof. In the case of capsules, tablets and pills, the dosage form may also comprise buffering agents. 
     Solid compositions of a similar type may also be employed as fillers in soft and hard-filled gelatin capsules using such carriers as lactose or milk sugar as well as high molecular weight polyethylene glycols and the like. 
     The solid dosage forms of tablets, dragees, capsules, pills and granules can be prepared with coatings and shells such as enteric coatings and other coatings well-known in the pharmaceutical formulating art. They may optionally contain opacifying agents and may also be of a composition such that they release the active ingredient(s) only, or preferentially, in a certain part of the intestinal tract, optionally, in a delayed manner. Examples of embedding compositions which can be used include polymeric substances and waxes. 
     The active compounds can also be in micro-encapsulated form, if appropriate, with one or more of the above-mentioned carriers. 
     Liquid dosage forms for oral administration include pharmaceutically acceptable emulsions, solutions, suspensions, syrups and elixirs. In addition to the active compounds, the liquid dosage forms may contain inert diluents commonly used in the art such as, for example, water or other solvents, solubilizing agents and emulsifiers such as ethyl alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylene glycol, dimethyl formamide, oils (in particular, cottonseed, groundnut, corn, germ, olive, castor and sesame oils), glycerol, tetrahydrofurfuryl alcohol, polyethylene glycols and fatty acid esters of sorbitan and mixtures thereof. 
     Besides inert diluents, the oral compositions may also include adjuvants such as wetting agents, emulsifying and suspending agents, sweetening, flavoring and perfuming agents. 
     Suspensions, in addition to the active compounds, may contain suspending agents as, for example, ethoxylated isostearyl alcohols, polyoxyethylene sorbitol and sorbitan esters, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar-agar, tragacanth and mixtures thereof. 
     Compositions for rectal or vaginal administration are preferably suppositories which can be prepared by mixing the compounds of this invention with suitable non-irritating carriers or carriers such as cocoa butter, polyethylene glycol or a suppository wax which are solid at room temperature but liquid at body temperature and therefore melt in the rectum or vaginal cavity and release the active compound. 
     Compounds of the present invention can also be administered in the form of liposomes. As is known in the art, liposomes are generally derived from phospholipids or other lipid substances. Liposomes are formed by mono- or multi-lamellar hydrated liquid crystals which are dispersed in an aqueous medium. Any non-toxic, physiologically acceptable and metabolizable lipid capable of forming liposomes can be used. The present compositions in liposome form can contain, in addition to a compound of the present invention, stabilizers, preservatives, excipients and the like. The preferred lipids are natural and synthetic phospholipids and phosphatidyl cholines (lecithins) used separately or together. 
     Methods to form liposomes are known in the art. See, for example, Prescott, Ed.,  Methods in Cell Biology , Volume XIV, Academic Press, New York, N.Y. (1976), p. 33 et seq. 
     Dosage forms for topical administration of a compound of the present invention include powders, sprays, ointments and inhalants. The active compound may be mixed under sterile conditions with a pharmaceutically acceptable carrier and any needed preservatives, buffers or propellants which may be required. Ophthalmic formulations, eye ointments, powders and solutions are also contemplated as being within the scope of this invention. 
     The compounds of the present invention can be used in the form of pharmaceutically acceptable salts derived from inorganic or organic acids. The phrase “pharmaceutically acceptable salt” means those salts which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of humans and lower animals without undue toxicity, irritation, allergic response and the like and are commensurate with a reasonable benefit/risk ratio. 
     Pharmaceutically acceptable salts are well known in the art. For example, S. M. Berge et al. describe pharmaceutically acceptable salts in detail in ( J. Pharmaceutical Sciences,  1977, 66: 1 et seq.). The salts can be prepared in situ during the final isolation and purification of the compounds of the invention or separately by reacting a free base function with a suitable organic acid. Representative acid addition salts include, but are not limited to acetate, adipate, alginate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, camphorate, camphorsulfonate, digluconate, glycerophosphate, hemisulfate, heptanoate, hexanoate, fumarate, hydrochloride, hydrobromide, hydroiodide, 2-hydroxyethansulfonate (isothionate), lactate, malate, maleate, methanesulfonate, nicotinate, 2-naphthalenesulfonate, oxalate, palmitoate, pectinate, persulfate, 3-phenylpropionate, picrate, pivalate, propionate, succinate, tartrate, thiocyanate, phosphate, glutamate, bicarbonate, p-toluenesulfonate and undecanoate. Also, the basic nitrogen-containing groups can be quaternized with such agents as lower alkyl halides such as, but not limited to, methyl, ethyl, propyl, and butyl chlorides, bromides and iodides; dialkyl sulfates like dimethyl, diethyl, dibutyl and diamyl sulfates; long chain halides such as, but not limited to, decyl, lauryl, myristyl and stearyl chlorides, bromides and iodides; arylalkyl halides like benzyl and phenethyl bromides and others. Water or oil-soluble or dispersible products are thereby obtained. Examples of acids which can be employed to form pharmaceutically acceptable acid addition salts include such inorganic acids as hydrochloric acid, hydrobromic acid, sulfuric acid, and phosphoric acid and such organic acids as acetic acid, fumaric acid, maleic acid, 4-methylbenzenesulfonic acid, succinic acid and citric acid. 
     Basic addition salts can be prepared in situ during the final isolation and purification of compounds of this invention by reacting a carboxylic acid-containing moiety with a suitable base such as, but not limited to, the hydroxide, carbonate or bicarbonate of a pharmaceutically acceptable metal cation or with ammonia or an organic primary, secondary or tertiary amine. Pharmaceutically acceptable salts include, but are not limited to, cations based on alkali metals or alkaline earth metals such as, but not limited to, lithium, sodium, potassium, calcium, magnesium and aluminum salts and the like and nontoxic quaternary ammonia and amine cations including ammonium, tetramethylammonium, tetraethylammonium, methylammonium, dimethylammonium, trimethylammonium, triethylammonium, diethylammonium, ethylammonium and the like. Other representative organic amines useful for the formation of base addition salts include ethylenediamine, ethanolamine, diethanolamine, piperidine, piperazine and the like. 
     The compounds of the present invention can exist in unsolvated as well as solvated forms, including hydrated forms, such as hemi-hydrates. In general, the solvated forms, with pharmaceutically acceptable solvents such as water and ethanol among others are equivalent to the unsolvated forms for the purposes of the invention. 
     The following examples serve to explain the invention without limiting it. 
     EXAMPLES 
     The compounds were either characterized via proton-NMR in d 6 -dimethylsulfoxide or d-chloroform or d 4 -methanol on a 400 MHz or 500 MHz NMR instrument (Bruker AVANCE), or by mass spectrometry, generally recorded via HPLC-MS in a fast gradient on C18-material (electrospray-ionisation (ESI) mode). 
     The magnetic nuclear resonance spectral properties (NMR) refer to the chemical shifts (6) expressed in parts per million (ppm). The relative area of the shifts in the  1 H-NMR spectrum corresponds to the number of hydrogen atoms for a particular functional type in the molecule. The nature of the shift, as regards multiplicity, is indicated as singlet (s), broad singlet (s. br.), doublet (d), broad doublet (d br.), triplet (t), broad triplet (t br.), quartet (q), quintet (quint.) and multiplet (m). 
     Enantiomers were separated/purified either by chiral supercritical fluid chromatography (SFC) (method A) or by chiral HPLC (method B). 
     Method A—Chiral Analytical SFC 
     Analytical SFC was performed on an Aurora A5 SFC Fusion and Agilent 1100 system running under Agilent Chemstation software control. The SFC system included a 10-way column switcher, CO2 pump, modifier pump, oven, and backpressure regulator. The mobile phase comprised of supercritical CO2 supplied by a beverage-grade CO2 cylinder with a modifier mixture of methanol at a flow rate of 3 mL/min. Oven temperature was at 35° C. and the outlet pressure at 150 bar. The UV detector was set to collect at wavelengths of 220 nm and 254 nm. The mobile phase gradient started with 5% modifier and held it for 0.1 minutes at a flow rate of 1 mL/min, then the flow rate was ramped up to 3 mL/min and held for 0.4 min. The modifier was ramped from 5% to 15% over the next 8 minutes at 3 mL/min then held for 1 minute at 15% modifier (3 mL/min). The gradient was ramped down from 15% to 5% modifier over 0.5 min (3 mL/min). The instrument was fitted with a Chiralpak AS-H column with dimensions of 4.6 mm i.d.×150 mm length with 5 μm particles. 
     Method B—Chiral HPLC 
     System: KNAUER preparative HPLC
 
Pump: Preparative pump 1800
 
Detector: Smartline UV detector 2600 257 nm
 
Sample pump: Knauer HPLC-Pump K-120
 
Fractional collector: Smartline Valves Drive S6
 
     Software: ChromGate® V3.1.7, KNAUER Instrument Control 
     Column: Whelk O 4.6 mm ID×250 mm 
     Column temperature: 25° C.
 
Mobile phase: hexane/isopropylamine 95/5
 
Flow rate: 1 ml/min
 
     I. PREPARATION EXAMPLES 
     Example 1 
     8,8-Dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-1 of Table B) 
     1.1 Preparation of tert-butyl 1-(3-methylbut-2-enoyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate 
     1 g (4.04 mmol) of tert-butyl 2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate was dissolved in 20 mL of dichloromethane and treated with 1.54 mL (8.86 mL) of triethylamine followed by 0.53 mL (4.83 mmol) of 3-methylbut-2-enoyl chloride. The reaction mixture was stirred over night at room temperature, poured onto water (50 mL) and extracted three times with 50 mL of dichloromethane each. The organic phases were combined, washed with a saturated solution of sodium chloride, dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 5-10% methanol in dichloromethane) to yield 1.27 g of the title compound as a white solid. 
     ESI-MS: m/z (%): 275.10 (100, [M-C 4 H 9 +H] + ). 
     1.2 Preparation of tert-butyl 8,8-dimethyl-6-oxo-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline-2(6H)-carboxylate 
     A solution of 0.33 g (1.0 mmol) of tert-butyl 1-(3-methylbut-2-enoyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate of step 1.1 was irradiated with a 150 W mercury lamp in an immersion well reactor with a pyrex filter in 20 mL of acetone until completion of the reaction monitored by liquid chromatography. The solution was concentrated in vacuo and the residue was purified by column chromatography on silica (eluent: 10-30% ethyl acetate in heptane) to yield 202 mg of the title compound as a beige solid. 
     ESI-MS: m/z (%): 275.10 (100, [M-C 4 H 9 +H] + ). 
     1.3 Preparation of tert-butyl 8,8-dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline-2(6H)-carboxylate 
     A solution of 38 mg (0.115 mmol) tert-butyl 8,8-dimethyl-6-oxo-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline-2(6H)-carboxylate of step 1.2 in 1 mL of tetrahydrofuran was treated with 0.46 mL of 1 molar solution of borohydride-tetrahydrofuran complex in tetrahydrofuran. The mixture was stirred over night, and then quenched with water and diluted hydrochloric acid. The pH was adjusted to pH 9 by addition of aqueous sodium hydroxide solution and the mixture extracted three times with 10 mL of dichloromethane each. The solution was dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 20-30% ethyl acetate in heptane) to yield 21 mg of the title compound as a clear oil. 
     ESI-MS: m/z (%): 317.20 (100, [M+H] + ). 
     1.4 Preparation of 8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline 
     287 mg (0.9 mmol) of tert-butyl 8,8-dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline-2(6H)-carboxylate of step 1.3 were dissolved in 5 mL of dichloromethane and treated with 2.5 mL of trifluoroacetic acid. The mixture was stirred over night at room temperature and then extracted once with water (10 mL). The organic phase was then extracted twice with a diluted solution of sodium hydroxide (10 mL each), dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 10-30% methanol in dichloromethane) to yield 141 mg of the title compound as a yellow oil. 
     ESI-MS: m/z (%): 217.15 (100, [M+H] + ). 
       1 H-NMR (500 MHz, CDCl 3 ): δ=7.15 (d, 1H), 6.85 (d, 1H), 6.75 (m, 1H), 3.80 (s, 2H), 3.15 (m, 2H), 3.00 (s, 4H), 1.65 (m, 2H), 1.20 (s, 6H). 
     Example 2 
     1,2,3,4-Tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopent[2]en]-6(7H)-one 2,2,2-trifluoroacetate (Compound of the Formula I.j, I.k or I.1 in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-481 of Table B) 
     2.1 Preparation of tert-butyl 6-oxo-3,4,6,7-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopent[2]ene]-2(1H)-carboxylate (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-401 of Table B, Wherein However R 1  is not H, but Boc) 
     A solution of 50 mg (0.128 mmol) tert-butyl 9-chloro-1-(2-cyclopentenylacetyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate was dissolved in 1 mL of degassed dry acetonitrile under argon, treated with 1.4 mg (0.006 mmol) of palladium acetate, 6.10 mg (0.013 mmol) dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine and 53 mg (0.384 mmol) potassium carbonate. The mixture was stirred for 10 hours at 120° C. in a synthesis microwave system. After cooling to room temperature the mixture was filtered over celite, diluted with dichloromethane and then extracted twice with a diluted solution of sodium chloride (10 mL each), dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 10-30% ethyl acetate in heptane) to yield 40 mg of the title compound as a yellow oil. 
     ESI-MS: m/z (%): 299.10 (100, [M-C 4 H 9 +H] + ). 
     2.2 Preparation of 1,2,3,4-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopent[2]en]-6(7H)-one 2,2,2-trifluoroacetate 
     Boc-deprotection of the compound obtained in step 2.1 analogously to example 1.4 yielded the title compound. 
     ESI-MS: m/z (%): 255 (100, [M+H] + ). 
     Example 3 
     8-Methyl-8-phenyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one, hydrochloride (Compound of the Formula I.j, I.k or I.l in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-161 of Table B) 
     392 mg (1 mmol) of tert-butyl 1-(3-phenylbut-2-enoyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate were treated with 1 g of polyphosphoric acid. The mixture was heated to 90° C. for 2 hours and then quenched with a saturated solution of potassium carbonate at 0° C. The mixture was extracted three times with ethyl acetate (20 mL each), the combined organic fractions dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 10-30% methanol in dichloromethane) to yield 86 mg of the title compound as a yellow foam. 
     ESI-MS: m/z (%): 293.1 (100, [M+H] + ). 
     1H-NMR (500 MHz, DMSO-d6): δ=10.05 (bs, 1H), 9.85 (bs, 1H), 7.40 (d, 1H), 7.35 (d, 1H), 7.25 (m, 2H), 7.20 (m, 2H), 7.10 (m, 2H), 4.55 (m, 1H), 4.35 (m, 1H), 4.15 (m, 1H), 3.55 (m, 1H), 3.25 (m, 2H), 3.10 (m, 1H), 2.70 (m, 1H), 1.60 (s, 3H). 
     The following example was prepared analogously to example 1. 
     Example 4 
     8,8-Dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one (Compound of the Formula I.j, I.k or I.l in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-1 of Table B) 
     ESI-MS: m/z (%): 231 (100, [M+H] + ). 
     1H-NMR (500 MHz, CDCl 3 ): δ=7.20 (d, 1H), 7.00 (m, 2H), 4.10 (s, 4H), 3.20 (m, 2H), 2.50 (s, 2H), 1.30 (s, 6H). 
     The following examples 5 and 6 were prepared analogously to example 2. 
     Example 5 
     1,2,3,4-Tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopentan]-6(7H)-one (Compound of the Formula I.j, I.k or I.l in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-361 of Table B) 
     ESI-MS: m/z (%): 257 (100, [M+H] + ). 
     Example 6 
     1,2,3,4,6,7-Hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopentane](Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-361 of Table B) 
     ESI-MS: m/z (%): 243 (100, [M+H] + ). 
       1 H-NMR (500 MHz, CDCl 3 ): δ=7.15 (d, 1H), 6.95 (d, 1H), 6.80 (m, 1H), 3.90 (s, 2H), 3.20 (m, 2H), 3.05 (m, 4H), 1.95-1.65 (m, 10H). 
     The following examples 7 to 13 were prepared analogously to example 1. 
     Example 7 
     12a-Methyl-4,5,6,7,10,11,12,12a-octahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinolin-9(9aH)-one (Racemic Cis Diastereomer of the Compound of the Formula I.j, I.k or I.l in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-521 of Table B) 
     ESI-MS: m/z (%): 257 (100, [M+H] + ). 
     Example 8 
     8-Methyl-8-(trifluoromethyl)-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Single Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-81 of Table B) 
     ESI-MS: m/z (%): 271 (100, [M+H] + ). 
     The retention time according to method A is 1.396 min. 
     Example 9 
     8-Methyl-8-(trifluoromethyl)-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Single Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-81 of Table B) 
     ESI-MS: m/z (%): 271 (100, [M+H] + ). 
     The retention time according to method A is 1.543 min. 
     Example 10 
     12a-Methyl-4,5,6,7,10,11,12,12a-octahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinolin-9(9aH)-one (Racemic Trans Diastereomer of the Compound of the Formula I.j, I.k or I.l in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-521 of Table B) 
     ESI-MS: m/z (%): 257 (100, [M+H] + ). 
     Example 11 
     12a-Methyl-4,5,6,7,9,9a, 10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline (Racemic Cis Diastereomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-521 of Table B) 
     ESI-MS: m/z (%): 243 (100, [M+H] + ). 
       1 H-NMR (500 MHz, CDCl 3 ): δ=7.15 (d, 1H), 6.90 (d, 1H), 6.80 (m, 1H), 3.90 (m, 2H), 3.15 (m, 1H), 3.05 (m, 3H), 2.95 (m, 1H), 2.80 (m, 1H), 1.95 (m, 1H), 1.90 (m, 1H), 1.80 (m, 2H), 1.60 (m, 1H), 1.55 (m, 1H), 1.30 (m, 1H), 1.20 (s, 3H). 
     Example 12 
     8-Methyl-8-(trifluoromethyl)-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one (Racemic Mixture of Compound of the Formula I.j, I.k or 1.1 in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-81 of Table B) 
     ESI-MS: m/z (%): 285 (100, [M+H] + ). 
     Example 13 
     12a-Methyl-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino-[6,7,1-ij]quinoline hydrochloride (Racemic Trans Diastereomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-521 of Table B) 
     ESI-MS: m/z (%): 243 (100, [M+H] + ). 
       1 H-NMR (500 MHz, CDCl 3 ): δ=9.45 (bs, 1H), 9.05 (bs, 1H), 7.05 (d, 1H), 7.00 (d, 1H), 6.70 (m, 1H), 4.30 (m, 1H), 3.95 (m, 1H), 3.55 (m, 2H), 3.35 (m, 1H), 3.25 (m, 2H), 2.95 (m, 1H), 1.95 (m, 1H), 1.85 (m, 1H), 1.80 (m, 1H), 1.70 (m, 1H), 1.55 (m, 1H), 1.40 (m, 1H), 1.25 (m, 1H), 0.90 (s, 3H). 
     The following examples 14 and 15 were prepared analogously to example 3. 
     Example 14 
     8-Methyl-8-phenyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline hydrochloride (Racemic Mixture in Form of the Salt of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-161 of Table B) 
     ESI-MS: m/z (%): 279 (100, [M+H] + ) 
       1 H-NMR (500 MHz, CDCl 3 ): δ=7.22-7.27 (m, 2H), 7.11-7.19 (m, 3H), 6.95-7.04 (m, 2H), 6.78 (dd, J=8.0, 7.5 Hz, 1H), 3.99 (d, J=14.4 Hz, 1H), 3.87 99 (d, J=14.5 Hz, 1H), 3.20-3.26 (m, 1H), 3.01-3.08 (m, 4H), 2.87-2.94 (m, 1H), 2.09-2.15 (m, 1H), 1.92-1.99 (m, 1H), 1.73 (s, 3H) ppm. 
     Example 15 
     8-Methyl-8-phenyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Racemic Mixture of Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R and R 9a  is as in Row B-161 of Table B) 
     ESI-MS: m/z (%): 279 (100, [M+H] + ). 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 7.25 (m, 2H), 7.15 (m, 3H), 7.05 (d, 1H), 6.95 (d, 1H), 6.80 (m, 1H), 4.00 (m, 1H), 3.90 (m, 1H), 3.25 (m, 1H), 3.05 (m, 4H), 2.90 (m, 1H), 2.10 (m, 1H), 1.95 (m, 1H), 1.75 (s, 3H). 
     Example 16 
     (R)-5,6,7,9,9a, 10,11,12-Octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (2,2,2-trifluoroacetate) (R-Enantiomer of the Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row A-865 of Table A) 
     16.1 Preparation of (R)-tert-butyl 9-oxo-6,7,9a, 10,11,12-hexahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline-5(9H)-carboxylate 
     65 mg of (R)-tert-butyl 9-chloro-1-(pyrrolidine-2-carbonyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate was stirred together with 1.8 mg of 2′-(di-tert-butylphosphino)-N,N-dimethylbiphenyl-2-amine, 2.5 mg Pd 2 (dba) 3  and 19 mg sodium 2-methylpropan-2-olate at 100° C. over 10 hours in toluene. The reaction mixture was then cooled to room temperature and evaporated. The residue was purified by column chromatography on silica (eluent: 10-25% ethyl acetate in heptane) to yield 20 mg of the title compound as a beige solid. 
     ESI-MS: m/z (%): 344.20 (100, [M+H] + ). 
     16.2 Preparation of (R)-tert-butyl 6,7,9a, 10,11,12-hexahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline-5(9H)-carboxylate (R-Enantiomer of the Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row A-121 of Table a, Wherein However R 1  is not H, but Boc) 
     Reduction of the compound obtained in step 16.1 analogously to example 1.3 yielded the title compound. 
     ESI-MS: m/z (%): 330.20 (100, [M+H] + ). 
     16.3 Preparation of (R)-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline bis(2,2,2-trifluoroacetate) (R-Enantiomer of the Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row A-121 of Table A) 
     Boc-deprotection of the compound obtained in step 16.2 analogously to example 1.4 yielded the title compound. 
     ESI-MS: m/z (%): 230.15 (100, [M+H] + ). 
     Example 17 was prepared analogously to example 16 employing (S)-tert-butyl 9-chloro-1-(pyrrolidine-2-carbonyl)-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate as starting material which was derived from (R)-1-(((9H-fluoren-9-yl)methoxy)carbonyl)pyrrolidine-2-carboxylic acid. 
     Example 17 
     (S)-5,6,7,9,9a, 10,11,12-Octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (2,2,2-trifluoroacetate) (S-Enantiomer of the Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row A-865 of Table A) 
     ESI-MS: m/z (%): 230 (100, [M+H] + ). 
     The following examples 18 to 23 were prepared analogously to example 1. 
     Example 18 
     9-Chloro-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline, (2,2,2-trifluoroacetate) (Compound of the Formula I.g in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-3 of Table B) 
     ESI-MS: m/z (%): 251 (100, [M+H] + ). 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.95 (bs, 2H), 7.35 (d, 1H), 7.25 (d, 1H), 4.15 (s, 2H), 3.30-3.20 (m, 6H), 1.65 (m, 2H), 1.25 (s, 6H). 
     Example 19 
     10-Chloro-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (2,2,2-trifluoroacetate) (Compound of the Formula I.h in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-3 of Table B) 
     ESI-MS: m/z (%): 251 (100, [M+H] + ). 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 9.10 (bs, 2H), 7.35 (m, 1H), 7.20 (m, 1H), 4.15 (s, 2H), 3.30-3.20 (m, 6H), 1.65 (m, 2H), 1.25 (s, 6H). 
     Example 20 
     9-Chloro-8,8-dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one 2,2,2-trifluoroacetate (Compound of the Formula I.j in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-3 of Table B) 
     ESI-MS: m/z (%): 265 (100, [M+H] + ). 
     Example 21 
     10-Chloro-8,8-dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one 2,2,2-trifluoroacetate (Compound of the Formula I.k in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-3 of Table B) 
     ESI-MS: m/z (%): 265 (100, [M+H] + ). 
     Example 22 
     9-Fluoro-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.g in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-2 of Table B) 
     ESI-MS: m/z (%): 235 (100, [M+H] + ). 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.95 (m, 1H), 6.55 (m, 1H), 3.95 (s, 2H), 3.20-3.10 (m, 6H), 1.70 (m, 2H), 1.40 (s, 6H). 
     Example 23 
     10-Fluoro-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (2,2,2-trifluoroacetate) (Compound of the Formula I.h in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-2 of Table B) 
     ESI-MS: m/z (%): 235 (100, [M+H] + ). 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 9.05 (bs, 2H), 7.05 (d, 1H), 6.80 (m, 1H), 4.20 (s, 2H), 3.35 (m, 2H), 3.30 (m, 3.25), 3.25 (m, 2H), 1.70 (m, 2H), 1.30 (s, 6H). 
     The following examples 24 to 26 were prepared analogously to example 2. 
     Example 24 
     1,2,3,4,6,7-Hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclohexane] (2,2,2-trifluoroacetate) (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-401 of Table B) 
     ESI-MS: m/z (%): 257.2 (100, [M+H] + ). 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 8.85 (bs, 2H), 7.45 (d, 1H), 7.15 (d, 1H), 6.90 (m, 1H), 4.15 (s, 2H), 3.25 (m, 4H), 3.15 (m, 2H), 1.80 (m, 2H), 1.70 (m, 4H), 1.55 (m, 4H), 1.30 (m, 2H). 
     Example 25 
     1′,2′,3′,4′,6′,7′-Hexahydrospiro[cyclobutane-1,8′-[1,4]diazepino[6,7,1-ij]quinoline], hydrochloride (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-321 of Table B) 
     ESI-MS [M+H + ]=229.20 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 8.80 (bs, 2H), 7.50 (d, 1H), 6.95 (d, 1H), 6.90 (m, 1H), 4.10 (s, 2H), 3.25 (m, 2H), 3.20 (m, 2H), 3.10 (m, 2H), 2.35 (m, 2H), 2.00 (m, 2H), 1.90 (m, 4H). 
     Example 26 
     9′-Fluoro-1′,2′,3′,4′,6′,7′-hexahydrospiro[cyclobutane-1,8′-[1,4]diazepino[6,7,1-ij]quinoline], hydrochloride (Compound of the Formula I.g in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-322 of Table B) 
     ESI-MS [M+H + ]=247.15 
       1 H NMR (DMSO-d 6 , 500 MHz): [ppm]: 9.00 (bs, 2H), 7.25 (m, 1H), 6.80 (m, 1H), 4.10 (s, 2H), 3.25 (m, 2H), 3.20 (m, 2H), 3.10 (m, 2H), 2.65 (m, 2H), 2.00 (m, 4H), 1.85 (m, 2H). 
     The following examples 27 and 28 were prepared analogously to example 1. 
     Example 27 
     Enantiomer of 7,8,8-trimethyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline](Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-25 of Table B) 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 7.25 (d, 1H), 7.00 (d, 1H), 6.85 (dd, 1H), 4.00 (m, 1H), 3.90 (m, 1H), 3.15 (m, 4H), 3.05 (m, 2H), 1.85 (m, 1H), 1.30 (s, 3H), 1.10 (s, 3H), 0.95 (d, 3H). 
     The retention time of the Boc-protected precursor according to method B is 10.363. 
     Example 28 
     Enantiomer of 7,8,8-trimethyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline](Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-25 of Table B) 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 7.25 (d, 1H), 7.00 (d, 1H), 6.85 (dd, 1H), 4.00 (m, 1H), 3.90 (m, 1H), 3.15 (m, 4H), 3.05 (m, 2H), 1.85 (m, 1H), 1.30 (s, 3H), 1.10 (s, 3H), 0.95 (d, 3H). 
     The retention time of the Boc-protected precursor according to method B is 11.410 min. 
     The following example 29 was prepared analogously to example 1. 
     Example 29 
     3-Methyl-1′,2′,3′,4′,6′,7′-hexahydrospiro[cyclobutane-1,8′-[1,4]diazepino[6,7,1-ij]quinoline], hydrochloride (Compound of the Formula I.p, I.q or I.r in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-321 of Table B) 
     ESI-MS [M+H + ]=243.20 
       1 H NMR (DMSO-d 6 , 500 MHz): [ppm]: 9.30 (bs, 1H), 8.55 (bs, 1H), 7.60 (d, 1H), 7.20 (d, 1H), 6.95 (dd, 1H), 4.20 (m, 1H), 4.05 (m, 1H), 3.35 (m, 1H), 3.20 (m, 2H), 2.90 (m, 1H), 2.40 (m, 1H), 2.25 (m, 1H), 2.05 (m, 1H), 1.95 (m, 6H), 1.2 (d, 3H). 
     Example 30 
     3-Benzyl-2′,3′,7′,8′,9′,10′-hexahydro-1H-3′,8′,10a′-triaza-cyclohepta[de]naphthalene (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row A-181 of Table A) 
     30.1 Preparation of 2-(4-benzyl-3,4-dihydro-2H-quinoxalin-1-yl)-acetamide 
     A solution of 1 g (4.46 mmol) 1-benzyl-1,2,3,4-tetrahydroquinoxaline in 10 ml of dimethylformamide was treated with 3.14 ml (18.15 mmol) of N-Ethyl-N-isopropylpropan-2-amine, and subsequently 863 mg (9.23 mmol) 2-chloroacetamide was added. The reaction mixture was heated in a microwave system at 100° C. for four hours. The resulting mixture was quenched with water and extracted once with ethylacetate. The aqueous phase was set to pH 10 with sodium hydroxide solution and extracted 3× with ethylacetate. The combined organic extracts were dried with magnesium sulfate, evaporated till dryness and directly purified by column chromatography on silica (eluent: starting with heptane and then up to 100% ethylacetate) to yield 1.224 g of the title compound. 
     ESI-MS: m/z (%): 282.10 (100, [M+H] + ). 
     30.2 Preparation of 2-(4-Benzyl-3,4-dihydro-2H-quinoxalin-1-yl)-ethylamine 
     To 1.224 g (4.35 mmol) of 2-(4-benzyl-3,4-dihydro-2H-quinoxalin-1-yl)-acetamide were added 10.88 ml (21.75 mmol) borane dimethylsulfide THF solution and subsequently heated to 60° C. for six hours in a microwave system. The mixture was quenched with 1 molar hydrochloric acid and methanol and heated for 15 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethylacetate and extracted 3× with 1 molar hydrochlorid acid. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and evaporated to yield 1.089 g of the title compound as an oil. 
     ESI-MS: m/z (%): 268.15 (100, [M+H] + ). 
     30.3 Preparation of 3-benzyl-2,3,7,8,9,10-hexahydro-1H-3,8,10a-triaza-cyclohepta[de]-naphthalene 
     A solution of 1.089 g (4.07 mmol) of 2-(4-benzyl-3,4-dihydro-2H-quinoxalin-1-yl)-ethylamine and 20 ml ethanol was treated with 122 mg (4.07 mmol) of formaldehyde and 511 mg (4.48 mmol) of trifluoroacetic acid and stirred over night at room temperature. The solvent was evaporated and dichloromethane was added to the crude mixture. The organic phase was washed with 1 molar sodium hydroxide solution. The organic phase was dried and purified by column chromatography on silica (eluent: starting with dichloromethane and then up to 100% methanol) to yield 448 mg of the title compound. 
     ESI-MS [M+H + ]=280.10 (100, [M+H] + ). 
       1 H NMR (CDCl 3 , 500 MHz): [ppm]: 7.35 (m, 3H), 7.30 (m, 2H), 6.80 (dd, 1H), 6.65 (d, 1H), 6.60 (d, 1H), 4.55 (s, 2H), 4.10 (s, 2H), 3.30 (m, 4H), 3.25 (m, 2H), 3.10 (m, 2H). 
     Example 31 
     9-Fluoro-1-methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane], Trifluoroacetic Acid Salt (Compound of the Formula I.m in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-322 of Table B) 
     31.1 Preparation of 2-cyclobutylidene-N-(3-fluorophenyl)-acetamide 
     1.5 g (13.50 mmol) of 3-fluoroaniline were dissolved in 20 ml of dichloromethane and treated with 5.19 g (29.7 mmol) of N-ethyl-N-isopropylpropan-2-amine. Within 10 min 12.82 g (16.20 mmol) of 2-cyclobutylideneacetyl chloride were added at 0° C. and the solution was stirred overnight at room temperature. The mixture was poured on ice water and extracted 2× with dichloromethane. The combined organic phases were washed once with saturated sodium chloride solution, dried with MgSO 4  and evaporated in vacuo. The crude oil was treated with heptane and decanted twice, redissolved in ether-dichloromethane and treated with heptane till crystallization, yielding 2.2 g (77%) of a beige solid. 
     ESI-MS: m/z (%): 206 (100, [M+H] + ). 
     31.2 Preparation of 5′-fluoro-1′H-spiro[cyclobutane-1,4′-quinolin]-2′(3′H)-one 
     A solution of 400 mg (1.94 mmol) of 2-cyclobutylidene-N-(3-fluorophenyl)-acetamide obtained in step 31.1 was dissolved in 19.5 ml of toluene and irradiated with a Hg middle pressure lamp in a suitable device till completion of the reaction indicated by liquid chromatography. The crude solution was concentrated in vacuo and the residue was purified by column chromatography on silica (eluent: 10-30% ethyl acetate in heptane) to yield 55 mg (14%) of the title compound as a beige solid. 
     ESI-MS: m/z (%): 206 (100, [M+H] + ). 
     31.3 Preparation of 5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinoline] 
     A solution of 50 mg (0.244 mmol) of 5′-fluoro-1′H-spiro[cyclobutane-1,4′-quinolin]-2′(3′H)-one obtained in step 31.2 in 1 mL of tetrahydrofuran was treated with 0.73 mL of 1 M solution of borohydride-tetrahydrofuran complex in tetrahydrofuran. The mixture was stirred at reflux for 2 h, quenched with water and evaporated till dryness. The crude compound was used in the subsequent step without purification. 
     ESI-MS: m/z (%): 192 (100, [M+H] + ). 
     31.4 Preparation of 2-(5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)-acetamide 
     A solution of 50 mg (0.26 mmol) of 5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinoline] obtained in step 31.3 in 1 ml of dimethylformamide was treated with 6.2 mg (0.26 mmol) of sodium hydride followed by 72 mg (0.52 mmol) 2-bromoacetamide and heated in a microwave system at 100° C. for one hour. The resulting mixture was quenched with water, evaporated till dryness and directly purified by column chromatography on silica (eluent: 10% methanol in dichloromethane) to yield 70 mg of the title compound with about 80% purity determined by LCMS. 
     ESI-MS: m/z (%): 249 (100, [M+H] + ). 
     31.5 Preparation of 2-(5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)ethanamine 
     A solution of 40 mg (0.16 mmol) of 2-(5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)-acetamide obtained in step 31.4 in 1 ml of tetrahydrofurane was treated with 38 μl (0.38 mmol) of borane dimethylsulfide and heated to 70° C. for two hours. The mixture was quenched with water and hydrochloric acid, diluted with dichloromethane and extracted twice with water. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and evaporated to yield 10 mg of the title compound as an oil. 
     ESI-MS: m/z (%): 235 (100, [M+H] + ). 
     31.6 Preparation of 9-fluoro-1-methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane], Trifluoroacetic Acid Salt 
     A solution of 10 mg (0.043 mmol) of 2-(5′-fluoro-2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)ethan-amine obtained in step 31.5 in 0.4 ml of acetonitrile/methanol was treated with 3.8 mg (0.085 mmol) of acetaldehyde and 6.5 μl (0.085 mmol) of trifluoroacetic acid and stirred over night at room temperature. The solvent was evaporated and the crude mixture purified with reversed phase liquid chromatography to yield 1.5 mg of the title compound as beige solid. 
     ESI-MS: m/z (%): 261 (100, [M+H] + ). 
       1 H-NMR (500 MHz, pyridine-d5): δ=7.05 (dd, 1H), 6.80 (dd, 1H), 4.20 (q, 1H), 3.05 (m, 2H), 3.00 (m, 2H), 2.85 (m, 2H), 2.75 (m, 2H), 2.05 (m, 2H), 1.90-1.70 (m, 4H), 1.50 (d, 3H) ppm. 
     Example 32 
     2,3,5,6,7,8-Hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-217 of Table A) 
     32.1 Preparation of tert-butyl 1-benzyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate 
     To a solution of 388 mg (1.39 mmol) of 1-benzyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (compound of example 30) in 15 ml of dichloromethane was treated with 0.49 ml (2.78 mmol) of N,N-diisopropylethylamine. 333 mg (1.53 mmol) of di-tert-butyl dicarbonate were dissolved in 5 ml of dichloromethane, slowly added to the reaction mixture and the solution was then stirred overnight at room temperature. The solution was diluted with dichloromethane and treated twice with 10% aqueous solution of citric acid. The organic phase was washed once with saturated sodium chloride solution, dried with MgSO 4  and concentrated in vacuo, yielding 559 mg of the crude product. The crude compound was used in the subsequent step without purification. 
     ESI-MS [M+H + ]=380.20 
     32.2 Preparation of tert-butyl 2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]-quinoxaline-7(8H)-carboxylate 
     559 mg (1.47 mmol) of tert-butyl 1-benzyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate (559 mg, 1,473 mmol) (from step 32.1) were dissolved in 10 ml of methanol. The solution was hydrogenated with a 10% Pd/C cartridge using the H-Cube apparatus (from Thales Nano) at 80 bar and 70° C. with a flow rate of 0.5 ml/min for 6 hours. The solution was concentrated in vacuo yielding 320 mg of the crude product. The crude compound was used in the subsequent step without purification. 
     ESI-MS [M+H + ]=290.20 
     32.3 Preparation of 2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline 
     30 mg (0.104 mmol) of tert-butyl 2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate (from step 32.2) were dissolved in 2 ml of dichloromethane and treated with 0.20 ml (2.59 mmol) of trifluoroacetic acid at 0° C. The solution was allowed to warm up to room temperature and stirred for 2 h. The reaction mixture was diluted with dichloromethane and extracted once with a 1 molar aqueous solution of sodium hydroxide. The aqueous phase was extracted 3× with ethyl acetate. The combined organic phases were dried with magnesium sulfate, and concentrated in vacuo yielding 14 mg (0.076 mmol) of the title compound. 
     ESI-MS [M+H + ]=190.10 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.75 (m, 1H), 6.55 (d, 1H), 6.50 (d, 1H), 3.90 (s, 2H), 3.25 (m, 4H), 3.10 (m, 2H), 2.95 (m, 2H). 
     Example 33 
     1-Cyclobutyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline 2,2,2-trifluoroacetate (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-433 of Table A) 
     33.1 Preparation of tert-butyl 1-cyclobutyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate 
     A solution of 79 mg (0.237 mmol) of tert-butyl 2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate (from step 32.2) in 2 ml THF was treated with 38.3 mg (0.546 mmol) of cyclobutanone and molecular sieves (4 Å). The reaction mixture was stirred at room temperature overnight. 231 mg (1.09 mmol) of sodium triacetoxyborohydride was added and the reaction mixture was stirred overnight at room temperature. The reaction mixture was diluted with ethyl acetate and extracted once with a 1 molar aqueous solution of sodium hydroxide. The organic phase was dried with magnesium sulfate, concentrated in vacuo and the residue was purified by column chromatography on silica (eluent: 0-10% methanol in dichloromethane) yielding 78 mg (0.205 mmol) of the title compound. 
     ESI-MS [M+H + ]=344.20 
     33.2 Preparation of 1-cyclobutyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline 2,2,2-trifluoroacetate 
     78.4 mg (0.228 mmol) of tert-butyl 1-cyclobutyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate (from step 33.1) were dissolved in 1 ml of dichloromethane and treated with 0.53 ml (6.85 mmol) of trifluoroacetic acid at 0° C. The solution was stirred for 2 h and then concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-30% methanol in dichloromethane) to yield 69 mg of crude product, which was purified again via preparative HPLC to yield 46 mg of the title compound. 
     ESI-MS [M+H + ]=244.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.70 (bs, 2H), 6.80 (m, 1H), 6.75 (d, 1H), 6.70 (d, 1H), 4.10 (m, 2H), 4.05 (m, 1H), 3.25 (m, 2H), 3.20 (m, 2H), 3.10 (m, 4H), 2.20 (m, 2H), 2.10 (m, 2H), 1.65 (m, 2H). 
     Example 34 
     1-Methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5 , R 5b , R 6  and R 9a  is as in row A-253 of Table A) 
     The title compound was prepared in analogy to example 33, using however formaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=204.10 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.85 (m, 1H), 6.65 (d, 1H), 6.55 (d, 1H), 3.90 (s, 2H), 3.35 (m, 2H), 3.15 (m, 2H), 3.10 (m, 2H), 2.95 (m, 5H). 
     Example 35 
     1-(Oxetan-3-yl)-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline 2,2,2-trifluoroacetate (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in row A-541 of Table A) 
     The title compound was prepared in analogy to example 33, using however oxetan-3-one instead of cyclobutanone. 
     ESI-MS [M+H + ]=246.15 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.80 (m, 2H), 6.75 (m, 2H), 6.30 (d, 1H), 4.80 (m, 2H), 4.65 (m, 3H), 4.10 (s, 2H), 3.35 (m, 2H), 3.20 (m, 4H), 3.10 (m, 2H). 
     Example 36 
     1-(Cyclopropylmethyl)-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-577 of Table A) 
     The title compound was prepared in analogy to example 33, using however cyclopropanecarboxaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=244.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.85 (m, 1H), 6.75 (m, 1H), 6.55 (m, 1H), 4.00 (m, 2H), 3.35-3.15 (m, 8H), 3.00 (m, 2H), 1.05 (m, 1H), 0.50 (m, 2H), 0.20 (m, 2H). 
     Example 37 
     1-(Cyclopentylmethyl)-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-649 of Table A) 
     The title compound was prepared in analogy to example 33, using however cyclopentanecarboxaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=272.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.80 (m, 1H), 6.65 (d, 1H), 6.50 (d, 1H), 3.95 (m, 2H), 3.30-3.20 (m, 6H), 3.15 (m, 2H), 2.95 (m, 2H), 2.30 (m, 1H), 1.90-1.55 (m, 6H), 1.25 (m, 2H). 
     Example 38 
     Cyclopropyl(2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxalin-1-yl)methanone (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-721 of Table A) 
     38.1 Preparation of tert-butyl 1-(cyclopropanecarbonyl)-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate 
     To 50 mg (0.173 mmol) of tert-butyl 2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate dissolved in 1 ml of dichloromethane were added 0.77 ml (4.43 mmol) of N,N-diisopropylethylamine in an inert atmosphere at 0° C. 19 μl (0.21 mmol) of cyclopropanecarbonyl chloride was dissolved in 1 ml of dichloromethane and slowly added to the reaction mixture. The reaction mixture was stirred at room temperature for 5 h. The solution was diluted with dichloromethane and treated twice with 10% aqueous solution of citric acid. The organic phase was washed once with saturated sodium chloride solution, dried with MgSO 4  and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-10% methanol in dichloromethane) yielding 35 mg (0.098 mmol) of the title compound. 
     ESI-MS [M-tert-butyl+H + ]=302.10 
     38.2 Preparation of cyclopropyl(2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]-quinoxalin-1-yl)methanone 
     35 mg (0.098 mmol) of tert-butyl 1-(cyclopropanecarbonyl)-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate were dissolved in 2 ml of dichloromethane and treated with 150 μl (1.96 mmol) of trifluoroacetic acid at 0° C. The solution was stirred overnight at room temperature. 100 μl (1.31 mmol) of trifluoroacetic acid were added and the reaction mixture was stirred for 1 h. The reaction mixture was treated 3× with acidified water. The combined aqueous phase was basified with 1 N sodium hydroxide solution and extracted 5× with dichloromethane. The combined organic phase was dried with MgSO 4  and concentrated in vacuo to yield 23 mg of the title compound. 
     ESI-MS [M+H + ]=258.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.30 (m, 1H), 7.05 (m, 1H), 6.80 (m, 1H), 4.10 (s, 2H), 3.90 (m, 2H), 3.45 (m, 4H), 3.30 (m, 2H), 2.10 (m, 1H), 1.15 (m, 2H), 0.85 (m, 2H). 
     Example 39 
     Cyclopentyl(2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxalin-1-yl)methanone (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in row A-793 of Table A) 
     The title compound was prepared in analogy to example 38 using cyclopentanecarbonyl chloride. 
     ESI-MS [M+H + ]=286.20  1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.00 (m, 2H), 6.80 (m, 1H), 4.10 (s, 2H), 3.90 (m, 2H), 3.45-3.20 (m, 7H), 1.80 (m, 6H), 1.55 (m, 2H). 
     Example 40 
     1-Cyclopropyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-397 of Table A) 
     40.1 Preparation of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)acetamide 
     A solution of 500 mg (2.87 mmol) of 1-cyclopropyl-1,2,3,4-tetrahydroquinoxaline in 5 ml dimethylformamide was treated with 2.0 ml (11.68 mmol) of N-ethyl-N-isopropylpropan-2-amine, and subsequently 555 mg (5.94 mmol) 2-chloroacetamide were added. The reaction mixture was heated in a microwave system at 100° C. for 12 hours. The reaction mixture was quenched with water and basified with 1 N sodium hydroxide solution. The aqueous phase was extracted 3× with dichloromethane. The combined organic extracts were dried with magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 620 mg of the title compound. 
     ESI-MS [M+H + ]=232.20 
     40.2 Preparation of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)ethanamine 
     To 620 mg (2.68 mmol) of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1 (2H)-yl)acetamide in 2 ml of THF was added 5.4 ml (10.80 mmol) of 2 molar borane dimethylsulfide THF solution and subsequently heated for 7 hours at 60° C. in a microwave system. An additional 2.7 ml (5.40 mmol) of 2 molar borane dimethylsulfide THF solution was added to the reaction mixture and heated for 10 hours at 60° C. in a microwave system. To the reaction mixture were added 2 ml of methanol, acidified with 2 molar hydrochloric acid and heated for 15 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethyl acetate and extracted twice with 1 molar hydrochloric acid. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-15% methanol in dichloromethane) to yield 347 mg of the title compound. 
     ESI-MS [M+ H ]=218.20 
     40.3 Preparation of 1-Cyclopropyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]-quinoxaline 
     A solution of 347 mg (1.6 mmol) of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)ethanamine in 5 ml of ethanol were treated with 119 μl (1.6 mmol) of 37% aqueous formaldehyde solution and 135 μl (1.76 mmol) of trifluoroacetic acid. The reaction mixture was stirred for 36 h at room temperature. Water was added and the reaction mixture was basified using 2 N aqueous sodium hydroxide solution. The aqueous phase was extracted three times with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 177 mg of the title compound. 
     ESI-MS [M+H + ]=230.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.10 (d, 1H), 6.80 (m, 1H), 6.60 (d, 1H), 3.85 (s, 2H), 3.20 (m, 2H), 3.10 (m, 2H), 3.00 (m, 4H), 2.25 (m, 1H), 0.80 (m, 2H), 0.55 (m, 2H). 
     Example 41 
     1-Cyclopentyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5b , R 5b , R 6  and R 9a  is as in Row A-469 of Table A) 
     The title compound was prepared in analogy to example 40 using 1-cyclopentyl-1,2,3,4-tetrahydroquinoxaline as starting material. 
     ESI-MS [M+H + ]=258.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.80 (d, 1H), 6.70 (m, 1H), 6.45 (d, 1H), 4.25 (m, 1H), 3.75 (s, 2H), 3.15 (m, 2H), 3.05 (m, 2H), 2.90 (m, 2H), 2.85 (m, 2H), 1.80 (m, 2H), 1.65 (m, 2H), 1.55 (m, 4H). 
     Example 42 
     1-Cyclopropyl-5-methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-397 of Table A) 
     42.1 Preparation of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1 (2H)-yl)propanamide 
     A solution of 300 mg (1.72 mmol) of 1-cyclopropyl-1,2,3,4-tetrahydroquinoxaline in 3 ml dimethylformamide was treated with 1.2 ml (7.0 mmol) of N-ethyl-N-isopropylpropan-2-amine, 387 mg (2.58 mmol) of sodium iodide and subsequently 523 mg (3.44 mmol) of 2-bromopropanamide were added. The reaction mixture was heated in a microwave system at 100° C. for 8 hours. The reaction mixture was quenched with water and basified with 1 N sodium hydroxide solution. The aqueous phase was extracted 3× with dichloromethane. The combined organic extracts were dried with magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 453 mg of the title compound. 
     ESI-MS [M+H + ]=246.20 
     42.2 Preparation of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)propan-1-amine 
     To 453 mg (1.85 mmol) of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)propanamide in 2 ml THF were added 4.3 ml (8.60 mmol) of 2 molar borane dimethylsulfide THF solution and subsequently heated for 9 hours at 60° C. and 2 hours at 70° C. in a microwave system. To the reaction mixture was added 2 ml of methanol, acidified with 2 molar hydrochloric acid and heated for 15 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethyl acetate and extracted twice with 1 molar hydrochloric acid. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-15% methanol in dichloromethane) to yield 209 mg of the title compound. 
     ESI-MS [M+H + ]=232.20 
     42.3 Preparation of 1-cyclopropyl-5-methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino-[1,7,6-de]quinoxaline 
     A solution of 209 mg (0.9 mmol) of 2-(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)propan-1-amine in 3 ml of ethanol were treated with 67 μl (0.9 mmol) of 37% aqueous formaldehyde solution and 76 μl (0.99 mmol) of trifluoroacetic acid. The reaction mixture was stirred for 36 h at room temperature. Water was added and the reaction mixture was basified using 2 N aqueous sodium hydroxide solution. The aqueous phase was extracted three times with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 136 mg of the title compound. 
     ESI-MS [M+H + ]=244.20 
     1H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.00 (d, 1H), 6.65 (m, 1H), 6.50 (d, 1H), 3.75 (d, 1H), 3.45 (d, 1H), 3.30-3.15 (m, 4H), 3.05 (m, 1H), 2.80 (d, 1H), 2.65 (d, 1H), 2.20 (m, 1H), 0.90 (d, 3H), 0.80 (m, 2H), 0.50 (m, 2H). 
     Example 43 
     1-Cyclopentyl-5-methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-469 of Table A) 
     The title compound was prepared in analogy to example using however 1-cyclopentyl-1,2,3,4-tetrahydroquinoxaline instead of 1-cyclopropyl-1,2,3,4-tetrahydroquinoxaline. 
     ESI-MS [M+H + ]=272.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.70 (d, 1H), 6.65 (m, 1H), 6.40 (d, 1H), 4.20 (m, 1H), 3.75 (d, 1H), 3.50 (d, 1H), 3.25-3.10 (m, 3H), 3.00 (m, 2H), 2.85 (d, 1H), 2.70 (d, 1H), 1.80 (m, 2H), 1.70-1.55 (m, 5H), 1.50 (m, 1H), 0.90 (d, 3H). 
     Example 44 
     5,6,7,9,9a,10,11,12,13,14-decahydro-4H-azepino[1,2-a][1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-937 of Table A) 
     44.1 Preparation of ethyl 1-(2-nitrophenyl)azepane-2-carboxylate 
     A solution of 450 mg (3.19 mmol) of 1-fluoro-2-nitrobenzene, 546 mg (3.19 mmol) of ethyl azepane-2-carboxylate and 0.89 ml (6.38 mmol) of triethylamine in 10 ml acetonitrile was stirred overnight at reflux. The reaction mixture was concentrated in vacuo. To the residue was added aqueous sodium bicarbonate solution and extracted twice with ethyl acetate. The combined organic extracts were dried with sodium sulfate and concentrated in vacuo to yield 780 mg of the crude title compound. The crude product was used without further purification in the next step. 
     ESI-MS [M+H + ]=293.10 
     44.2 Preparation of 6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-6(5H)-one 
     780 mg (2.67 mmol) of ethyl 1-(2-nitrophenyl)azepane-2-carboxylate were dissolved in 30 ml methanol and treated with 284 mg of 10% Pd/C in a hydrogen atmosphere. The solution was stirred at room temperature for 1 h. The catalyst was filtered off and the solution was concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-50% ethyl acetate in heptane) to yield 159 mg of the title compound. 
     ESI-MS [M+H + ]=217.10 
     44.3 Preparation of 5,6,6a,7,8,9,10,11-octahydroazepino[1,2-a]quinoxaline 
     To 105 mg (0.485 mmol) 6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-6(5H)-one in 4 ml of THF (tetrahydrofuran) were added 0.97 ml (0.97 mmol) of 1 molar borane dimethylsulfide THF solution and subsequently heated for 1 h at 80° C. in a microwave system. The reaction mixture was poured on ice water, acidified with hydrochloric acid solution to pH=5 and extracted twice with ethyl acetate. The combined organic phases were dried and concentrated in vacuo. The residue was acidified with hydrochloric acid solution and extracted once with ether. The aqueous phase was basified with aqueous sodium bicarbonate solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo to yield 85 mg of the crude title compound. 
     ESI-MS [M+H + ]=203.20 
     44.4 Preparation of 2-(6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-5(6H)-yl)-acetamide 
     A solution of 85 mg (0.40 mmol) of 5,6,6a,7,8,9,10,11-octahydroazepino[1,2-a]quinoxaline in 2 ml of dimethylformamide was treated with 16 mg (0.40 mmol) of sodium hydride (60% in mineral oil) and stirred for 15 min at room temperature. 112 mg (1.2 mmol) of 2-chloroacetamide were added and the reaction mixture was heated in a microwave system at 100° C. for 4 hours. 209 μl (1.2 mmol) of N-ethyl-N-isopropylpropan-2-amine were added to the reaction mixture and heated at 100° C. for 2 hours. 110 mg (0.8 mmol) of 2-bromoacetamide were added and the reaction mixture was heated in a microwave system at 100° C. for 2 hours. The reaction mixture was basified with sodium bicarbonate solution and extracted 2× with ethyl acetate. The combined organic extracts were dried with magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-50% ethyl acetate in heptane) to yield 42 mg of the title compound. 
     ESI-MS [M+H + ]=260.20 
     44.5 Preparation of 2-(6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-5(6H)-yl)-ethanamine 
     To 42 mg (0.146 mmol) of 2-(6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-5(6H)-yl)acetamide in 1 ml of THF were added 292 μl (8.60 mmol) of 2 molar borane dimethylsulfide THF solution and subsequently heated for 6 hours at 60° C. in a microwave system. Additional 292 μl (8.60 mmol) of 2 molar borane dimethylsulfide THF solution were added to the reaction mixture and heated for 4 hours at 60° C. in a microwave system. To the reaction mixture was added 2 ml of methanol, acidified with 2 molar aqueous hydrochloric acid solution and heated for 15 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethyl acetate and extracted twice with 1 molar hydrochloric acid. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo to yield 36 mg of the title compound. 
     ESI-MS [M+H + ]=246.20 
     44.6 Preparation of 5,6,7,9,9a,10,11,12,13,14-decahydro-4H-azepino[1,2-a][1,4]-diazepino[1,7,6-de]quinoxaline 
     A solution of 36 mg (0.147 mmol) of 2-(6a,7,8,9,10,11-hexahydroazepino[1,2-a]quinoxalin-5(6H)-yl)ethanamine in 2 ml of ethanol were treated with 11 μl (0.147 mmol) of 37% aqueous formaldehyde solution and 12 μl (0.161 mmol) of trifluoroacetic acid. The reaction mixture was stirred overnight at room temperature. The reaction mixture was concentrated in vacuo, treated with aqueous sodium bicarbonate solution and extracted twice with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 12.7 mg of the title compound. 
     ESI-MS [M+H + ]=258.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.65 (m, 1H), 6.50 (d, 1H), 6.35 (d, 1H), 3.70 (m, 1H), 3.60 (m, 1H), 3.20 (m, 2H), 3.10 (m, 1H), 3.00 (m, 3H), 2.95 (m, 1H), 2.85 (m, 1H), 2.80 (m, 1H), 1.80 (m, 2H), 1.65-1.50 (m, 4H), 1.40 (m, 2H). 
     Example 45 
     7-Methyl-5,6,7,9,9 a , 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-865 of Table A) 
     The title compound was prepared in analogy to example 42, using however 1,2,3,3a,4,5-hexahydropyrrolo[1,2-a]quinoxaline and 2-bromopropanamide. 
     ESI-MS [M+H + ]=244.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.80 (m, 1H), 6.50 (d, 1H), 6.45 (d, 1H), 3.95 (d, 1H), 3.70 (d, 1H), 3.50 (m, 2H), 3.15 (m, 2H), 2.85 (m, 2H), 2.75 (m, 1H), 2.20 (m, 1H), 2.10 (m, 1H), 2.00 (m, 1H), 1.90 (m, 1H), 1.35 (m, 1H), 1.20 (d, 3H). 
     Example 46 
     1-Fluoro-7-methyl-5,6,7,9,9 a ,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (Compound of the Formula I.gg in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-866 of Table A) 
     The title compound was prepared in analogy to example 42, using however 9-fluoro-1,2,3,3a,4,5-hexahydropyrrolo[1,2-a]quinoxaline and 2-bromopropanamide. 
     ESI-MS [M+H + ]=262.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.60 (m, 1H), 6.55 (m, 1H), 3.90 (d, 1H), 3.80 (m, 1H), 3.55 (d, 1H), 3.20 (d, 1H), 3.00 (m, 2H), 2.80 (m, 2H), 2.55 (m, 1H), 2.15 (m, 2H), 1.80 (m, 2H), 1.50 (m, 1H), 1.25 (d, 3H). 
     Example 47 
     1,2,3,4,6,7-Hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopropane](Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-281 of Table B) 
     47.1 Preparation of 2-(2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinolin]-1′-yl)-acetamide 
     A solution of 500 mg (3.14 mmol) of 2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinoline] in 5 ml of dimethylformamide was treated with 2.2 ml (12.8 mmol) of N-ethyl-N-isopropylpropan-2-amine and 706 mg (4.71 mmol) of sodium iodide; and subsequently 670 mg (7.16 mmol) of 2-chloroacetamide were added. The reaction mixture was heated in a microwave system at 100° C. for 10 hours. The reaction mixture was quenched with water and basified with 1 N sodium hydroxide solution. The aqueous phase was extracted 3× with dichloromethane. The combined organic extracts were dried with magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 624 mg of the title compound. 
     ESI-MS [M+H + ]=217.20 
     47.2 Preparation of 2-(2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinolin]-1′-yl)ethan-amine 
     To 624 mg (2.89 mmol) of 2-(2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinolin]-1′-yl)acetamide in 2 ml of THF were added 5.77 ml (11.54 mmol) of 2 molar borane dimethylsulfide THF solution and subsequently heated for 9 hours at 60° C. in a microwave system. To the reaction mixture were added 2 ml of methanol, acidified with 2 molar hydrochloric acid and heated for 15 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethyl acetate and extracted twice with 1 molar hydrochloric acid. The combined aqueous phases were set to pH 10 with sodium hydroxide solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 299 mg of the title compound. 
     ESI-MS [M+H + ]=203.20 
     47.3 Preparation of 1,2,3,4,6,7-Hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopropane] 
     A solution of 299.6 mg (1.48 mmol) of 2-(2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinolin]-1′-yl)ethanamine in 3 ml of ethanol was treated with 110 μl (1.48 mmol) of 37% aqueous formaldehyde solution and 126 μl (1.63 mmol) of trifluoroacetic acid. The reaction mixture was stirred overnight at room temperature. Water was added and the reaction mixture was basified using 2 N aqueous sodium hydroxide solution. The aqueous phase was extracted three times with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 131 mg of the title compound. 
     ESI-MS [M+H + ]=215.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.90 (d, 1H), 6.70 (m, 1H), 6.55 (d, 1H), 3.75 (s, 2H), 3.25 (m, 2H), 3.00 (m, 2H), 2.90 (m, 2H), 1.60 (m, 2H), 0.95 (s, 2H), 0.80 (s, 2H). 
     Example 48 
     4-Methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclopropane](Compound of the Formula I.s, I.t or I.u in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-281 of Table B) 
     The title compound was prepared in analogy to example 47, using however 2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-quinoline] and 2-bromopropanamide. 
     ESI-MS [M+H + ]=229.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.85 (d, 1H), 6.65 (m, 1H), 6.55 (d, 1H), 3.80 (d, 1H), 3.50 (d, 1H), 3.25 (m, 3H), 2.85 (d, 1H), 2.70 (d, 1H), 1.70 (m, 1H), 1.60 (m, 1H), 1.05 (m, 1H), 0.90 (m, 3H), 0.85 (m, 1H), 0.75 (m, 2H). 
     Example 49 
     11-Fluoro-8,8-Dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-2 of Table B) 
     The title compound was prepared in analogy to example 47, using however 7-fluoro-4,4-dimethyl-1,2,3,4-tetrahydroquinoline and 2-bromoacetamide. 
     ESI-MS [M+H + ]=235.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.15 (dd, 1H), 6.55 (dd, 1H), 3.80 (s, 2H), 3.20 (m, 2H), 3.10 (m, 2H), 2.90 (m, 2H), 1.60 (m, 2H), 1.20 (s, 6H). 
     Example 50 
     10-Methoxy-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline, trifluoroacetic acid (Compound of the Formula I.h in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-7 of Table B) 
     The title compound was prepared in analogy to example 1, using however 7-methoxy-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate and 3-methylbut-2-enoyl chloride. 
     ESI-MS [M+H + ]=247.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.75 (bs, 2H), 6.95 (s, 1H), 6.85 (s, 1H), 4.15 (m, 2H), 3.70 (s, 3H), 3.20 (m, 2H), 3.15 (m, 4H), 1.65 (m, 2H), 1.25 (s, 6H). 
     Example 51 
     4,8,8-Trimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline 2,2,2-trifluoroacetate (Compound of the Formula I.s, I.t or I.u in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-1 of Table B) 
     The title compound was prepared in analogy to example 47, using however 4,4-dimethyl-1,2,3,4-tetrahydroquinoline and 2-bromopropanamide. 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 9.90 (bs, 1H), 9.20 (bs, 1H); 7.35 (d, 1H), 7.10 (d, 1H), 6.90 (m, 1H), 4.30 (d, 1H), 4.05 (d, 1H), 3.45 (m, 1H), 3.25 (m, 3H), 3.15 (m, 1H), 1.70 (m, 2H), 1.30 (m, 9H). 
     Example 52 
     4-Ethyl-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.v, I.w or I.x in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-1 of Table B) 
     The title compound was prepared in analogy to example 47, using however 4,4-dimethyl-1,2,3,4-tetrahydroquinoline and 2-bromobutanamide. 
     ESI-MS [M+H + ]=245.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.15 (d, 1H), 6.85 (d, 1H), 6.70 (m, 1H), 3.85 (d, 1H), 3.50 (d, 1H), 3.20 (m, 2H), 3.00 (d, 1H), 2.95 (m, 1H), 2.75 (d, 1H), 1.60 (m, 2H), 1.40 (m, 2H), 1.25 (s, 3H), 1.30 (s, 3H), 0.80 (m, 3H). 
     Example 53 
     6,8,8-Trimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.y, I.z or I.Zz in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-1 of Table B) 
     The title compound was prepared in analogy to example 47, using however 2,4,4-trimethyl-1,2,3,4-tetrahydroquinoline and 2-chloroacetamide. 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.05 (d, 1H), 6.90 (d, 1H), 6.65 (m, 1H), 3.85 (d, 1H), 3.45 (d, 1H), 3.30 (m, 3H), 3.00 (m, 1H), 2.70 (m, 1H), 1.65 (m, 1H), 1.40 (m, 1H), 1.25 (s, 3H), 1.15 (s, 6H). 
     Example 54 
     One Enantiomer of 8-ethyl-8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]-quinoline, Trifluoroacetic Acid (Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-41 of Table B) 
     The title compound was prepared in analogy to example 1, using however tert-butyl 2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate and (Z)-3-methylpent-2-enoyl chloride. 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.90 (bs, 1H), 8.65 (bs, 1H), 7.30 (d, 1H), 7.15 (d, 1H), 6.90 (m, 1H), 4.20 (m, 1H), 4.10 (m, 1H), 3.25 (m, 6H), 1.85 (m, 1H), 1.70 (m, 1H), 1.60 (m, 1H), 1.45 (m, 1H), 1.20 (s, 3H), 0.70 (m, 3H). 
     Example 55 
     Other enantiomer of 8-ethyl-8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline, Trifluoroacetic Acid (Enantiomer of the Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in row B-41 of Table B) 
     The title compound was prepared in analogy to example 1, using however tert-butyl 2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate and (Z)-3-methylpent-2-enoyl chloride. 
     ESI-MS [M+H + ]=231.10 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 8.90 (bs, 1H), 8.65 (bs, 1H), 7.30 (d, 1H), 7.15 (d, 1H), 6.90 (m, 1H), 4.20 (m, 1H), 4.10 (m, 1H), 3.20 (m, 6H), 1.85 (m, 1H), 1.70 (m, 1H), 1.60 (m, 1H), 1.45 (m, 1H), 1.20 (s, 3H), 0.70 (m, 3H). 
     Example 56 
     4-Methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane](Compound of the Formula I.s, I.t or I.u in which the Combination of R 5a , R 5b , R, R 8  and R 9a  is as in row B-321 of Table B) 
     56.1 Preparation of 2-cyclobutylidene-N-phenylacetamide 
     3.35 g (36 mmol) of aniline were dissolved in 60 ml of dichloromethane and treated with 13.83 ml (79 mmol) of N-ethyl-N-isopropylpropan-2-amine. Within 10 min 19.80 ml of a 1 molar solution of 2-cyclobutylideneacetyl chloride in dichloromethane was added at 0° C. and the solution was stirred overnight at room temperature. The reaction mixture was poured on ice water and extracted 2× with dichloromethane. The combined organic phases were washed once with saturated sodium chloride solution, dried with magnesium sulfate and concentrated in vacuo. The crude oil was dissolved in dichloromethane and treated with ether till crystallization, yielding 5.5 g of the title compound. 
     ESI-MS [M+H + ]=188.10 
     56.2 Preparation of 1′H-spiro[cyclobutane-1,4′-quinolin]-2′(3′H)-one 
     A solution of 2.0 g (10.68 mmol) of 2-cyclobutylidene-N-phenylacetamide in 214 ml of toluene was irradiated with a 700 W mercury lamp in a flow reactor (FEP-tubing, pyrex filter) with a flow rate of 1 ml per min at a temperature range of 0° C. to 20° C. with a residence time of 5 to 7 min. The reaction mixture was concentrated in vacuo and the residue was purified by column chromatography on silica (eluent: 0-55% ethyl acetate in cyclohexane) to yield 940 mg of the title compound. 
     ESI-MS [M+H + ]=188.10 
     56.3 Preparation of 2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinoline] 
     To 850 mg (4.54 mmol) of 1′H-spiro[cyclobutane-1,4′-quinolin]-2′(3′H)-one in 5 ml of THF were added 9.08 ml (9.08 mmol) of 1 molar borane dimethylsulfide THF solution and subsequently heated for 30 min at 80° C. in a microwave system. The reaction mixture was acidified with 6 molar hydrochloric acid solution and treated with ethyl acetate. The organic phase was extracted twice with 1 molar hydrochloric acid solution. The combined aqueous phases were set to pH 10 with sodium bicarbonate and extracted 3× with ethyl acetate. The combined organic phases were dried and concentrated in vacuo to yield 565 mg of the crude title compound. 
     ESI-MS [M+H + ]=174.10 
     56.4 Preparation of 2-(2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)propanamide 
     ESI-MS [M+H + ]=245.20 
     A solution of 300 mg (1.73 mmol) of 2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinoline] in 10 ml dimethylformamide was treated with 69 mg (1.73 mmol) of sodium hydride (60% in mineral oil) and stirred for 15 min at 50° C., then transferred to a microwave vial and stirred for 5 min at 70° C. in a microwave system. Subsequently 790 mg (5.19 mmol) of 2-bromoacetamide were added and the reaction mixture was heated in a microwave system at 100° C. for 7 hours. Additional 263 mg (1.73 mmol) of 2-bromoacetamide were added and the reaction mixture was heated in a microwave system at 100° C. for 2 hours. The reaction mixture was quenched with ice water, acidified to pH=5 and extracted with ether. The aqueous phase was basified with sodium bicarbonate solution and extracted 3× with dichloromethane. The combined organic extracts were dried with magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-55% ethyl acetate in heptane) to yield 258 mg of the title compound. 
     56.5 Preparation of 2-(2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)propan-1-amine 
     To 258 mg (0.348 mmol) of 2-(2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)propanamide in 2 ml THF were added 1.05 ml (2.10 mmol) of 2 molar borane dimethylsulfide THF solution and subsequently heated for 6 hours at 60° C. in a microwave system. Subsequently 348 μl (0.70 mmol) of 2 molar borane dimethylsulfide THF solution was added to the reaction mixture and heated for 2 hours at 60° C. in a microwave system. Subsequently 697 μl (1.39 mmol) of 2 molar borane dimethylsulfide THF solution was added to the reaction mixture and heated for 3 hours at 60° C. in a microwave system. To the reaction mixture was added 2 ml of methanol, acidified with 2 molar hydrochloric acid and heated for 5 minutes at 60° C. in a microwave system. The reaction mixture was diluted with ethyl acetate and extracted twice with 1 molar hydrochloric acid. The combined aqueous phases were set to pH 10 with sodium bicarbonate solution and extracted 3× with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-20% methanol in dichloromethane) to yield 90 mg of the title compound. 
     ESI-MS [M+H + ]=231.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.35 (d, 1H), 6.95 (dd, 1H), 6.70 (d, 1H), 6.55 (dd, 1H), 3.80 (m, 1H), 3.05 (m, 1H), 3.00 (m, 1H), 2.70 (m, 1H), 2.55 (m, 1H), 2.35 (m, 1H), 2.25 (m, 1H), 2.00 (m, 1H), 1.90 (m, 5H), 1.05 (d, 3H). 
     56.6 Preparation of 4-methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]-quinoline-8,1′-cyclobutane] 
     A solution of 90 mg (0.313 mmol) of 2-(2′,3′-dihydro-1′H-spiro[cyclobutane-1,4′-quinolin]-1′-yl)propan-1-amine in 2 ml of ethanol was treated with 23 μl (0.313 mmol) of 37% aqueous formaldehyde solution and 26 μl (0.344 mmol) of trifluoroacetic acid. The reaction mixture was stirred overnight at room temperature. Further 12 μl (0.156 mmol) of 37% aqueous formaldehyde solution and 12 μl (0.156 mmol) of trifluoroacetic acid were added to the reaction mixture and stirring was continued overnight at room temperature. The reaction mixture was concentrated in vacuo and to the residue was added aqueous sodium bicarbonate solution. The aqueous phase was extracted twice with dichloromethane. The combined organic phases were dried and concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-10% methanol in dichloromethane) to yield 38 mg of the title compound. 
     ESI-MS [M+H + ]=243.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 7.35 (d, 1H), 6.90 (d, 1H), 6.75 (d, 1H), 3.80 (m, 1H), 3.40 (m, 1H), 3.20 (m, 2H), 3.10 (m, 1H), 2.80 (m, 1H), 2.70 (m, 1H), 2.40 (m, 1H), 2.15 (m, 1H), 2.00 (m, 4H), 1.85 (m, 1H), 1.70 (m, 1H), 0.80 (s, 3H). 
     Example 57 
     1-Fluoro-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, Trifluoroacetic Acid (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-866 of Table A) 
     57.1 Preparation of methyl pyrrolidine-2-carboxylate 
     To a solution of pyrrolidine-2-carboxylic acid (75 g, 651 mmol) in methanol (750 ml), SOCl 2  (250 ml) was added dropwise at 0° C., and the reaction mixture was stirred for 16 hrs at 20° C. One additional vial was set up in the same way. Both reaction mixtures were combined and concentrated under reduced pressure to give the title compound (90 g, 543 mmol, yield 50%). 
       1 H NMR (400 MHz, DMSO-d 6 ): δ[ppm]: 9.83 (s, 1H), 4.32 (t, J=7.6 Hz, 1H), 3.72 (s, 3H), 3.21-3.15 (m, 2H), 2.22-2.20 (m, 1H), 1.96-1.87 (m, 3H) 
     57.2 Preparation of methyl 1-(2-fluoro-6-nitro-phenyl)-pyrrolidine-2-carboxylate 
     To a mixture of methyl pyrrolidine-2-carboxylate (17.18 g, 104 mmol) in acetonitril (500 mL), triethylamine (26.3 mL, 189 mmol) and 1,2-difluoro-3-nitrobenzene (15 g, 94 mmol) were added at 20° C., and the reaction mixture was stirred for 12 h at 80° C. Then the mixture was cooled to 20° C., concentrated under reduced pressure, and the residue was purified by column chromatography on silica gel (petrol ether:ethyl acetate=20:1 to 10:1) to give the title compound (20 g, 74.6 mmol, yield 79%). 
       1 H NMR (400 MHz, CDCl 3 ): δ[ppm]: 7.36 (d, J=8 Hz, 1H), 7.15-7.11 (m, 1H), 6.99-6.96 (m, 1H), 4.35-4.31 (m, 1H), 3.55 (s, 3H), 3.52-3.49 (m, 1H), 3.06-3.04 (m, 1H), 2.29-2.26 (m, 1H), 2.06-1.89 (m, 3H) 
     57.3 Preparation of 9-fluoro-2,3,3a,5,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-4-one 
     To a solution of methyl 1-(2-fluoro-6-nitro-phenyl)-pyrrolidine-2-carboxylate (10 g, 37.3 mmol) in methanol (200 ml), Pd/C (3.97 g, 37.3 mmol) was added under Ar protection, then the reaction mixture was stirred for 12 h at 20° C. at 15 psi under H 2  atmosphere. One additional vial was set up as described above. The two reaction mixtures were combined, filtered, and the filtrate was concentrated under reduced pressure to give the title compound (10 g, 48.5 mmol, yield 65%). 
       1 H NMR (400 MHz, CDCl 3 ): δ[ppm]: 9.33 (s, 1H), 6.73-6.63 (m, 2H), 6.55-6.53 (m, 1H), 3.89-3.86 (m, 1H), 3.72-3.68 (m, 1H), 3.40-3.39 (m, 1H), 2.30-2.22 (m, 2H), 1.92-1.84 (m, 2H) 
     57.4 Preparation of 9-fluoro-1,2,3,3a,4,5,5a,6-octahydropyrrolo[1,2-a]quinoxaline 
     To a solution of 9-fluoro-2,3,3a,5,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-4-one (10 g, 48.5 mmol) in THF (200 ml), a solution of BH 3 .THF (12.5 g, 145 mmol) was added at 0° C., then the reaction solution was stirred 12 h at 70° C. After cooling to 0° C., methanol (100 ml) was added dropwise at 0° C., and the reaction solution was stirred for 30 minutes at 20° C., concentrated under reduced pressure, and the residue was purified by column chromatography on silica gel (petrol ether:ethyl acetate=20:1 to 10:1) to give the title compound (5 g, 26 mmol, yield 53.6%). 
       1 H NMR (400 MHz, CDCl 3 ): δ[ppm]: 6.54-6.49 (m, 1H), 6.40-6.37 (m, 1H), 6.28 (d, J=8 Hz, 1H), 3.92 (s, 1H), 3.78-3.76 (m, 1H), 3.34-3.20 (m, 1H), 3.20-3.17 (m, 1H), 2.99-2.97 (m, 1H), 2.66-2.61 (m, 1H), 2.13-2.11 (m, 1H), 1.86-1.78 (m, 2H), 1.50-1.47 (m, 1H) 
     57.5 Preparation of 2-(9-fluoro-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)acetamide 
     To a solution of 9-fluoro-1,2,3,3a,4,5,5a,6-octahydropyrrolo[1,2-a]quinoxaline (5.6 g, 29.1 mmol), diisopropylethyl amine (30.5 mL, 175 mmol) in dimethylformamide (DMF) (100 ml), 2-bromoacetamide (16.08 g, 117 mmol) was added and the reaction solution was stirred 12 h at 100° C. After cooling to 20° C., water (300 ml) was added, and the mixture was extracted with ethyl acetate (3×200 ml); the organic layer was dried over anhydrous Na 2 SO 4 , concentrated under reduced pressure, and the residue was purified by column chromatography on silica gel (dichloromethane: methanol=100:1 to 50:1) to give the title compound (3 g, 12.03 mmol, yield 41.3%). 
     LCMS (ESI+): m/z 250 (M+H) +   
     57.6 Preparation of 2-(9-fluoro-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)ethanamine 
     To a solution of 2-(9-fluoro-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)acetamide (3 g, 12.03 mmol) in THF (20 ml), a solution of BH 3 .THF (3.1 g, 36.1 mmol) was added at 0° C., then the reaction solution was stirred for 12 h at 70° C. After cooling to 0° C., methanol (100 ml) was added at 0° C., and the reaction solution was stirred for 30 minutes at 20° C. Then the solution was concentrated under reduced pressure, and the residue was purified by column chromatography on silica gel (petrol ether/ethyl acetate=20:1 to 10:1) to give title compound (1.3 g, 5.52 mmol, yield 45.9%). 
       1 H NMR (400 MHz, CD 3 OD): δ[ppm]: 6.63-6.59 (m, 1H), 6.48 (d, J=8.4 Hz, 1H), 6.34-6.29 (m, 1H), 3.73-3.70 (m, 1H), 3.34-3.25 (m, 3H), 3.11-3.08 (m, 1H), 2.84-2.79 (m, 3H), 2.64-2.61 (m, 1H), 2.13-2.09 (m, 1H), 1.80-1.76 (m, 2H), 1.55-1.51 (m, 1H) 
     57.7 Preparation of 1-fluoro-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of 2-(9-fluoro-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)ethanamine (1.1 g, 4.67 mmol) and formaldehyde (2.106 g, 70.1 mmol) in ethanol (20 ml), trifluoroacetic acid (TFA) (2.88 mL, 37.4 mmol) was added, and the reaction solution was stirred for 12 h at 90° C. After cooling to 40° C., the solution was concentrated under reduced pressure, and the residue was purified by prep-HPLC to give the title compound as TFA salt (1.087 g, yield 94%). 
     Prep-HPLC Method: 
     Instrument: Shimadzu LC-20AP preparative HPLC 
     Column: Luna(2) C18 250*50 mm i.d. 10 u 
     Mobile phase: A for H 2 O (0.09% TFA1) and B for CH 3 CN 
     Gradient: B from 0% to 20% in 20 min 
     Flow rate: 80 ml/min 
     Wavelength: 220 &amp;254 nm 
     Injection amount: 1.1 g per injection 
       1 H NMR (400 MHz, CD 3 OD): δ[ppm]: 6.79-6.71 (m, 2H), 4.23 (s, 2H), 4.01-3.96 (m, 1H), 3.36-3.32 (m, 3H), 3.29-3.27 (m, 2H), 3.15-3.12 (m, 2H), 2.49-2.43 (m, 1H), 2.29-2.21 (m, 1H), 1.95-1.90 (m, 2H), 1.58-1.54 (m, 1H) 
     Example 58 
     1-Bromo-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-868 of Table A) 
     58.1 Preparation of 1-(2-bromo-6-nitro-phenyl)-pyrrolidine-2-carboxylate 
     A mixture of 1-bromo-2-fluoro-3-nitrobenzene (60 g, 273 mmol), methyl pyrrolidine-2-carboxylate (54.2 g, 327 mmol; see example 57.1) and triethylamine (83 g, 818 mmol) was heated at 70° C. for 16 h. Then the mixture was cooled, diluted with ethyl acetate (1000 ml), washed with 2N HCl (500 ml), aqueous K 2 CO 3  (300 ml) and brine (300 ml) sequentially, and the aqueous phase was extracted with ethyl acetate (500 ml) again. The ethyl acetate layer was dried over Na 2 SO 4 , filtered, concentrated, and the residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=50:1 to 10:1) to afford the title compound (66 g, yield 74%) as yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.80-7.78 (m, 1H), 7.64-7.62 (m, 1H), 7.19 (t, J=8.2 Hz, 1H), 4.26-4.16 (m, 1H), 3.70-3.65 (m, 1H), 3.59 (s, 3H), 3.36-3.23 (m, 1H), 2.40-2.23 (m, 2H), 2.15-2.04 (m, 2H) 
     58.2 Preparation of 9-bromo-2,3,3a,5,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-4-one 
     To a solution of 1-(2-bromo-6-nitro-phenyl)-pyrrolidine-2-carboxylate (45 g, 137 mmol) in methanol (225 ml) was added a solution of NH 4 Cl (65.8 g, 1230 mmol) in water (225 ml) and Fe powder (53.4 g, 957 mmol) at 23° C., and the resulting mixture was heated at 85° C. for 1.5 h. Then the reaction was cooled, diluted with methanol (1000 ml), and the resulting mixture was stirred for 10 minutes, filtered, and the filter cake was washed with methanol (500 ml). The filtrate was concentrated under reduced pressure, the residue was put into water, extracted with ethyl acetate (3×800 ml), the extracts were washed with brine (400 ml), dried over Na 2 SO 4 , filtered, and concentrated to afford the title compound (33 g, yield 90%) as a light yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 9.78 (s, 1H), 7.27-7.17 (m, 1H), 6.91-6.75 (m, 2H), 4.10-3.90 (m, 2H), 3.09-3.06 (m, 1H), 2.86-2.68 (m, 1H), 2.37-2.20 (m, 1H), 2.04-2.02 (m, 1H), 1.88-1.68 (m, 1H) 
     58.3 Preparation of 9-bromo-1,2,3,3a,4,5,5a,6-octahydropyrrolo[1,2-a]quinoxaline 
     To a solution of 9-bromo-2,3,3a,5,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-4-one (24 g, 90 mmol) in THF (360 ml) was added dropwise BH 3 .DMS (50 ml, 500 mmol, 10 M in dimethylsulfide (DMS)) at 23° C., and the resulting solution was stirred at 70° C. for 2 h. The reaction was then cooled, and quenched with methanol. One additional reaction was set up and quenched as described above. The two resulting mixtures were combined, concentrated to about one third of volume, 6N HCl (250 mL) was added, and the resulting solution was heated at 70° C. for 20 minutes. Then the solution was cooled, adjusted to pH 9 by addition of saturated aqueous K 2 CO 3 , extracted with ethyl acetate (3×400 mL), the extracts were washed with brine, dried over Na 2 SO 4 , concentrated to give the residue, which was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=20:1 to 5:1) to afford the title compound (40 g, yield 88%) as a white solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 6.93-6.91 (m, 1H), 6.66 (t, J=7.7 Hz, 1H), 6.54-6.51 (m, 1H), 4.24-4.20 (m, 1H), 4.08 (s, 1H), 3.37-3.35 (m, 1H), 3.14-.311 (m, 1H), 2.89-2.76 (m, 1H), 2.76-2.62 (m, 1H), 2.37-2.22 (m, 1H), 1.96-1.93 (m, 1H), 1.89-1.77 (m, 1H), 1.75-1.63 (m, 1H). 
     58.4 Preparation of 2-(9-bromo-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)acetamide 
     A mixture of 9-bromo-1,2,3,3a,4,5,5a,6-octahydropyrrolo[1,2-a]quinoxaline (20 g, 79 mmol), 2-bromoacetamide (32.7 g, 237 mmol), and DIEA (51.1 g, 395 mmol) in DMF (200 mL) was stirred at 100° C. for 15 h. The reaction was cooled, diluted with water (600 ml), and extracted with ethyl acetate (3×400 ml). The organic layers were washed with brine (200 ml), dried over Na 2 SO 4  and filtered, concentrated to give a residue, which was recrystallized from ethyl acetate to afford the title compound (22 g, yield 90%) as a light yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.04 (d, J=7.9 Hz, 1H), 6.75 (t, J=7.9 Hz, 1H), 6.55 (d, J=7.9 Hz, 1H), 6.39 (s, 1H), 5.69 (s, 1H), 4.28-4.25 (m, 1H), 3.96-3.75 (m, 2H), 3.55-3.42 (m, 1H), 3.13-3.04 (m, 1H), 3.03-2.91 (m, 1H), 2.77-2.65 (m, 1H), 2.39-2.23 (m, 1H), 2.04-1.90 (m, 1H), 1.90-1.78 (m, 1H), 1.71-1.67 (m, 1H) 
     58.5 Preparation of 2-(9-bromo-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)ethanamine 
     To a solution of 2-(9-bromo-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)acetamide (11 g, 35.5 mmol) in THF (165 ml) was added dropwise BH 3 .DMS (18 ml, 180 mmol, 10 M in DMS) at 23° C., and the resulting solution was heated at 70° C. for 4 h. The reaction was then quenched with methanol. One additional reaction was set up and quenched as described above. The two resulting mixtures were combined, concentrated to about one third of volume, 6N HCl (200 mL) was added, and the resulting solution was heated at 70° C. for 20 minutes. The solution was then cooled, adjusted to pH 9 by addition of saturated aqueous K 2 CO 3 , and extracted with ethyl acetate (3×300 m). The extracts were washed with brine, dried over Na 2 SO 4  and concentrated to give a residue, which was purified by column chromatography on silica gel (eluted with dichloromethane/methanol=60:1 to 15:1) to afford the title compound (15 g, yield 71%) as a light yellow oil. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 6.94-6.87 (m, 1H), 6.78-6.67 (m, 2H), 4.25-4.21 (m, 1H), 3.51-3.40 (m, 1H), 3.39-3.28 (m, 2H), 3.07-3.05 (m, 1H), 3.02-2.84 (m, 3H), 2.67-2.57 (m, 1H), 2.29-2.27 (m, 1H), 2.00-1.87 (m, 1H), 1.87-1.74 (m, 1H), 1.71-1.60 (m, 1H), 1.26 (s, 2H) 
     58.6 Preparation of 1-bromo-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of 2-(9-bromo-2,3,3a,4,5a,6-hexahydro-1H-pyrrolo[1,2-a]quinoxalin-5-yl)ethanamine (13 g, 43.9 mmol) in ethanol (390 ml) was added formaldehyde (7.1 g, 88 mmol, 37% aqueous) and TFA (15 g, 132 mmol), and the resulting solution was heated at 80° C. for 2 h. Then the reaction was concentrated, the residue was dissolved in ethyl acetate (300 ml), and washed with saturated aqueous K 2 CO 3  (150 ml), and brine (100 ml). The ethyl acetate layer was dried over Na 2 SO 4 , filtered, and concentrated to afford the title compound (13 g, crude) as a yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.17-7.08 (m, 1H), 6.69-6.60 (m, 1H), 4.40-4.27 (m, 1H), 3.96-3.78 (m, 2H), 3.24-3.14 (m, 1H), 3.13-3.02 (m, 2H), 3.01-2.88 (m, 3H), 2.79-2.70 (m, 1H), 2.66-2.58 (m, 1H), 2.36-2.28 (m, 1H), 2.23 (s, 1H), 1.99-1.88 (m, 1H), 1.83-1.71 (m, 1H), 1.71-1.61 (m, 1H) 
     Analytical Method: The gradient was 1-90% B in 3.4 min, 90-100% B in 0.45 min, 100-1% B in 0.01 min, and then held at 1% B for 0.65 min (0.8 mL/min flow rate). Mobile phase A was 0.0375% TFA in water, mobile phase B was 0.018% TFA in acetonitril. 
     The column used for the chromatography was a 2.1×50 mm Venusil XBP-C18 column (5 m particles). Detection methods are diode array (DAD) and evaporative light scattering (ELSD) detection as well as positive/negative electrospray ionization.). 
     Example 59 
     1-Methyl-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, trifluoroacetic acid (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-869 of Table A) 
     59.1 Preparation of boc-protected 1-bromo-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of 1-bromo-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (13 g, 42.2 mmol) in dichloromethane (DCM) (260 ml) were added triethylamine (6.4 g, 63.3 mmol) and a solution of Boc 2 O (10.1 g, 46.4 mmol) in DCM (20 ml) at 0° C., then it was allowed to warm to 23° C. and stirred for 16 h. The reaction was diluted with DCM (250 ml), washed with 2 N HCl (200 ml), saturated aqueous K 2 CO 3  (150 ml) and brine (150 ml), and the water phase was extracted with DCM (200 mL) again. The combined organic layers were dried over Na 2 SO 4 , filtered, and concentrated, and the residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=30:1 to 4:1) to give the boc-protected compound (6 g, yield 35%, 2 steps). 
     LCMS (ESI+): m/z 408 (M+H) +   
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 7.11 (d, J=7.50 Hz, 1H), 6.73 (d, J=7.94 Hz, 1H), 4.67-4.50 (m, 1H), 4.36-4.24 (m, 1H), 4.18-4.01 (m, 1H), 3.91 (d, J=11.91 Hz, 1H), 3.27 (s, 1H), 3.20-2.90 (m, 4H), 2.76-2.55 (m, 2H), 2.27-2.25 (m, 1H), 1.97-1.66 (m, 3H), 1.46 (m, 9H) 
     59.2 Preparation of boc-protected 1-methyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a mixture of boc-protected 1-bromo-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (500 mg, 1.2 mmol), tricyclohexylphosphine (34.3 mg, 0.12 mmol), and Pd(OAc) 2  (13.7 mg, 0.06 mmol) in toluene (20 ml) under N 2  atmosphere was added methylboronic acid (366 mg, 6.1 mmol), K 3 PO 4  (1.04 g, 4.9 mmol) and Water (2 mL). The reaction mixture was heated at 100° C. for 16 h. After cooling, the reaction mixture was diluted with ethyl acetate (100 ml) and washed with brine. The organic layer was dried over Na 2 SO 4 , filtered and concentrated. The residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=25:1 to 4:1) to afford the title compound (0.35 g, yield 73%) as white solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 6.95-6.49 (m, 2H), 4.81-4.48 (m, 1H), 4.20-3.68 (m, 3H), 3.52-3.17 (m, 2H), 3.11-2.81 (m, 3H), 2.78-2.51 (m, 2H), 2.32 (s, 3H), 2.01-1.86 (m, 1H), 1.86-1.71 (m, 1H), 1.71-1.60 (m, 1H), 1.44 (s, 9H) 
     59.3 Preparation of 1-methyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of boc-protected 1-methyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (350 mg, 0.9 mmol) in DCM (6 ml) was added TFA (3 ml), and the resulting solution was stirred at 20° C. for 5 h. The reaction was then concentrated and the residue was purified by Prep-HPLC and lyophilized to afford the title compound (242 mg, yield 92%, TFA salt) as a light gray solid. 
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 7.12 (d, J=7.5 Hz, 1H), 6.97-6.86 (m, 1H), 4.34-4.22 (m, 2H), 4.16-4.11 (m, 1H), 3.69-3.66 (m, 1H), 3.54-3.43 (m, 1H), 3.39-3.33 (m, 2H), 3.30-3.23 (m, 2H), 3.10-2.97 (m, 2H), 2.43 (s, 3H), 2.41-2.31 (m, 1H), 2.13-1.98 (m, 2H), 1.95-1.85 (m, 1H) 
     Example 60 
     1-Cyclopropyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, trifluoroacetic acid (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-873 of Table A) 
     The compound was prepared in analogy to example 59. 
     LCMS (ESI+): m/z 270 (M+H) +   
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 7.10 (d, J=7.9 Hz, 1H), 6.67 (d, J=7.9 Hz, 1H), 4.41-4.38 (m, 1H), 4.26 (s, 2H), 3.67-3.66 (m, 1H), 3.52-3.42 (m, 1H), 3.39-3.33 (m, 2H), 3.29-3.21 (m, 2H), 3.15-3.09 (m, 1H), 3.00-2.87 (m, 1H), 2.46-2.31 (m, 1H), 2.17-1.94 (m, 3H), 1.93-1.82 (m, 1H), 1.20-1.17 (m, 1H), 1.07-0.93 (m, 2H), 0.69-0.54 (m, 1H). 
     Example 61 
     1-Cyclobutyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-874 of Table A) 
     61.1 Preparation of boc-protected 1-(1-hydroxy-cyclobut-1-yl)-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of boc-protected 1-bromo-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (800 mg, 1.96 mmol) in THF (16 ml) was added dropwise n-BuLi (1.6 ml, 3.92 mmol, 2.5 M in hexane) at −70° C. with stirring under N 2  atmosphere, and the resulting solution was stirred at −70° C. for 1 hour. A solution of cyclobutanone (275 mg, 3.92 mmol) in THF (0.5 ml) was added dropwise at −70° C., and the reaction solution was stirred for 2 h at same temperature. Then it was allowed to warm slowly to 20° C. and stirred for 16 h. The reactiont was quenched by saturated aqueous NH 4 Cl, extracted with ethyl acetate (2×100 ml), the organic layers were dried over Na 2 SO 4 , concentrated, and the residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=10:1 to 2:1) to afford the title compound (0.5 g, yield 64%) as white solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.07-6.90 (m, 2H), 4.64-4.48 (m, 1H), 4.23 (d, J=14.1 Hz, 1H), 3.86 (d, J=11.5 Hz, 1H), 3.68-3.67 (m, 1H), 3.52-3.31 (m, 1H), 3.25-3.11 (m, 2H), 3.10-2.94 (m, 2H), 2.94-2.76 (m, 2H), 2.60-2.47 (m, 2H), 2.46-2.33 (m, 2H), 2.29-2.16 (m, 1H), 2.01-1.82 (m, 3H), 1.82-1.68 (m, 1H), 1.68-1.54 (m, 1H), 1.41 (s, 9H). 
     61.2 Preparation of 1-cyclobutyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of boc-protected 1-(1-hydroxy-cyclobut-1-yl)-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (380 mg, 0.95 mmol) in DCM (3 ml) was added triethylsilane (1.66 g, 14.3 mmol), and the resulting solution was stirred for 0.5 h. Then TFA (10 ml) was added, and the resulting solution was stirred at 60° C. overnight. The solvent was removed under reduced pressure. The residue was dissoved in 3 N HCl (50 ml), and washed with DCM (3×50 ml). The aqueous phase was adjusted to pH 9 by addition of saturated aqueous K 2 CO 3 , the resulting mixture was extracted with DCM (2×100 ml), the DCM layers were washed with brine (30 ml), dried over Na 2 SO 4 , filtered, and concentrated to afford the title compound (160 mg, yield 60%) as a gray solid. 
     LCMS (ESI+): m/z 284 (M+H) +   
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 6.91 (d, J=7.9 Hz, 1H), 6.79 (d, J=7.5 Hz, 1H), 3.89-3.71 (m, 3H), 3.69-3.60 (m, 1H), 3.17-3.05 (m, 1H), 3.05-2.84 (m, 5H), 2.68-2.48 (m, 2H), 2.48-2.36 (m, 1H), 2.33-2.18 (m, 2H), 2.17-1.93 (m, 3H), 1.93-1.74 (m, 3H), 1.68-1.54 (m, 1H) 
     Example 62 
     1-Cyclopentyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, trifluoroacetic acid (Compound of the Formula I.a in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-875 of Table A) 
     62.1 Preparation of boc-protected 1-(1-hydroxy-cyclopent-1-yl)-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of boc-protected 1-bromo-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (100 mg, 0.25 mmol) in THF (2 ml) was added dropwise n-BuLi (0.2 ml, 0.5 mmol, 2.5 M in hexane) at −70° C. with stirring under N 2  atmosphere, and the resulting solution was stirred at −70° C. for 1 hour. A solution of cyclopentanone (40 mg, 0.5 mmol) in THF (0.2 ml) was added dropwise at −70° C., and the reaction solution was stirred for 8 h at same temperature. It was then allowed to warm slowly to 20° C. and stirred for 16 h. The reaction was quenched by saturated aqueous NH 4 Cl, extracted with ethyl acetate (2×50 ml), the organic layers were dried over Na 2 SO 4 , concentrated, and the residue was purified by Prep-TLC (petrol ether/ethyl acetate=2:1) to afford the title compound (16 mg, yield 22%) as white solid. 
       1 H NMR (400 MHz; DMSO-d 6  (T=273+80 K)): δ[ppm]: 7.50 (s, 1H), 6.81-6.75 (m, 1H), 6.74-6.68 (m, 1H), 4.46-4.24 (m, 2H), 3.75-3.66 (m, 2H), 3.42-3.26 (m, 2H), 3.24-3.12 (m, 2H), 2.93 (d, J=9.7 Hz, 1H), 2.63-2.51 (m, 2H), 2.15-2.03 (m, 4H), 1.99-1.90 (m, 1H), 1.83-1.82 (m, 5H), 1.72-1.55 (m, 3H), 1.34 (s, 9H) 
     62.2 Preparation of boc-protected 1-cyclopent-1-enyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     A mixture of boc-protected 1-(1-hydroxy-cyclopent-1-yl)-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (100 mg, 0.25 mmol), 2-(cyclopent-1-en-1-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (95 mg, 0.49 mmol), Pd(PPh 3 ) 2 Cl 2  (12 mg, 0.017 mmol) and Cs 2 CO 3  (160 mg, 0.49 mmol) in dioxane (2 ml) and water (0.6 ml) was placed in a microwave tube under N 2  atmosphere. The reaction mixture was heated at 100 C for 1 hour in microwave reactor. Six additional reactions were set up as described above. All seven reaction mixtures were combined, was put into water, extracted with ethyl acetate (2×100 ml); the extracts were washed with brine, dried over Na 2 SO 4 , andconcentrated to give crude product, which was purified by column chromatography on silica gel (eleted with petrol ether/ethyl acetate=25:1 to 5:1) to afford the title compound (400 mg, yield 58%) as light yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 6.93-6.68 (m, 2H), 5.94-5.78 (m, 1H), 4.81-4.52 (m, 1H), 4.15 (d, J=13.7 Hz, 1H), 4.08-3.78 (m, 1H), 3.71-3.58 (m, 1H), 3.45-3.17 (m, 2H), 3.15-2.85 (m, 4H), 2.69-2.41 (m, 4H), 2.38-2.18 (m, 2H), 2.02-1.96 (m, 2H), 1.86-1.66 (m, 2H), 1.59-1.51 (m, 1H), 1.44 (s, 9H) 
     62.3 Preparation of boc-protected 1-cyclopentyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     A mixture of 1-cyclopent-1-enyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (0.3 g, 0.76 mmol), and Pd/C (0.09 g, 5%) in methanol (20 ml) was stirred at 20° C. under a H 2  balloon for 16 h. Then the reaction was filtered, and concentrated to afford the title compound (0.29 g, yield 96%) as light yellow solid. 
     LCMS (ESI+): m/z 398 (M+H) +   
     62.4 Preparation of 1-cyclopentyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline 
     To a solution of boc-protected 1-cyclopentyl-5,6,7,9,9a, 10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline (0.29 g, 0.74 mmol) in DCM (6 ml) was added TFA (3 ml), and the resulting solution was stirred for 3 h at 25° C. The reaction was concentrated and lyophilized to afford the title compound (351 mg, yield 90%, TFA salt) as brown oil. 
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 7.34 (d, J=8.4 Hz, 1H), 7.13 (d, J=7.9 Hz, 1H), 4.37-4.25 (m, 2H), 4.24-4.14 (m, 1H), 3.96-3.87 (m, 1H), 3.62-3.52 (m, 1H), 3.44-3.32 (m, 4H), 3.30-3.19 (m, 3H), 2.48-2.35 (m, 1H), 2.25-2.04 (m, 4H), 2.04-1.85 (m, 3H), 1.85-1.70 (m, 2H), 1.70-1.56 (m, 2H) 
     Example 63 
     8-Methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-241 of Table B) 
     63.1 Preparation of boc-protected ethyl 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoate 
     To a solution of 4-boc-protected 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine (7 g, 28.2 mmol) in acetic acid (14 ml) was added ethyl acrylate (14.1 g, 141 mmol) and the reaction mixture was heated at 100° C. for 16 hrs. Then it was cooled, concentrated, and the residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=25:1 to 5:1) to give the title compound (5 g, yield 51%) as light yellow oil. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.32-7.14 (m, 2H), 7.03-6.88 (m, 2H), 4.43-4.26 (m, 2H), 4.20-4.08 (m, 2H), 3.64-3.51 (m, 4H), 3.10-2.99 (m, 2H), 2.63-2.53 (m, 2H), 1.49-1.38 (m, 9H), 1.30-1.19 (m, 3H) 
     63.2 Preparation of boc-protected 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoic acid 
     To a solution of boc-protected ethyl 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoate (7.5 g, 21.5 mmol) in THF (70 mL), H 2 O (50 mL) and methanol (23 ml) was added a solution of NaOH (2.6 g, 64.6 mmol) in H 2 O (20 mL) at 5° C., and the resulting solution was stirred at 25° C. for 3 h. Then the solution was cooled to 5° C., adjusted to pH 3 by addition of 1N HCl, and the resulting mixture was extracted with ethyl acetate three times. The ethyl acetate layers were combined, dried over Na 2 SO 4 , filtered, and concentrated to give the title compound (6.7 g, yield 97%) as yellow oil. 
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: δ 7.23-7.06 (m, 2H), 6.98-6.85 (m, 2H), 4.39-4.21 (m, 2H), 3.65-3.41 (m, 4H), 3.05-2.91 (m, 2H), 2.56 (t, J=6.6 Hz, 2H), 1.40-1.31 (m, 9H). 
     63.3 Preparation of boc-protected 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoyl chloride 
     To a solution of boc-protected 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoic acid (6.5 g, 20.3 mmol) in dichloromethane (300 ml) were added dimethylformamide (0.15 g, 2 mmol) and dropwise a solution of (COCl) 2  (7.7 g, 60.9 mmol) in dichloromethane (30 ml) at 0° C. The the reaction was stirred for 1 hour at 25° C., and concentrated under reduced pressure below 30° C. to give the title compound as a residue which was used directly in the next step without further purification. 
     63.4 Preparation of boc-protected 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one 
     To a solution of boc-protected 3-(2,3,4,5-tetrahydro-1,4-benzodiazepin-1-yl)propanoyl chloride (6.6 g, crude, −20 mmol) in dichloroethane (400 ml) was added A1Cl 3  (10.4 g, 78 mmol) in portions at 0-5° C., then the resulting mixture was stirred at 65° C. for 7 hrs. 
     The reaction was quenched with water (100 ml), adjusted to pH 9 by addition of aqueous saturated K 2 CO 3 , then Boc 2 O (6.4 g, 29.2 mmol) was added, and the resulting mixture was stirred for 2 hrs. The mixture was extracted with dichloromethane twice, the organic phase was washed with brine, dried over Na 2 SO 4 , concentrated, and the residue was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=10:1 to 2:1) to give the title compound (4.2 g, yield 71%) as yellow solid. 
       1 H NMR (400 MHz, CDCl 3 ): δ[ppm]: 7.85 (d, J=7.5 Hz, 1H), 7.40-7.20 (m, 1H), 6.83 (t, J=7.5 Hz, 1H), 4.58-4.40 (m, 2H), 3.74 (d, J=3.5 Hz, 2H), 3.60-3.50 (m, 2H), 3.44-3.37 (m, 2H), 2.72-2.62 (m, 2H), 1.47-1.29 (m, 9H). 
     63.5 Preparation of 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one 
     To a solution of boc-protected 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one (500 mg, 1.7 mmol) in dichloromethane (10 ml) was added trifluoroacetic acid (5 ml), and then the resulting mixture was stirred at 25° C. for 3 hrs. This was concentrated and lyophilized to give the title compound (500 mg, yield 100%, trifluoroacetic acid salt) as yellow solid. 
       1 H NMR (400 MHz; CD 3 OD): δ[ppm]: 7.92-790 (m, 1H), 7.49 (d, J=6.6 Hz, 1H), 6.97 (t, J=7.7 Hz, 1H), 4.40 (s, 2H), 3.71-3.63 (m, 4H), 3.55-3.47 (m, 2H), 2.75-2.67 (m, 2H). 
     63.6 Preparation of Cbz-protected 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one 
     To a solution of 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one (2 g, 6.92 mmol) (TFA salt) in DCM (30 ml) were added triethylamine (1.4 g, 13.8 mmol) and a solution of CbzCl (Cbz=benzyloxycarbonyl; 1.5 g, 9 mmol) in DCM (5 mL) at 0-5° C., then the reaction mixture was stirred at 25° C. for 2 hrs. Then it was diluted with DCM (100 ml), washed with aqueous K 2 CO 3  (50 mL) and brine (50 ml); the water phase was extracted with DCM again, the DCM layer was dried over Na 2 SO 4 , filtered, and concentrated under reduced pressure to give the title compound (1.5 g, yield 64%) as brown oil. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.79 (d, J=7.6 Hz, 1H), 7.30-7.11 (m, 6H), 6.76-6.72 (m, 1H), 5.04-5.01 (m, 2H), 4.55-4.48 (m, 2H), 3.75-3.74 (m, 2H), 3.48-3.38 (m, 4H), 2.60-2.55 (m, 2H) 
     63.7 Preparation of Cbz-protected 8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol 
     To a solution of Cbz-protected 1,2,3,4,6,7-hexahydro[1,4]diazepino[6,7,1-ij]-quinolin-8-one (1.5 g, 4.5 mmol) in THF (45 ml) was added dropwise methyllithium (3.7 ml, 5.8 mmol, 1.6 M in ether) at −70° C., and the resulting solution was stirred at −70° C. for 2 h. Then it was quenched with aqueous NH 4 Cl (20 ml), extracted with ethyl acetate (50 ml) three times, the ethyl acetate layers were washed with brine (30 ml), dried over Na 2 SO 4 , filtered, concentrated, and the residue was purified by column chromatography on silica gel (eluted with DCM/methanol=150:1 to 50:1) to give the title compound (1 g, yield 64%) as light yellow oil. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.47 (d, J=7.5 Hz, 1H), 7.39-7.25 (m, 5H), 7.25-6.99 (m, 1H), 6.93-6.80 (m, 1H), 5.18-5.02 (m, 2H), 4.62-4.35 (m, 2H), 3.79 s, 1H), 3.73-3.59 (m, 1H), 3.45-3.34 (m, 1H), 3.29-3.15 (m, 3H), 2.00-1.89 (m, 2H), 1.59 (s, 3H) 
     63.8 Preparation of 8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol 
     A mixture of Cbz-protected 8-hydroxy-8-methyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline (0.5 g, 1.42 mmol), NH 3 —H 2 O (1 ml) and Pd/C (168 mg, 10%) in THF (30 ml) was stirred under a H 2  balloon for 2 h. Then it was filtered, concentrated, and the residue was purified by Prep-HPC (basic method) and lyophilized to give the title compound (214 mg, yield 69%) as white solid. 
     LCMS (ESI+): m/z 219 (M+H) +   
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.44 (d, J=7.5 Hz, 1H), 7.01 (d, J=7.1 Hz, 1H), 6.83 (t, J=7.5 Hz, 1H), 3.92-3.81 (m, 2H), 3.43-3.32 (m, 1H), 3.29-3.17 (m, 1H), 3.14-3.00 (m, 4H), 1.99-1.91 (m, 2H), 1.59 (s, 3H) 
     Example 64 
     8-Methoxy-8-methyl-2,3,4,6,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline (Compound of the Formula I.g, I.h or I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-201 of Table B) 
     64.1 Preparation of Cbz-protected 8-methoxy-8-methyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline 
     To a solution of Cbz-protected 8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol (0.5 mg, 1.42 mmol; see example 63.2) in DMF (10 ml) was added NaH (113 mg, 2.84 mmol) in portions at 0-5° C., and then the resulting mixture was stirred at 25° C. for 0.5 hrs. A solution of MeI (403 mg, 2.84 mmol) in DMF (2 ml) was added dropwise at 0-5° C., then the reaction mixture was stirred at 25° C. for 16 h. It was quenched with water (30 ml), and extracted with ethyl acetate (60 ml) twice. The ethyl acetate layer was washed with brine, dried over Na 2 SO 4 , and concentrated to give a residue, which was purified by column chromatography on silica gel (eluted with petrol ether/ethyl acetate=15:1 to 4:1) to give the title compound (200 mg, yield 39%) as light yellow oil. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.41-7.24 (m, 6H), 7.23-7.01 (m, 1H), 6.93-6.79 (m, 1H), 5.12 (s, 2H), 4.64-4.49 (m, 1H), 4.44-4.34 (m, 1H), 3.88-3.75 (m, 1H), 3.69-3.58 (m, 1H), 3.40-3.26 (m, 2H), 3.23-3.12 (m, 2H), 3.08 (s, 3H), 2.28-2.19 (m, 1H), 1.72-1.63 (m, 1H), 1.53 (s, 3H) 
     64.2 Preparation of 8-methoxy-8-methyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline 
     A mixture of Cbz-protected 8-methoxy-8-methyl-1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline (160 mg, 0.44 mmol), NH 3 —H 2 O (0.5 ml) and Pd/C (50 mg, 10%) in THF (20 ml) was stirred under a H 2  balloon at 25° C. for 2 hrs. Then it was filtered, concentrated, and the residue was purified by Prep-HPC (basic method) and lyophilized to give the title compound (55 mg, yield 54%) as yellow oil. 
     LCMS (ESI+): m/z 233 (M+H) +   
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.30-7.27 (m, 1H), 7.02 (d, J=7.1 Hz, 1H), 6.83 (t, J=7.5 Hz, 1H), 3.94-3.84 (m, 2H), 3.38-3.24 (m, 2H), 3.16-3.01 (m, 7H), 2.27-2.22 (m, 1H), 1.69-1.63 (m, 1H), 1.54 (s, 3H) 
     Example 65 
     2,8-Dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol 
     A mixture of Cbz-protected 8-methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol (50 mg, 0.14 mmol; see example 63.2), formaldehyde (21 mg, 0.28 mmol, 40% in water) and Pd/C (17 mg, 10%) in methanol (5 ml) was stirred under a H 2  balloon for 6 hrs. Then it was filtered, concentrated, and the residue was purified by Prep-HPC (basic method) and lyophilized to give the title compound (12 mg, yield 36%) as light yellow solid. 
       1 H NMR (400 MHz; CDCl 3 ): δ[ppm]: 7.44-7.42 (m, 1H), 7.07-7.00 (m, 1H), 6.83 (t, J=7.5 Hz, 1H), 3.71-3.57 (m, 2H), 3.40-3.31 (m, 1H), 3.25-3.17 (m, 1H), 3.17-3.04 (m, 2H), 2.82 (t, J=5.1 Hz, 2H), 2.37 (s, 3H), 1.94 (t, J=6.0 Hz, 2H), 1.58 (s, 3H) 
     Example 66 
     11-Methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane], 2,2,2-trifluoroacetic acid (Compound of the Formula I.i in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-325 of Table B) 
     The title compound was prepared in analogy to example 1, using however tert-butyl 6-methyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-4-carboxylate and 2-cyclobutylidene-acetic acid as starting materials. 
     ESI-MS [M+H + ]=243.20 
       1 H NMR (DMSO-d 6 , 500 MHz) [ppm]: 7.28 (d, J=7.9 Hz, 1H), 6.71 (d, J=7.9 Hz, 1H), 3.74 (s, 2H), 3.10-3.03 (m, 2H), 2.99-2.94 (m, 2H), 2.90-2.84 (m, 2H), 2.34-2.25 (m, 2H), 2.22 (s, 3H), 2.09-1.96 (m, 1H), 1.92-1.83 (m, 5H). 
     Example 67 
     9-Methyl-1,2,3,4,6,7-Hexahydrospiro[[1,4]Diazepino[6,7,1-Ij]Quinoline-8,1′-Cyclobutane], Trifluoroacetic Acid (Compound of the Formula I.g in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-325 in Table B) 
     The intermediate tert-butyl 9-chloro-3,4,6,7-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane]-2(1H)-carboxylate was prepared in analogy to example 1, steps 1.1 to 1.3 using tert-butyl 8-chloro-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate and 2-cyclobutylideneacetyl chloride as starting materials. 
     67.1 Preparation of tert-butyl 9-methyl-3,4,6,7-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane]-2(1H)-carboxylate 
     75 mg (0.21 mmol) of tert-butyl 9-chloro-3,4,6,7-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane]-2(1H)-carboxylate were dissolved in 0.5 ml of tetrahydrofurane, 0.5 ml toluene and 5 μl water. To this solution 35 μl (0.25 mmol) trimethylboroxine, 0.2 mg (0.4 μmol) of dicyclohexyl(2′,4′,6′-triisopropyl-[1,1′-biphenyl]-2yl)phosphine and 65.8 mg (0.31 mmol) of potassium phosphate were added and the solution was degassed with Argon. 0.1 mg (0.4 μmol) of palladium(II)acetate were added and the reaction mixture was heated at 100° C. for 10 minutes in a microwave unit. The reaction mixture was concentrated in vacuo. The residue was purified by column chromatography on silica (eluent: 0-30% methanol in dichloromethane) to yield 40 mg of the title compound. 
     ESI-MS [M+H + ]=343.20 
     67.2 Preparation of 9-methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]-quinoline-8,1′-cyclobutane], trifluoroacetic acid 
     To 40 mg (0.12 mmol) of tert-butyl 9-methyl-3,4,6,7-tetrahydrospiro[[1,4]diazepino-[6,7,1-ij]quinoline-8,1′-cyclobutane]-2(1H)-carboxylate in 3 ml dichloromethane were added 90 μl (1.2 mmol) of trifluoroacetic acid at 0° C. The solution was stirred for 2 h at room temperature. The reaction mixture was concentrated in vacuo. The residue was purified by preparative HPLC to yield 4.6 mg of the title compound. 
     ESI-MS [M+H + ]=243.20 
       1 H NMR (CDCl 3 , 500 MHz): δ[ppm]: 9.15 (bs, 2H), 6.95 (d, 1H), 6.80 (d, 1H), 4.15 (m, 2H), 3.30 (m, 2H), 3.25 (m, 2H), 3.10 (m, 2H), 2.85 (m, 2H), 2.70 (s, 3H), 2.20 (m, 2H), 2.00 (m, 2H), 1.85 (m, 2H). 
     Example 68 
     4,5,6,7,9,9a,9b,10,10a, 11-Decahydrocyclopropa[3,4]pyrrolo[1,2-a][1,4]diazepino[1,7,6-de]quinoxaline 
     
       
         
         
             
             
         
       
     
     The title compound was prepared in analogy to example 44 using however 1-fluoro-2-nitrobenzene and ethyl 3-azabicyclo[3.1.0]hexane-2-carboxylate as starting materials. 
     ESI-MS [M+H + ]=242.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.65 (m, 1H), 6.35 (d, 1H), 6.30 (d, 1H), 3.65 (m, 1H), 3.60 (m, 1H), 3.35 (m, 4H), 3.30 (m, 1H), 2.90 (m, 3H), 2.55 (m, 1H), 1.65 (m, 1H), 1.60 (m, 1H), 0.50 (m, 1H), 0.15 (m, 1H). 
     Example 69 
     1-Ethyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-289 in Table A) 
     The title compound was prepared in analogy to example 33, using however acetaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=218.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.70 (m, 1H), 6.60 (d, 1H), 6.40 (d, 1H), 3.65 (s, 2H), 3.35 (m, 2H), 3.15 (m, 2H), 3.10 (m, 2H), 2.90 (m, 2H), 2.80 (m, 2H), 1.05 (t, 3H). 
     Example 70 
     1-Propyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.a, I.b or I.c in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-325 in Table A) 
     The title compound was prepared in analogy to example 33, using however propionaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=232.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.70 (m, 1H), 6.60 (d, 1H), 6.40 (d, 1H), 3.65 (s, 2H), 3.25 (m, 2H), 3.15 (m, 4H), 2.90 (m, 2H), 2.80 (m, 2H), 1.50 (m, 2H), 0.90 (t, 3H). 
     Example 71 
     1-Cyclobutyl-5-methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-433 in Table A) 
     The title compound was prepared in analogy to example 33, using tert-butyl 5-methyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate and cyclobutanone. tert-Butyl 5-methyl-2,3,5,6-tetrahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline-7(8H)-carboxylate was prepared in analogy to example 30 however using 2-bromopropaneamide instead of 2-chloroacetamide and in analogy to example 32. 
     ESI-MS [M+H + ]=258.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.65 (m, 1H), 6.55 (d, 1H), 6.45 (d, 1H), 3.90 (m, 1H), 3.80 (m, 1H), 3.55 (m, 1H), 3.30-3.15 (m, 3H), 3.10 (m, 1H), 2.95 (m, 1H), 2.85 (m, 1H), 2.75 (m, 1H), 2.20 (m, 1H), 2.15 (m, 1H), 2.05 (m, 2H), 1.65 (m, 2H), 0.9 (d, 3H). 
     Example 72 
     5-Methyl-1-(oxetan-3-yl)-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-541 in Table A) 
     The title compound was prepared in analogy to example 71, using however oxetane-3-one instead of cyclobutanone. 
     ESI-MS [M+H + ]=260.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.60 (m, 1H), 6.55 (d, 1H), 6.05 (d, 1H), 4.80 (m, 1H), 4.75 (m, 1H), 4.65 (m, 1H), 4.60 (m, 1H), 4.45 (m, 1H), 3.80 (d, 1H), 3.50 (d, 1H), 3.35 (m, 2H), 3.15 (m, 2H), 2.90 (m, 1H), 2.85 (m, 1H), 2.75 (m, 1H), 0.9 (d, 3H). 
     Example 73 
     1-Ethyl-5-methyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-289 in Table A) 
     The title compound was prepared in analogy to example 71, using however acetaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=232.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.80 (m, 1H), 6.65 (d, 1H), 6.50 (d, 1H), 3.95 (d, 1H), 3.80 (d, 1H), 3.45-3.05 (m, 8H), 2.85 (m, 1H), 1.15 (t, 3H), 1.00 (d, 3H). 
     Example 74 
     5-Methyl-1-propyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline (Compound of the Formula I.gg, I.hh or I.ii in which the Combination of R 5a , R 5b , R 6  and R 9a  is as in Row A-325 in Table A) 
     The title compound was prepared in analogy to example 71, using however propionaldehyde instead of cyclobutanone. 
     ESI-MS [M+H + ]=246.20 
       1 H NMR (DMSO-d 6 , 500 MHz): δ[ppm]: 6.80 (m, 1H), 6.60 (d, 1H), 6.50 (d, 1H), 3.95 (d, 1H), 3.80 (d, 1H), 3.30 (m, 4H), 3.20 (m, 2H), 3.10 (m, 1H), 3.00 (m, 1H), 2.80 (m, 1H), 1.60 (m, 2H), 0.95 (d, 3H), 0.90 (t, 3H). 
     Example 75 
     9-Chloro-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-Cyclobutane], Trifluoroacetic Acid (Compound of the Formula I.g in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-323 in Table B) 
     The title compound was prepared in analogy to example 1 using tert-butyl 8-chloro-2,3-dihydro-1H-benzo[e][1,4]diazepine-4(5H)-carboxylate and 2-cyclobutylideneacetyl chloride as starting materials. 
     ESI-MS [M+H + ]=236.10 
       1 H NMR (CDCl 3 , 500 MHz): δ[ppm]: 9.60 (bs, 2H), 7.00 (m, 2H), 4.15 (s, 2H), 3.25 (m, 6H), 3.10 (m, 2H), 2.15 (m, 2H), 2.05 (m, 2H), 1.75 (m, 2H). 
     Example 76 
     10-Methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane], trifluoroacetic acid (Compound of the Formula I.h in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-325 in Table B) ESI-MS [M+H + ]=243.20 
       1 H NMR (CDCl 3 , 500 MHz): δ[ppm]: 9.35 (bs, 2H), 7.40 (s, 1H), 6.90 (s, 1H), 4.15 (m, 2H), 3.35 (m, 2H), 3.25 (m, 2H), 3.15 (m, 2H), 2.40 (m, 2H), 2.30 (s, 3H), 2.15-1.90 (m, 6H). 
     Example 77 
     10-Chloro-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1′-cyclobutane], trifluoroacetic acid (Compound of the Formula I.h in which the Combination of R 5a , R 5b , R 7 , R 8  and R 9a  is as in Row B-323 in Table B) 
     ESI-MS [M+H + ]=236.10 
       1 H NMR (CDCl 3 , 500 MHz): δ[ppm]: 9.65 (bs, 2H), 7.55 (s, 1H), 7.05 (s, 1H), 4.15 (s, 2H), 3.30 (m, 4H), 3.20 (m, 2H), 2.35 (m, 2H), 2.15-1.90 (m, 6H). 
     II. BIOLOGICAL TESTS 
     Functional Activity 
     The functional activity of compounds of formula I was assayed by incubation with U2OS_HTR 2C _β-Arrestin cells (DiscoverX, 93-0289C3) to induce beta-arrestin2 recruitment to the 5-HT 2C  receptor. The agonist-induced recruitment and proximity of the receptor and beta-arrestin2 leads to complementation and formation of active β-galactosidase. The enzyme complementation results in enzyme activity, which is measured following the termination of the agonist incubation using DiscoveRx&#39;s detection reagent, which contains a chemiluminescent substrate which produces a high intensity signal. Cells were plated and a medium-change to a 1% serum containing medium was performed 24 h later. The next day, test compounds were added and incubated for 1.5 h before addition of detection reagent. 
     The response produced was measured and compared with the response produced by 10 [mu]M 5-HT or the maximal effect induced by 5-HT (defined as 100%) to which it was expressed as a percentage response (relative efficacy). Dose response curves were constructed using Graphpad Prism (Graph Software Inc.) or using in house adapted software using a 4 parameter dose response model with variable slope (fit=(Bottom+(Top−Bottom)/(1+10{circumflex over ( )}((LogEC50−x)*HillSlope))res=(y−fit)). Results are compiled in the table below. 
     
       
         
           
               
               
               
             
               
                 TABLE 
               
               
                   
               
               
                 # 
                 Potency (EC50) in functional assay 
                 % efficacy 
               
               
                   
               
             
            
               
                   
               
            
           
           
               
               
               
            
               
                 1 
                 ++ 
                 71 
               
               
                 6 
                 ++ 
                 63 
               
               
                 8 
                 ++ 
                 40 
               
               
                 9 
                 +++ 
                 61 
               
               
                 16 
                 + 
                 55 
               
               
                 17 
                 ++ 
                 84 
               
               
                 19 
                 ++ 
                 25 
               
               
                 22 
                 ++ 
                 69 
               
               
                 25 
                 ++ 
                 90 
               
               
                 26 
                 +++ 
                 107 
               
               
                 27 
                 + 
                 87 
               
               
                 28 
                 ++ 
                 55 
               
               
                 33 
                 + 
                 78 
               
               
                 35 
                 ++ 
                 112 
               
               
                 36 
                 + 
                 31 
               
               
                 37 
                 + 
                 21 
               
               
                 40 
                 ++ 
                 131 
               
               
                 41 
                 + 
                 75 
               
               
                 42 
                 +++ 
                 163 
               
               
                 43 
                 + 
                 59 
               
               
                 44 
                 ++ 
                 55 
               
               
                 45 
                 ++ 
                 77 
               
               
                 46 
                 + 
                 71 
               
               
                 47 
                 ++ 
                 59 
               
               
                 48 
                 ++ 
                 105 
               
               
                 49 
                 + 
                 78 
               
               
                 51 
                 ++ 
                 102 
               
               
                 54 
                 + 
                 24 
               
               
                 55 
                 + 
                 26 
               
               
                 56 
                 +++ 
                 124 
               
               
                 57 
                 + 
                 35 
               
               
                 59 
                 ++ 
                 51 
               
               
                 66 
                 + 
                 53 
               
               
                 67 
                 +++ 
                 116 
               
               
                 68 
                 ++ 
                 76 
               
               
                 69 
                 + 
                 54 
               
               
                 70 
                 ++ 
                 63 
               
               
                 76 
                 +++ 
                 98 
               
               
                   
               
               
                 Potency (EC50): 
               
               
                 + from 200 nM to &lt;1 μM 
               
               
                 ++ from 20 nM to &lt;200 nM 
               
               
                 +++ &lt;20 nM