Patent Publication Number: US-2010119599-A1

Title: Polyhydroquinoline compounds and dihydropyridine compounds for inhibiting beta-amyloid production

Description:
FIELD OF THE INVENTION 
     The present invention relates to methods of treatment and diagnosis of diseases associated with cerebral accumulation of Alzheimer&#39;s amyloid, such as Alzheimer&#39;s disease, using polyhydroquinoline and dihydropyridine compounds provided herein. 
     BACKGROUND 
     Alzheimer&#39;s disease (AD) is the most common neurodegenerative disorder of aging, afflicting approximately 1% of the population over the age of 65. Characteristic features of the disease include neurofibrillary tangles composed of abnormal tau protein, paired helical filaments, neuronal loss, and alteration in multiple neurotransmitter systems. The hyperphosphorylation of microtubule-associated tau protein is a known marker of the pathogenic neuronal pre-tangle stage in AD brain (Tan et al., “Microglial Activation Resulting from CD40R/CD40L Interaction after Beta-Amyloid Stimulation,” Science 286:2352-55, 1999). 
     A significant pathological feature of AD is an overabundance of diffuse and compact senile plaques in association with limbic areas of the brain. Although these plaques contain multiple proteins, their cores are composed primarily of β-amyloid protein, a 39-43 amino acid proteolytic fragment that is proteolytically derived from amyloid precursor protein (APP), a transmembrane glycoprotein. Additionally, C-terminal fragments (CTF) of APP are known to accumulate intraneuronally in AD. 
     β-amyloid is derived from APP, a single-transmembrane protein with a 590 to 680 amino acid extracellular amino terminal domain and an approximately 55 amino acid cytoplasmic tail. Messenger RNA from the APP gene on chromosome 21 undergoes alternative splicing to yield eight possible isoforms, three of which (the 695, 751 and 770 amino acid isoforms) predominate in the brain. APP undergoes proteolytic processing via three enzymatic activities, termed α-, β- and γ-secretase. Alpha-secretase cleaves APP at amino acid 17 of the β-amyloid domain, thus releasing the large soluble amino-terminal fragment α-APP for secretion. Because α-secretase cleaves within the β-amyloid domain, this cleavage precludes β-amyloid formation. Alternatively, APP can be cleaved by β-secretase to define the amino terminus of β-amyloid and to generate the soluble amino-terminal fragment β-APP. Subsequent cleavage of the intracellular carboxy-terminal domain of APP by γ-secretase results in the generation of multiple peptides, the two most common being a 40 amino acid β-amyloid (Aβ1-40) and 42 amino acid β-amyloid (Aβ1-42). Aβ1-40 comprises 90-95% of the secreted β-amyloid and is the predominant species recovered from cerebrospinal fluid (Seubert et al., Nature, 359:325-7, 1992). In contrast, less than 10% of secreted β-amyloid is Aβ1-42. Despite the relative paucity of Aβ1-42 production, Aβ1-42 is the predominant species found in plaques and is deposited initially, perhaps due to its ability to form insoluble amyloid aggregates more rapidly than Aβ1-40 (Jarrett et al., Biochemistry, 32:4693-7, 1993). The abnormal accumulation of β-amyloid in the brain is believed to be due to decreased clearance of β-amyloid from the brain to the periphery or excessive production of β-amyloid. Various studies suggest excessive production of β-amyloid is due to either overexpression of APP or altered processing of APP, or mutation in the γ-secretases or APP responsible for β-amyloid formation. 
     β-Amyloid peptides are thus believed to play a critical role in the pathobiology of AD, as all the mutations associated with the familial form of AD result in altered processing of these peptides from APP. Indeed, deposits of insoluble, or aggregated, fibrils of β-amyloid in the brain are a prominent neuropathological feature of all forms of AD, regardless of the genetic predisposition of the subject. It also has been suggested that AD pathogenesis is due to the neurotoxic properties of β-amyloid. The cytotoxicity of β-amyloid was first established in primary cell cultures from rodent brains and also in human cell cultures. The work of Mattson et al. (J. Neurosci., 12:376-389, 1992) indicates that β-amyloid, in the presence of the excitatory neurotransmitter glutamate, causes an immediate pathological increase in intracellular calcium, which is believed to be very toxic to the cell through its greatly increased second messenger activities. 
     Concomitant with β-amyloid production and β-amyloid deposition, there exists robust activation of inflammatory pathways in AD brain, including production of pro-inflammatory cytokines and acute-phase reactants in and around β-amyloid deposits (McGeer et al., J. Leukocyte Biol. 65:409-15, 1999). Activation of the brain&#39;s resident innate immune cells, the microglia, is thought to be intimately involved in this inflammatory cascade. It has been demonstrated that reactive microglia produce pro-inflammatory cytokines, such as inflammatory proteins and acute phase reactants, such as alpha-1-antichymotrypsin, transforming growth factor β, apolipoprotein E and complement factors, all of which have been shown to be localized to β-amyloid plaques and to promote β-amyloid plaque “condensation” or maturation (Nilsson et al., J. Neurosci. 21:1444-5, 2001), and which at high levels promote neurodegeneration. Epidemiological studies have shown that patients using non-steroidal anti-inflammatory drugs (NSAIDS) have as much as a 50% reduced risk for AD (Rogers et al., Neurobiol. Aging 17:681-6, 1996), and post-mortem evaluation of AD patients who have undergone NSAID treatment has demonstrated that risk reduction is associated with diminished numbers of activated microglia (Mackenzie et al., Neurology 50:986-90, 1998). Further, when Tg APPsw mice, a mouse model for Alzheimer&#39;s disease, are given an NSAID (ibuprofen), these animals show reduction in β-amyloid deposits, astrocytosis, and dystrophic neurites correlating with decreased microglial activation (Lim et al., J. Neurosci. 20:5709-14, 2000). 
     At present, treatment for AD is limited. However, there are several drugs approved by the FDA to improve or stabilize symptoms of AD (Alzheimer&#39;s Disease Medications Fact Sheet: (July 2004) U.S. Department of Health and Human Services), including ARICEPT® (donepezil), EXELON® (rivastigmine), REMINYL® or RAZADYNE® (galantamine), COGNEX® (tacrine) and NAMENDA® (memantine). The effect achieved with many drugs currently in use is small (Tariot et al., JAMA 291: 317-24, 2004). Treatments for AD remain a largely unmet clinical need. 
     U.S. Patent Application No. 2005009885 (Jan. 13, 2005) (Mullan et al.) discloses a method for reducing β-amyloid deposition using nilvadipine, as wells as methods of diagnosing cerebral amyloidogenic diseases using nilvadipine. Nimodipine has been studied for the treatment of dementia. (Fritze et al., J. Neural Transm. 46: 439-453, 1995; and Forette et al., Lancet 352: 1347-1351, 1998). 
     There continues to be a need to identify compounds that can treat the inexorable progression of brain degeneration which is a hallmark of AD, wherein the treatment addresses β-amyloid production and the concomitant β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau), microglial-activated inflammation, and altered or over expression of APP which is seen in AD patients. 
     SUMMARY 
     The present inventors have found polyhydroquinoline and dihydropyridine compounds that inhibit β-amyloid production, particularly, Aβ1-40 and Aβ1-42 production individually and total production of Aβ1-40+Aβ1-42. These compounds may be used in methods of treating, preventing, managing, slowing the progression of, delaying the onset of and/or ameliorating one or more symptoms of a disease associated with accumulation of β-amyloid, such as, but not limited to Alzheimer&#39;s Disease, or AD, in a subject in need thereof. Polyhydroquinoline compounds useful in the methods of the invention are listed in Table 1. Dihydropyridine and related compounds useful in the methods of the invention are listed in Tables 2 and 3. 
     Tables 1, 2, and 3 provide a list of polyhydroquinoline, dihydropyridine, and related compounds and report the activity of each compound to alter the levels of β-amyloid peptides, particularly Aβ1-40 and Aβ1-42, in cells that overexpress APP, e.g., Chinese Hamster Ovary (CHO) cells that overexpress APP751 (e.g., as described in Example 1, infra.) The compounds used in the methods of the invention reduce Aβ1-40 and/or Aβ1-42 production, and optionally both, and reduce one of Aβ1-40 and/or Aβ1-42 (or both) by at least 1%, 2%, 5%, 15%, 20%, 25%, 30%, 40%, 50%, 60%, 70%, 80%, 90%, 95%, or even at least 99%. An entry of “0” indicates no detectable amount of Aβ1-40 or Aβ1-42 according to the assay conditions. The data in tables 1, 2, and 3 may be rounded to the nearest 0.1%. The β-amyloid concentrations may be measured intracellularly or extracellularly (e.g., in the culture medium). The compounds may be tested at a range of concentrations, for example, from about 1 mM to 10 mM, about 500 nM to 50 μM, or about 5 μM to 30 μM. 
     The invention provides methods of treating, preventing managing, slowing the progression of, delaying the onset of, and/or ameliorating one or more symptoms of a disease or disorder associated with increased accumulation of β-amyloid, preferably cerebral accumulation of β-amyloid, such as, but not limited to AD, by administering an effective amount of a compound in Tables 1, 2, and 3, or a pharmaceutically acceptable salt, prodrug or derivative thereof, to a non-human animal or human subject. The invention provides pharmaceutical compositions comprising a therapeutically effective amount of a compound listed in Tables 1, 2, and 3, or pharmaceutically acceptable salt, prodrug or derivative thereof, and a pharmaceutically acceptable carrier, for use in the methods of the invention described herein, as well as unit dosage forms thereof. Also provided is the use of a compound disclosed in Tables 1, 2, and 3, or a pharmaceutically acceptable salt, prodrug or derivative thereof, in the manufacture of a medicament for the treatment of a disease associated with cerebral accumulation of β-amyloid. 
     In specific embodiments, the disease associated with cerebral accumulation of Alzheimer&#39;s amyloid is AD. In other embodiments, the disease is cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis Dutch-type, other forms of familial Alzheimer&#39;s disease and familial cerebral Alzheimer&#39;s amyloid angiopathy, transmissible spongiform encephalopathy, scrapie (and any other prion-based diseases), traumatic brain injury and Gerstmann-Straussler-Scheinker syndrome. 
     The method may, in one embodiment, include one or more of reducing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis. Because most diseases having cerebral accumulation of Alzheimer&#39;s amyloid, such as AD, are chronic, progressive, intractable brain dementias, it is contemplated that the duration of treatment with at least one of the active agents can optionally last for up to the lifetime of the animal or human. 
     Also provided is a method for treating head injury, and, optionally, reducing the risk of β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) or microgliosis, in animals or humans suffering from traumatic brain injury, the method comprising administering to the animal or human a therapeutically effective amount in unit dosage form of a compound listed in Tables 1, 2, or 3, or a pharmaceutically acceptable salt, prodrug, or derivative thereof. In particular embodiments, the compound is administered immediately after the head injury, e.g., no more than 1 hour, 2 hours, 3 hours, 4 hours, 5 hours, 6 hours, 7 hours, 8 hours, 10 hours, 12 hours, 15 hours, 18 hours, or 24 hours after the injury has occurred, then, optionally, continuing treatment with the compound for a prescribed period of time thereafter. In one embodiment, the compound reduces the risk of β-amyloid production, Aβ deposition, β-amyloid neurotoxicity and/or microgliosis. 
     In specific embodiments, the invention provides methods of delaying the onset of or slowing the progression of a disease or disorder associated with increased β-amyloid accumulation. For example, the methods may slow the mental deterioration and loss of cognitive function that occurs in many such diseases, such as AD. In specific embodiments, human subjects suffering from AD retain mental function (e.g., can live unassisted) for at least 6 months, 1 year, 18 months, 2 years, 3 years, 4 years, 5 years, 7 years, 10 years, 12 years, 15 years, 18 years or even at least 20 years longer, on average, than comparable patients not subject to a method of the invention or for at least that period of time after diagnosis. In certain embodiments, the subject is elderly, specifically, at least 65, 75 or 85 years old. 
     In other embodiments, the invention provides methods of delaying the onset of diseases or disorders associated with accumulation of β-amyloid in subjects exhibiting early signs of such a disease or disorder or having a predisposition for such a disease or disorder. For example, subjects may exhibit early signs of memory loss or other loss of cognitive function, or behavioral or physical changes associated with early AD, or other disease or disorder associated with cerebral accumulation of β-amyloid. In these early stage subjects, methods of the invention may show the progression of the disease and delay onset of later stages of the disease by at least, on average, 6 months, 1 year, 18 months, 2 years, 3 years, 4 years, 5 years, 7 years, 10 years, 12 years, 15 years, 18 years or even at least 20 years. Subjects predisposed to a disease or disorder associated with accumulation of β-amyloid may be over the age of 65, 70, 75, 80 or 85, have a family history of such a disease or disorder, particularly, early onset AD (e.g., have at least a first degree relative or at least a second degree relative having been diagnosed with such a disease or disorder), have the ApoE epsilon 4 genotype, and/or have a history of head injury (particularly repeated head injury). In subjects having such a predisposition, methods of the invention may delay the onset of the disease or disorder by, on average, 1 year, 2 years, 5 years, 10 years, 15 years or 20 years or reduce risk of developing such a disease or disorder by at least 10%, 20%, 30%, 40%, 50%, 60%, 70%, 80% or 90%. 
     In another embodiment, a diagnostic method for a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid in an animal or human is provided, comprising: taking a first measurement of plasma, urine, serum, whole blood, or cerebral spinal fluid (CSF) concentration of β-amyloid in the peripheral circulation of the animal or human; administering a diagnostically effective amount in unit dosage form of at least one active agent selected from the compounds listed in Tables 1, 2, or 3, or pharmaceutically acceptable salt, prodrug or derivative thereof, to the animal or human; taking a second measurement of plasma, serum, whole blood, urine or CSF concentration of β-amyloid in the peripheral circulation of the animal or human; and calculating the difference between the first measurement and the second measurement, wherein a change in the plasma, serum, whole blood, urine or CSF concentration of β-amyloid in the second measurement compared to the first measurement, in particular, an increase in concentration, indicates a possible diagnosis of a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid in the animal or human. 
    
    
     DETAILED DESCRIPTION OF THE INVENTION 
     The invention provides methods of treating, preventing, managing, delaying the onset of, slowing the progression of, and ameliorating one or more symptoms of a disease or disorder associated with β-amyloid accumulation, particularly, cerebral β-amyloid accumulation, by administration to a subject in need thereof an effective amount of a pharmaceutical composition comprising a compound selected from the compounds listed in Tables 1, 2, and 3, supra, and pharmaceutically acceptable salts, prodrugs and derivatives thereof. The invention further provides pharmaceutical compositions comprising a compound selected from the compounds listed in Tables 1, 2, and 3, and pharmaceutically acceptable salts, prodrugs and derivatives thereof; and a pharmaceutically acceptable carrier, and methods of diagnosis using the compounds listed in Tables 1, 2, and 3, and pharmaceutically acceptable salts, prodrugs and derivatives thereof. 
     DEFINITIONS 
     As used herein, the term “Alzheimer&#39;s amyloid” is defined as a β-amyloid amino acid fragment that is for example proteolytically derived from amyloid precursor protein (APP). A β-amyloid amino acid fragment may include, for example, about 5 to 47 consecutive amino acids of the β-amyloid sequence. As used herein, the terms “β-amyloid,” “β-amyloid protein” and “Aβ” are used interchangeably with Alzheimer&#39;s amyloid that accumulates cerebrally in an animal or human. 
     As used herein the phrase a cell that “overexpresses APP or fragment thereof” refers to a cell that overexpresses an amyloid precursor protein, or fragment thereof, that in one preferred embodiment, includes a β-amyloid sequence and β- and γ-secretase cleavage sites. The cell that overexpresses APP or a fragment thereof preferably expresses an APP or fragment thereof that produces β-amyloid in the cell in which it is expressed. 
     As used herein, the term “amyloidogenic disease” includes a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid. 
     The terms “host,” “subject,” and “patient,” as used herein, unless otherwise specified, include mammals (e.g., cats, dogs, horses, mice, cows, sheep, etc.), humans, or other organisms in need of treatment, all of which can be treated or diagnosed using the methods described herein. 
     The term “elderly,” as used herein, means a human who is 65 years or older. 
     As used herein, the phrase “in combination” refers to the use of more than one therapeutic agent. The use of the term “in combination” does not restrict the order in which therapeutic agents are administered to a subject with a disease or disorder. A first therapeutic agent can be administered prior to (e.g., 5 minutes, 15 minutes, 30 minutes, 45 minutes, 1 hour, 2 hours, 4 hours, 6 hours, 12 hours, 24 hours, 48 hours, 72 hours, 96 hours, 1 week, 2 weeks, 3 weeks, 4 weeks, 5 weeks, 6 weeks, 8 weeks, or 12 weeks before), concomitantly with, or subsequent to (e.g., 5 minutes, 15 minutes, 30 minutes, 45 minutes, 1 hour, 2 hours, 4 hours, 6 hours, 12 hours, 24 hours, 48 hours, 72 hours, 96 hours, 1 week, 2 weeks, 3 weeks, 4 weeks, 5 weeks, 6 weeks, 8 weeks, or 12 weeks after) the administration of a second therapeutic agent (different from the first therapeutic agent) to a subject with a disease or disorder. 
     The terms “treatment,” “treat” and “treating,” as used herein, include any manner in which one or more of the symptoms of a disease or disorder are ameliorated or otherwise beneficially altered. 
     The terms “prevent,” “preventing” and “prevention,” as used herein, refer to the prevention of the onset of one or more symptoms of a disease or disorder associated with accumulation of β-amyloid in a subject resulting from the administration of a prophylactic or therapeutic agent. 
     As used herein, the term “therapeutically effective amount” refers to that amount of a therapeutic agent sufficient to result in amelioration of one or more symptoms of a disorder. 
     The term “pharmaceutically acceptable salt,” as used herein, unless otherwise specified, includes those salts which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of hosts without undue toxicity, irritation, allergic response and the like, and are commensurate with a reasonable benefit/risk ratio and effective for their intended use. The salts can be prepared in situ during the final isolation and purification of one or more compounds of the composition, or separately by reacting the free base function with a suitable organic acid. Non-pharmaceutically acceptable acids and bases also find use herein, as for example, in the synthesis and/or purification of the compounds of interest. Nonlimiting examples of such salts are (a) acid addition salts formed with inorganic salts (for example hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, nitric acid, and the like), and salts formed with organic salts such as acetic acid, oxalic acid, tartaric acid, succinic acid, ascorbic acid, benzoic acid, tannic acid, and the like; (b) base addition salts formed with metal cations such as zinc, calcium, magnesium, aluminum, copper, nickel and the like; (c) combinations of (a) and (b). 
     The term “pharmaceutically acceptable prodrugs,” as used herein, unless otherwise specified, includes those prodrugs of one or more compounds of the composition which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of hosts without undue toxicity, irritation, allergic response and the like, are commensurate with a reasonable benefit/risk ratio, and are effective for their intended use. Pharmaceutically acceptable prodrugs also include zwitterionic forms, where possible, of one or more compounds of the composition. The term “prodrug” includes compounds that are transformed in vivo to yield the parent compound, for example by hydrolysis in blood or in the digestive system. 
     As used herein, the term “pharmaceutically acceptable derivative” means any salt, ester, or salt of such ester or any other compound which upon administration to an individual is capable of providing (directly or indirectly) a compound of the invention. The phrase includes active metabolites or residues of the compounds according to the invention. 
     The term “enantiomerically enriched,” as used herein, refers to a compound that is a mixture of enantiomers in which one enantiomer is present in excess, and preferably present to the extent of 95% or more, and more preferably 98% or more, including 100%. 
     By the term “about” is meant within ±10% of the stated amount, or within experimental error of the measuring technique. 
     Methods of Treatment 
     The invention provides methods for treating an animal or human afflicted with a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid, such as Alzheimer&#39;s disease (AD), comprising administering a therapeutically effective amount of a compound disclosed herein, or a pharmaceutically acceptable salt, prodrug or derivative thereof. Administration of the compound in one embodiment results in reducing one or more of β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) or microgliosis, or combination thereof. In one embodiment, the compound is characterized in that it reduces β-amyloid production, for example, by at least about 5%, 10%, 15%, 20%, 25%, 30%, 50%, 70%, 80%, 90%, 95% or more in cultured cells that overexpress APP or a fragment thereof, as measured, for example, in a culture medium comprising the cells or as measured intracellularly. 
     As used herein, reference to a compound that reduces β-amyloid production, refers to a compound that reduces β-amyloid production, either Aβ1-40 or Aβ1-42, or both, in cells that overexpress APP or a fragment thereof, and the cells may be, for example, Chinese hamster ovary (CHO) cells that overexpress APP, for example, 7W WT APP751 CHO cells; 7W (wt APP 751 ) cells; 7W ΔC  cells; 7W SW  cells; or 7W VF  cells. In one embodiment, the compound and method according to the invention achieve a greater relative reduction in Aβ1-42 compared to reduction in Aβ1-40. In other words, where Aβ1-42 is more pathogenic than Aβ1-40, compounds and methods according to one embodiment of the invention selectively reduce production of Aβ1-42. For example, Aβ1-42 may be selectively reduced by at least about 5%, 10%, 15%, 20%, 25%, 30%, 50%, 70%, 80%, 90%, 95% or more compared to the reduction in Aβ1-40 in cultured cells that overexpress APP or a fragment thereof, as measured, for example, in a culture medium comprising the cells or as measured intracellularly. 
     It is noted that wherever the embodiments disclosed herein refer to a reduction in β-amyloid in cells that overexpress APP, alternatively, an increase in αCTF (α C-terminal APP fragment, also known as CTF-α) and/or APPSα soluble fragment can be measured for example, in the cell culture or intracellularly. Alpha-CTF and APPSα soluble fragment are produced in increased amounts from APP when the production of β-amyloid decreases. 
     It is further noted that wherever the embodiments disclosed herein refer to a reduction in β-amyloid in cells that overexpress APP, alternatively, a decrease in β CTF (β C-terminal APP fragment, also known as CTF-β) or APPSβ soluble fragment can be measured, e.g., in the cell culture media or intracellularly, as they are produced in decreased amounts from APP as the compound causes the production of β-amyloid to decrease. 
     In a further embodiment, a method is provided for treating animals or humans suffering from traumatic brain injury (TBI). In one embodiment, β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and/or microgliosis is reduced. The method includes administering to the animal or human, for example, immediately (30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, 5 hours, 6 hours, 8 hours, 10 hours, 12 hours, 15 hours, 18 hours, 24 hours, 36 hours or 48 hours) after the TBI, a therapeutically effective amount of a compound selected from the compounds listed in Tables 1, 2, and 3, and pharmaceutically acceptable salts, prodrugs and derivatives thereof. The method may include continuing treatment with the compound for a prescribed period of time thereafter. It has been shown that TBI increases the susceptibility to AD, and thus it is believed, without being bound by the theory, that TBI accelerates brain β-amyloid accumulation and oxidative stress, which may work synergistically to promote the onset or drive the progression of AD. Treatment with the compound of animals or humans suffering from one or more TBIs can continue, for example, for about one hour, 24 hours, a week, two weeks, 1-6 months, one year, two years or three years. Such treatment reduces the risk of developing AD by 10%, 20%, 30%, 40%, 50%, 60%, 70% or even 80% or delays the onset of AD by, on average, 1 year, 2 years, 5 years, 10 years, 15 years, 20 years, or 25 years or reduce the risk of developing the disease or disorder by 10%, 20%, 30%, 40%, 50%, 60%, 70%, 80%, or 90%. 
     Amyloidogenic diseases which can be treated according to the methods of the present invention can include, without limitation, Alzheimer&#39;s disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis Dutch-type, or other forms of familial AD and familial cerebral Alzheimer&#39;s amyloid angiopathy. 
     In specific embodiments, the invention provides methods of delaying the onset of or slowing the progression of a disease or disorder associated with increased β-amyloid accumulation. For example, the methods may slow the mental deterioration and loss of cognitive function, adverse changes in behavior and/or physical deterioration that occurs in many such diseases, such as AD. In specific embodiments, human or animal subjects suffering from an amyloidogenic disease, such as AD, retain mental function (e.g., can live unassisted) for at least 6 months, 1 year, 18 months, 2 years, 3 years, 4 years, 5 years, 7 years, 10 years, 12 years, 15 years, 18 years or even at least 20 years longer, on average, than comparable patients not subject to a method of the invention. In certain embodiments, the subject is at least 65, 75 or 85 years old. 
     In other embodiments, the invention provides methods of delaying the onset of diseases or disorders associated with accumulation of β-amyloid in subjects exhibiting early signs of such a disease or disorder or having a predisposition to such a disease or disorder. For example, subjects may exhibit early signs of memory loss or other loss of cognitive function, adverse behavioral changes, or other signs of physical impairment associated with a disease or disorder characterized by accumulation of β-amyloid, particularly AD. Subjects predisposed to a disease or disorder associated with accumulation of β-amyloid may be over the age of 65, 70, 75, 80 or 85, have a family history (e.g., having at least a first degree relative or at least a second degree relative with such a disease or disorder) of such a disease or disorder, particularly, early onset AD, have the ApoE epsilon 4 genotype, and/or have a history of head injury (particularly repeated head injury). In subjects having such a predisposition, methods of the invention may delay the onset of the disease or disorder by, on average, 1 year, 2 years, 5 years, 10 years, 15 years or 20 years or reduce the risk of developing the disease or disorder by 10%, 20%, 30%, 40%, 50%, 60%, 70%, 80% or 90%. 
     The compounds of the invention may be administered in combination with other therapeutic agents that are useful for the treatment, prevention, management, delaying the onset, slowing the progression or amelioration of one or more symptoms of a disease or disorder associated with accumulation of β-amyloid, either when administered alone or in combination with a compound of the invention. Such therapeutic agents useful for such combination therapy include, but are not limited to ARICEPT® (donepezil), EXELON® (rivastigmine), REMINYL® or RAZADYNE® (galantamine), COGNEX® (tacrine) and NAMENDA® (memantine), NSAIDS such as ibuprofen, etc., and agents that have efficacy in the treatment of depression, continency and other symptoms of diseases and disorders associated with accumulation of β-amyloid. The effects of the combination may be additive or, preferably, are synergistic. 
     Exemplary dosages of compound that can be administered include 0.001-1.0 mg/kg body weight. An exemplary dose of compound is about 1 to 50 mg/kg body weight per day, 1 to 20 mg/kg body weight per day, or 0.1 to about 100 mg per kilogram body weight of the recipient per day. Lower doses may be preferable, for example doses of 0.5-100 mg, 0.5-50 mg, 0.5-10 mg, or 0.5-5 mg per kilogram body weight per day, or e.g., 0.01-0.5 mg per kilogram body weight per day. The effective dosage range can be calculated based on the activity of the compound and other factors known in the art of pharmacology. 
     The compound is conveniently administered in any suitable dosage form, including but not limited to one containing 1 to 3000 mg, or 10 to 1000 mg of active ingredient per unit dosage form. An oral dosage of 50-1000 mg is possible. Lower doses may be preferable, for example from 10-100 or 1-50 mg, or 0.1-50 mg, or 0.1-20 mg or 0.01-10.0 mg. Furthermore, lower doses may be utilized in the case of administration by a non-oral route, as, for example, by injection or inhalation. 
     In another embodiment, the dosage can range from about 0.05 mg to 20 mg per day, from between about 2 mg to 15 mg per day, about 4 mg to 12 mg per day, and or about 8 mg per day. 
     In another embodiment, the dosage ranges, e.g. from about one day to twelve months, from about one week to six months, or from about two weeks to four weeks. 
     Because most diseases having cerebral accumulation of Alzheimer&#39;s amyloid, such as AD, are chronic, progressive, intractable brain dementias, it is contemplated that the duration of treatment with compounds disclosed herein can last for up to the lifetime of the animal or human. 
     In another embodiment of the present invention, a method is provided for increasing cerebral blood flow in an animal or human to improve cognition or slow the progress of an impairment of cognition by administering a compound according to Formulas I or II or selected from the compounds listed in Tables 1, 2, and 3, and pharmaceutically acceptable salts, prodrugs and derivatives thereof. Impairment of cognition includes MCI (Mild Cognitive Impairment). A condition of MCI may exist irrespective of a patient&#39;s status with respect to a diagnosis related to Alzheimer&#39;s amyloid. Without wishing to be bound by theory, the administration of compounds according to the invention may yield increased cerebral blood flow compared to baseline cerebral blood flow, and such increased blood flow may reduce β-amyloid deposition or provide other clinical benefit. Diseases associated with decreased cerebral blood flow can include without limitation stroke, such as ischemic stroke, ischemia, depression, including subcortical ischemic depression, giant cell arteritis, temporal arteritis, cerebral vasospasm, infarction, obstruction of a cerebral blood vessel, hemorrhage, such as subarachnoid hemorrhage, or any other indication related to restricted cerebral blood flow. 
     Methods of Diagnosis 
     In a further embodiment, a method is provided for diagnosing or determining the risk for developing a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid, such as AD, in an animal or human, by taking a first measurement of β-amyloid concentration from a peripheral body fluid such as plasma, serum, whole blood, urine or cerebral spinal fluid (CSF) of the animal or human. Subsequently, the method includes administering to the animal or human a diagnostically effective amount of a compound selected from the compounds listed in Tables 1, 2, and 3, and pharmaceutically acceptable salts, prodrugs and derivatives thereof. In one embodiment, the compound decreases β-amyloid production, for example, by at least about 5%, 10%, 15%, 20%, 25%, 30%, 50%, or more, as measured, for example, in the medium of cultured cells which overexpress APP or a fragment thereof, or as measured intracellularly. A second (selected endpoint) measurement of β-amyloid concentration is taken from plasma, serum, whole blood, urine or CSF of the animal or human at a later time, and the difference between the first measurement and the second measurement is determined. A change in the concentration of β-amyloid in plasma, serum, whole blood, urine or CSF in the second measurement compared to the first measurement indicates a risk of developing or a possible diagnosis of a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid in the animal or human. In particular, an increase in peripheral β-amyloid indicates the presence of an accumulation of cerebral β-amyloid, and therefore the risk of disease or the presence of the disease. 
     It is believed, without being bound by any theory, that the compounds can cause an increase in β-amyloid concentration in plasma, urine, serum, whole blood or CSF by facilitating the clearance of already produced β-amyloid from the central nervous system into the periphery, thus increasing β-amyloid concentration in the peripheral fluid being assayed. 
     The duration of time of administration of the compound after the first peripheral body fluid measurement, up until the second (selected endpoint) peripheral body fluid measurement, is, e.g., any suitable time period, e.g. about 1-12 hours, about 1-7 days, about 1-4 weeks; about 2-6 months, or more. The time length can be adjusted as needed depending, for example, on the progression of the disease, and the patient. A suitable periodic (e.g., daily) dosage of the compound is administered, e.g. orally or intravenously, and the β-amyloid levels in the individual can be monitored periodically up until the endpoint. In one preferred embodiment, the compound is administered daily for about 3 days to 4 weeks from the start of administration to the endpoint measurement. The change in concentration indicative of the risk or presence of a disease associated with β-amyloid accumulation is, e.g. about 10-20% or more between the first and endpoint measurements. 
     Exemplary dosages of compound that can be administered include 0.001-1.0 mg/kg body weight, for example daily. An exemplary dose of compound is about 1 to 50 mg/kg body weight per day, 1 to 20 mg/kg body weight per day, or 0.1 to about 100 mg per kilogram body weight of the recipient per day. Lower doses may be preferable, for example doses of 0.5-100 mg, 0.5-50 mg, 0.5-10 mg, or 0.5-5 mg per kilogram body weight per day, or e.g., 0.01-0.5 mg per kilogram body weight per day. The effective dosage range can be calculated based on the activity of the compound and other factors known in the art of pharmacology. 
     The compound is conveniently administered in any suitable dosage form, including but not limited to, one containing 1 to 3000 mg, or 10 to 1000 mg of active ingredient per unit dosage form. An oral dosage of 50-1000 mg is possible. Lower doses may be preferable, for example from 10-100 or 1-50 mg, or 0.1-50 mg, or 0.1-20 mg or 0.01-10.0 mg. Furthermore, lower doses may be utilized in the case of administration by a non-oral route, as, for example, by injection or inhalation. 
     In one embodiment, the invention comprises a method for diagnosing a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid in an animal or human subject, comprising: taking a first measurement of plasma, urine, serum, whole blood, or cerebral spinal fluid (CSF) concentration of β-amyloid or fragment thereof in the peripheral circulation of the animal or human subject; (a) administering to the animal or human subject a diagnostically effective amount of a compound selected from the compounds listed in Tables 1, 2, and 3, and derivatives, salts and prodrugs thereof; (b) taking a second measurement of plasma, serum, whole blood, urine or CSF concentration of β-amyloid in the peripheral circulation of the animal or human; and (c) calculating the difference between the first measurement and the second measurement; wherein a change in the plasma, serum, whole blood, urine or CSF concentration of β-amyloid in the second measurement compared to the first measurement indicates a possible diagnosis of a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid in the animal or human subject. 
     Compounds 
     A variety of compounds are provided herein in Tables 1, 2, and 3, which can be used in methods described herein, including the treatment or diagnosis of diseases associated with cerebral accumulation of Alzheimer&#39;s amyloid. Compounds useful in the methods and compositions described herein are in one embodiment available from commercially sources or can be synthesized using methods routine in the art. 
     Optionally, the compounds listed in Tables 1, 2, and 3 can be represented by the following formulas. 
     Polyhydroquinoline compounds according to Formula I: 
     
       
         
         
             
             
         
       
     
     wherein
 
R1 through R11 may be the same or different from each other and each represent hydrogen atom, alkyl, alkenyl, alkynyl, alkoxy, carboxy, carboxamido, amino, aminocarboxy, cyano, halogen, aryl, alkaryl, alkenaryl, azido, heteroaryl, cycloalkyl, heterocycloalkyl, carbamoyl, methyl thiocarbamoyl, alkyl ester, aryl ester, alkyloxyalkylester, alkylthioalkylester, and thiolalkyl groups, in which each group is optionally further substituted. In addition, adjacent R groups (i.e. R1 and R2, R2 and R3, R7 and R8, etc.) may together form cyclo, heterocyclo, aryl, or heteroaryl groups.
 
     Representative aryl and heteroaryl groups include phenyl, benzyl, chromene, 1-naphthyl, 2-naphthyl, thiophene-3-yl, thiophene-2-yl, furan-3-yl, furan-2-yl, pyrrolo, pyridine-4-yl, pyridine-3-yl, pyridine-2-yl, pyridine-4-ylmethyl, pyridine-3-ylmethyl, pyridine-2-ylmethyl, 1-naphthyl, 2-naphthyl, thiophene-3-yl, thiophene-2-yl, furan-3-yl, furan-2-yl, pyridine-4-yl, pyridine-3-yl, pyridine-2-yl, carbazolyl, indole-2-yl, and indole-3-yl groups. 
     In one embodiment, R4 is an optionally substituted aromatic or heteroaromatic ring, and R5 is hydrogen. In another embodiment, R4 is an unsubstituted aromatic or heteroaromatic ring, and R5 is hydrogen. 
     In one embodiment, R4 is a nonaromatic substituent and R5 is hydrogen. 
     In one embodiment, R2 and R3 together form a ring which may optionally be fused with one or more additional rings. 
     In one embodiment, R1, R6, R7, R8, R9, R10, and R11 are hydrogen. Alternatively, R8 and R9 are hydrogen, methyl, optionally substituted phenyl, or thienyl. 
     In one embodiment, R2 is selected from lower alkyl, including methyl, amino, and thiol, and aryl, such as phenyl group, each group being optionally substituted. R2 may optionally form a ring together with R1 or R3. In one embodiment R1 and R2 join together with the main ring to form a 1,3-thiazolidino[3,2-a]pyridine ring. 
     In one embodiment, R3 is selected from a cyano group or carboxylate esters, such as alkyl esters, including methyl, ethyl, propyl, butyl, pentyl, hexyl, branched alkyls; cycloalkyl esters, including cyclopentyl, cyclohexyl, and cycloheptyl; aryl esters, including phenyl, benzyl; allyl esters; and optional substitutions, such as methoxyethyl esters, ethoxyethyl esters, phenoxyethyl esters, phenylethylesters, methoxybenzyl esters; aryl-substituted amides, and the like. 
     In one embodiment, R4 is an aromatic group selected from phenyl, pyridinyl, furyl, pyrrolo, and thienyl, optionally unsubstituted or optionally with one or more substitutions, including alkoxy, nitro, halogen, acetoxy, trifluoromethyl, phenoxy, dialkylamino, 1,3-dioxalenyl, and alkyl substituents. 
     Dihydropyridine compounds according to Formula II: 
     
       
         
         
             
             
         
       
     
     wherein
 
R1 through R7 may be the same or different from each other and each represent hydrogen atom, alkyl, alkenyl, alkynyl, alkoxy, carboxy, carboxamido, amino, aminocarboxy, cyano, halogen, aryl, alkaryl, alkenaryl, azido, sulfonyl, heteroaryl, cycloalkyl, heterocycloalkyl, carbamoyl, methylthiocarbamoyl, alkyl ester, and aryl ester, in which each group is optionally further substituted. In addition, adjacent R groups (i.e. R1 and R2, R2 and R3, R6 and R7, R1 and R7, etc.) may together form cyclo, heterocyclo, aryl, or heteroaryl groups.
 
     Representative aryl and heteroaryl groups include phenyl, benzyl, chromene, 1-naphthyl, 2-naphthyl, thiophene-3-yl, thiophene-2-yl, furan-3-yl, furan-2-yl, pyrrolo, pyridine-4-yl, pyridine-3-yl, pyridine-2-yl, pyridine-4-ylmethyl, pyridine-3-ylmethyl, pyridine-2-ylmethyl, 1-naphthyl, 2-naphthyl, thiophene-3-yl, thiophene-2-yl, furan-3-yl, furan-2-yl, pyridine-4-yl, pyridine-3-yl, pyridine-2-yl, carbazolyl, indole-2-yl, and indole-3-yl groups. 
     In one embodiment, R1 is hydrogen. In one embodiment, R1 is a substituted or unsubstituted phenyl, benzyl or thienyl group. In one embodiment, R1 is an adamantyl group. In one embodiment, R1 is an alkyl group such as methyl. In embodiment, R1 is a 1-phenylethyl group. 
     In one embodiment, R2 or R7 are independently hydrogen, methyl, ethyl, propyl, amino, thiol, cyano, thioether, phenyl, thioacetamide, thioacetate, optionally substituted, for example at the nitrogen of the thioacetamide with an optionally substituted phenyl ring. 
     In one embodiment R1 and (R2 or R7) join together with the dihydropyridine ring to form a 1,3-thiazolidino[3,2-a]pyridine ring. 
     In one embodiment, (R2 or R7) and (R3 or R6) together form a fused sulfur-containing heteroaromatic ring. 
     In one embodiment, R3 or R6 are independently hydrogen, cyano, sulfonyl, carboxylate esters, such as alkyl esters, including methyl, ethyl, propyl, butyl, pentyl, hexyl, branched alkyls, such as t-butyl; cycloalkyl esters, including cyclopentyl, cyclohexyl, and cycloheptyl; aryl esters, including phenyl, benzyl; allyl esters; and optional substitutions, such as methoxyethyl esters, ethoxyethyl esters, phenoxyethyl esters, phenylethylesters, methoxybenzyl esters; aryl-substituted amides, phenylcarbamoyl, and the like. 
     In one embodiment, R4 is an optionally substituted aromatic or heteroaromatic ring, and R5 is hydrogen. In one embodiment, R4 is an unsubstituted aromatic or heteroaromatic ring and R5 is hydrogen. In one embodiment, R4 is an aromatic group selected from phenyl, pyridinyl, furyl, pyrrolo, and thienyl, optionally with one or more substitutions, including alkoxy, nitro, halogen, acetoxy, trifluoromethyl, phenoxy, dialkylamino, 1,3-dioxalenyl, additional aromatic rings, and alkyl substituents. 
     In one embodiment, R4 is a nonaromatic substituent and R5 is hydrogen. 
     In one embodiment, R4 and R5 together form a double bond to an oxygen atom. 
     In one embodiment, R4 and R5 together form a double bond to a nitrogen atom which together with R3 forms a fused heteroaromatic ring. 
     It is not envisioned that every compound within Formulas I and 2 will have the same level of efficacy in the methods described herein, including the treatment or diagnosis of diseases associated with cerebral accumulation of Alzheimer&#39;s amyloid. Certain compounds within Formulas I and 2 are preferred embodiments, such as the compounds listed in Tables 1, 2, and 3. Preferred embodiments can be readily determined by one of ordinary skill in the art using the assays described herein. As a general guide, preferred embodiments according to the invention alter the levels of β-amyloid peptides, particularly Aβ1-40 and Aβ1-42, in cells that overexpress APP, e.g., Chinese Hamster Ovary (CHO) cells that overexpress APP751 (e.g., as described in Example 1, infra.). Guidance for the amount of alteration of production of β-amyloid peptides is provided above. In one embodiment of the invention, treated cells produce 90% or less Aβ1-40 and/or Aβ1-42 compared to control cells. 
     It is to be understood that the compounds disclosed herein may contain chiral centers. Such chiral centers may be of either the (R) or (S) configuration, or may be a mixture thereof. Thus, the compounds provided herein may be enantiomerically pure, or be stereoisomeric or diastereomeric mixtures. It is understood that the disclosure of a compound herein encompasses any racemic, optically active, polymorphic, or steroisomeric form, or mixtures thereof, which preferably possesses the useful properties described herein, it being well known in the art how to prepare optically active forms and how to determine activity using the standard tests described herein, or using other similar tests which are will known in the art. Examples of methods that can be used to obtain optical isomers of the compounds include the following: 
     i) physical separation of crystals—a technique whereby macroscopic crystals of the individual enantiomers are manually separated. This technique can be used if crystals of the separate enantiomers exist, i.e., the material is a conglomerate, and the crystals are visually distinct; 
     ii) simultaneous crystallization—a technique whereby the individual enantiomers are separately crystallized from a solution of the racemate, possible only if the latter is a conglomerate in the solid state; 
     iii) enzymatic resolutions—a technique whereby partial or complete separation of a racemate by virtue of differing rates of reaction for the enantiomers with an enzyme 
     iv) enzymatic asymmetric synthesis, a synthetic technique whereby at least one step of the synthesis uses an enzymatic reaction to obtain an enantiomerically pure or enriched synthetic precursor of the desired enantiomer; 
     v) chemical asymmetric synthesis—a synthetic technique whereby the desired enantiomer is synthesized from an achiral precursor under conditions that produce asymmetry (i.e., chirality) in the product, which may be achieved using chiral catalysts or chiral auxiliaries; 
     vi) diastereomer separations—a technique whereby a racemic compound is reacted with an enantiomerically pure reagent (the chiral auxiliary) that converts the individual enantiomers to diastereomers. The resulting diastereomers are then separated by chromatography or crystallization by virtue of their now more distinct structural differences and the chiral auxiliary later removed to obtain the desired enantiomer; 
     vii) first- and second-order asymmetric transformations a technique whereby diastereomers from the racemate equilibrate to yield a preponderance in solution of the diastereomer from the desired enantiomer or where preferential crystallization of the diastereomer from the desired enantiomer perturbs the equilibrium such that eventually in principle all the material is converted to the crystalline diastereomer from the desired enantiomer. The desired enantiomer is then released from the diastereomer; 
     viii) kinetic resolutions—this technique refers to the achievement of partial or complete resolution of a racemate (or of a further resolution of a partially resolved compound) by virtue of unequal reaction rates of the enantiomers with a chiral, non-racemic reagent or catalyst under kinetic conditions; 
     ix) enantiospecific synthesis from non-racemic precursors—a synthetic technique whereby the desired enantiomer is obtained from non-chiral starting materials and where the stereochemical integrity is not or is only minimally compromised over the course of the synthesis; 
     x) chiral liquid chromatography, a technique whereby the enantiomers of a racemate are separated in a liquid mobile phase by virtue of their differing interactions with a stationary phase. The stationary phase can be made of chiral material or the mobile phase can contain an additional chiral material to provoke the differing interactions; 
     xi) chiral gas chromatography, a technique whereby the racemate is volatilized and enantiomers are separated by virtue of their differing interactions in the gaseous mobile phase with a column containing a fixed non-racemic chiral adsorbent phase; 
     xii) extraction with chiral solvents—a technique whereby the enantiomers are separated by virtue of preferential dissolution of one enantiomer into a particular chiral solvent; and 
     xiii) transport across chiral membranes—a technique whereby a racemate is placed in contact with a thin membrane barrier. The barrier typically separates two miscible fluids, one containing the racemate, and a driving force such as concentration or pressure differential causes preferential transport across the membrane barrier. Separation occurs as a result of the non-racemic chiral nature of the membrane which allows only one enantiomer of the racemate to pass through. 
     Additional information on certain embodiments of the invention can be seen in the following tables. Data from Tables 1, 2, and 3 can be rounded to the nearest 0.1%. Values of zero indicate that the level of Aβ1-40 or Aβ1-42 was below the detection limit for the assay. Where nitrogen is shown with only two bonds, a third bond to an H atom is assumed. 
     
       
         
           
               
             
               
                 TABLE 1 
               
             
            
               
                   
               
               
                 Polyhydroquinoline Compounds 
               
            
           
           
               
               
               
               
               
            
               
                   
                   
                   
                 Aβ1-40 
                 Aβ1-42 
               
               
                   
                   
                   
                 (% of 
                 (% of 
               
               
                 ID 
                 IUPAC Name 
                 Structure 
                 control) 
                 control) 
               
               
                   
               
            
           
           
               
               
               
               
               
            
               
                 ST013049 
                 phenylmethyl 4-[4- (diethylamino)phenyl]-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.81322327 
                 94.14198698 
               
               
                   
               
               
                 ST013052 
                 phenylmethyl 2,7,7-trimethyl-4-(6- nitro(2H-benzo[d]1,3-dioxolan-5- yl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.80972594 
                 72.35237417 
               
               
                   
               
               
                 ST013054 
                 pentyl 4-(4-chlorophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 8.35898154 
               
               
                   
               
               
                 ST013059 
                 methyl 2,7,7-trimethyl-5-oxo-4-(3- pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.68792349 
                 76.11236215 
               
               
                   
               
               
                 ST013060 
                 ethyl 2,7,7-trimethyl-4-(6-nitro(2H- benzo[d]1,3-dioxolan-5 -yl))-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 32.67242471 
                 99.38781622 
               
               
                   
               
               
                 ST013066 
                 ethyl 4-[4-(dimethylamino)phenyl]- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.42450704 
                 96.6696344 
               
               
                   
               
               
                 ST013070 
                 ethyl 2-methyl-5-oxo-4-(3-pyridyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 33.96416417 
                 82.4138992 
               
               
                   
               
               
                 ST013073 
                 methyl 4-(2,5-dimethoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.45771019 
                 93.16887134 
               
               
                   
               
               
                 ST013077 
                 methylethyl 2-methyl-5-oxo-4-(3- pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.44265943 
                 97.83491993 
               
               
                   
               
               
                 ST013081 
                 cyclopentyl 4-(4-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0.188081173 
               
               
                   
               
               
                 ST013083 
                 cyclopentyl 4-[4- (diethylamino)phenyl]-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 91.60943309 
               
               
                   
               
               
                 ST013086 
                 cyclopentyl 4-(2,4- dimethoxyphenyl)-2,7,7-trimethyl- 5-oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 73.73926838 
               
               
                   
               
               
                 ST013090 
                 methylethyl 2-methyl-5-oxo-4-(4- pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 41.06768443 
                 87.31382264 
               
               
                   
               
               
                 ST013092 
                 ethyl 4-(3-iodophenyl)-2-methyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 58.2381888 
                 82.02138197 
               
               
                   
               
               
                 ST013103 
                 cyclopentyl 4-(2-bromophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 68.18024309 
               
               
                   
               
               
                 ST013115 
                 methyl 4-(4-hydroxy-3- methoxyphenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 94.68997542 
                 65.74282147 
               
               
                   
               
               
                 ST013117 
                 methyl 4-(2,5-dimethoxyphenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 22.41281981 
                 46.14772075 
               
               
                   
               
               
                 ST013129 
                 methyl 4-[4-(diethylamino)phenyl]- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.2775198 
                 90.55369977 
               
               
                   
               
               
                 ST013137 
                 cyclopentyl 4-(3-bromo-4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 18.68706182 
                 30.01990755 
               
               
                   
               
               
                 ST013138 
                 phenylmethyl 4-(3,4- dimethoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.68041519 
                 56.82154064 
               
               
                   
               
               
                 ST013140 
                 methyl 4-(2,3-dimethoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.99016662 
                 51.10571245 
               
               
                   
               
               
                 ST013141 
                 methyl 4-(3-bromo-4-hydroxy-5- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 89.7204771 
                 23.67513581 
               
               
                   
               
               
                 ST013145 
                 methyl 4-(3-bromophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.90330511 
                 43.26618754 
               
               
                   
               
               
                 ST013146 
                 ethyl 4-(3-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 87.68642447 
                 67.67756521 
               
               
                   
               
               
                 ST013147 
                 methyl 2-methyl-5-oxo-4-(2,3,4- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 72.0021852 
                 45.36289098 
               
               
                   
               
               
                 ST013148 
                 ethyl 4-(3-hydroxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.10762087 
                 49.93352903 
               
               
                   
               
               
                 ST013151 
                 methyl 4-(2,3-dichlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 52.07684603 
                 61.61082431 
               
               
                   
               
               
                 ST013152 
                 pentyl 4-(3-chlorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 22.01766366 
                 33.22536019 
               
               
                   
               
               
                 ST013153 
                 methyl 4-(3-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 91.3939725 
                 66.25906806 
               
               
                   
               
               
                 ST013156 
                 cyclopentyl 4-(3-chlorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 13.69436853 
               
               
                   
               
               
                 ST013158 
                 ethyl 4-(3-ethoxy-4- hydroxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 75.02868069 
                 67.80645814 
               
               
                   
               
               
                 ST013162 
                 ethyl 4-(3-fluorophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 33.37521624 
                 36.28032527 
               
               
                   
               
               
                 ST013170 
                 pentyl 4-(3-bromo-4-hydroxy-5- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.83346991 
                 49.80328643 
               
               
                   
               
               
                 ST013173 
                 methyl 4-[3-(ethoxycarbonyl)-2- methyl-5-oxo-4-1,4,6,7,8- pentahydroquinolyl]benzoate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.19147774 
                 78.10034754 
               
               
                   
               
               
                 ST013174 
                 methylethyl 4-(3-hydroxyphenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.28571429 
                 73.08566994 
               
               
                   
               
               
                 ST013183 
                 prop-2-enyl 4-(3-methoxy-4- propoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 78.71437676 
                 66.25906806 
               
               
                   
               
               
                 ST013184 
                 ethyl 4-(2,3-dimethoxyphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 73.71392152 
                 60.31784594 
               
               
                   
               
               
                 ST013188 
                 cyclohexyl 4-(2,3-dichlorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 47.06279313 
               
               
                   
               
               
                 ST013191 
                 methylethyl 4-(4-ethylphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 33.37521624 
                 97.99507373 
               
               
                   
               
               
                 ST013192 
                 4-{2-methyl-3- [(methylethyl)oxycarbonyl]-5-oxo- 4-1,4,6,7,8-pentahydroquinolyl} phenyl acetate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.50213967 
                 82.46786112 
               
               
                   
               
               
                 ST013199 
                 prop-2-enyl 4-(3-methoxyphenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.48577567 
                 86.67952236 
               
               
                   
               
               
                 ST013202 
                 propyl 4-(3-bromophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 39.14929912 
               
               
                   
               
               
                 ST013206 
                 propyl 4-(2,3-dichiorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 62.53695129 
               
               
                   
               
               
                 ST013208 
                 butyl 2,7,7-tnmethyl-4-naphthyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 20.19103421 
               
               
                   
               
               
                 ST013212 
                 phenylmethyl 4-[4- (dimethylamino)phenyl]-2-methyl- 5-oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 50.84142151 
                 93.67934224 
               
               
                   
               
               
                 ST013213 
                 ethyl 4-(2,4-dimethoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 78.23840694 
                 69.34764412 
               
               
                   
               
               
                 ST013214 
                 phenylmethyl 2,7,7-trimethyl-4-(4- nitrophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 4.363166315 
               
               
                   
               
               
                 ST013215 
                 phenylmethyl 2,7,7-trimethyl-5- oxo-4-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 88.64072218 
               
               
                   
               
               
                 ST013216 
                 ethyl 2-methyl-5-oxo-4-[2- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 88.75568176 
               
               
                   
               
               
                 ST013227 
                 cyclopentyl 4-(4-ethylphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 92.65318231 
               
               
                   
               
               
                 ST013230 
                 phenylmethyl 4-(2,3- dichlorophenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 69.46790138 
               
               
                   
               
               
                 ST013235 
                 cyclohexyl 4-(2-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 43.00070989 
               
               
                   
               
               
                 ST013239 
                 butyl 4-(2,3-dichlorophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 59.45264407 
               
               
                   
               
               
                 ST013242 
                 phenylmethyl 4-(3-ethoxy-4- hydroxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 81.24629031 
                 64.37418548 
               
               
                   
               
               
                 ST013244 
                 propyl 4-(4-ethylphenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 32.20558607 
                 57.5873322 
               
               
                   
               
               
                 ST013247 
                 propyl 2-methyl-4-(4- methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.51944089 
                 54.95756561 
               
               
                   
               
               
                 ST013249 
                 phenylmethyl 4-(3-bromo-4- hydroxy-5-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 68.02004641 
               
               
                   
               
               
                 ST013251 
                 2-methoxyethyl 4-[4- (dimethylamino)phenyl]-2-methyl- 5-oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 89.42392095 
                 58.58382513 
               
               
                   
               
               
                 ST013253 
                 2-methoxyethyl 2-methyl-5-oxo-4- phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 50.23449452 
                 85.75401829 
               
               
                   
               
               
                 ST013254 
                 2-methoxyethyl 4-(4- hydroxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.6225516 
                 76.86398746 
               
               
                   
               
               
                 ST013256 
                 2-methoxyethyl 4-[4- (diethylamino)phenyl]-2-methyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.24795392 
                 92.76708236 
               
               
                   
               
               
                 ST013258 
                 cyclohexyl 2-methyl-4-naphthyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 47.04760492 
               
               
                   
               
               
                 ST013269 
                 cyclohexyl 4-(3,4-dichlorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 12.32832094 
                 1.354161377 
               
               
                   
               
               
                 ST013270 
                 cyclohexyl 4-(2,5- dimethoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 19.69762771 
                 34.97746754 
               
               
                   
               
               
                 ST013271 
                 cyclohexyl 2-methyl-5-oxo-4-[2- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 6.9200912 
                 39.85192766 
               
               
                   
               
               
                 ST013320 
                 cyclohexyl 4-(4-ethylphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.23152923 
                 71.76951132 
               
               
                   
               
               
                 ST013322 
                 propyl 2-methyl-4-[2- (methylethoxy)phenyl]-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.57423593 
                 99.72356879 
               
               
                   
               
               
                 ST013323 
                 methylethyl 4-(4-ethoxy-3- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.67309049 
                 80.07468721 
               
               
                   
               
               
                 ST013324 
                 butyl 4-(2-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.26551219 
                 93.68192572 
               
               
                   
               
               
                 ST013325 
                 butyl 2-methyl-5-oxo-4-(2- propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.46208132 
                 69.39399976 
               
               
                   
               
               
                 ST013328 
                 cyclopentyl 2,7,7-trimethyl-5-oxo- 4-(2,3,4-trimethoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.10840888 
                 93.41265594 
               
               
                   
               
               
                 ST013330 
                 butyl 4-(2-butoxyphenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.99196569 
                 86.50382876 
               
               
                   
               
               
                 ST013332 
                 methyl 7-(4-methoxyphenyl)-2- methyl-4-(4-methylphenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.08034309 
                 67.99192191 
               
               
                   
               
               
                 ST013333 
                 methyl 7-(4-methoxyphenyl)-2- methyl-4-(3-nitrophenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.38228109 
                 51.55865277 
               
               
                   
               
               
                 ST013339 
                 cyclohexyl 4-(2-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.6404104 
                 6.873410651 
               
               
                   
               
               
                 ST013341 
                 2-ethoxyethyl 4-(3,4- dimethoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 73.01313718 
                 73.85700316 
               
               
                   
               
               
                 ST013342 
                 2-ethoxyethyl 4-(3- hydroxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.74512784 
                 55.47322081 
               
               
                   
               
               
                 ST013343 
                 2-ethoxyethyl 4-(4-hydroxy-3- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.10146029 
                 82.95488429 
               
               
                   
               
               
                 ST013344 
                 2-ethoxyethyl 4-(4-ethylphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.38086966 
                 86.63976573 
               
               
                   
               
               
                 ST013345 
                 2-ethoxyethyl 2-methyl-5-oxo-4- (3,4,5-trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 58.35595245 
                 75.38303887 
               
               
                   
               
               
                 ST013346 
                 pentyl 2-methyl-5-oxo-4-(2,3,4- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 16.27626079 
                 77.73355052 
               
               
                   
               
               
                 ST013350 
                 cyclohexyl 4-(3,4-dichlorophenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.07464307 
                 95.56681419 
               
               
                   
               
               
                 ST013352 
                 cyclohexyl 4-(4-chlorophenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 22.38613539 
                 84.04915085 
               
               
                   
               
               
                 ST013356 
                 2-methoxyethyl 2,7,7-trimethyl-5- oxo-4-(3,4,5-trimethoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.71375061 
                 82.54446923 
               
               
                   
               
               
                 ST013357 
                 2-methoxyethyl 4-(3-bromo-4- hydroxy-5-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.39346398 
                 95.16316994 
               
               
                   
               
               
                 ST013365 
                 2-methoxyethyl 4-(2- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 84.53802725 
                 56.04978106 
               
               
                   
               
               
                 ST013387 
                 cyclohexyl 4-(4-hydroxy-3- methoxyphenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.97475707 
                 26.3587512 
               
               
                   
               
               
                 ST013389 
                 cyclohexyl 4-(4-ethylphenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.41382118 
                 94.35588142 
               
               
                   
               
               
                 ST013390 
                 phenylmethyl 4-(4-ethylphenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.36870962 
                 98.25117871 
               
               
                   
               
               
                 ST013410 
                 4-(4-chlorophenyl)-2,7,7-trimethyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 21.9857771 
                 26.03843995 
               
               
                   
               
               
                 ST013428 
                 butyl 4-(3-chlorophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.07464307 
                 40.90661104 
               
               
                   
               
               
                 ST013429 
                 cyclohexyl 4-(3-bromo-4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 31.93773411 
                 45.38628104 
               
               
                   
               
               
                 ST013435 
                 4-{3-[(2-ethoxyethyl)oxycarbonyl]- 2-methyl-5-oxo-4-1,4,6,7,8- pentahydroquinolyl}phenyl acetate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.72232778 
                 70.09399703 
               
               
                   
               
               
                 ST013438 
                 cyclohexyl 2-methyl-4-(4- methylphenyl)-5-oxo-7-phenyl- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 31.45594702 
                 93.54703042 
               
               
                   
               
               
                 ST013439 
                 methylethyl 4-(2,3-dichlorophenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 19.69762771 
                 80.34968613 
               
               
                   
               
               
                 ST014138 
                 2-amino-7,7-dimethyl-5-oxo-1- benzylspiro[1,4,6,7,8- pentahydroquinoline-4,4′-2′ H- 3′,4,5′,6′-tetrahydropyran]-3- carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.09261169 
                 65.31693236 
               
               
                   
               
               
                 ST014234 
                 [4-(2-amino-3-cyano-7,7-dimethyl- 5-oxo-1-phenyl-6,8-dihydro-4H- quinolin-4-yl)phenoxy]sodium 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 83.72509636 
                 63.62006398 
               
               
                   
               
               
                 ST014875 
                 methylethyl 4-[4- (diethylamino)phenyl]-2-methyl-5- oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.1884249 
                 95.73807992 
               
               
                   
               
               
                 ST014881 
                 phenylmethyl 2,7,7-trimethyl-5- oxo-4-[2-(trifluoromethyl)phenyl]- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 49.88766565 
               
               
                   
               
               
                 ST014882 
                 cyclohexyl 2-methyl-5-oxo-4-[2- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.46178615 
                 91.81548227 
               
               
                   
               
               
                 ST014884 
                 2-phenylethyl 4-(2,4- dichlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.97300589 
                 52.78225692 
               
               
                   
               
               
                 ST014885 
                 2-phenylethyl 4-(6-bromo(2H- benzo[d]1,3-dioxolen-5-yl))-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.46178615 
                 87.49242738 
               
               
                   
               
               
                 ST014886 
                 2-phenoxyethyl 4-(4-ethylphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 21.59695691 
                 65.06737638 
               
               
                   
               
               
                 ST014890 
                 2-phenoxyethyl 4-(4- bromophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.21343366 
                 67.45959598 
               
               
                   
               
               
                 ST014891 
                 2-phenoxyethyl 4-(4-fluorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.76095697 39.34284581 
               
               
                   
               
               
                 ST014899 
                 2-phenoxyethyl 2-methyl-5-oxo-4- [4-(phenylmethoxy)phenyl]- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.6115384 
                 65.46783361 
               
               
                   
               
               
                 ST014907 
                 2-phenylethyl 4-(2-butoxyphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.56680959 
                 83.50391768 
               
               
                   
               
               
                 ST014919 
                 2-phenoxyethyl 2-methyl-4-[2- (methylethoxy)phenyl]-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.42614992 
                 85.12900968 
               
               
                   
               
               
                 ST014923 
                 2-phenylethyl 2,7,7-trimethyl-4-(4- nitrophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 28.35824306 
               
               
                   
               
               
                 ST014957 
                 phenylmethyl 2-methyl-5-oxo-4-(2- propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 62.7831639 
               
               
                   
               
               
                 ST014958 
                 propyl 4-(2,3-dichlorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 18.22853234 
                 61.15530249 
               
               
                   
               
               
                 ST014959 
                 propyl 4-(3-hydroxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.0017351 
                 70.21959374 
               
               
                   
               
               
                 ST014969 
                 prop-2-enyl 2-methyl-5-oxo-4- (2,3,4-trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.6569846 
                 83.25356268 
               
               
                   
               
               
                 ST015031 
                 phenylmethyl 4-(4-ethylphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 33.05193614 
                 71.26310885 
               
               
                   
               
               
                 ST015043 
                 methylethyl 4-(3-ethoxy-4- hydroxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.93419977 
                 68.77783694 
               
               
                   
               
               
                 ST015048 
                 2-phenylethyl 2,7,7-trimethyl-5- oxo-4-(2-propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.87517309 
                 88.7314631 
               
               
                   
               
               
                 ST015049 
                 2-phenylethyl 2,7,7-trimethyl-4-[2- (methylethoxy)phenyl]-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 62.37716785 
               
               
                   
               
               
                 ST015054 
                 2-phenylethyl 2,7,7-trimethyl-5- oxo-4-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.87871002 
                 44.20316696 
               
               
                   
               
               
                 ST015055 
                 2-phenoxyethyl 2,7,7-trimethyl-5- oxo-4-(3-phenoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.61050401 
                 78.20602915 
               
               
                   
               
               
                 ST015060 
                 2-phenylethyl 2-methyl-5-oxo-4-(2- propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST015061 
                 2-phenylethyl 4-(3-bromo-5- ethoxy-4-hydroxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.81482841 
                 33.53150797 
               
               
                   
               
               
                 ST015062 
                 2-phenylethyl 4-(2,3- dichlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.57608569 
                 20.81712938 
               
               
                   
               
               
                 ST015067 
                 2-phenoxyethyl 4-(2,4- dichlorophenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 4.89497656 
                 43.89631592 
               
               
                   
               
               
                 ST015068 
                 ethyl 4-(2,3-dichlorophenyl)-7-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.32042577 
                 83.75427269 
               
               
                   
               
               
                 ST015070 
                 methyl 7-(2-chlorophenyl)-2- methyl-4-(3-nitrophenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.42818532 
                 96.95883751 
               
               
                   
               
               
                 ST015071 
                 2-phenoxyethyl 4-[3-methoxy-4- (phenylmethoxy)phenyl]-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.82552896 
                 88.32224232 
               
               
                   
               
               
                 ST015072 
                 2-phenoxyethyl 2-methyl-4-(4- methylthiophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 19.33402706 
                 59.38239758 
               
               
                   
               
               
                 ST015075 
                 2-phenoxyethyl 4-[4- (diethylamino)phenyl]-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.66666667 
                 42.20603587 
               
               
                   
               
               
                 ST015076 
                 2-phenylethyl 2-methyl-4-(4- methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 58.90912244 
                 98.56122264 
               
               
                   
               
               
                 ST015084 
                 2-phenylethyl 4-(3-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.46063129 
                 80.23086604 
               
               
                   
               
               
                 ST015085 
                 2-phenylethyl 4-(2-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.89594173 
                 72.88944673 
               
               
                   
               
               
                 ST015087 
                 2-phenylethyl 4-(4-ethoxyphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.27055151 
                 43.7042733 
               
               
                   
               
               
                 ST015090 
                 2-phenylethyl 4-(2,4- dimethoxyphenyl)-2,7,7-trimethyl- 5-oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 15.37807839 
                 34.94397117 
               
               
                   
               
               
                 ST015091 
                 2-phenoxyethyl 4-(3-chlorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.44536941 
                 75.84121477 
               
               
                   
               
               
                 ST015093 
                 2-phenoxyethyl 4-(4-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST015094 
                 2-phenylethyl 4-(4-hydroxy-3- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.26257371 
                 59.8054359 
               
               
                   
               
               
                 ST015095 
                 2-phenoxyethyl 2,7,7-trimethyl-4- (4-methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.7346514 
                 0 
               
               
                   
               
               
                 ST015096 
                 2-phenoxyethyl 4-(2-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.05931322 
                 79.96653694 
               
               
                   
               
               
                 ST015098 
                 2-phenylethyl 4-(3,4- dichlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.85848075 
                 0 
               
               
                   
               
               
                 ST015099 
                 2-phenylethyl 2,7,7-trimethyl-4-(4- methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 14.8491155 
                 33.8235064 
               
               
                   
               
               
                 ST015103 
                 2-phenoxyethyl 4-(2H-benzo[3,4- d]1,3-dioxolan-5-yl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.27055151 
                 73.49466536 
               
               
                   
               
               
                 ST015105 
                 2-phenoxyethyl 2,7,7-trimethyl-5- oxo-4-(2-propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 52.9778009 
                 99.75042416 
               
               
                   
               
               
                 ST015106 
                 2-phenylethyl 4-(4-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.2049948 
                 0 
               
               
                   
               
               
                 ST015108 
                 2-phenoxyethyl 4-(2- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 32.95178633 
                 92.11729282 
               
               
                   
               
               
                 ST015110 
                 2-phenylethyl 4-(2- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.79916753 
                 90.13454519 
               
               
                   
               
               
                 ST015159 
                 cyclohexyl 4-(3-chlorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 2.977800902 
                 0 
               
               
                   
               
               
                 ST015174 
                 pentyl 4-(2-ethoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 17.16441207 
                 0 
               
               
                   
               
               
                 ST015176 
                 methyl 7-(2-chlorophenyl)-2- methyl-4-(4-nitrophenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 17.41068332 
                 76.41122678 
               
               
                   
               
               
                 ST015182 
                 methyl 4-[4-(diethylamino)phenyl]- 7-(2-chlorophenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.86992716 
                 61.44841168 
               
               
                   
               
               
                 ST015214 
                 methyl 7-(4-chlorophenyl)-2- methyl-4-(4-methylphenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.69025321 
                 66.69363978 
               
               
                   
               
               
                 ST015215 
                 methyl 4-(3,4-dichlorophenyl)-7-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.14429414 
                 39.7605726 
               
               
                   
               
               
                 ST015216 
                 methyl 7-(4-chlorophenyl)-4-(2- fluorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.3593479 
                 93.19472728 
               
               
                   
               
               
                 ST015218 
                 methyl 7-(4-chlorophenyl)-2- methyl-5-oxo-4-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.32362123 
                 0 
               
               
                   
               
               
                 ST015219 
                 2-methoxyethyl 4-(3- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 83.70620881 
                 45.79375848 
               
               
                   
               
               
                 ST015234 
                 2-phenylethyl 4-(2-bromophenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.81408255 
                 54.83794894 
               
               
                   
               
               
                 ST015254 
                 ethyl 4-(2,5-dimethoxyphenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.87304891 
                 33.8235064 
               
               
                   
               
               
                 ST015255 
                 2-phenylethyl 2-methyl-4-(4- nitrophenyl)-5-oxo-7-phenyl- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.52896289 
                 74.68219037 
               
               
                   
               
               
                 ST015256 
                 ethyl 4-(2-fluorophenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.7693375 
                 75.84121477 
               
               
                   
               
               
                 ST016953 
                 methyl 7-(4-chlorophenyl)-2- methyl-5-oxo-4-[4- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.91432536 
                 69.73817449 
               
               
                   
               
               
                 ST016959 
                 (4-methoxyphenyl)methyl 4-(3- fluorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.83801596 
                 57.18729253 
               
               
                   
               
               
                 ST016960 
                 2-methoxyethyl 4-(4- bromophenyl)-7-(4-chlorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.52098508 
                 76.41122678 
               
               
                   
               
               
                 ST016961 
                 methylethyl 7-(4-methoxyphenyl)- 2-methyl-5-oxo-4-[4- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 41.83489421 
                 89.46114865 
               
               
                   
               
               
                 ST016962 
                 methyl 4-(2-bromophenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.36593826 
                 28.45868754 
               
               
                   
               
               
                 ST016964 
                 (4-methoxyphenyl)methyl 4-(3- ethoxy-4-hydroxyphenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 36.42611897 
                 40.04974668 
               
               
                   
               
               
                 ST016969 
                 2-methylpropyl 4-(3-chlorophenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.25476324 
                 60.19647081 
               
               
                   
               
               
                 ST016970 
                 2-methylpropyl 4-(4-ethylphenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.67223813 
                 27.78307022 
               
               
                   
               
               
                 ST016971 
                 2-methoxyethyl 7-(4- chlorophenyl)-2-methyl-4-(4- nitrophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.27539181 
                 86.20182491 
               
               
                   
               
               
                 ST016974 
                 methyl 4-(4-ethoxyphenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.63449508 
                 57.35636803 
               
               
                   
               
               
                 ST016978 
                 2-methylpropyl 4-(2H-benzo[3,4- d]1,3-dioxolen-5-yl)-2-methyl-5- oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.93600834 
                 99.50423316 
               
               
                   
               
               
                 ST016979 
                 (4-methoxyphenyl)methyl 4-(3- methoxy-4-propoxyphenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 53.71335879 
                 90.10594628 
               
               
                   
               
               
                 ST016983 
                 (4-methoxyphenyl)methyl 4-(4- ethylphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.56489887 
                 72.60730112 
               
               
                   
               
               
                 ST016984 
                 2-methylpropyl 2-methyl-5-oxo-7- phenyl-4-(2-propoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.36373702 
                 56.15200343 
               
               
                   
               
               
                 ST016990 
                 methyl 7-(4-methoxyphenyl)-2- methyl-5-oxo-4-(4-propoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.30077198 
                 22.04955492 
               
               
                   
               
               
                 ST016999 
                 methyl 4-(2,3-dimethoxyphenyl)-7- (4-methoxyphenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 67.25265727 
                 82.83569657 
               
               
                   
               
               
                 ST017011 
                 methylethyl 4-(4-ethoxyphenyl)-7- (4-methoxyphenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.72432595 
                 74.04122392 
               
               
                   
               
               
                 ST017025 
                 (4-methoxyphenyl)methyl 4-(4- hydroxy-3-methoxyphenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.10402677 
                 32.17785865 
               
               
                   
               
               
                 ST017026 
                 2-methylpropyl 7-(4-chlorophenyl)- 2-methyl-5-oxo-4-(2- propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.58672465 
                 80.58036883 
               
               
                   
               
               
                 ST017027 
                 2-methoxyethyl 2-methyl-4-(4- nitrophenyl)-5-oxo-7-phenyl- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.05227702 
                 82.13179062 
               
               
                   
               
               
                 ST017038 
                 2-methyipropyl 7-(4-chlorophenyl)- 4-(2-ethoxyphenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.71052705 
                 81.85001064 
               
               
                   
               
               
                 ST017045 
                 4-(2-bromo-4,5-dimethoxyphenyl)- 7-(4-chlorophenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.55374251 
                 45.98126952 
               
               
                   
               
               
                 ST017050 
                 cyclohexyl 4-(3-chloro-4-hydroxy- 5-methoxyphenyl)-2-methyl-5-oxo- 7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.64973931 
                 22.24049078 
               
               
                   
               
               
                 ST017054 
                 (4-methoxyphenyl)methyl 2,7,7- trimethyl-4-(6-nitro(2H- benzo[d]1,3-dioxolan-5-yl))-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.5375585 
                 9.539176868 
               
               
                   
               
               
                 ST017060 
                 2-methoxyethyl4-(3-bromo-5- ethoxy-4-hydroxyphenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.96351619 
                 61.68043948 
               
               
                   
               
               
                 ST017066 
                 methylethyl 4-(4-fluorophenyl)-7- (4-methoxyphenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.86267784 
                 57.35636803 
               
               
                   
               
               
                 ST017070 
                 2-methylpropyl 4,7-bis(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.42134154 
                 89.11011598 
               
               
                   
               
               
                 ST017078 
                 ethyl 7-(4-methoxyphenyl)-2- methyl-5-oxo-4-[4- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.81160551 
                 49.37881673 
               
               
                   
               
               
                 ST017084 
                 2-phenoxyethyl 2-methyl-5-oxo-7- phenyl-4-(4-pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.26688983 
                 84.68712533 
               
               
                   
               
               
                 ST017089 
                 methylpropyl 4,7-bis(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.87153374 
                 82.52158164 
               
               
                   
               
               
                 ST017091 
                 methylpropyl 7-(4-chlorophenyl)-2- methyl-5-oxo-4-(3,4,5- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.65736656 
                 91.03019648 
               
               
                   
               
               
                 ST017092 
                 methylpropyl 4-(4-ethylphenyl)-7- (4-methoxyphenyl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 41.34196678 
                 30.88880794 
               
               
                   
               
               
                 ST017093 
                 methylpropyl 7-(4-chlorophenyl)-2- methyl-5-oxo-4-(4-propoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.78699593 
                 94.96982242 
               
               
                   
               
               
                 ST017094 
                 2-methoxyethyl 4-(2H-benzo[3,4- d]1,3-dioxolen-5-yl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.89519298 
                 73.76168695 
               
               
                   
               
               
                 ST017095 
                 methylpropyl 4-(3,4- dichlorophenyl)-7-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.27785421 
                 37.14055748 
               
               
                   
               
               
                 ST017097 
                 2-methoxyethyl 4-(3- methoxyphenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.17903292 
                 80.92025428 
               
               
                   
               
               
                 ST017099 
                 2-methoxyethyl 4-(4- bromophenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 84.49922696 
                 56.98584879 
               
               
                   
               
               
                 ST017106 
                 methyl 4-{3-[(2- ethylthioethyl)oxycarbonyl]-2- methyl-5-oxo-4-1,4,6,7,8- pentahydroquinolyl}benzoate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 36.83309457 
                 0 
               
               
                   
               
               
                 ST017113 
                 2-ethylthioethyl 4-[4-(2- hydroxyethoxy)-3-methoxyphenyl]- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 82.57372236 
                 74.11068674 
               
               
                   
               
               
                 ST017116 
                 2-ethylthioethyl 4-(3-methoxy-4- propoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.53427611 
                 43.00724393 
               
               
                   
               
               
                 ST017117 
                 2-methylpropyl 7-(4-chlorophenyl)- 4-(3-ethoxy-4-hydroxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.71963518 
                 81.72120879 
               
               
                   
               
               
                 ST017133 
                 phenylmethyl 4-(2H-benzo[3,4- d]1,3-dioxolen-5-yl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.21220976 
                 79.19910365 
               
               
                   
               
               
                 ST017136 
                 ethyl 4,7-bis(4-methoxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 87.67237344 
                 66.10346826 
               
               
                   
               
               
                 ST017144 
                 ethyl 4-(3-chlorophenyl)-7-(4- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.42051886 
                 55.61544295 
               
               
                   
               
               
                 ST017167 
                 butyl 4-(4-bromophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 79.03484317 
                 50.53395172 
               
               
                   
               
               
                 ST017170 
                 cyclohexyl 4-(4-bromophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 3.468382474 
                 1.380068974 
               
               
                   
               
               
                 ST017171 
                 cyclopentyl 2-methyl-5-oxo-4-(2- thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.5408814 
                 63.41479367 
               
               
                   
               
               
                 ST017175 
                 butyl 4-(4-chlorophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.76125573 
                 34.51599477 
               
               
                   
               
               
                 ST017176 
                 cyclopentyl 4-(2-methoxyphenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.20809985 
                 49.78415983 
               
               
                   
               
               
                 ST017183 
                 propyl 4-(3,4-dichlorophenyl)-7-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 50.10659331 
                 67.88024735 
               
               
                   
               
               
                 ST017199 
                 2-ethylthioethyl 4-(2- bromophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 47.8978375 
                 99.98691878 
               
               
                   
               
               
                 ST017201 
                 2-ethylthioethyl 4-(4- bromophenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.45410609 
                 85.21108336 
               
               
                   
               
               
                 ST017212 
                 methylethyl 2-methyl-5-oxo-4,7- diphenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.4069575 
                 57.14591509 
               
               
                   
               
               
                 ST017213 
                 methylethyl 4-(4-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 44.3672627 
                 91.43833987 
               
               
                   
               
               
                 ST017220 
                 methylethyl 4-(2-methoxyphenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.94615877 
                 99.5938875 
               
               
                   
               
               
                 ST017226 
                 propyl 4-(2,4-dimethoxyphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.5578961 
                 26.46509692 
               
               
                   
               
               
                 ST017228 
                 phenylmethyl 4-(3-ethoxy-4- hydroxyphenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.63601709 
                 60.15875847 
               
               
                   
               
               
                 ST017229 
                 methylethyl 4-(2,4- dimethoxyphenyl)-2-methyl-5-oxo- 7-phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.05280778 
                 98.67522892 
               
               
                   
               
               
                 ST017230 
                 4-{2-methyl-5-oxo-7-phenyl-3-[(2- phenoxyethyl)oxycarbonyl]-4- 1,4,6,7,8- pentahydroquinolyl}phenyl acetate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.12491375 
                 84.67891545 
               
               
                   
               
               
                 ST017233 
                 phenylmethyl 2-methyl-5-oxo-4-(2- thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.89928247 
                 27.40397193 
               
               
                   
               
               
                 ST017236 
                 methylpropyl 7-(4- methoxyphenyl)-2-methyl-4-(6- nitro(2H-benzo[d]1,3-dioxolan-5- yl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.98461891 
                 98.06922004 
               
               
                   
               
               
                 ST017242 
                 oxolan-2-ylmethyl 4-(3- chlorophenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.55527527 
                 0 
               
               
                   
               
               
                 ST017243 
                 2-ethylthioethyl 7-(4- chlorophenyl)-4-(3-ethoxy-4- hydroxyphenyl)-2-methyl-5-ox o- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.61170535 
                 15.61606433 
               
               
                   
               
               
                 ST017244 
                 phenylmethyl 7-(4- methoxyphenyl)-2-methyl-5-oxo-4- (3,4,5-trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.41671444 
                 24.37973506 
               
               
                   
               
               
                 ST017249 
                 propyl 2,7,7-trimethyl-5-oxo-4-(4- pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.9793936 
                 75.13869511 
               
               
                   
               
               
                 ST017250 
                 propyl 2-methyl-5-oxo-4-(3- pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.45419253 
                 49.21913677 
               
               
                   
               
               
                 ST017251 
                 ethyl 2-methyl-5-oxo-7-phenyl-4- (2-pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 90.43637078 
                 34.33817904 
               
               
                   
               
               
                 ST017252 
                 2-methoxyethyl 2,7,7-trimethyl-5- oxo-4-(3-pyridyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 89.56698717 
                 70.50722355 
               
               
                   
               
               
                 ST017259 
                 propyl 4-(4-bromophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.46995037 
                 86.97001065 
               
               
                   
               
               
                 ST017262 
                 propyl 2,7,7-trimethyl-5-oxo-4- phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.11933037 
                 85.99906987 
               
               
                   
               
               
                 ST017264 
                 propyl 4-(4-ethylphenyl)-2-methyl- 5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.71383643 
                 48.22359242 
               
               
                   
               
               
                 ST017266 
                 phenylmethyl 7-(4- methoxyphenyl)-2-methyl-5-oxo-4- (4-pyridyl)-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.50598699 
                 64.58856534 
               
               
                   
               
               
                 ST017293 
                 propyl 4-(2,4-dichlorophenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.71634261 
                 95.21340594 
               
               
                   
               
               
                 ST017304 
                 cyclohexyl 4-(2-ethoxyphenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.96645318 
                 57.24530057 
               
               
                   
               
               
                 ST017312 
                 2-ethoxyethyl 4-(2-fluorophenyl)-2- methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 15.34382218 
                 71.23632927 
               
               
                   
               
               
                 ST017313 
                 2-ethoxyethyl 4-(4-bromophenyl)- 2-methyl-5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 44.23209225 
                 85.4427892 
               
               
                   
               
               
                 ST017315 
                 2-phenoxyethyl 4-(3- hydroxyphenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.82586119 
                 53.92921974 
               
               
                   
               
               
                 ST017319 
                 methylpropyl 4-(3,4- dichlorophenyl)-2-methyl-5-oxo-7- phenyl-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.79773624 
                 97.52674138 
               
               
                   
               
               
                 ST017324 
                 methylethyl 4-(2,3- dimethoxyphenyl)-7-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.21651789 
                 99.21799131 
               
               
                   
               
               
                 ST017331 
                 methylethyl 7-(4-chlorophenyl)-2- methyl-5-oxo-4-(3-pyridyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 1.107133987 
                 0 
               
               
                   
               
               
                 ST017336 
                 pentyl 4-(3-hydroxyphenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.87916198 
                 72.74895647 
               
               
                   
               
               
                 ST017342 
                 2-methylpropyl 2-methyl-5-oxo-4- [4-(phenylmethoxy)phenyl]- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.80345377 
                 93.48894 
               
               
                   
               
               
                 ST018638 
                 4-(2,5-dimethoxyphenyl)-2-methyl- 5-oxo-7-phenyl-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.37496165 
                 53.78765937 
               
               
                   
               
               
                 ST018645 
                 (4-methoxyphenyl)methyl 4-(4- bromophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 7.025874034 
                 18.01175569 
               
               
                   
               
               
                 ST018648 
                 (4-methoxyphenyl)methyl 4-(4- chlorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 7.486522419 
                 10.98560354 
               
               
                   
               
               
                 ST020008 
                 ethyl 4-(2,4-dichlorophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.71899426 
                 95.6946929 
               
               
                   
               
               
                 ST020910 
                 ethyl 4-(4-bromo-5-methyl(2- thienyl))-2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 47.34597572 
                 69.8003805 
               
               
                   
               
               
                 ST024431 
                 butyl 4-(4-chlorophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST024440 
                 ethyl 4-(4-chlorophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.06565518 
                 97.73536632 
               
               
                   
               
               
                 ST024444 
                 ethyl 4-(2,4-dichlorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.43806116 
                 16.59578882 
               
               
                   
               
               
                 ST024487 
                 cycloheptyl 4-(3-bromophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 5.065882814 
                 3.7720845 
               
               
                   
               
               
                 ST024504 
                 cycloheptyl 2,7,7-trimethyl-5-oxo- 4-(2,3,4-trimethoxyphenyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0.415307894 
                 0 
               
               
                   
               
               
                 ST024574 
                 methyl 7-(3,4-dimethoxyphenyl)-2- methyl-5-oxo-4-(3,4,5- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.26567529 
                 83.64969056 
               
               
                   
               
               
                 ST028547 
                 methyl 4-(4-bromophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 72.08053638 
                 45.31341839 
               
               
                   
               
               
                 ST028591 
                 ethyl 4-{4-[(2- chlorophenyl)methoxy]-3- methoxyphenyl}-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 98.28146176 
                 69.5640148 
               
               
                   
               
               
                 ST028592 
                 methyl 4-{4-[(3- chlorophenyl)methoxy]-3- methoxyphenyl}-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.31808795 
                 97.06716982 
               
               
                   
               
               
                 ST028595 
                 methyl 4-{4-[(4- chlorophenyl)methoxy]-3- methoxyphenyl}-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.41174592 
                 98.90009509 
               
               
                   
               
               
                 ST028598 
                 ethyl 4-{4-[(4- chlorophenyl)methoxy]-3- methoxyphenyl}-2-methyl-5-oxo- 1,4,6,7,8 -pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.41755785 
                 71.56195482 
               
               
                   
               
               
                 ST028606 
                 ethyl 4-{3-methoxy-4-[(4- methylphenyl)methoxy]phenyl}-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.21851161 
                 51.9808022 
               
               
                   
               
               
                 ST028607 
                 methyl 4-(3-methoxy-4-{[3- (trifluoromethyl)phenyl]methoxy} phenyl)-2,7,7-trimethyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.78243931 
                 63.29282628 
               
               
                   
               
               
                 ST040993 
                 2-amino-1-(4-fluorophenyl)-5-oxo- 7-phenyl-4-(3-thienyl)-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.71884708 
                 46.89023024 
               
               
                   
               
               
                 ST041668 
                 5-(4-fluorophenyl)-4,8-dioxo- 1,2,3,5,7,9,10,11,12,13,15- undecahydrocyclohepta[1,2- b]quinolino[1′,2′- 2,1]pyrimidino[5,6-d]thiophene-6- carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 88.72375581 
                 27.87197958 
               
               
                   
               
               
                 ST045143 
                 methyl 4-(4-bromo-2,5- dimethoxyphenyl)-2-methyl-5-oxo- 7-(2-thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 22.85871287 
                 16.01058456 
               
               
                   
               
               
                 ST046868 
                 2-amino-4-(5-bromo(2-thienyl))-1- [2-chloro-5- (trifluoromethyl)phenyl]-7,7- dimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.77636602 
                 84.03754489 
               
               
                   
               
               
                 ST047623 
                 2-amino-4-(4-chlorophenyl)-7,7- dimethyl-5-oxo-1-benzyl-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.44262887 
                 44.40610034 
               
               
                   
               
               
                 ST050407 
                 N-(4-bromophenyl)-2-[4-(2- chlorophenyl)-3-cyano-5-oxo(2- 1,4,6,7,8- pentahydroquinolylthio)]acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.71913217 
                 44.28752729 
               
               
                   
               
               
                 ST051161 
                 N-(3-chloro-2-methylphenyl)-2-(3- cyano-7,7-dimethyl-5-oxo-4-(2- thienyl)(2-1,4,6,7,8- pentahydroquinolylthio))acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 12.98647518 
                 25.37366361 
               
               
                   
               
               
                 ST051557 
                 cyclopentyl 2-methyl-5-oxo-7-(2- thienyl)-4-(2,4,5- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.31234626 
                 93.1349412 
               
               
                   
               
               
                 ST051566 
                 2-methylpropyl 4-(2-fluorophenyl)- 2-methyl-5-oxo-7-(2-thienyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.386505 
                 96.06415423 
               
               
                   
               
               
                 ST051567 
                 cyclopentyl 2-methyl-4-(5- methyl(2-furyl))-5-oxo-7-(2- thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.41444083 
                 84.9935221 
               
               
                   
               
               
                 ST051570 
                 2-ethylthioethyl 4-(3- chlorophenyl)-2-methyl-5-oxo-7- (2-thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 31.74108215 
                 93.76903374 
               
               
                   
               
               
                 ST051571 
                 cyclopentyl 2-methyl-5-oxo-7-(2- thienyl)-4-(2,3,4- trimethoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.40342551 
                 62.05920904 
               
               
                   
               
               
                 ST051818 
                 oxolan-2-ylmethyl 4-(3- chlorophenyl)-2-methyl-5-oxo-7- (2-thienyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.02511988 
                 72.9336363 
               
               
                   
               
               
                 ST051958 
                 2-amino-1-(2-chlorophenyl)-4-(3- hydroxy-4-methoxyphenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.63072196 
                 80.22743306 
               
               
                   
               
               
                 ST051960 
                 2-amino-1-(2,6-difluorophenyl)-5- oxo-4-(3-thienyl)-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.77920508 
                 86.27816587 
               
               
                   
               
               
                 ST052026 
                 2-amino-4-[5-(tert-butyl)(2- thienyl)]-1-(4-bromophenyl)-7,7- dimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.47181156 
                 25.25628719 
               
               
                   
               
               
                 ST052048 
                 2-amino-4-(2,4-dichlorophenyl)-1- (4-bromo-2-fluorophenyl)-7,7- dimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 58.87022635 
                 33.02478711 
               
               
                   
               
               
                 ST052173 
                 cyclopentyl 4-(9-ethylcarbazol-3- yl)-2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.69964635 
                 32.49464416 
               
               
                   
               
               
                 ST052207 
                 oxolan-2-ylmethyl 4-(9- ethylcarbazol-3-yl)-2-methyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 52.33723425 
                 59.6367503 
               
               
                   
               
               
                 ST052219 
                 2-phenoxyethyl 4-(2- bromophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 14.02589013 
                 24.66723947 
               
               
                   
               
               
                 ST052221 
                 2-phenylethyl 4-(3-bromophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.4228721 
                 46.11550641 
               
               
                   
               
               
                 ST052224 
                 oxolan-2-ylmethyl 4-(5-bromo-2- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 76.93285628 
                 68.09608191 
               
               
                   
               
               
                 ST052225 
                 2-phenylethyl 4-(2-fluorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.71751104 
                 29.68237443 
               
               
                   
               
               
                 ST052228 
                 2-phenylethyl 2-methyl-5-oxo-4-[2- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.3610207 
                 36.85619602 
               
               
                   
               
               
                 ST052231 
                 2-phenylethyl 4-[4- (dimethylamino)phenyl]-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.78591365 
                 63.51753527 
               
               
                   
               
               
                 ST052247 
                 2-phenoxyethyl 2-methyl-4-[4- (methylethyl)phenyl]-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 97.96630805 
                 64.11567858 
               
               
                   
               
               
                 ST052262 
                 cyclopentyl 2-methyl-4-(5- methyl(2-thienyl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.20949446 
                 19.65801715 
               
               
                   
               
               
                 ST052267 
                 cyclopentyl 4-(3,4-difluorophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 50.68946733 
                 52.83315426 
               
               
                   
               
               
                 ST052271 
                 (4-methoxyphenyl)methyl 2- methyl-5-oxo-4-[2- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.80335494 
                 23.93528692 
               
               
                   
               
               
                 ST052272 
                 2-(methylethoxy)ethyl 2,7,7- trimethyl-4-(4-nitrophenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.83638636 
                 29.2186425 
               
               
                   
               
               
                 ST052280 
                 2-phenoxyethyl 2-methyl-4-(5- methyl(2-thienyl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 73.5680602 
                 37.71978644 
               
               
                   
               
               
                 ST052292 
                 [4-(4-chlorophenyl)-2-methyl-5- oxo(3-1,4,6,7,8- pentahydroquinolyl)]-N-(2- methoxyphenyl)carboxamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 85.75817374 
                 68.19182074 
               
               
                   
               
               
                 ST052308 
                 methyl 2-methyl-4-(5-methyl(2- thienyl))-5-oxo-7-(2-thienyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.43761682 
                 74.20625461 
               
               
                   
               
               
                 ST052313 
                 2-methoxyethyl 2,7,7-trimethyl-4- [4-(methylethyl)phenyl]-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.29321855 
                 23.35997928 
               
               
                   
               
               
                 ST052320 
                 2-phenylethyl 2-methyl-5-oxo-4-[4- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 9.443192378 
                 0 
               
               
                   
               
               
                 ST052323 
                 phenylmethyl 2-methyl-5-oxo-4-[4- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 4.907047414 
                 0 
               
               
                   
               
               
                 ST052325 
                 cyclohexyl 4-(3-hydroxy-4- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 41.72492336 
                 32.95713848 
               
               
                   
               
               
                 ST052330 
                 2-phenoxyethyl 2-methyl-4-(6- methyl-4-oxochromen-3-yl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.56005469 
                 15.51604302 
               
               
                   
               
               
                 ST052342 
                 2-ethylthioethyl 2,7,7-trimethyl-4- (2-methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.73300364 
                 9.883006394 
               
               
                   
               
               
                 ST052344 
                 2-phenylethyl 2,7,7-trimethyl-4-(5- methyl(2-thienyl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.06700277 
                 24.39135774 
               
               
                   
               
               
                 ST052345 
                 2-methylpropyl 4-(3,4- difluorophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentanydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.63551157 
                 7.814628893 
               
               
                   
               
               
                 ST052347 
                 methyl 2-methyl-5-oxo-4-[3- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.15903143 
                 64.31361292 
               
               
                   
               
               
                 ST052351 
                 2-methylpropyl 4-(2-chloro-5- nitrophenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 19.30975829 
                 20.27266892 
               
               
                   
               
               
                 ST052354 
                 (4-methoxyphenyl)methyl 2- methyl-4-(3-methylphenyl)-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.14929558 
                 57.23929616 
               
               
                   
               
               
                 ST052357 
                 (4-methoxyphenyl)methyl 4-(4- chloro-3-nitrophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 13.28519701 
                 23.35997928 
               
               
                   
               
               
                 ST052359 
                 methyl 2,7,7-trimethyl-5-oxo-4-[4- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.96795125 
                 29.53660736 
               
               
                   
               
               
                 ST052360 
                 methyl 2,7,7-trimethyl-5-oxo-4-[3- (phenylmethoxy)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.67061513 
                 61.6422263 
               
               
                   
               
               
                 ST052361 
                 methyl 4-(4-chloro-3-nitrophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 84.08150241 
                 63.23164915 
               
               
                   
               
               
                 ST052362 
                 (4-methoxyphenyl)methyl 2- methyl-5-oxo-4-[4- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 7.114037149 
                 0 
               
               
                   
               
               
                 ST052364 
                 propyl 4-(5-bromo-2- methoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.01642774 
                 13.49721803 
               
               
                   
               
               
                 ST052365 
                 2-methylpropyl 2-methyl-4- naphthyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.11246646 
                 72.76954338 
               
               
                   
               
               
                 ST052368 
                 methyl 4-(2,5-difluorophenyl)-2- methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.34915709 
                 74.15741075 
               
               
                   
               
               
                 ST052370 
                 2-ethoxyethyl 2-methyl-5-oxo-4-(4- oxochromen-3-yl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.59445701 
                 69.66595611 
               
               
                   
               
               
                 ST052371 
                 (4-methoxyphenyl)methyl 2- methyl-5-oxo-4-(2-thienyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.75365895 
                 92.5233839 
               
               
                   
               
               
                 ST052373 
                 2-phenylethyl 4-(2,5- dimethoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.43108557 
                 37.44000798 
               
               
                   
               
               
                 ST052381 
                 2-phenoxyethyl 4-(2- ethoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.11735174 
                 61.9981966 
               
               
                   
               
               
                 ST052389 
                 methyl 4-(2,5-dimethoxyphenyl)-2- methyl-5-oxo-7-(2-thienyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 78.29681056 
                 44.92036384 
               
               
                   
               
               
                 ST052392 
                 2-phenoxyethyl 2,7,7-trimethyl-4- (6-methyl-4-oxochromen-3-yl)-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.07507108 
                 11.87540774 
               
               
                   
               
               
                 ST052393 
                 methyl 2-methyl-5-oxo-7-(2- thienyl)-4-[3- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.24523485 
                 48.179359 
               
               
                   
               
               
                 ST052398 
                 2-phenylethyl 2,7,7-trimethyl-4-(5- methyl(2-furyl))-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 44.28019761 
                 55.55832575 
               
               
                   
               
               
                 ST052408 
                 phenylmethyl 4-(2-bromophenyl)- 2-methyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.99228166 
                 63.43883619 
               
               
                   
               
               
                 ST052414 
                 methyl 4-(3,4-dichlorophenyl)-2- methyl-5-oxo-7-(2-thienyl)- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.15989769 
                 66.92471027 
               
               
                   
               
               
                 ST052422 
                 2-phenoxyethyl 4-(3-hydroxy-4- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8-pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.34653926 
                 44.8314406 
               
               
                   
               
               
                 ST052437 
                 2-propoxyethyl 4-(4-bromophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 5.308983702 
                 16.47157573 
               
               
                   
               
               
                 ST052446 
                 2-propoxyethyl 4-(3,4- dichlorophenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 58.11351259 
                 45.18796461 
               
               
                   
               
               
                 ST052454 
                 2-propoxyethyl 4-(2-chlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.59167479 
                 33.17510998 
               
               
                   
               
               
                 ST052457 
                 2-ethylthioethyl 2,7,7-trimethyl-4- (3-methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.1018675 
                 63.89802834 
               
               
                   
               
               
                 ST052462 
                 2-methoxyethyl 4-(2-bromo-4,5- dimethoxyphenyl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.83051252 
                 94.27942282 
               
               
                   
               
               
                 ST052468 
                 phenylmethyl 4-(6-chloro-4- oxochromen-3-yl)-2-methyl-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.93110718 
                 31.931645 
               
               
                   
               
               
                 ST052493 
                 methyl 2-methyl-5-oxo-7-(2- thienyl)-4-[4- (trifluoromethyl)phenyl]-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.85078857 
                 57.11442672 
               
               
                   
               
               
                 ST056056 
                 butyl 4-(3-iodophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 6.563115292 
                 12.30239302 
               
               
                   
               
               
                 ST211289 
                 ethyl 4-(4-bromophenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 89.12708458 
                 63.58389823 
               
               
                   
               
               
                 ST212479 
                 ethyl 2-methyl-4-(6-nitro(2H- benzo[d]1,3-dioxolan-5-yl))-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.24790334 
                 29.26397197 
               
               
                   
               
               
                 ST213781 
                 ethyl 4-(4-ethoxyphenyl)-2-methyl- 5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.83271428 
                 81.30884997 
               
               
                   
               
               
                 ST215419 
                 butyl 4-(3,4-dichlorophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST215449 
                 methylethyl 4-(3-bromo-4- methoxyphenyl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.51134321 
                 25.74257426 
               
               
                   
               
               
                 ST215464 
                 butyl 2,7,7-trimethyl-4-(2- nitrophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.6959546 
                 90.72035885 
               
               
                   
               
               
                 ST216053 
                 butyl 2,7,7-trimethyl-4-(6-nitro(2H- benzo[d]1,3-dioxolen-5-yl))-5-oxo- 1,4,6,7,8-pentahydroquinoline-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 22.16999362 
                 6.37350288 
               
               
                   
               
               
                 ST216061 
                 pentyl 4-(3,4-dichlorophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST216079 
                 pentyl 4-(2-bromophenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.79796228 
                 20.45245061 
               
               
                   
               
               
                 ST216093 
                 pentyl 2,7,7-trimethyl-4-(4- nitrophenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0 
                 0 
               
               
                   
               
               
                 ST216568 
                 pentyl 4-(6-bromo(2H-benzo[d]1,3- dioxolan-5-yl))-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 14.78651761 
                 24.71178625 
               
               
                   
               
               
                 ST216581 
                 pentyl 4-(2H-benzo[3,4-d]1,3- dioxolan-5-yl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 28.62736478 
                 41.64007119 
               
               
                   
               
               
                 ST216602 
                 pentyl 2,7,7-trimethyl-4-(4- methylphenyl)-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 2.651500512 
                 5.008345397 
               
               
                   
               
               
                 ST216606 
                 pentyl 4-(4-methoxyphenyl)-2,7,7- trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 1.398215424 
                 9.561084708 
               
               
                   
               
               
                 ST216854 
                 phenylmethyl 4-(2-bromophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.44984444 
                 60.00769493 
               
               
                   
               
               
                 ST216858 
                 phenylmethyl 4-(2-iodophenyl)- 2,7,7-trimethyl-5-oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.07449419 
                 61.52564376 
               
               
                   
               
               
                 ST216875 
                 methyl 2,7,7-trimethyl-5-oxo-4-(4- phenylphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 14.18179578 
                 32.99019866 
               
               
                   
               
               
                 ST216920 
                 cyclohexyl 4-(2H-benzo[3,4-d]1,3- dioxolen-5-yl)-2,7,7-trimethyl-5- oxo-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 1.398215424 
                 3.822551671 
               
               
                   
               
               
                 ST217244 
                 pentyl 2,7,7-trimethyl-5-oxo-4-(4- propoxyphenyl)-1,4,6,7,8- pentahydroquinoline-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.92584398 
                 41.48949421 
               
               
                   
               
               
                 ST024318 
                 3,3-dimethyl-5-(2-methylphenyl)- 11-phenyl-2,3,4,5,11- pentahydroindeno[3,2-b]quinoline- 1,10-dione 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.94486384 
                 99.52632853 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 2 
               
               
                   
               
             
            
               
                 Dihydropyridine Compounds 
               
            
           
           
               
               
               
               
               
            
               
                   
                   
                   
                 Aβ1-40 
                 Aβ1-42 
               
               
                   
                   
                   
                 (% of 
                 (% of 
               
               
                 ID 
                 IUPAC Name 
                 Structure 
                 control) 
                 control) 
               
               
                   
               
               
                 ST003359 
                 5-amino-7-(2-methylphenyl)-2-[(2- methylphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.16135647 
                 98.22334844 
               
               
                   
               
               
                 ST003360 
                 5-amino-7-(2,4-dichlorophenyl)-2- [(2,4-dichlorophenyl)methylene]-3- oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.36955577 
                 72.55108602 
               
               
                   
               
               
                 ST003361 
                 5-amino-7-(1-methylpyrrol-2-yl)-2- [(1-methylpyrrol-2-yl)methylene]- 3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 43.90448665 
                 90.24380022 
               
               
                   
               
               
                 ST003836 
                 ethyl 5-(ethoxycarbonyl)-2,6- dimethyl-4-[3-(2,2,2- trifluoroacetylamino)phenyl]-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.33858962 
                 83.98396812 
               
               
                   
               
               
                 ST006952 
                 5-amino-7-(3-methyl(2-thienyl))-2- [(3-methyl(2-thienyl))methylene]- 3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.23610569 
                 77.09937943 
               
               
                   
               
               
                 ST006953 
                 5-amino-7-(2-chlorophenyl)-2-[(2- chlorophenyl)methylene[-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 47.74097379 
                 83.98396812 
               
               
                   
               
               
                 ST007526 
                 (5-cyano-2-methyl-4-(4-pyridyl)-6- sulfanyl(3-1,4-dihydropyridyl))-N- benzamide, 4-methylmorpholine salt 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 72.49756883 
                 81.23471202 
               
               
                   
               
               
                 ST011325 
                 ethyl 5-amino-7-(2- methoxyphenyl)-2-[(2- methoxyphenyl)methylene[-3-oxo- 8-(phenylsulfonyl)-4,7-dihydro- 1,3-thiazolidino[3,2-a]pyridine-6- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.34579468 
                 98.99938771 
               
               
                   
               
               
                 ST011326 
                 ethyl 5-amino-7-[4- (methylethyl)phenyl]-2-{[4- methylethyl)phenyl[methylene}-3- oxo-8-(phenylsulfonyl)-4,7- dihydro-1,3-thiazolidino[3,2- a]pyridine-6-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.93556481 
                 72.94687422 
               
               
                   
               
               
                 ST011596 
                 prop-2-enyl 5-cyano-2-methyl-4-(3- pyridyl)-6-sulfanyl-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.76848449 
                 86.13954192 
               
               
                   
               
               
                 ST011628 
                 5-acetyl-6-methyl-4-(2- nitrophenyl)-2-sulfanyl-1,4- dihydropyridine-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.06670777 
                 76.90148533 
               
               
                   
               
               
                 ST011764 
                 ethyl 5-amino-6-(ethoxycarbonyl)- 7-[4-(methylethyl)phenyl]-2-{[4- (methylethyl) phenyl]methylene}- 3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-8- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 83.40407892 
                 70.36852666 
               
               
                   
               
               
                 ST011765 
                 ethyl 5-amino-6-(ethoxycarbonyl)- 7-(2-furyl)-2-(2-furylmethylene)-3- oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-8- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.57087557 
                 29.42161973 
               
               
                   
               
               
                 ST011766 
                 ethyl 5-amino-6-cyano-7-(5- methyl(2-thienyl))-2-[(5-methyl(2- thienyl))methylene[-3-oxo-4,7- dihydro-1,3-thiazolidino[3,2- a]pyridine-8-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 21.0970155 
                 9.557794585 
               
               
                   
               
               
                 ST011768 
                 methyl 5-amino-6- (methoxycarbonyl)-3-oxo-7-(3- pyridyl)-2-(3-pyridylmethylene)- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-8-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.70591154 
                 97.83491993 
               
               
                   
               
               
                 ST011769 
                 methyl 5-amino-7-(2,4- dichlorophenyl)-2-[(2,4- dichlorophenyl)methylene]-6- (methoxycarbonyl)-3-oxo-4,7-dihydro- 1,3-thiazolidino[3,2-a]pyridine-8- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.30080362 
                 71.55916226 
               
               
                   
               
               
                 ST014038 
                 methyl 2-(5-acetyl-3-cyano-6- methyl-4-(2-thienyl)-2-1,4- dihydropyridylthio)acetate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.98208566 
                 21.81866477 
               
               
                   
               
               
                 ST014052 
                 methyl 4-(2H,3H-benzo[3,4-e]1,4- dioxan-6-yl)-5-cyano-2-methyl-6- (2-oxo-2-(2-thienyl)ethylthio)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.00114 
                 74.68981241 
               
               
                   
               
               
                 ST014065 
                 6-amino-4-(3-bromophenyl)-2- sulfanyl-1,4-dihydropyridine-3,5- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 18.60105315 
                 30.00509113 
               
               
                   
               
               
                 ST014144 
                 2-amino-4-(4-chlorophenyl)-5-oxo- 1,4-dihydrochromeno[4,3- b]pyridine-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 66.07676022 
                 66.02213793 
               
               
                   
               
               
                 ST014147 
                 2-amino-4-(4-bromophenyl)-5-oxo- 1,4-dihydrochromeno[4,3- b]pyridine-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 82.08702025 
                 68.55337805 
               
               
                   
               
               
                 ST014245 
                 2-amino-1-benzyl-4-(3-pyridyl)-8- (3-pyridylmethylene)-1,4,7- trihydro-5H-pyrano[4,3- b]pyridine-3-carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 75.4356441 
                 53.59354065 
               
               
                   
               
               
                 ST024405 
                 ethyl 5-amino-8-cyano-3-oxo-7-(4- pyridyl)-2-(4-pyridylmethylene)- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.66259211 
                 77.40725374 
               
               
                   
               
               
                 ST024552 
                 methyl 5-(methoxycarbonyl)-1,2,6- trimethyl-4-(3-phenoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.25769736 
                 74.81070428 
               
               
                   
               
               
                 ST024568 
                 methyl 5-(methoxycarbonyl)-1,2,6- trimethyl-4-(2-pyridyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 67.61180756 
                 70.13103758 
               
               
                   
               
               
                 ST024836 
                 methyl 4-(4-chlorophenyl)-1-[(4- fluorophenyl)methyl]-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.40699115 
                 82.553677 
               
               
                   
               
               
                 ST024841 
                 5-amino-7-(3-bromophenyl)-2-[(3- bromophenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.77605667 
                 95.58309996 
               
               
                   
               
               
                 ST025017 
                 5-amino-7-(2,4-dimethoxyphenyl)- 2-[(2,4- dimethoxyphenyl)methylene]-3- oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.5355116 
                 72.3852989 
               
               
                   
               
               
                 ST025022 
                 5-amino-7-(4-ethoxy-3- methoxyphenyl)-2-[(4-ethoxy-3- methoxyphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.31389759 
                 76.11070774 
               
               
                   
               
               
                 ST025023 
                 5-amino-7-[3-(2- methylpropoxy)phenyl]-2-{[3-(2- methylpropoxy)phenyl]methylene}- 3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.12915573 
                 85.2885247 
               
               
                   
               
               
                 ST025026 
                 5-amino-7-[4- (methylethoxy)phenyl]-2-{[4- (methylethoxy)phenyl]methylene}- 3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 26.82031382 
                 0 
               
               
                   
               
               
                 ST025029 
                 5-amino-7-[3-methoxy-4- (methylethoxy)phenyl]-2-{[3- methoxy-4-(methylethoxy)phenyl] methylene}-3-oxo-4,7-dihydro- 1,3-thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.70242356 
                 73.69394599 
               
               
                   
               
               
                 ST025030 
                 5-amino-7-(5-bromo-2- hydroxyphenyl)-2-[(5-bromo-2- hydroxyphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.28510927 
                 33.92801577 
               
               
                   
               
               
                 ST025031 
                 5-amino-3-oxo-7-(3,4,5- trimethoxyphenyl)-2-[(3,4,5- trimethoxyphenyl)methylene]-4,7- dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.16845248 
                 77.59222764 
               
               
                   
               
               
                 ST025032 
                 5-amino-7-(4-hydroxy-3- methoxyphenyl)-2-[(4-hydroxy-3- methoxyphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.77083686 
                 32.98067282 
               
               
                   
               
               
                 ST025033 
                 5-amino-7-(3-ethoxy-4- hydroxyphenyl)-2-[(3-ethoxy-4- hydroxyphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 53.66167097 
                 57.59775957 
               
               
                   
               
               
                 ST025034 
                 5-amino-7-(4-hydroxyphenyl)-2- [(4-hydroxyphenyl)methylene]-3- oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.9007655 
                 85.10700826 
               
               
                   
               
               
                 ST025037 
                 2-[4-(5-amino-2-{[4- (carbamoylmethoxy)-3- ethoxyphenyl]methylene}-6,8- dicyano-3-oxo(4,7-dihydro-1,3- thiazolidino[3,2-a]pyridin-7-yl))-2- ethoxyphenoxy]acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80.02022277 
                 67.09884867 
               
               
                   
               
               
                 ST025089 
                 ethyl 5-amino-6-cyano-3-oxo-7-[2- (trifluoromethyl)phenyl]-2-{[2- (trifluoromethyl)phenyl]methylene}- 4,7-dihydro- 1,3-thiazolidino[3,2-a]pyridine-8- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.7065634 
                 33.69290876 
               
               
                   
               
               
                 ST025482 
                 6-amino-2-(dicyanomethyl)-4-(3,4- dimethoxyphenyl)-1,4- dihydropyridine-3,5-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.82901703 
                 45.10078484 
               
               
                   
               
               
                 ST026470 
                 ethyl 1-[4-(acetylamino)(1,2,5- oxadiazol-3-yl)]-6-amino-4-(2,4- dichlorophenyl)-5-cyano-2-methyl- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 81.69535088 
                 67.47916883 
               
               
                   
               
               
                 ST026471 
                 ethyl 1-[4-(acetylamino)(1,2,5- oxadiazol-3-yl)]-6-amino-4-(2- chlorophenyl)-5-cyano-2-methyl- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 4.367482636 
                 0 
               
               
                   
               
               
                 ST038081 
                 methyl 4-(2,4-dimethoxyphenyl)-1- [(4-fluorophenyl)methyl]-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 36.22274105 
                 92.93110807 
               
               
                   
               
               
                 ST038110 
                 methyl 1-(2H-benzo[3,4-d]1,3- dioxolen-5-ylmethyl)-4-(2,3- dimethoxyphenyl)-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 39.35067209 
                 74.78258485 
               
               
                   
               
               
                 ST038112 
                 methyl 1-(2H-benzo[3,4-d]1,3- dioxolen-5-ylmethyl)-5- (methoxycarbonyl)-4-(2-thienyl)- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 47.6979228 
                 99.51994629 
               
               
                   
               
               
                 ST038114 
                 methyl 1-(2H-benzo[3,4-d]1,3- dioxolen-5-ylmethyl)-4-(3,4- dimethoxyphenyl)-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.00059392 
                 95.91618031 
               
               
                   
               
               
                 ST038115 
                 methyl 1-[(3,4- dimethoxyphenyl)methyl]-5- (methoxycarbonyl)-4-(2-thienyl)- 1,4-d ihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.44553189 
                 90.99691958 
               
               
                   
               
               
                 ST038162 
                 methyl 4-(3,4-dimethoxyphenyl)-1- [(3,4-dimethoxyphenyl)methyl]-5- (methoxycarbo nyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.64720096 
                 58.6241508 
               
               
                   
               
               
                 ST038735 
                 methyl 1-cyclopropyl-4-(3- fluorophenyl)-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.36287539 
                 98.51948067 
               
               
                   
               
               
                 ST038738 
                 methyl 4-(4-chlorophenyl)-1- cyclopropyl-5-(methoxycarbonyl)- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 94.48516721 
                 52.58896601 
               
               
                   
               
               
                 ST041706 
                 N-(3,4-dimethylphenyl)-2-[3- cyano-6-methyl-5-(N- phenylcarbamoyl)-4-(2-thienyl) (2- 1,4-dihydropyridylthio)]acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.73375602 
                 50.1272459 
               
               
                   
               
               
                 ST045237 
                 methyl 4-(3,4-dichlorophenyl)-5- (methoxycarbonyl)-1-(oxolan-2- ylmethyl)-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.45503462 
                 50.7708875 
               
               
                   
               
               
                 ST045329 
                 methyl 1-adamantanyl-5- (methoxycarbonyl)-4-(3- nitrophenyl)-1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 82.59951979 
                 68.51596076 
               
               
                   
               
               
                 ST045410 
                 methyl 4-[4-(2,4-dichlorophenyl)(2- furyl)]-5-(methoxycarbonyl)-2,6- dimethyl-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 75.12601779 
                 69.44433016 
               
               
                   
               
               
                 ST048506 
                 2-[5-acetyl-3-cyano-6-methyl-4-(4- methyl(2-thienyl))(2-1,4- dihydropyridylthio)]-N-(2,4- dibromo-6-methylphenyl)acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 91.15791889 
                 65.5758358 
               
               
                   
               
               
                 ST050424 
                 tert-butyl 6-{[N-(2,3- dimethylphenyl)carbamoyl]methylthio}- 4-(4-chlorophenyl)-5-cyano- 2-methyl-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 41.20893606 
                 52.28527934 
               
               
                   
               
               
                 ST050428 
                 tert-butyl 6-{[N-(2,5- dimethylphenyl)carbamoyl]methylthio}- 4-(4-chlorophenyl)-5-cyano- 2-methyl-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.73847964 
                 65.46912006 
               
               
                   
               
               
                 ST050837 
                 2-[3-cyano-6-methyl-5-(N- phenylcarbamoyl)-4-(2-thienyl)(2- 1,4-dihydropyridylthio)]-N-(2- methylphenyl)acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 95.44262887 
                 41.28911135 
               
               
                   
               
               
                 ST050838 
                 2-{3-cyano-6-methyl-5-[N-(2- methylphenyl)carbamoyl]-4-(2- thienyl)(2-1,4-dihydropyridylthio)}- N-(4-ethoxyphenyl)acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.7588621 
                 56.65716641 
               
               
                   
               
               
                 ST050840 
                 N-(3-chloro-4-methylphenyl)-2-{3- cyano-6-methyl-5-[N-(2- methylphenyl)carbamoyl]-4-(2- thienyl)(2-1,4- dihydropyridylthio)}acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 52.30260749 
                 38.84354225 
               
               
                   
               
               
                 ST050842 
                 N-(3-chloro-4-methylphenyl)-2-[3- cyano-6-methyl-5-(N- phenylcarbamoyl)-4-(2-thienyl)(2- 1,4-dihydropyridylthio)]acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.46466634 
                 52.05801433 
               
               
                   
               
               
                 ST050859 
                 2-[6-amino-4-(2-chlorophenyl)-3,5- dicyano-2-1,4- dihydropyridylthio]acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 75.54080641 
                 35.46766877 
               
               
                   
               
               
                 ST050862 
                 methyl 2-{5-[(tert- butyl)oxycarbonyl]-4-(4- chlorophenyl)-3-cyano-6-methyl-2- 1,4-dihydropyridylthio}acetate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.24095239 
                 56.21301154 
               
               
                   
               
               
                 ST050983 
                 tert-butyl 4-(4-chlorophenyl)-5- cyano-2-methyl-6-methylthio-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.29788657 
                 0 
               
               
                   
               
               
                 ST051142 
                 tert-butyl 4-(4-chlorophenyl)-5- cyano-2-methyl-6-{[N-(4- methylphenyl)carbamoyl]methylthio}- 1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 94.84873043 
                 46.05871219 
               
               
                   
               
               
                 ST051153 
                 2-{5-[N-(4- chlorophenyl)carbamoyl]-3-cyano- 6-methyl-4-phenyl(2-1,4- dihydropyridylthio)}-N-(3- methylphenyl)acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 4.932798914 
                 0 
               
               
                   
               
               
                 ST051156 
                 N-(3-chloro-2-methylphenyl)-2-{3- cyano-4-(2-furyl)-6-methyl-5-[N- (2-methylphenyl)carbamoyl](2- 1,4-dihydropyridylthio)}acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 86.63960397 
                 68.02140491 
               
               
                   
               
               
                 ST051158 
                 2-{3-cyano-4-(2-furyl)-6-methyl-5- [N-(2-methylphenyl)carbamoyl](2- 1,4-dihydropyridylthio)}-N-(4- ethoxyphenyl)acetamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 17.68147711 
                 15.86902619 
               
               
                   
               
               
                 ST051458 
                 methyl 4-(6-chloro(2H- benzo[d]1,3-dioxolan-5-yl))-1- cyclopropyl-5-(methoxycarbonyl)- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 77.80704152 
                 59.89749054 
               
               
                   
               
               
                 ST051459 
                 methyl 4-(2,3-dimethoxyphenyl)-5- (methoxycarbonyl)-1-(oxolan-2- ylmethyl)-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.09383722 
                 85.95722149 
               
               
                   
               
               
                 ST051569 
                 methyl 4-(3-bromophenyl)-5- (methoxycarbonyl)-1-(oxolan-2- ylmethyl)-1,4-dihydropyridine-3- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.02435792 
                 72.76818319 
               
               
                   
               
               
                 ST052261 
                 methyl 5-(methoxycarbonyl)-4-(3- methoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.04473794 
                 57.23929616 
               
               
                   
               
               
                 ST052273 
                 methyl 5-(methoxycarbonyl)-4-[3- (phenylmethoxy)phenyl]-1,4- dihydropyridine-3 -carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 84.65948538 
                 57.9217965 
               
               
                   
               
               
                 ST052274 
                 methyl 4-(4-ethylphenyl)-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 4.951507642 
                 0 
               
               
                   
               
               
                 ST052284 
                 ethyl 5-(ethoxycarbonyl)-4-(2- ethoxyphenyl)-1-(4-methylphenyl)- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.7133824 
                 55.60852182 
               
               
                   
               
               
                 ST052316 
                 ethyl 5-(ethoxycarbonyl)-4-(2- ethoxyphenyl)-1-(4-fluorophenyl)- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.08983904 
                 40.0250317 
               
               
                   
               
               
                 ST052327 
                 ethyl 5-(ethoxycarbonyl)-1-(4- fluorophenyl)-4-(2-thienyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.73821604 
                 84.32974201 
               
               
                   
               
               
                 ST052366 
                 ethyl 5-(ethoxycarbonyl)-1,2,6- trimethyl-4-(2-pyridyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.21321027 
                 89.75762184 
               
               
                   
               
               
                 ST052391 
                 methyl 4-(2,3-dimethoxyphenyl)-5- (methoxycarbonyl)-1- (phenylethyl)-1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 29.94609178 
                 16.18693826 
               
               
                   
               
               
                 ST052415 
                 methyl 4-(3-ethoxyphenyl)-5- (methoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.57396989 
                 72.15123599 
               
               
                   
               
               
                 ST052438 
                 methyl 4-(3-chlorophenyl)-5- (methoxycarbonyl)-1- (phenylethyl)-1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 47.39643815 
                 65.74128324 
               
               
                   
               
               
                 ST052440 
                 methyl 4-(2-chlorophenyl)-5- (methoxycarbonyl)-1- (phenylethyl)-1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.28977295 
                 79.81317809 
               
               
                   
               
               
                 ST052450 
                 ethyl 4-(2,3-dimethoxyphenyl)-1- (2,5-dimethylphenyl)-5- (ethoxycarbonyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 5.248627712 
                 12.04080917 
               
               
                   
               
               
                 ST052464 
                 methyl 4-(4-chlorophenyl)-5- (methoxycarbonyl)-1- (phenylethyl)-1,4-dihydropyridine- 3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.08487301 
                 77.31121101 
               
               
                   
               
               
                 ST052471 
                 ethyl 1-(2,5-dimethylphenyl)-5- (ethoxycarbonyl)-4-(4-ethoxy-3- methoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.26430958 
                 57.75436544 
               
               
                   
               
               
                 ST052474 
                 ethyl 1-(2,5-dimethylphenyl)-5- (ethoxycarbonyl)-4-(2,4,5- trimethoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 5.403755892 
                 3.498108487 
               
               
                   
               
               
                 ST052487 
                 ethyl 1-(2,5-dimethylphenyl)-5- (ethoxycarbonyl)-4-(2,3,4- trimethoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 11.56301585 
                 15.09861973 
               
               
                   
               
               
                 ST052488 
                 ethyl 1-(2,5-dimethylphenyl)-5- (ethoxycarbonyl)-4-(2- ethoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.30421531 
                 57.75436544 
               
               
                   
               
               
                 ST052491 
                 ethyl 1-(2,5-dimethylphenyl)-5- (ethoxycarbonyl)-4-(3,4,5- trimethoxyphenyl)-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.28611702 
                 28.34522581 
               
               
                   
               
               
                 ST063245 
                 ethyl 4-(4-bromophenyl)-5- (methoxycarbonyl)-2,6-dimethyl- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 8.423161831 
                 0 
               
               
                   
               
               
                 ST208633 
                 methyl 4-(4-bromophenyl)-5- (methoxycarbonyl)-2,6-dimethyl- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 9.119741444 
                 0 
               
               
                   
               
               
                 ST208634 
                 methyl 4-(3-bromophenyl)-5- (methoxycarbonyl)-2,6-dimethyl- 1,4-dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80.50155559 
                 32.51078812 
               
               
                   
               
               
                 ST211423 
                 ethyl 4-(2,6-dichlorophenyl)-5- (ethoxycarbonyl)-2,6-dimethyl-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 2.731212197 
                 0 
               
               
                   
               
               
                 ST211424 
                 methyl 4-(3,5-dichloro-2- methoxyphenyl)-5- (ethoxycarbonyl)-2,6-dimethyl-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.45627935 
                 91.28508042 
               
               
                   
               
               
                 ST211500 
                 ethyl 5-(ethoxycarbonyl)-4-(4- fluorophenyl)-2,6-dimethyl-1,4- dihydropyridine-3-carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 20.66923999 
                 19.53293456 
               
               
                   
               
               
                 ST211853 
                 5-amino-3-oxo-7-(4-pyridyl)-2-(4- pyridylmethylene)-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.00185955 
                 18.36946417 
               
               
                   
               
               
                 ST215651 
                 ethyl 5-amino-7-(2-chlorophenyl)- 2-[(2-chlorophenyl)methylene]-8- cyano-3-oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6- carboxylate 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80.91612637 
                 42.29873608 
               
               
                   
               
               
                 ST215709 
                 5-amino-7-(4-methylphenyl)-2-[(4- methylphenyl)methylene]-3-oxo- 4,7-dihydro-1,3-thiazolidino[3,2- a]pyridine-6,8-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.90767387 
                 78.42869721 
               
               
                   
               
               
                 ST215713 
                 5-amino-7-(3-methoxyphenyl)-2- [(3-methoxyphenyl)methylene]-3- oxo-4,7-dihydro-1,3- thiazolidino[3,2-a]pyridine-6,8- dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 69.19835524 
                 80.48369993 
               
               
                   
               
               
                 ST217080 
                 [4-(2,6-dichlorophenyl)-2,6- dimethyl-5-(N- phenylcarbamoyl)(3-1,4- dihydropyridyl)]-N-benzamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 65.54257087 
                 0 
               
               
                   
               
            
           
           
               
               
               
               
            
               
                 ID 
                 Structure 
                 Aβ1-40 (% of control) 
                 Aβ1-42 (% of control) 
               
               
                   
               
               
                 RI_1 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 93.2 
                 75.4 
               
               
                   
               
               
                 RI_2 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 100.9 
                 44.4 
               
               
                   
               
               
                 RI_3 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 97.4 
                 51.2 
               
               
                   
               
               
                 RI_4 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 92.2 
                 64.7 
               
               
                   
               
               
                 RI_5 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 81.4 
                 82.2 
               
               
                   
               
               
                 RI_6 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 77.7 
                 65.1 
               
               
                   
               
               
                 RI_7 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.1 
                 58.8 
               
               
                   
               
               
                 RI_8 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.1 
                 26.4 
               
               
                   
               
               
                 RI_9 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.3 
                 27.6 
               
               
                   
               
               
                 RI_10 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 78.8 
                 70.6 
               
               
                   
               
               
                 RI_11 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 52.1 
                 35.8 
               
               
                   
               
               
                 RI_12 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.4 
                 82.5 
               
               
                   
               
               
                 RI_13 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 53.8 
                 41.3 
               
               
                   
               
               
                 RI_14 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56.3 
                 64.1 
               
               
                   
               
               
                 RI_15 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.9 
                 41.2 
               
               
                   
               
               
                 RI_16 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.2 
                 105 
               
               
                   
               
               
                 RI_17 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 18.2 
                 24.1 
               
               
                   
               
               
                 RI_18 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.2 
                 44.1 
               
               
                   
               
               
                 RI_19 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.4 
                 44.4 
               
               
                   
               
               
                 RI_20 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.6 
                 41.9 
               
               
                   
               
               
                 RI_21 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 18.7 
                 22.1 
               
               
                   
               
               
                 RI_22 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.9 
                 47.6 
               
               
                   
               
               
                 RI_23 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.3 
                 35.9 
               
               
                   
               
               
                 RI_24 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80.8 
                 44.1 
               
               
                   
               
               
                 RI_25 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.9 
                 36.5 
               
               
                   
               
               
                 RI_26 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 37.6 
                 26.7 
               
               
                   
               
               
                 RI_27 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.4 
                 26.5 
               
               
                   
               
               
                 RI_28 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 77.1 
                 68.5 
               
               
                   
               
               
                 RI_29 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 79.7 
                 100 
               
               
                   
               
               
                 RI_30 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 94.9 
                 48.2 
               
               
                   
               
               
                 RI_31 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 53.9 
                 73.3 
               
               
                   
               
               
                 RI_32 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.9 
                 62.8 
               
               
                   
               
               
                 RI_33 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 11.9 
                 13.7 
               
               
                   
               
               
                 RI_34 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 31.4 
                 26.1 
               
               
                   
               
               
                 RI_35 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.4 
                 78.6 
               
               
                   
               
               
                 RI_36 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 35.9 
                 72.9 
               
               
                   
               
               
                 RI_37 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.4 
                 75.8 
               
               
                   
               
               
                 RI_38 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 62.5 
                 103.4 
               
               
                   
               
               
                 RI_39 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 72 
                 72 
               
               
                   
               
               
                 RI_40 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 25.7 
                 43.2 
               
               
                   
               
               
                 RI_41 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 36.4 
                 30.7 
               
               
                   
               
               
                 RI_42 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.2 
                 36.2 
               
               
                   
               
               
                 RI_43 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 61.2 
                 75.1 
               
               
                   
               
               
                 RI_44 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 93.1 
                 60.1 
               
               
                   
               
               
                 RI_45 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 82.7 
                 61.3 
               
               
                   
               
               
                 RI_46 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.4 
                 70.2 
               
               
                   
               
               
                 RI_47 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 30.5 
                 28.1 
               
               
                   
               
               
                 RI_48 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 86.5 
                 100 
               
               
                   
               
               
                 RI_49 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.9 
                 37.7 
               
               
                   
               
               
                 RI_50 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.2 
                 38.2 
               
               
                   
               
               
                 RI_51 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 53.5 
                 58 
               
               
                   
               
               
                 RI_52 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 50.3 
                 61.6 
               
               
                   
               
               
                 RI_53 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 56 
                 99.2 
               
               
                   
               
               
                 RI_54 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 45.89 
                 52.6 
               
               
                   
               
               
                 RI_55 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 48.1 
                 40.3 
               
               
                   
               
               
                 RI_56 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 54.5 
                 100 
               
               
                   
               
               
                 RI_57 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 49.1 
                 37.3 
               
               
                   
               
               
                 RI_58 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 23.1 
                 25.6 
               
               
                   
               
               
                 RI_59 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.7 
                 30.6 
               
               
                   
               
               
                 RI_60 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.4 
                 71.1 
               
               
                   
               
               
                 RI_61 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 68.5 
                 51.4 
               
               
                   
               
               
                 RI_62 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 91.6 
                 62.4 
               
               
                   
               
               
                 RI_63 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 38.2 
                 38.8 
               
               
                   
               
               
                 RI_64 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.1 
                 41.3 
               
               
                   
               
               
                 RI_65 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 51.7 
                 38.1 
               
               
                   
               
               
                 RI_66 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 20.6 
                 23.6 
               
               
                   
               
               
                 RI_67 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.6 
                 51.8 
               
               
                   
               
               
                 RI_68 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.6 
                 100 
               
               
                   
               
               
                 RI_69 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 89.1 
                 69.8 
               
               
                   
               
               
                 RI_70 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.1 
                 58.2 
               
               
                   
               
               
                 RI_71 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 34.5 
                 25.1 
               
               
                   
               
               
                 RI_72 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 40.2 
                 50.9 
               
               
                   
               
               
                 RI_73 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 24.3 
                 34.9 
               
               
                   
               
               
                 RI_74 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 31.4 
                 41.6 
               
               
                   
               
               
                 RI_75 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 27.3 
                 38.6 
               
               
                   
               
               
                 RI_76 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 46.2 
                 54.6 
               
               
                   
               
               
                 RI_77 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 16.9 
                 25.4 
               
               
                   
               
               
                 RI_78 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 77.32 
                 88.1 
               
               
                   
               
               
                 RI_79 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.46 
                 51.6 
               
               
                   
               
               
                 RI_80 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.37 
                 54.3 
               
               
                   
               
               
                 RI_81 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 73.6 
                 100 
               
               
                   
               
               
                 RI_82 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 67.5 
                 67.9 
               
               
                   
               
               
                 RI_83 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 44.1 
                 55.4 
               
               
                   
               
               
                 RI_84 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.2 
                 44.5 
               
               
                   
               
               
                 RI_85 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 98.5 
                 46.7 
               
               
                   
               
               
                 RI_86 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 32.8 
                 21.8 
               
               
                   
               
               
                 RI_87 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 77.1 
                 49 
               
               
                   
               
               
                 RI_88 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.1 
                 54.6 
               
               
                   
               
               
                 RI_89 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.7 
                 55.1 
               
               
                   
               
               
                 RI_90 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 63.9 
                 42.9 
               
               
                   
               
               
                 RI_91 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 55.9 
                 60.7 
               
               
                   
               
               
                 RI_92 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 60.7 
                 47.3 
               
               
                   
               
               
                 RI_93 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 42.6 
                 58 
               
               
                   
               
               
                 RI_94 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 73.2 
                 81.2 
               
               
                   
               
               
                 RI_95 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 67.9 
                 69.9 
               
               
                   
               
               
                 RI_96 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 71.3 
                 70.5 
               
               
                   
               
               
                 RI_97 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 76.7 
                 74.9 
               
               
                   
               
               
                 RI_98 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 74.6 
                 78.2 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 3 
               
             
            
               
                   
               
               
                 Additional Dihydropyridine Compounds 
               
            
           
           
               
               
               
               
               
            
               
                   
                   
                   
                 Aβ1-40 
                 Aβ-42 
               
               
                 ID 
                 IUPAC Name 
                 Structure 
                 (% of control) 
                 (% of control) 
               
               
                   
               
            
           
           
               
               
               
               
               
            
               
                 ST002431 
                 1-[(aminothioxomethyl)amino]-2,6- dimethylhydropyridin-4-one 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 16.91194712 
                 97.64111454 
               
               
                   
               
               
                 ST014350 
                 4-oxo-2-sulfanyl-6- (trifluoromethyl)hydropyridine-3- carbonitrile, 4-methylmorpholine salt 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 81.81151946 
                 46.12690315 
               
               
                   
               
               
                 ST056312 
                 (2S)-2-amino-3-(3-hydroxy-4- oxohydropyridyl)propanoic acid 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 70.68288717 
                 37.1465806 
               
               
                   
               
               
                 ST007544 
                 3,5-bis(ethoxycarbonyl)-2,6- dimethyl-1,4-dihydropyridine-4- carboxylic acid 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 78.73644014 
                 80.05470709 
               
               
                   
               
               
                 ST019328 
                 [2-(1-cyclohexyl-4- hydropyridylidene)ethylidene[methane- 1,1-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 59.02172484 
                 92.16457961 
               
               
                   
               
               
                 ST208051 
                 {2-[1-benzyl-4- hydropyridylidene]ethylidene}methane- 11-dicarbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 57.06516875 
                 74.97997576 
               
               
                   
               
               
                 ST026819 
                 2-(5-nitro-2-phenyl-1-(4-pyridyl)(4- 6-hydropyridylidene))-N-(3-pyridyl)- 2-azaace tamide 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 64.94486384 
                 57.79483456 
               
               
                   
               
               
                 ST020165 
                 ethyl 3,6,7,8-tetramethyl-4-pentyl- 6-hydropyrrolo[4,5-f]indolizine-2- carboxyla te, chloride 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 90.94364983 
                 23.138825 
               
               
                   
               
               
                 ST044920 
                 2-[2-amino-4,4- bis(trifluoromethyl)-3-cyano- 1,4,5,6,7-pentahydrocyclopenta[1,2- b]pyridinyl]-4,5,6,7- tetrahydrobenzo[b]thiophene-3- carbonitrile 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 76.92072428 
                 48.18900702 
               
               
                   
               
            
           
         
       
     
     Pharmaceutical Formulations and Methods of Administration 
     Compounds disclosed herein can be administered in an effective amount for the treatment of a disease associated with cerebral accumulation of β-amyloid, such as Alzheimer&#39;s disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis Dutch-type, other forms of familial Alzheimer&#39;s disease and familial cerebral Alzheimer&#39;s amyloid angiopathy. Such compounds are also referred to herein as “active agents.” Dosage amounts and pharmaceutical formulations can be selected using methods known in the art. The compound can be administered by any route known in the art including parenteral, oral or intraperitoneal administration. 
     The compounds disclosed herein that are administered to animals or humans are dosed in accordance with standard medical practice and general knowledge of those skilled in the art. In particular, therapeutically effective amounts of compounds or more, can be administered in unit dosage form to animals or humans afflicted with a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid or suffering from a traumatic brain injury, as well as administered diagnostically for the purpose of determining the risk of developing and/or a diagnosis of a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid. 
     Parenteral administration includes the following routes: intravenous; intramuscular; interstitial; intra-arterial; subcutaneous; intraocular; intracranial; intraventricular; intrasynovial; transepithelial, including transdermal, pulmonary via inhalation, ophthalmic, sublingual and buccal; topical, including ophthalmic, dermal, ocular, rectal, or nasal inhalation via insufflation or nebulization. The nasal inhalation is conducted, for example, using aerosols, atomizers or nebulizers. 
     Examples of suitable dosage amounts are, e.g., about 0.02 mg to 1000 mg per unit dose, about 0.5 mg to 500 mg per unit dose, or about 20 mg to 100 mg per unit dose. The daily dosage can be administered in a single unit dose or divided into two, three or four unit doses per day. The duration of treatment of the active agent is, for example, on the order of hours, weeks, months, years or a lifetime. The treatment may have a duration, for example, of 1-7 days, 1-4 weeks, 1-6 months, 6-12 months, or more. 
     The compound can be administered to the CNS, parenterally or intraperitoneally. Solutions of compound, e.g., as a free base or a pharmaceutically acceptable salt can be prepared in water mixed with a suitable surfactant, such as hydroxypropylcellulose. Dispersions also can be prepared in glycerol, liquid polyethylene glycols, and mixtures thereof, and in oils. Under ordinary conditions of storage and use, these preparations can contain a preservative and/or antioxidants to prevent the growth of microorganisms or chemical degeneration. 
     The compounds which are orally administered can be enclosed in hard or soft shell gelatin capsules, or compressed into tablets. The compounds also can be incorporated with an excipient and used in the form of ingestible tablets, buccal tablets, troches, capsules, sachets, lozenges, elixirs, suspensions, syrups, wafers, and the like. Further, compounds can be in the form of a powder or granule, a solution or suspension in an aqueous liquid or non-aqueous liquid, or in an oil-in-water or water-in-oil emulsion. 
     The tablets, troches, pills, capsules and the like also can contain, for example, a binder, such as gum tragacanth, acacia, corn starch; gelating excipients, such as dicalcium phosphate; a disintegrating agent, such as corn starch, potato starch, alginic acid and the like; a lubricant, such as magnesium stearate; a sweetening agent, such as sucrose, lactose or saccharin; or a flavoring agent. When the dosage unit form is a capsule, it can contain, in addition to the materials described above, a liquid carrier. Various other materials can be present as coatings or to otherwise modify the physical form of the dosage unit. For example, tablets, pills, or capsules can be coated with shellac, sugar or both. A syrup or elixir can contain a compound as disclosed herein, sucrose as a sweetening agent, methyl and propylparabens as preservatives, a dye and flavoring. Additionally, a compound can be incorporated into sustained-release preparations and formulations. 
     Evaluating Therapeutic Efficacy 
     Compounds can be evaluated for potential efficacy in the treatment and diagnosis of diseases associated with β-amyloid accumulation using in vitro assays, particularly cultured cell-based assays, and then in vivo assays in animal models using methods known in the art. 
     Compounds can be tested for a reduction in β-amyloid production in cells exposed to the test compound. In the method, the concentration of β-amyloid (e.g., Aβ1-40 and/or Aβ1-42) in cells exposed to the compound can be measured and compared with a measurement of β-amyloid production in unexposed cells, for example, in a control run in parallel. A decrease in the production β-amyloid, alone or in combination, for example of about 5%, 10%, 15%, 20%, 25%, 30%, 50%, or more in the exposed cells compared to the control cells indicates the potential therapeutic effectiveness of the compound to treat animals or humans afflicted with a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid. In one embodiment, total β-amyloid concentration (Aβ1-40+Aβ1-42) is measured. The β-amyloid is measured, e.g. in the culture medium comprising the cells, or intracellularly. 
     The method of measuring β-amyloid may include testing an array of compounds, e.g., in a 96 well plate, as well as one or more control samples. In the assay, the compound is often required to be incubated with the cells for about 4-48 hours, or e.g., 18-36 hours. β-amyloid can be detected using an ELISA sandwich assay using quantitatively commercially available enzymatically labeled (with horseradish peroxidase) antibodies to Aβ1-40 and Aβ1-42 as described in the Example. The labeled antibody ELISA assay also can require on the order of 24 hours to complete. The compounds which are tested for their ability to reduce AB production may be screened in a range of concentrations, for example of about 1 nM to 10 mM, about 500 nM to 50 μM, or about 5 μM to 30 μM. 
     Cells which can be used in the assays described herein for measuring a reduction in β-amyloid production include mammalian or non-mammalian cells that overexpress APP or a fragment thereof, including but not limited to Chinese hamster ovary (CHO) cells, for example, 7W WT APP751 CHO cells. See, e.g., Koo and Squazzo, J. Biol. Chem., Vol. 269, Issue 26, 17386-17389, July, 1994. Cell lines transfected with APP have been described in the art and include 7W (wt APP 751 ); 7W ΔC  (APP 751  with deletion of almost the entire cytoplasmic tail (residue 710-751); 7W SW  (APP 751  with the “Swedish” KM651/652NL double-mutation); and 7W VF  (APP 751  with the V698F mutation). See, e.g. Xia et al., Proc. Natl. Acad. Sci. USA 94:8208-8213, 1997; and Pérez, R. &amp; Koo, E. (1997) in  Processing of the β - Amyloid Precursor Protein Effects of C - Terminal Mutations on Amyloid Production , eds. Iqbal, K., Winblad, B., Nishimura, T., Takeda, M. &amp; Wisniewski, H. M. (J. Wiley &amp; Sons, London), pp. 407-416. The APP which is overexpressed can include transcripts of APP, such as, without limitation, APP751. 
     Compounds can also be tested using transgenic animal models for example, for AD, such as, without limitation, PDAPP and TgAPPsw mouse models, which can be useful for screening compounds for ability to reduce β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis in the central nervous system of such animals or in humans. Transgenic animal models for AD can be constructed using standard methods known in the art, as set forth for example, without limitation, in U.S. Pat. Nos. 5,487,992; 5,464,764; 5,387,742; 5,360,735; 5,347,075; 5,298,422; 5,288,846; 5,221,778; 5,175,385; 5,175,384; 5,175,383; and 4,736,866. 
     Also provided is the use of a compound selected from Tables 1, 2, and 3, for the manufacture of a medicament for the treatment of a disease associated with cerebral accumulation of Alzheimer&#39;s amyloid, such as Alzheimer&#39;s disease (AD). 
     EXAMPLES 
     The invention will be understood in further detail in view of the following non-limiting examples. 
     Example 1 
     Measurement of Aβ1-40 and Aβ1-42 
     1. Materials and Methods 
     Chinese hamster ovary (CHO) cells, stably transfected with human APP751 (7W WT APP751 CHO cells) were used. See, e.g., Koo and Squazzo, J. Biol. Chem., 269(26): 17386-17389, 1994. The cells were maintained in DMEM medium supplemented with 10% fetal bovine serum and 1× mixture of penicillin/streptomycin/fungizone/glutamine mixture (Cambrex, Md.) geneticin as selecting agent in 75 cm 2  cell culture flasks. 
     The 7W WT APP751 CHO cells were plated in 96-well cell culture plates in quadruplicate, containing 200 microliters of culture medium, for 18 hours at 37° C. and 5% CO 2 . All test compounds were placed in dimethyl sulfoxide (DMSO) before being added to the cultured confluent 7W WT APP751 CHO cells to a concentration of the test compound of 5 μM. The culture medium was collected and diluted before being assayed by ELISAs for Aβ1-40 at 10-fold dilution and Aβ1-42 at 2-fold dilution, respectively. Concentrations of Aβ1-40 and Aβ1-42, expressed in pg/ml, were determined using commercially available ELISAs (Biosource, Calif.) in a colorimetric assay using labeled antibodies detected spectrophotometrically. For compounds with an identification beginning “RI”, the compounds were tested at a concentration of 10 μM for 24 hours. Control cells were treated with DMSO containing no compound. 
     2. Results 
     The percentage reduction in levels of Aβ1-40 and Aβ1-42 as compared to control cells not exposed to the test compounds are reported for the compounds in Tables 1, 2, and 3, supra. An entry of “0” indicates no detectable amount of Aβ1-40 or Aβ1-42 according to the assay conditions. The data in Tables 1, 2, and 3 may be rounded to the nearest 0.1%. 
     Example 2 
     Synthesis of Compounds 
     General techniques: All reactions requiring anhydrous conditions were conducted in oven-dried glass apparatus under an atmosphere of nitrogen. Preparative chromatographic separations were performed on Combiflash Companion, Isco Inc.; reactions were followed by TLC analysis using silica plates with fluorescent indicator (254 nm) and visualized with UV, phosphomolybdic acid or 4-hydroxy-3-methoxybenzaldehyde. All commercially available reagents were purchased from Aldrich and Acros and were typically used as supplied. 
     Purity of compounds was checked with Agilent 1100 series system using analytical HPLC column (Eclipse XDB-C18, 5 micron, 4.6 mm i.d) in two different solvent systems (methanol/water and acetonitrile/water) using a gradient program and found to be &gt;98% pure.  1 H and  13 C NMR spectra were recorded in Fourier transform mode at the field strength specified on a Varian AS500 spectrometer and chemical shifts are expressed in ppm relative to tetramethylsilane as an internal standard. Multiplicities in the  1 H NMR spectra are described as: s=singlet, d=doublet, t=triplet, q=quartet, m=multiplet, br=broad; coupling constants are reported in Hz. Low (MS) resolution mass spectra were measured on a Micromass Q-T of API-US spectrometer utilizing an Advion Bioscience Nanomate electrospray source. Ion mass/charge (m/z) ratios are reported as values in atomic mass units. 
     
       
         
         
             
             
         
       
     
     General Synthesis: 
     Piperidine (1.1 mol equivs.) was added to a solution of 3-oxo-N-pheylbutanamide 
     (1.0 mol equiv.), substituted/unsubstituted alkyl/aryl aldehyde (1.0 mol equiv.) and 2-cyanothioacetamide (1.0 mol equiv.) in absolute EtOH (12.5 or 25 mL). The reaction mixture was sequentially heated (&lt;5 min), cooled to room temperature and the 2-halo substituted N-alkyl/aryl acetamide (1.1 mol equiv.) (except where 2-halo substituted N-alkyl/aryl acetamide═CH 3 I) was added. The resulting solution was heated (&lt;10 min) and cooled to room temperature. The product was precipitated by adding HCl/EtOH (3 M) to the reaction mixture and refluxing for 5 min. The reaction mixture was then cooled to room temperature. The precipitate so formed was filtered, rinsed with H 2 O, EtOH, hexane/EtOAc (1:1) or hexane, and dried under vacuum with heat to afford the desired product. 
     Synthesis of Cyclic Analog of STO51153: 
     
       
         
         
             
             
         
       
     
     To suspension of compound ST51153 (1 mmol) in EtOH (10 mL), aqueous KOH (4 M in H 2 O, 0.5 mL) was added dropwise. The reaction mixture was heated to reflux for 10 min and then stirred at room temperature for 45 min. A precipitate formed which was filtered, rinsed with H 2 O (3×10 mL) and hexane (5×10 mL), and dried under vacuum and heat to afford compound “RI — 43” as a yellow solid (0.320 g, 61% yield).):  1 HNMR (DMSO-d 6 ) δ 2.32 (s, 3H, CH 3 ), 2.68 (s, 3H, CH 3 ), 5.77 (s, 2H, NH 2 ), 6.91-7.50 (m, 13H, ArH), 9.49 (s, 1H, NH), 10.52 (s, 1H, NH). Ref: Heterocylic Communications 2001, 7(4), 375-380. 
     
       
         
         
             
             
         
       
     
     General Synthesis: 
     Piperidine (1.1 mol equivs) was added to a solution of 3-oxo-N-pheylbutanamide (1.0 mol equiv.), 2 or 3-thiophenecarboxaldehyde (1.0 mol equiv) and 2-cyanothioacetamide (1.0 mol equiv.) in absolute EtOH (12.5 or 25 mL). The reaction mixture was sequentially heated (&lt;5 min), cooled to room temperature and the 2-halo substituted N-alkyl/aryl acetamide (1.1 mol equiv) was added. The resulting solution was heated (&lt;10 min) and cooled to room temperature. The product was precipitated by adding HCl/EtOH (3 M) to the reaction mixture and refluxation for 5 min. The reaction mixture was then cooled to room temperature. The precipitate so formed was filtered, rinsed with H 2 O, EtOH, hexane/EtOAc (9:1) or hexane, and dried under vacuum with heat to afford the desired product. 
     
       
         
         
             
             
         
       
     
     General Synthesis: 
     The substituted/unsubstituted aryl aldehyde (1.0 mol equiv.) was added to malononitrile (1.0 mol equiv.) in absolute EtOH followed by a few drops of piperidine. The reaction mixture was then heated at reflux for 2 h, half the solvent was removed, a drop of hexane was added and a precipitate formed. The precipitate was filtered and rinsed with hexane to afford the crude benzylidenemalononitrile intermediate. Triethylamine (1.0 mol equiv.) was then added to the above intermediate (2.0 mol equivs.) in EtOH and the resulting mixture heated at reflux for 2 h. A precipitate formed, was filtered, rinsed with H 2 O, EtOH and hexane to afford the desired product. 
     
       
         
         
             
             
         
       
     
     General Synthesis: 
     5,5-dimethyl-1,3-cyclohexanedione (1.0 mol equiv.), aldehyde (1.0 mol equiv.), benzylacetoacetate (1.0 mol equiv.), 0.5 mmol/g HClO 4 —SiO 2  (0.250 g), and NH 4 OAc (1.5 mol equivs.) mixture was heated at 95° C. for 1 h. Ethyl acetate was added, the mixture was heated to dissolve solids, cooled, filtered and concentrated. Hexane/EtOAc (9:1) was added to the crude product and vigorously stirred at room temperature until all solvent evaporated leaving behind a yellow solid. The solid was suspended in the same solvent, filtered, collected and purified by flash chromatography using hexane/EtOAc (1:1) to afford the product. 
     
       
         
         
             
             
         
       
     
     General Synthesis: 
     Acetoacetaniline (3.58 g, 20 mmol) and 2-cyanothioacetamide (2.06 g, 20 mmol) were dissolved in absolute EtOH (20 mL). To this solution was added the corresponding carboxaldehyde (20 mmol) dropwise, followed by piperidine (2.0 mL). The resulting suspension was heated to reflux for 1 h and cooled down to rt. The yellow solid was filtered and washed with EtOH and hexanes and dried, affording the corresponding salt. 200 mg of this salt and 2-chloroacetamide (1 equiv.) were dissolved in dry DMF (2 mL). The solution was heated to 90° C. for 2 h and poured into ice. The resulting solid was filtered and recrystallization from EtOH gave the titled compound. 
     It should be understood that the embodiments described herein are for illustrative purposes only and that various modifications or changes in light thereof will be suggested to persons skilled in the art and are to be included within the spirit and purview of this application. All references cited herein are incorporated by reference in their entirety.