Patent Publication Number: US-2004053786-A1

Title: Insecticidal 1,8-naphthalenedicarboxamides

Description:
BACKGROUND OF THE INVENTION  
       [0001] This invention relates to certain 1,8-naphthalenedicarboxamides, their agriculturally suitable salts and compositions, and methods of their use for controlling invertebrate pests in both agronomic and nonagronomic environments.  
       [0002] The control of invertebrate pests is extremely important in achieving high crop efficiency. Damage by invertebrate pests to growing and stored agronomic crops can cause significant reduction in productivity and thereby result in increased costs to the consumer. The control of invertebrate pests in forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health is also important. Many products are commercially available for these purposes, but the need continues for new compounds that are more effective, less costly, less toxic, environmentally safer or have different modes of action.  
       [0003] EP919542 discloses phthalic diamides of Formula i as insecticides  
                 
 
       [0004] wherein, among others, Z 1  and Z 2  are O or S; and R 1 , R 2  and R 3  are, among others, H, alkyl or substituted alkyl.  
       SUMMARY OF THE INVENTION  
       [0005] This invention is directed to compounds of Formula I and Formula II including all geometric and stereoisomers, N-oxides and agriculturally suitable salts thereof:  
                 
 
       [0006] wherein  
       [0007] each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 5 R 5 ;  
       [0008] A and B are independently O or S;  
       [0009] n is 0 to 4;  
       [0010] R 1  is H; or C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl or C 3 -C 6  cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 2 -C 4  alkoxycarbonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino and C 3 -C 6  cycloalkylamino; or  
       [0011] R 1  is C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl or C 3 -C 8  dialkylaminocarbonyl;  
       [0012] R 2  is H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  alkoxy, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 2 -C 6  alkoxycarbonyl or C 2 -C 6  alkylcarbonyl;  
       [0013] R 3  is H; or C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl or C 3 -C 6  cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl and C 1 -C 4  alkylsulfonyl; or  
       [0014] R 2  and R 3  can be taken together with the nitrogen to which they are attached to form a ring containing 2 to 6 atoms of carbon and optionally one additional atom of nitrogen, sulfur or oxygen, said ring may be optionally substituted with 1 to 4 substituents selected from the group consisting of C 1 -C 2  alkyl, halogen, CN, NO 2  and C 1 -C 2  alkoxy; and  
       [0015] each R 4  and each R 5  is independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 6  haloalkyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkynyl, C 3 -C 6  halocycloalkyl, halogen, CN, CO 2 H, CONH 2 , NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl, C 2 -C 4  alkoxycarbonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl, C 3 -C 8  dialkylaminocarbonyl, or C 3 -C 6  trialkylsilyl; or  
       [0016] each R 4  and each R 5  is independently a phenyl, benzyl, phenoxy, 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system, each ring optionally substituted with one to three substituents independently selected from the group consisting of C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  haloalkyl, C 2 -C 4  haloalkenyl, C 2 -C 4  haloalkynyl, C 3 -C 6  halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 3 -C 6  (alkyl)cycloalkylamino, C 2 -C 4  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl, C 3 -C 8  dialkylaminocarbonyl or C 3 -C 6  trialkylsilyl; or  
       [0017] (R 5 ) 2  when attached to adjacent carbon atoms can be taken together as —OCF 2 O—, —CF 2 CF 2 O— or —OCF 2 CF 2 O—.  
       [0018] This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I or Formula II and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. This invention also pertains to a composition comprising a biologically effective amount of a compound of Formula I or Formula II and an effective amount of at least one additional biologically active compound or agent.  
       [0019] This invention also pertains to a method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I or Formula rT (e.g., as a composition described herein). This invention also relates to such a method wherein the invertebrate pest or its environment is contacted with composition comprising a biologically effective amount of a compound of Formula I or Formula II or with a composition comprising a compound of Formula I or Formula II and a biologically effective amount of at least one additional compound or agent for controlling invertebrate pests.  
       DETAILS OF THE INVENTION  
       [0020] In the above recitations, the term “alkyl”, used either alone or in compound words such as “alkylthio” or “haloalkyl” includes straight-chain or branched alkyl, such as, methyl, ethyl, ni-propyl, i-propyl, or the different butyl, pentyl or hexyl isomers. “Alkenyl” includes straight-chain or branched alkenes such as 1-propenyl, 2-propenyl, and the different butenyl, pentenyl and hexenyl isomers. “Alkenyl” also includes polyenes such as 1,2-propadienyl and 2,4-hexadienyl. “Alkynyl” includes straight-chain or branched alkynes such as 1-propynyl, 2-propynyl and the different butynyl, pentynyl and hexynyl isomers. “Alkynyl” can also include moieties comprised of multiple triple bonds such as 2,5-hexadiynyl. “Alkoxy” includes, for example, methoxy, ethoxy, n-propyloxy, isopropyloxy and the different butoxy, pentoxy and hexyloxy isomers. “Alkylthio” includes branched or straight-chain alkylthio moieties such as methylthio, ethylthio, and the different propylthio, butylthio, pentylthio and hexylthio isomers. “Cycloalkyl” includes, for example, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. “Alkylamino”, “alkenylthio”, “alkenylsulfinyl”, “alkenylsulfonyl”, “alklynylsulfinyl”, “alkynylsulfonyl”, and the like, are defined analogously to the above examples. Examples of “alkoxycarbonyl” include CH 3 OC(═O), CH 3 CH 2 OC(—O), CH 3 CH 2 CH 2 OC(—O), (CH 3 ) 2 CHOC(—O) and the different butoxy- or pentoxycarbonyl isomers. Examples of “alkylaminocarbonyl” include CH 3 NHC(═O), CH 3 CH 2 NHC(═O), CH 3 CH 2 CH 2 NHC(═O), (CH 3 ) 2 CHNHC(═O) and the different butylamino- or pentylaminocarbonyl isomers. The term “dialkylamino” includes amino functions substituted with two alkyl groups that may be the same or different. “Dialkylaminocarbonyl” is defined analogously, and examples include (CH 3 ) 2 NC(═O) and CH 3 CH 2 NCH 3 C(═O).  
       [0021] The term “heterocyclic ring” or “heterocyclic ring system” denotes rings or ring systems in which at least one ring atom is not carbon and comprises 1 to 4 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, provided that each heterocyclic ring contains no more than 4 nitrogens, no more than 2 oxygens and no more than 2 sulfurs. The heterocyclic ring can be attached through any available carbon or nitrogen by replacement of hydrogen on said carbon or nitrogen. The term “aromatic ring system” denotes fully unsaturated carbocycles and heterocycles in which the polycyclic ring system is aromatic (where aromatic indicates that the Hückel rule is satisfied for the ring system). The term “heteroaromatic ring” denotes fully aromatic rings in which at least one ring atom is not carbon and comprises 1 to 4 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, provided that each heterocyclic ring contains no more than 4 nitrogens, no more than 2 oxygens and no more than 2 sulfurs (where aromatic indicates that the Hückel rule is satisfied). The heterocyclic ring can be attached through any available carbon or nitrogen by replacement of hydrogen on said carbon or nitrogen. The term “aromatic heterocyclic ring system” includes fully aromatic heterocycles and heterocycles in which at least one ring of a polycyclic ring system is aromatic (where aromatic indicates that the Hückel rule is satisfied). The term “fused heterobicyclic ring system” includes a ring system comprised of two fused rings in which at least one ring atom is not carbon and can be aromatic or non aromatic, as defined above.  
       [0022] The term “halogen”, either alone or in compound words such as “haloalkyl”, includes fluorine, chlorine, bromine or iodine. Further, when used in compound words such as “haloalkyl”, said alkyl may be partially or fully substituted with halogen atoms which may be the same or different. Examples of “haloalkyl” include F 3 C, ClCH 2 , CF 3 CH 2  and CF 3 CCl 2 . The terms “haloalkenyl”, “haloalkynyl”, “haloalkoxy”, and the like, are defined analogously to the term “haloalkyl”. Examples of “haloalkenyl” include (Cl) 2 C═CHCH 2  and CF 3 CH 2 CH═CHCH 2 . Examples of “haloalkynyl” include HC≡CCHCl, CF 3 C≡C, CCl 3 C≡C and FCR 2 C≡CCH 2 . Examples of “haloalkoxy” include CF 3 O, CCl 3 CH 2 O, HCF 2 CH 2 CH 2 O and CF 3 CH 2 O.  
       [0023] The total number of carbon atoms in a substituent group is indicated by the “C i -C j ” prefix where i and j are numbers from 1 to 6. For example, C 1 -C 3  alkylsulfonyl designates methylsulfonyl through propylsulfonyl; C 2  alkoxyalkyl designates CH 3 OCH 2 ; C 3  alkoxyalkyl designates, for example, CH 3 CH(OCH 3 ), CH 3 OCH 2 CH 2  or CH 3 CH 2 OCH 2 ; and C 4  alkoxyalkyl designates the various isomers of an alkyl group substituted with an alkoxy group containing a total of four carbon atoms, examples including CH 3 CH 2 CH 2 OCH 2  and CH 3 CH 2 OCH 2 CH 2 . In the above recitations, when a compound of Formula I contains a heterocyclic ring, all substituents are attached to this ring through any available carbon or nitrogen by replacement of a hydrogen on said carbon or nitrogen.  
       [0024] When a group contains a substituent which can be hydrogen, for example R 3 , then, when this substituent is taken as hydrogen, it is recognized that this is equivalent to said group being unsubstituted. When the number of optional substituents on a group is 0, for example when n is 0, then it is recognized that this is equivalent to said group being unsubstituted. When a bond is depicted as floating, the substituent may be attached to any of the available carbons on the ring by replacement of hydrogen; for bicyclic ring systems, the substituent or substituents may be attached to either ring of the bicyclic ring system, or both rings. For example, when n is 1, a single R 4  substituent may be attached to Formula I or Formula II at any of the indicated positions 2, 3, 4, 5, 6 or 7; and when n is 2, two independent R 4  substituents may be attached at the 2,3; 2,4; 2,5; 2, 6 or 2,7 positions or any other combination of 2 positions. When R 2  and R 3  are taken together with the nitrogen to which they are attached to form a ring, said ring can be optionally substituted on any available carbon or optionally nitrogen in said ring.  
       [0025] Compounds of this invention can exist as one or more stereoisomers. The various stereoisomers include enantiomers, diastereomers, atropisomers and geometric isomers. One skilled in the art will appreciate that one stereoisomer may be more active and/or may exhibit beneficial effects when enriched relative to the other stereoisomer(s) or when separated from the other stereoisomer(s). Additionally, the skilled artisan knows how to separate, enrich, and/or to selectively prepare said stereoisomers. The compounds of the invention may be present as a mixture of stereoisomers, individual stereoisomers, or as an optically active form.  
       [0026] The present invention comprises compounds selected from Formula I or Formula II, N-oxides and agriculturally suitable salts thereof. One skilled in the art will appreciate that not all nitrogen containing heterocycles can form N-oxides since the nitrogen requires an available lone pair for oxidation to the oxide; one skilled in the art will recognize those nitrogen containing heterocycles which can form N-oxides. One skilled in the art will also recognize that tertiary amines can form N-oxides. Synthetic methods for the preparation of N-oxides of heterocycles and tertiary amines are very well known by one skilled in the art including the oxidation of heterocycles and tertiary amines with peroxy acids such as peracetic and m-clhloroperbenzoic acid (MCPBA), hydrogen peroxide, alkyl hydroperoxides such as t-butyl hydroperoxide, sodium perborate, and dioxiranes such as dimethydioxirane. These methods for the preparation of N-oxides have been extensively described and reviewed in the literature, see for example: T. L. Gilchrist in  Comprehensive Organic Synthesis , vol. 7, pp 748-750, S. V. Ley, Ed., Pergamon Press; M. Tisler and B. Stanovnik in  Comprehensive Hetetrocyclic Chemistry , vol. 3, pp 18-19, A. J. Boulton and A. McKillop, Eds., Pergamon Press; M. R. Grimmett and B. R. T. Keene in Advances in  Heterocyclic Chemistry , vol. 43, pp 139-151, A. R. Katritzky, Ed., Academic Press; M. Tisler and B. Stanovnik in  Advances in Heterocyclic Chemistry , vol. 9, pp 285-291, A. R. Katritzky and A. J. Boulton, Eds., Academic Press; and G. W. H. Cheeseman and E. S. G. Werstiuk in  Advances in Heterocyclic Chemistry , vol. 22, pp 390-392, A. R. Katritzky and A. J. Boulton, Eds., Academic Press.  
       [0027] The salts of the compounds of the invention include acid-addition salts with inorganic or organic acids such as hydrobromic, hydrochloric, nitric, phosphoric, sulfuric, acetic, butyric, fumaric, lactic, maleic, malonic, oxalic, propionic, salicylic, tartaric, 4-toluenesulfonic or valeric acids.  
       [0028] Preferred for reasons including ease of synthesis and/or greater arthropodicidal efficacy are:  
       [0029] Preferred 1. Compounds of Formula I wherein  
       [0030] A and B are both O;  
       [0031] R 1  is H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 2 -C 6  alkylcarbonyl or C 2 -C 6  alkoxycarbonyl; and  
       [0032] n is 0 to 2.  
       [0033] Preferred 2. Compounds of Formula II wherein  
       [0034] A and B are both O;  
       [0035] R 1  is H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 2 -C 6  alkylcarbonyl or C 2 -C 6  alkoxycarbonyl; and  
       [0036] n is 0 to 2.  
       [0037] Preferred 3. Compounds of Preferred 1 or Preferred 2 wherein  
       [0038] J is a phenyl ring or a 5- or 6-membered heteroaromatic ring selected from the group consisting of J-1, J-2, J-3 and J-4, each J ring optionally substituted with 1 to 3 R 5  
                 
 
       [0039]  Q is O, S or NR 5 ;  
       [0040] W, X, Y and Z are independently N or CR 5 , provided that in J-3 and J-4 at least one of W, X, Y or Z is N;  
       [0041] R 2  is H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 2 -C 6  alkylcarbonyl or C 2 -C 6  alkoxycarbonyl;  
       [0042] R 3  is C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl or C 3 -C 6  cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, C 1 -C 2  alkoxy, C 1 -C 2  alkylthio, C 1 -C 2  alkylsulfinyl and C 1 -C 2  alkylsulfonyl;  
       [0043] one R 4  group is attached to the naphthyl ring system at the 2-position or 7-position, and said R 4  is C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl or C 1 -C 4  haloalkylsulfonyl;  
       [0044] each R 5  is independently H, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl, C 3 -C 8  dialkylaminocarbonyl; or  
       [0045] each R 5  is independently a phenyl, benzyl or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted with C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  haloalkyl, C 2 -C 4  haloalkenyl, C 2 -C 4  haloalkynyl, C 3 -C 6  halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 3 -C 6  (alkyl)cycloalkylamino, C 2 -C 4  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl, C 3 -C 8  dialkylaminocarbonyl or C 3 -C 6  trialkylsilyl; or  
       [0046] (R 5 ) 2  when attached to adjacent carbon atoms can be taken together as —OCF 2 O—, —CF 2 CF 2 O— or —OCF 2 CF 2 O—; and  
       [0047] n is 1 to 2.  
       [0048] Preferred 4. Compounds of Formula I of Preferred 3 wherein R 2  is H; R 3  is C 1 -C 4  alkyl; and at least one of the R 5  substituents is ortho to the NR 1 C(═B) moiety.  
       [0049] Preferred 5. Compounds of Preferred 4 wherein R 3  is methyl.  
       [0050] Preferred 6. Compounds of Formula II of Preferred 3 wherein  
       [0051] R 1  is H or C 1 -C 4  alkyl;  
       [0052] R 2  is H or C 1 -C 4  alkyl;  
       [0053] R 3  is C 1 -C 4  alkyl optionally substituted with halogen, CN, OCH 3 , or S(O) p CH 3 ;  
       [0054] one R 5  group is attached to the J at the position ortho to the C(═B)NR 1  moiety, and said R 5  is C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl; C 3 -C 8  dialkylaminocarbonyl or a phenyl, benzyl, or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted with halogen, CN, NO 2 , C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  haloalkyl, C 1 -C 4  alkoxy or C 1 -C 4  haloalkoxy;  
       [0055] and a second optional R 5  group is independently C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl; C 3 -C 8  dialkylaminocarbonyl or a phenyl, benzyl, or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted with halogen, CN, NO 2 , C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  haloalkyl, C 1 -C 4  alkoxy or C 1 -C 4  haloalkoxy.  
       [0056] Preferred 7. Compounds of Preferred 6 wherein J is phenyl, pyrazole, pyrrole, pyridine or pyrimidine, each substituted with one R 5  attached to the J at the position ortho to the C(═B)NR 1  moiety and a second optional R 5 .  
       [0057] Preferred 8. Compounds of Preferred 7 wherein  
       [0058] R 1  and R 2  are each H;  
       [0059] one R 4  is attached at the 7-position ortho to the NR 1 C(═X)J moiety and is selected from the group consisting of C 1 -C 3  alkyl, CF 3 , OCF 3 , OCHF 2 , S(O) p CF 3 , S(O) p CHF 2  and halogen and an optional second R 4  is attached at the 5-position pair to the NR 1 C(═X)J moiety and is selected from the group consisting of halogen, C 1 -C 3  alkyl and C 1 -C 3  haloalkyl.  
       [0060] Preferred 9. Compounds of Preferred 8 wherein  
       [0061] J is J-1;  
       [0062] Q is NR 5a ;  
       [0063] X is N or CH;  
       [0064] Y is CH;  
       [0065] Z is CR 5b ;  
       [0066] R 5a  is a phenyl or 2-pyridyl ring substituted with one or two substituents selected from the group consisting of halogen, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl or C 1 -C 4  haloalkoxy; and  
       [0067] R 5b  is halogen or CF 3 .  
       [0068] Specifically preferred compounds are those selected from the group consisting of  
       [0069] N-methyl —N′-(2-bromo-4-fluoropheny)-1,8-naphthalene-dicarboxamide,  
       [0070] N-methyl 8-[(3,4-difluorophenyl)carbonylamino]-1-naphthalenecarboxamide and  
       [0071] N-methyl 8-[(2-thienyl)carbonylamino]-1-naphthalenecarboxamide.  
       [0072] This invention also pertains to a composition for controlling invertebrates comprising a biologically effective amount of a compound of Formula I or Formula II and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. This invention also pertains to a composition comprising a biologically effective amount of a compound of Formula I or Formula II and an effective amount of at least one additional biologically active compound or agent. Preferred compositions are those comprising compounds of Formula I or Formula II as preferred in Preferred 1 through 9, and the specifically preferred compounds above.  
       [0073] This invention also pertains to a method for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula I or Formula II, and N-oxide or agriculturally suitable salts thereof (e.g. as a composition comprising a compound of Formula I or Formula II). This invention also relates to such a method wherein the invertebrate pest or its environment is contacted with a biologically effective amount of a compound of Formula I or Formula II or a composition comprising a compound of Formula I or Formula II and a biologically effective amount of at least one additional compound or agent for controlling invertebrate pests. Preferred methods are those comprising compounds of Formula I or Formula II as preferred in Preferred 1 through 9, and the specifically preferred compounds above.  
       [0074] Of note are certain compounds of Formula Ih and Formula IIc including all geometric and stereoisomers, and agriculturally suitable salts thereof  
                 
 
       [0075] wherein:  
       [0076] A and B are independently O or S;  
       [0077] m is 1 to 5;  
       [0078] n is 0 to 4;  
       [0079] R 1  is H; or C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl or C 3 -C 6  cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 2 -C 4  alkoxycarbonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino and C 3 -C 6  cycloalkylamino; or  
       [0080] R 1  is C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl or C 3 -C 8  dialkylaminocarbonyl;  
       [0081] R 2  is H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  alkoxy, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 2 -C 6  alkoxycarbonyl or C 2 -C 6  alkylcarbonyl;  
       [0082] R 3  is H; or C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl or C 3 -C 6  cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl and C 1 -C 4  alkylsulfonyl; or  
       [0083] R 2  and R 3  can be taken together with the nitrogen to which they are attached to form a ring containing 2 to 6 atoms of carbon and optionally one additional atom of nitrogen, sulfur or oxygen, said ring may be optionally substituted with 1 to 4 substituents selected from the group consisting of C 1 -C 2  alkyl, halogen, CN, NO 2  and C 1 -C 2  alkoxy; and  
       [0084] each R 4  and each R 5  is independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 6  haloalkyl, C 2 -C 6  haloalkenyl, C 2 -C 6  haloalkynyl, C 3 -C 6  halocycloalkyl, halogen, CN, CO 2 H, CONH 2 , NO 2 , hydroxy, C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl, C 2 -C 4  alkoxycarbonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl, C 3 -C 8  dialkylaminocarbonyl, or C 3 -C 6  trialkylsilyl; or  
       [0085] each R 4  and each R 5  is independently phenyl optionally substituted with C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 1 -C 4  haloalkyl, C 2 -C 4  haloalkenyl, C 2 -C 4  haloalkynyl, C 3 -C 6  halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  alkylamino, C 2 -C 8  dialkylamino, C 3 -C 6  cycloalkylamino, C 3 -C 6  (alkyl)cycloalkylamino, C 2 -C 4  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 2 -C 6  alkylaminocarbonyl, C 3 -C 8  dialkylaminocarbonyl or C 3 -C 6  trialkylsilyl.  
       [0086] Also of note are arthropodicidal compositions comprising an arthropodicidally effective amount of a compound of Formula Ih or Formula IIc noted above and at least one additional component selected from the group consisting of surfactants, solid diluents or liquid diluents.  
       [0087] Also of note are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula Ih or Formula IIc noted above.  
       [0088] Selection 1. Of note are selected compounds of Formula Ih wherein  
       [0089] A and B are both O;  
       [0090] m is 1 to 3;  
       [0091] n is 0 to 2;  
       [0092] R 1  is H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 2 -C 6  alkylcarbonyl or C 2 -C 6  alkoxycarbonyl; and  
       [0093] each R 4  and each R 5  is independently H, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl.  
       [0094] Selection 2. Of note are selected compounds of Selection I wherein  
       [0095] R 2  is H;  
       [0096] R 3  is C 1 -C 4  alkyl;  
       [0097] each R 4  and each R 5  is independently H, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl; and  
       [0098] at least one of the R 5  substituents is ortho to the amide linkage.  
       [0099] Selection 3. Of note are selected compounds of Selection 2 wherein R 3  is methyl.  
       [0100] Selection 4. Of note are selected compounds of Formula IIc wherein  
       [0101] A and B are both O;  
       [0102] m is 1 to 3;  
       [0103] n is 0 to 2;  
       [0104] R 1  is H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 3 -C 6  cycloalkyl, C 2 -C 6  alkylcarbonyl or C 2 -C 6  alkoxycarbonyl; and  
       [0105] each R 4  and each R 5  is independently H, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl.  
       [0106] Selection 5. Of note are selected compounds of Selection 4 wherein  
       [0107] R 2  is H;  
       [0108] R 3  is C 1 -C 6  alkyl optionally substituted with C 1 -C 4  alkoxy or C 1 -C 4  alkylthio;  
       [0109] each R 4  and each R 5  is independently H, C 1 -C 4  alkyl, C 1 -C 4  haloalkyl, halogen, CN, NO 2 , C 1 -C 4  alkoxy, C 1 -C 4  haloalkoxy, C 1 -C 4  alkylthio, C 1 -C 4  alkylsulfinyl, C 1 -C 4  alkylsulfonyl, C 1 -C 4  haloalkylthio, C 1 -C 4  haloalkylsulfinyl, C 1 -C 4  haloalkylsulfonyl or C 2 -C 4  alkoxycarbonyl; and  
       [0110] at least one of the R 5  substituents is ortho to the amide linkage.  
       [0111] As noted above, each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 5 R 5 . The term “optionally substituted” in connection with these J groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the arthropodicidal activity possessed by the unsubstituted analog. An example of phenyl optionally substituted with 1 to 5 R 5  is the ring illustrated as U-1 in Exhibit 1, wherein R v  is R 5  and r is an integer from 1 to 5. An example of a naphthyl group optionally substituted with 1 to 5 R 5  is illustrated as U-85 in Exhibit 1, wherein R v  is R 5  and r is an integer from 1 to 5. Examples of 5- or 6-membered heteroaromatic rings optionally substituted with 1 to 5 R 5  include the rings U-2 through U-53 illustrated in Exhibit 1 wherein R v  is R 5  and r is an integer from 1 to 5. Note that J-1 through J-4 below also denote 5- or 6-membered heteroaromatic rings. Note that U-2 through U-20 are examples of J-1, U-2 1 through U-35 and U-40 are examples of J-2, U-41 through U-48 are examples of J-3 and U-49 through U-53 are examples of J-4. Examples of aromatic 8-, 9- or 10-membered fused heterobicyclic ring systems optionally substituted with 1 to 4 R 3  include U-54 through U-84 illustrated in Exhibit 1 wherein R v  is R 5  and r is an integer from 1 to 5.  
       [0112] Although R v  groups are shown in the structures U-I through U-85, it is noted that they do not need to be present since they are optional substituents. Note that when R v  is H when attached to an atom, this is the same as if said atom is unsubstituted. The nitrogen atoms that require substitution to fill their valence are substituted with H or R v . Note that some U groups can only be substituted with less than 5 R v  groups (e.g. U-14, U-1 5, U-18 through U-21 and U-32 through U-34 can only be substituted with one R v ). Note that when the attachment point between (R v ) r  and the U group is illustrated as floating, (R v ) r  can be attached to any available carbon atom of the U group. Note that when the attachment point on the U group is illustrated as floating, the U group can be attached to the remainder of Formula I through any available carbon of the U group by replacement of a hydrogen atom.  
       Exhibit 1 
       [0113]                                                                                                                                                 
       [0114] The compounds of Formula I and Formula II can be prepared by one or more of the following methods and variations as described in Schemes 1-2 1. The definitions of R 1 , R 2 , R 3 , R 4 , A, B, m and n in the compounds described in the Schemes below are as defined above in the Summary of the Invention or their subsets.  
       [0115] Compounds of Formula I can be prepared by procedures outlined in Schemes 1-9. Compounds of Formulae Ia-h are various subsets of the compounds of Formula I.  
       [0116] Typical procedures are described in Scheme 1 and involve either coupling of a isonaphthalimide of Formula 2 with an amine of Formula 3 or coupling of a compound of Formula 4 with an amine of Formula 5 with or without the presence of a base. Typical bases include amine bases such as triethylamine, diisopropylethylamine and pyridine. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. The amines of Formula 3 and Formula 5 are either commercially available, well represented in the chemical literature, or readily available from established literature procedures. Amides of Formula Ia can be converted to thioamides of Formula Ib using a variety of standard thio transfer reagents including phosphorus pentasulfide and Lawesson&#39;s reagent.  
                 
 
       [0117] Compounds of Formula 2 and Formula 4 are typically prepared by coupling of a 1,8-naphthaloyl chloride of the Formula 6 with an amine of Formula 7 or an amine of Formula 8 respectively (Scheme 2). Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. In some instances, the amine of Formula 7 can serve as the acid scavenger when used in excess. The compounds of 1,8-naphthaloyl chloride of the Formula 6 are well represented in the chemical literature and are typically prepared from the corresponding 1,8-naphthalic acids or the anhydrides with the use of chlorinating reagents commonly used for the transformation of carboxylic acid to carboxylic acid chloride. These commonly used chlorinating reagents include phosphorous oxychloride and phosphorous pentachloride.  
                 
 
       [0118] An alternate procedure for the preparation of compounds of Formula 2 and Formula 4 involves the cyclization of compounds of 8-aminocarbonyl-1-naphthalenecarboxylic acid of Formula 9 and Formula 10 respectively (Scheme 3) with the use of a dehydration reagent in an inert solvent at a temperature in the range of-30 to 30° C., with or without the presence of an acid scavenger. Typical dehydration reagents include dicyclohexylcarbodiimide and trifluoroacetic anhydride. Polymer supported reagents such as polymer-bound cyclohexylcarboduimide are useful. Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Typical inert solvents include aprotic solvents such as dichloromethane and 1-chlorobutane. A typical range of reaction temperature is from −5 to 25° C.  
                 
 
       [0119] The preparation of 8-aminocarbonyl-1-naphthalenecarboxylic acids of Formula 9 and Formula 10 involves the coupling of 1,8-naphthalic anhydrides of Formula 11 with amines of Formula 7 or amines of Formula 8 respectively (Scheme 4) in an inert solvent at a temperature in the range of 0 to 30° C. A typical inert solvent is dimethylformamide. The reaction is commonly conducted in the temperature range of 5 to 10° C.  
                 
 
       [0120] Alternate procedures for the preparation of compounds of 8-aminocarbonyl-1-naphthalenecarboxylic acid of Formula 9 and Formula 10 involve the hydrolysis of 10 compounds of 1,8-naphthalimide of Formula 12 and Formula 13 respectively (Scheme 5) using a hydroxide such as sodium hydroxide or potassium hydroxide in a protic solvent system such as water-methanol or water-dioxane at elevated temperature. The reaction is usually conducted at the reflux temperature of the reaction mixture. The compounds of 1,8-naphthalimide of Formula 12 and Formula 13 are typically prepared by condensing a 1,8-naphthalic anhydride of Formula II with an amine of Formula 7 or Formula 8 respectively at an elevated temperature, usually in the presence of an acid. A typical reaction involves refluxing the 1,8-naphthalic anhydride of Formula 11 and the amine of Formula 7 or Formula 8 in acetic acid.  
                 
 
       [0121] An alternate procedure for the preparation of compounds of Formula I involves the coupling of 8-aminocarbonyl-1-naphthoyl chlorides of Formula 14 and Formula 15 with an amine of Formula 3 or an amine of Formula 5 respectively (Scheme 6), in the presence of an acid scavenger. Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Typically, the reaction temperature range is 0 to 25° C.  
       [0122] 8-Aminocarbonyl-1-naphthoyl chlorides of Formula 14 and Formula 15 are available from coupling the corresponding 1,8-naphthaloyl dichloride of Formula 6 with an amine of Formula 5 or Formula 3 respectively in the presence of an acid scavenger (Scheme 7). Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine.  
                 
 
                 
 
       [0123] Another procedure for the preparation of compounds of Formula I involves the stepwise carbamoylation or thiocarbamoylation of a naphthalene of Formula 20 (Schemes 8 and 9). Upon treatment with a Lewis acid under Friedel-Crafts reaction conditions, compounds of 1-naphthalenecarboxamide or 1-naphthalenethiocarboxamide of Formula 16 or Formula 17 couple with a carbamoyl chloride or thiocarbamoyl chloride of Formula 18 or Formula 19 to provide a compound of Formula I (Scheme 8). Commonly used Lewis acids include aluminum chloride and stannic chloride.  
       [0124] The preparation of compounds of 1-naphthalenecarboxamides or 1-naphthalenethiocarboxamides of Formula 16 or Formula 17 (Scheme 9) involves the coupling of a naphthalene of Formula 20 and a carbamoyl chloride or thiocarbamoyl chloride of Formula 19 or Formula 18 respectively in the presence of a Lewis acid such as aluminum chloride and stannic chloride under Friedel-Crafts reaction conditions. The naphthalenes of Formula 20, the carbamoyl chlorides and the thiocarbamoyl chlorides of Formula 18 and Formula 19 are commercially available, well described in the chemical literature, or can be prepared following established literature procedures.  
                 
 
                 
 
       [0125] The compounds of Formula II can be prepared by one or more of the following methods and variations as described in Schemes 10-13. Compounds of Formulae IIa-b are subsets of the compounds of Formula II.  
       [0126] A typical procedure is described in Scheme 10 and involves coupling of an 8-amino-naphthalene-1-carboxamide of Formula 21 with a carbonyl chloride of Formula 22 in the presence of an acid scavenger to provide the compounds of Formula IIa, or with thiocarbonyl chloride of Formula 22 in the presence of an areneselenolate to provide the compounds of Formula IIb. Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine, other scavengers include hydroxides such as sodium and potassium hydroxide and carbonates such as sodium carbonate and potassium carbonate. In certain instances it is useful to use polymer supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Typical areneselenolates include sodium phenylselenolate. The carbonyl chlorides and the thiocarbonyl chlorides of Formula 22 are commercially available, well represented in the chemical literature, or readily prepared according to established literature procedures. Amides of Formula IIa can be converted to thioamides of Formula IIb using standard thio transfer reagents such as phosphorus pentasulfide and Lawesson&#39;s reagent.  
                 
 
       [0127] Another procedure for the preparation of compounds of Formula IIa involves coupling of an 1-amino-naphthalene-8-carboxamide or 1-amino-naphthalene-8-thiocarboxamide of Formula 21 with a carboxylic acid of Formula 23 in the presence of a dehydration reagent such as dicyclohexylcarbodiimide (DCC). Polymer supported reagents such as polymer-bound cyclohexylcarboduimide are useful. Benzoic acids of Formula 23 are commercially available, well represented in the chemical literature, or readily prepared according to established literature procedures. The procedures of Scheme 10 and Scheme 11 are only representative examples of useful methods for the preparation of Formula II compounds as the literature is extensive for the preparation of carboxamides.  
                 
 
       [0128] 8-Amino-naphthalene-1-carboxamides and 8-amino-naphthalene-1-thiocarboxamides of Formula 21a are typically available from the corresponding 8-nitro-naphthalene-1-carboxamides and 8-nitro-naphthalene-1-thiocarboxamides of Formula 24 respectively via reduction of the nitro group. Typical procedures involve reduction with hydrogen in the presence of a metal catalyst such as palladium on carbon or platinum oxide and in hydroxylic solvents such as ethanol and isopropanol. These procedures are well documented in the chemical literature. R 1  substituents such as alkyl, substituted alkyl and the like can generally be introduced at this stage through known procedures including either direct alkylation or through the generally preferred method of reductive alkylation of the amine. A commonly employed procedure is to combine the aminonaphthalene 21a with an aldehyde in the presence of a reducing agent such as sodium cyanoborohydride to produce the compounds of Formula 21 where R 1  is other than H.  
                 
 
       [0129] The intermediate amides of Formula 24 are readily prepared from 8-nitro-naphthalene-1-carboxylic acids that are commercially available, known in the literature, or can be prepared by established literature procedures for the derivatization of naphthalenes or aromatic groups in general. Typical methods for amide formation can be applied here. These include direct dehydrative coupling of acids of Formula 25 with amines of Formula 5 using for example DCC, and conversion of the acids to an activated form such as the acid chlorides or anhydrides and subsequent coupling with amines to form amides of formula 24a. Also, diethyl cyanophosphonate is a useful reagent for this type of reaction involving activation of the acid. The chemical literature is extensive on this type of reaction. Amides of Formula 24a are readily converted to thioamides of Formula 24b by using commercially available thio transfer reagents such as phosphorus pentasulfide and Lawesson&#39;s reagent.  
                 
 
       [0130] Benzoic acids of Formula 23a, (compounds of Formula 23 wherein J is an optionally substituted phenyl ring) are well known in the art. Preparation of certain heterocyclic acids of Formula 4 are described in Schemes 14-21. A variety of heterocyclic acids and general methods for their synthesis may be found in World Patent Application WO 98/57397.  
       [0131] The synthesis of representative pyridine acids (23b) is depicted in Scheme 14. This procedure involves the known synthesis of pyridines from β-ketoesters and 4-aminobutenones (29). Substituent groups R 5 (c) and R 5 (d) include e.g. alkyl and haloalkyl.  
                 
 
       [0132] The synthesis of representative pyrimidine acids (23c) is depicted in Scheme 15. This procedure involves the known synthesis of pyrimidines from vinylidene-β-ketoesters (33) and amidines (34). Substituent groups R 5 (c) and R 5 (d) include e.g. alkyl and haloalkyl.  
                 
 
       [0133] Syntheses of representative pyrazole acids (23d) are depicted in Schemes 16-21. The synthesis of 23d in Scheme 16 involves as the key step introduction of the R 5 (c) substituent via arylation or alkylation of the pyrazole. The arylating or alkylating agent R 5 (c)-Lg (wherein Lg is a leaving group such as Cl, Br, I, sulfonates such as p-toluenesulfonate or methanesulfonate or sulfates such as —SO 2 OR 5 (c)) includes R 5 (c) groups such as C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 2 -C 6  alkylcarbonyl, C 2 -C 6  alkoxycarbonyl, C 3 -C 8  dialkylaminocarbonyl, C 3 -C 6  trialkylsilyl; or phenyl, benzyl, benzoyl, 5- or 6-membered heteroaromatic ring each ring or ring system optionally substituted. Oxidation of the methyl group affords the pyrazole carboxylic acid. Some of the more preferred R 5 (d) groups include haloalkyl.  
                 
 
       [0134] Synthesis of pyrazoles of Formula 23d are described in Scheme 17. These acids may be prepared via metallation of compounds of Formula 40 with lithium diisopropylamide (LDA) followed by quenching of the lithium salt with carbon dioxide affords metallation using lithium diisoprylamide (LDA) and carboxylation of compounds of Formula 40 as the key step. The R 5 (c) group is introduced in a manner similar to that of Scheme 16, i.e. via alkylation or arylation with a compound of Formula 37. Representative R 5 (d) groups include e.g. cyano, haloalkyl and halogen.  
                 
 
       [0135] This procedure is particularly useful for preparing 1-(2-pyridinyl)pyrazolecarboxylic acids of Formula 23e as shown in Scheme 18. Reaction of a pyrazole of Formula 39 with a 2,3-dihalopyridine of Formula 37a affords good yields of the l-pyridylpyrazole of Formula 40a with good specificity for the desired regiochemistry. Metallation and carboxylation of compounds of Formula 40a as described above affords the 1-(2-pyridinyl)pyrazolecarboxylic acid of Formula 23e.  
                 
 
       [0136] The synthesis of pyrazoles of Formula 4c is described in Scheme 19. They can be prepared via reaction of an optionally substituted phenyl hydrazine of Formula 41 with a ketopyruvate of Formula 42 to yield pyrazole esters of Formula 43. Hydrolysis of the esters affords the pyrazole acids of Formula 23d. This procedure is particularly useful for the preparation of compounds in which R 5 (c) is optionally substituted phenyl and R 5 (d) is haloalkyl.  
                 
 
       [0137] An alternate synthesis of pyrazole acids of Formula 23d is described in Scheme 20. They can be prepared via 3+2 cycloaddition of an appropriately substituted nitrilimine with either substituted propiolates of Formula 45 or acrylates of Formula 47. Cycloaddition with an acrylate requires additional oxidation of the intermediate pyrazoline to the pyrazole. Hydrolysis of the esters affords the pyrazole acids of Formula 23d. Preferred iminohalides for this reaction include the trifluoromethyl iminochloride of Formula 48 and the iminodibromide of Formula 49. Compounds such as 48 are known ( J. Heterocycl. Chem.  1985, 22(2), 565-8). Compounds such as 49 are available by known methods ( Tetrahedron Letters  1999, 40, 2605). These procedures are particularly useful for the preparation of compounds where R 5 (c) is optionally substituted phenyl and R 5 (d) is haloalkyl or bromo.  
                 
 
       [0138] The starting pyrazoles of Formula 39 are known compounds. The pyrazole of Formula 39a (the compound of Formula 39 wherein R 5 (d) is CF 3 ) is commercially available. The pyrazoles of Formula 39c (compounds of Formula 39 wherein R 5 (d) is Cl or Br) can be prepared by literature procedures ( Chem. Ber.  1966, 99(10), 33507). A useful alternative method for the preparation of compound 39c is depicted in Scheme 21. Metallation of the sulfamoyl pyrazole of Formula 50 with n-butyllithium followed by direct halogenation of the anion with either hexachloroethane (for R 5 (d) being Cl) or 1,2-dibromotetrachloroethane (for R 5 (d) being Br) affords the halogenated derivatives of Formula 51. Removal of the sulfamoyl group with trifluoroacetic acid (TFA) at room temperature proceeds cleanly and in good yield to afford the pyrazoles of Formula 39c. One skilled in the art will recognize that Formula 39c is a tautomer of Formula 39b.  
                 
 
       [0139] It is recognized that some reagents and reaction conditions described above for preparing compounds of Formula I and Formula II may not be compatible with certain functional groups present in the intermediates. In these instances, the incorporation of protection/deprotection sequences or functional group interconversions into the synthesis will aid in obtaining the desired products. The use and choice of the protecting groups will be apparent to one skilled in chemical synthesis (see, for example, Greene, T. W.; Wuts, P. G. M.  Protective Groups in Organic Synthesis,  2nd ed.; Wiley: New York, 1991). One skilled in the art will recognize that, in some cases, after the introduction of a given reagent as it is depicted in any individual scheme, it may be necessary to perform additional routine synthetic steps not described in detail to complete the synthesis of compounds of Formula I and II. One skilled in the art will also recognize that it may be necessary to perform a combination of the steps illustrated in the above schemes in an order other than that implied by the particular sequence presented to prepare the compounds of Formula I and II.  
       [0140] One skilled in the art will also recognize that compounds of Formula I and II and the intermediates described herein can be subjected to various electrophilic, nucleophilic, radical, organometallic, oxidation, and reduction reactions to add substituents or modify existing substituents.  
       [0141] Without further elaboration, it is believed that one skilled in the art using the preceding description can utilize the present invention to its fullest extent. The following Examples are, therefore, to be construed as merely illustrative, and not limiting of the disclosure in any way whatsoever.  1 H NMR spectra are reported in ppm downfield from tetramethylsilane: s is singlet, d is doublet, t is triplet, q is quartet, m is multiplet, dd is doublet of doublets, dt is doublet of triplets, br s is broad singlet. m.p. is melting point. 
     
    
    
     EXAMPLE 1  
     Preparation of N-methyl-N′-(2-bromo-4-fluoropheny)-1,8-naphthalene-dicarboxamide  
     [0142] Step A: Preparation of 8-[(methylamino)carbonyl]-1-naphthalenecarboxylic Acid  
     [0143] To a stirred solution of 1,8-naphthalic anhydride (5 g, 25.3 mmole) in N,N-dimethylformarnmide (50 mL) at room temperature, methylamine (0.82 g, 26.5 mmole) in N,N-dimethylformamide (5 mL) was added. The reaction mixture was stirred for 2.5 hours. The solvent was removed under reduced pressure. The crude solid thus obtained was washed with a small amount of diethyl ether and air dried to give the product (5 g), containing 8-[(methylamino)carbonyl]-1-naphthalenecarboxylic acid and 1,8-naphthalic anhydride in a ratio of ˜7 to 1 determined by NMR analysis. This material was used for the subsequent reaction without further purification.  
     [0144] 1 H NMR (DMSO-d6) δ: 2.77 (doublet, 3H), 7.55-7.65 (multiplet, 3H), 7.83 (doublet, 1H), 8.03-8.12 (multiplet, 2H), 8.39 (quartet, 1H).  
     [0145] Step B: Preparation of N-methyl —N′-(2-bromo-4-fluoropheny)-1,8-naphthalene-dicarboxamide  
     [0146] To a stirred solution of 8-[(methylamino)carbonyl]-1-naphthalenecarboxylic acid (22.3 g, 97.4 mmole) prepared as described in Step A and pyridine (15.4 g, 0.195 mole) in dichloromethane (300 mL) cooled to −5° C. under nitrogen atmosphere, trifluroacetic anhydride (22.5 g, 0.107 mole) diluted in dichloromethane (50 mL) was added in a dropwise manner. After the addition, the reaction mixture was further stirred at ambient temperature for one half of an hour. A small amount of solid was filtered off. The filtrate was concentrated under reduced pressure to a solid that was extracted with hot hexane (3×250 ml). The hexane extracts were combined and concentrated under reduced pressure to give a crude product of 3-(methylimino)-1H,3H-naphtho[1,8-cd]pyran-1-one (15 g).  
     [0147] The 3-(methylimino)-1H,3H-naphtho[1,8-cd]pyran-1-one (0.25 g, 1.19 mmole) thus obtained was dissolved in dichloromethiane (3 ml) and 2-bromo-4-fluoroaniline (0.17 g, 1.45 mmole) was added. The reaction mixture was stirred at room temperature for 48 hours. The solid was filtered, collected and washed with a small amount of methanol in dichloromethane and air dried to give N-methyl N′-(2-methyl-4-fluoropheny)-1,8-naphthalene-dicarboxamide (0.12 g, m.p. 249° C.).  
     [0148] 1 H NMR (DMSO-d 6 ) δ: 2.37 (singlet, 3H), 2.72 (doublet, 3H), 7.05-7.12 (multiplet, 2H), 7.54-7.64 (multiplet, 3H), 7.75-7.83 (multiplet, 2H), 8.05-8.10 (multiplet, 2H), 8.33 (quartet, 1H.), 9.84 (singlet, 1H).  
     EXAMPLE 2  
     Preparation of N-methyl 8-[(3,4-difluorophenyl)carbonylamino]-1-naphthalenecarboxamide  
     [0149] Step A: Preparation of N-methyl 8-nitro-1-naphthalenecarboxamide  
     [0150] To a stirred solution of 8-nitro-1-naphthalenecarboxylic acid (1.5 g, 6.9 mmole), methylamine (0.22 g, 7.3 mmole), and imidazole (0.68 g, 8.3 mmole) in N,N-dimethylformamide (12 mL) at room temperature, diethyl cyanophosphonate (1.24 g, 7.6 mmole) was added. The reaction mixture was stirred overnight, poured into water (100 mL) and extracted with ethyl acetate (3×100 mL). The ethyl acetate extracts were combined, dried over anhydrous magnesium sulfate, filtered, and concentrated under reduced pressure to give a solid which was washed with a small amount of methanol to give the product (0.64 g) which was used without further purification.  
     [0151] 1 H NMR (DMSO-d 6 ) δ: 2.76 (doublet, 3H), 7.72-8.37 (multiplet, 6H), 8.66 (broad quartet, 1H).  
     [0152] Step B: Preparation of N-methyl 8-amino-1-naththalenecarboxamide  
     [0153] N-methyl 8-nitro-1-naphthalenecarboxamide (0.5 g, 2.17 mmole) in methanol (5 mL) and dichlomethane (15 mL) was hydrogenated with a catalytic amount of palladium (10% on charcoal) under 30 psi hydrogen pressure for 1 hour. The reaction mixture was suction filtered through celite and concentrated under reduced pressure to provide the product (0.42 g) which was used without further purification.  
     [0154] 1 H NMR (DMSO-d6) δ: 2.82 (doublet, 3H), 5.46 (singlet, 2H), 6.81-7.85 (multiplet, 6H), 8.59 (broad quartet, 1H).  
     [0155] Step C: Preparation of N-methyl 8-[(3,4-difluorophenyl)carbonylamino]-1-naphthalenecarboxamide  
     [0156] To a stirred solution of N-methyl 8-amino-1-naphthalenecarboxamide (0.2 g, 1 mmole) and pyridine (0.24 g, 3 mmole) in dichloromethane (10 mL), actyl chloride (94.2 mg, 1.2 mmole) in dichloromethane (2 mL) was added in portions. The mixture was stirred for 3 hours. The solid was collected with suction filtration (110 mg, m.p. &gt;250° C.).  
     [0157] 1 H NMR (DMSO-d6) δ: 2.43 (doublet, 3H), 7.46-8.10 (multiplet, 9H), 8.51 (broad quartet, 1H), 10.13 (singlet, 1H).  
     EXAMPLE 3  
     Preparation of N-methyl 8-[(2-thienyl)carbonylamino]-1-naphthalenecarboxamide  
     [0158] To a stirred solution of N-methyl 8-amino-1-naphthalenecarboxamide (0.2 g, 1 mmole) and pyridine (0.24 g, 3 mmole) in dichloromethane (10 mL), 2-thiophenecarboxylic acid chloride (176 mg, 1.2 mmole) in dichloromethane (2 mL) was added in portions. The mixture was stirred for 3 hours. The reaction mixture was washed sequentially with dilute hydrochloric acid, saturated sodium bicarbonate aqueous solution, and water. The solvent was partially removed under reduced pressure. The solid thus formed was collected with suction filtration (36 mg, m.p. 210° C.).  1 H NMR (DMSO-d6) δ: 2.53 (doublet, 3H), 7.26-8.10 (multiplet, 9H), 8.66 (broad quartet, 1H), 10.07 (singlet, 1H).  
     [0159] By the procedures described herein together with methods known in the art, the following compounds of Tables 1 to 10 can be prepared. The following abbreviations are used in the Tables: 1 is tertiary, s is secondary, z is normal, i is iso, c is cyclo, Me is methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, t-Bu is tert butyl, Ph is phenyl, OMe is methoxy, OEt is ethoxy, SMe is methylthio, SEt is ethylthio, CN is cyano, NO 2  is nitro, TMS is trimethylsilyl, S(O)Me is methylsulfinyl, and S(O) 2 Me is methylsulfonyl.  
               TABLE 1                                                                                              R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3         Me   H   Me   H   OCF 3         Et   H   Me   H   OCF 3         Me   H   Me   Me   Br       Me   H   Me   Et   Br       Me   H   Me   Me   Cl       Me   H   Me   Et   Cl       Me   H   Me   Me   I       Me   H   Me   Me   CF 3         Me   H   Me   Me   OCF 3         Et   H   Me   Me   CF 3         Me   H   Me   Me   SCF 3         Me   H   Me   Me   SCHF 2         Me   H   Me   Me   OCHF 2         n-Pr   H   Me   Me   CF 3         Me   H   Me   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5         Me   H   Me   Et   CF 3         Me   H   Me   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3         Me   H   Me   Cl   CF 3         Me   H   Me   F   CF 3         Me   H   Me   Me   SMe       Me   H   Me   Me   OMe       Me   H   Me   Me   OEt       Me   H   Me   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7         Me   H   Me   Me   Et       Me   H   Me   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2         Me   H   Me   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3         Me   H   Me   CF 3     Me       Me   H   Me   OMe   CF 3         Me   H   Me   H   CF 3         Me   H   Me   H   OCHF 2         Me   H   Me   H   C 2 F 5         Et   H   Me   H   C 2 F 5         Me   H   Me   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7         Me   H   Me   H   Br       Me   H   Me   H   Cl       Me   H   Me   H   SCF 3         Me   H   Me   Ph   CF 3         Me   H   Me   Ph   Cl       Me   H   Me   Ph   Br       Me   H   Me   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br       Me   H   Me   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3                     pyridyl           Me   H   Me   3-Me-2-   CF 3                     pyridyl           Me   H   Me   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3         Me   Me   H   H   OCF 3         Et   Me   H   H   OCF 3         Me   Me   H   Me   Br       Me   Me   H   Et   Br       Me   Me   H   Me   Cl       Me   Me   H   Et   Cl       Me   Me   H   Me   I       Me   Me   H   Me   CF 3         Me   Me   H   Me   OCF 3         Et   Me   H   Me   CF 3         Me   Me   H   Me   SCF 3         Me   Me   H   Me   SCHF 2         Me   Me   H   Me   OCHF 2         n-Pr   Me   H   Me   CF 3         Me   Me   H   Me   C 2 F 5         Et   Me   H   Me   C 2 F 5         Me   Me   H   Et   CF 3         Me   Me   H   n-Pr   CF 3         Me   Me   H   i-Pr   CF 3         Me   Me   H   Cl   CF 3         Me   Me   H   F   CF 3         Me   Me   H   Me   SMe       Me   Me   H   Me   OMe       Me   Me   H   Me   OEt       Me   Me   H   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   Et       Me   Me   H   Me   OCF 2 CHF 2         Me   Me   H   Me   SCF 2 CHF 2         Me   Me   H   Me   SO 2 Me       Me   Me   H   Me   SO 2 CF 3         Me   Me   H   CF 3     CF 3         Me   Me   H   CF 3     Me       Me   Me   H   OMe   CF 3         Me   Me   H   H   CF 3         Me   Me   H   H   OCHF 2         Me   Me   H   H   C 2 F 5         Et   Me   H   H   C 2 F 5         Me   Me   H   H   OCF 3         Me   Me   H   H   OCF 2 CHF 2         Me   Me   H   H   SCF 2 CHF 2         Me   Me   H   H   n-C 3 F 7         Me   Me   H   H   i-C 3 F 7         Me   Me   H   H   Br       Me   Me   H   H   Cl       Me   Me   H   H   SCF 3         Me   Me   H   Ph   CF 3         Me   Me   H   Ph   Cl       Me   Me   H   Ph   Br       Me   Me   H   2-pyridyl   CF 3         Me   Me   H   2-pyridyl   Cl       Me   Me   H   2-ClPh   CF 3         Me   Me   H   2-ClPh   OCF 3         Me   Me   H   2-ClPh   Br       Me   Me   H   2-ClPh   Cl       Me   Me   H   2-ClPh   SCHF 2         Me   Me   H   2-BrPh   CF 3         Me   Me   H   2-MePh   CF 3         Me   Me   H   2-CNPh   CF 3         Me   Me   H   2-FPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3         Me   Me   H   2-MeOPh   CF 3         Me   Me   H   3-Cl-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   OCF 3         Me   Me   H   3-CF 3 -2-   CF 3                     pyridyl           Me   Me   H   3-Me-2-   CF 3                     pyridyl           Me   Me   H   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-F-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Br-2-pyridyl   Br       Me   Me   H   3-Br-2-pyridyl   Cl       Me   Cl   H   Me   Br       Me   Cl   H   Et   Br       Me   Cl   H   Me   Cl       Me   Cl   H   Et   Cl       Me   Cl   H   Me   I       Me   Cl   H   Me   CF 3         Me   Cl   H   Me   OCF 3         Et   Cl   H   Me   CF 3         Me   Cl   H   Me   SCF 3         Me   Cl   H   Me   SCHF 2         Me   Cl   H   Me   OCHF 2         n-Pr   Cl   H   Me   CF 3         Me   Cl   H   Me   C 2 F 5         Et   Cl   H   Me   C 2 F 5         Me   Cl   H   Et   CF 3         Me   Cl   H   n-Pr   CF 3         Me   Cl   H   i-Pr   CF 3         Me   Cl   H   Cl   CF 3         Me   Cl   H   F   CF 3         Me   Cl   H   Me   SMe       Me   Cl   H   3-Me-2-   CF 3                     pyridyl           Me   Cl   H   Me   OEt       Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   Et       Me   Cl   H   Me   OCF 2 CHF 2         Me   Cl   H   Me   SCF 2 CHF 2         Me   Cl   H   Me   SO 2 Me       Me   Cl   H   Me   SO 2 CF 3         Me   Cl   H   CF 3     CF 3         Me   Cl   H   CF 3     Me       Me   Cl   H   OMe   CF 3         Me   Cl   H   H   CF 3         Me   Cl   H   H   OCHF 2         Me   Cl   H   H   C 2 F 5         Et   Cl   H   H   C 2 F 5         Me   H   H   H   CF 3         Me   H   H   H   OCF 3         Et   H   H   H   OCF 3         Me   H   H   Me   Br       Me   H   H   Et   Br       Me   H   H   Me   Cl       Me   H   H   Et   Cl       Me   H   H   Me   I       Me   H   H   Me   CF 3         Me   H   H   Me   OCF 3         Et   H   H   Me   CF 3         Me   H   H   Me   SCF 3         Me   H   H   Me   SCHF 2         Me   H   H   Me   OCHF 2         n-Pr   H   H   Me   CF 3         Me   H   H   Me   C 2 F 5         Et   H   H   Me   C 2 F 5         Me   H   H   Et   CF 3         Me   H   H   n-Pr   CF 3         Me   H   H   i-Pr   CF 3         Me   H   H   Cl   CF 3         Me   H   H   F   CF 3         Me   H   H   Me   SMe       Me   H   H   Me   OMe       Me   H   H   Me   OEt       Me   H   H   Me   n-C 3 F 7         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   Et       Me   H   H   Me   OCF 2 CHF 2         Me   H   H   Me   SCF 2 CHF 2         Me   Me   H   Me   SO 2 Me       Me   H   H   Me   SO 2 CF 3         Me   H   H   CF 3     CF 3         Me   H   H   CF 3     Me       Me   H   H   OMe   CF 3         Me   H   H   H   CF 3         Me   H   H   H   OCHF 2         Me   H   H   H   C 2 F 5         Et   H   H   H   C 2 F 5         Me   H   H   H   OCF 3         Me   H   H   H   OCF 2 CHF 2         Me   H   H   H   SCF 2 CHF 2         Me   H   H   H   n-C 3 F 7         Me   H   H   H   i-C 3 F 7         Me   H   H   H   Br       Me   H   H   H   Cl       Me   H   H   H   SCF 3         Me   H   H   Ph   CF 3         Me   H   H   Ph   Cl       Me   H   H   Ph   Br       Me   H   H   2-pyridyl   CF 3         Me   H   H   2-pyridyl   Cl       Me   H   H   2-ClPh   CF 3         Me   H   H   2-ClPh   OCF 3         Me   H   H   2-ClPh   Br       Me   H   H   2-ClPh   Cl       Me   H   H   2-ClPh   SCHF 2         Me   H   H   2-BrPh   CF 3         Me   H   H   2-MePh   CF 3         Me   H   H   2-CNPh   CF 3         Me   H   H   2-FPh   CF 3         Me   H   H   2,6-F 2 Ph   CF 3         Me   H   H   2,4-F 2 Ph   CF 3         Me   H   H   2,5-F 2 Ph   CF 3         Me   H   H   2-MeOPh   CF 3         Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   H   3-Cl-2-pyridyl   Br       Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   H   3-F-2-pyridyl   CF 3         Me   H   H   3-CF 3 -2-   CF 3                     pyridyl       Me   H   H   3-Me-2-   CF 3                     pyridyl       Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   H   3-Br-2-pyridyl   Br       Me   H   H   3-Br-2-pyridyl   Cl       Me   H   Cl   Et   Br       Me   H   Cl   Me   Cl       Me   H   Cl   Et   Cl       Me   H   Cl   Me   I       Me   H   Cl   Me   CF 3         Me   H   Cl   Me   OCF 3         Et   H   Cl   Me   CF 3         Me   H   Cl   Me   SCF 3         Me   H   Cl   Me   SCHF 2         Me   H   Cl   Me   OCHF 2         n-Pr   H   Cl   Me   CF 3         Me   H   Cl   Me   C 2 F 5         Et   H   Cl   Me   C 2 F 5         Me   H   Cl   Et   CF 3         Me   H   Cl   n-Pr   CF 3         Me   H   Cl   i-Pr   CF 3         Me   H   Cl   Cl   CF 3         Me   H   Cl   F   CF 3         Me   H   Cl   Me   SMe       Me   H   Cl   Me   OMe       Me   H   Cl   Me   OEt       Me   H   Cl   Me   n-C 3 F 7         Me   H   Cl   Me   i-C 3 F 7         Me   H   Cl   Me   Et       Me   H   Cl   Me   OCF 2 CHF 2         Me   H   Cl   Me   SCF 2 CHF 2         Me   H   Cl   Me   SO 2 Me       Me   H   Cl   Me   SO 2 CF 3         Me   H   Cl   CF 3     CF 3         Me   H   Cl   CF 3     Me       Me   H   Cl   OMe   CF 3         Me   H   Cl   H   CF 3         Me   H   Cl   H   OCHF 2         Me   H   Cl   H   C 2 F 5         Et   H   Cl   H   C 2 F 5         Me   H   Cl   H   OCF 3         Me   H   Cl   H   OCF 2 CHF 2         Me   H   Cl   H   SCF 2 CHF 2         Me   H   Cl   H   n-C 3 F 7         Me   H   Cl   H   i-C 3 F 7         Me   H   Cl   H   Br       Me   H   Cl   H   Cl       Me   H   Cl   H   SCF 3         Me   H   Cl   Ph   CF 3         Me   H   Cl   Ph   Cl       Me   H   Cl   Ph   Br       Me   H   Cl   2-pyridyl   CF 3         Me   H   Cl   2-pyridyl   Cl       Me   H   Cl   2-ClPh   CF 3         Me   H   Cl   2-ClPh   OCF 3         Me   H   Cl   2-ClPh   Br       Me   H   Cl   2-ClPh   Cl       Me   H   Cl   2-ClPh   SCHF 2         Me   H   Cl   2-BrPh   CF 3         Me   H   Cl   2-MePh   CF 3         Me   H   Cl   2-CNPh   CF 3         Me   H   Cl   2-FPh   CF 3         Me   H   Cl   2,6-F 2 Ph   CF 3         Me   H   Cl   2,4-F 2 Ph   CF 3         Me   H   Cl   2,5-F 2 Ph   CF 3         Me   H   Cl   2-MeOPh   CF 3         Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   H   Cl   3-Cl-2-pyridyl   Br       Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   H   Cl   3-F-2-pyridyl   CF 3         Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl       Me   H   Cl   3-Me-2-   CF 3                     pyridyl       Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   H   Cl   3-Br-2-pyridyl   Br       Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Cl   H   Ph   CF 3         Me   Cl   H   Ph   Cl       Me   Cl   H   Ph   Br       Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   2-ClPh   OCF 3         Me   Cl   H   2-ClPh   Br       Me   Cl   H   2-ClPh   Cl       Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   2-MePh   CF 3         Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   2-FPh   CF 3         Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   2,5-F,Ph   CF 3         Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   3-CF 3 -2-   CF 3                     pyridyl       Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   3-Br-2-pyridyl   Cl       Me   Cl   H   H   OCF 3         Me   Cl   H   H   OCF 2 CHF 2         Me   Cl   H   H   SCF 2 CHF 2         Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   H   Br       Me   Cl   H   H   Cl       Me   Cl   H   H   SCF 3         Me   Cl   H   Ph   CF 3         Me   Cl   H   Me   OMe                  
 
     [0160]               TABLE 2                                                                                              R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3         Me   H   Me   H   OCF 3         Et   H   Me   H   OCF 3         Me   H   Me   Me   Br       Me   H   Me   Et   Br       Me   H   Me   Me   Cl       Me   H   Me   Et   Cl       Me   H   Me   Me   I       Me   H   Me   Me   CF 3         Me   H   Me   Me   OCF 3         Et   H   Me   Me   CF 3         Me   H   Me   Me   SCF 3         Me   H   Me   Me   SCHF 2         Me   H   Me   Me   OCHF 2         n-Pr   H   Me   Me   CF 3         Me   H   Me   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5         Me   H   Me   Et   CF 3         Me   H   Me   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3         Me   H   Me   Cl   CF 3         Me   H   Me   F   CF 3         Me   H   Me   Me   SMe       Me   H   Me   Me   OMe       Me   H   Me   Me   OEt       Me   H   Me   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7         Me   H   Me   Me   Et       Me   H   Me   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3         Me   H   Me   CF 3     Me       Me   H   Me   OMe   CF 3         Me   H   Me   H   CF 3         Me   H   Me   H   OCHF 2         Me   H   Me   H   C 2 F 5         Et   H   Me   H   C 2 F 5         Me   H   Me   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7         Me   H   Me   H   Br       Me   H   Me   H   Cl       Me   H   Me   H   SCF 3         Me   H   Me   Ph   CF 3         Me   H   Me   Ph   Cl       Me   H   Me   Ph   Br       Me   H   Me   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br       Me   H   Me   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3-2-     CF 3                     pyridyl           Me   H   Me   3-Me-2-   CF 3                     pyridyl           Me   H   Me   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3         Me   Me   H   H   OCF 3         Et   Me   H   H   OCF 3         Me   Me   H   Me   Br       Me   Me   H   Et   Br       Me   Me   H   Me   Cl       Me   Me   H   Cl   Et       Me   Me   H   Me   I       Me   Me   H   Me   CF 3         Me   Me   H   Me   OCF 3         Et   Me   H   Me   CF 3         Me   Me   H   Me   SCF 3         Me   Me   H   Me   SCHF 2         Me   Me   H   Me   OCHF 2         n-Pr   Me   H   Me   CF 3         Me   Me   H   Me   C 2 F 5         Et   Me   H   Me   C 2 F 5         Me   Me   H   Et   CF 3         Me   Me   H   n-Pr   CF 3         Me   Me   H   i-Pr   CF 3         Me   Me   H   Cl   CF 3         Me   Me   H   F   CF 3         Me   Me   H   Me   SMe       Me   Me   H   Me   OMe       Me   Me   H   Me   OEt       Me   Me   H   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   Et       Me   Me   H   Me   OCF 2 CHF 2         Me   Me   H   Me   SCF 2 CHF 2         Me   Me   H   Me   SO 2 Me       Me   Me   H   Me   SO 2 CF 3         Me   Me   H   CF 3     CF 3         Me   Me   H   CF 3     Me       Me   Me   H   OMe   CF 3         Me   Me   H   H   CF 3         Me   Me   H   H   OCHF 2         Me   Me   H   H   C 2 F 5         Et   Me   H   H   C 2 F 5         Me   Me   H   H   OCF 3         Me   Me   H   H   OCF 2 CHF 2         Me   Me   H   H   SCF 2 CHF 2         Me   Me   H   H   n-C 3 F 7         Me   Me   H   H   i-C 3 F 7         Me   Me   H   H   Br       Me   Me   H   H   Cl       Me   Me   H   H   SCF 3         Me   Me   H   Ph   CF 3         Me   Me   H   Ph   Cl       Me   Me   H   Ph   Br       Me   Me   H   2-pyridyl   CF 3         Me   Me   H   2-pyridyl   Cl       Me   Me   H   2-ClPh   CF 3         Me   Me   H   2-ClPh   OCF 3         Me   Me   H   2-ClPh   Br       Me   Me   H   2-ClPh   Cl       Me   Me   H   2-ClPh   SCHF 2         Me   Me   H   2-BrPh   CF 3         Me   Me   H   2-MePh   CF 3         Me   Me   H   2-CNPh   CF 3         Me   Me   H   2-FPh   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3         Me   Me   H   2-MeOPh   CF 3         Me   Me   H   3-Cl-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   OCF 3         Me   Me   H   3-CF 3-2-     CF 3                     pyridyl           Me   Me   H   3-Me-2-   CF 3                     pyridyl           Me   Me   H   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-F-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Br-2-pyridyl   Br       Me   Me   H   3-Br-2-pyridyl   Cl       Me   Cl   H   Me   Br       Me   Cl   H   Et   Br       Me   Cl   H   Me   Cl       Me   Cl   H   Et   Cl       Me   Cl   H   Me   Cl       Me   Cl   H   Me   CF 3         Me   Cl   H   Me   OCF 3         Et   Cl   H   Me   CF 3         Me   Cl   H   Me   SCF 3         Me   Cl   H   Me   SCHF 2         Me   Cl   H   Me   OCHF 2         n-Pr   Cl   H   Me   CF 3         Me   Cl   H   Me   C 2 F 5         Et   Cl   H   Me   C 2 F 5         Me   Cl   H   Et   CF 3         Me   Cl   H   n-Pr   CF 3         Me   Cl   H   i-Pr   CF 3         Me   Cl   H   Cl   CF 3         Me   Cl   H   F   CF 3         Me   Cl   H   Me   SMe       Me   Cl   H   Me   OMe       Me   Cl   H   Me   OEt       Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   Et       Me   Cl   H   Me   OCF 2 CHF 2         Me   Cl   H   Me   SCF 2 CHF 2         Me   Cl   H   Me   SO 2 Me       Me   Cl   H   Me   SO 2 CF 3         Me   Cl   H   3-CF 3-2-     CF 3                     pyridyl           Me   Cl   H   CF 3     Me       Me   Cl   H   OMe   CF 3         Me   Cl   H   H   CF 3         Me   Cl   H   H   OCHF 2         Me   Cl   H   H   C 2 F 5         Me   H   H   H   CF 3         Me   H   H   H   OCF 3         Et   H   H   H   OCF 3         Me   H   H   Me   Br       Me   H   H   Et   Br       Me   H   H   Me   Cl       Me   H   H   Et   Cl       Me   H   H   Me   I       Me   H   H   Me   CF 3         Me   H   H   Me   OCF 3         Et   H   H   Me   CF 3         Me   H   H   Me   SCF 3         Me   H   H   Me   SCHF 2         Me   H   H   Me   OCHF 2         n-Pr   H   H   Me   CF 3         Me   H   H   Me   C 2 F 5         Et   H   H   Me   C 2 F 5         Me   H   H   Et   CF 3         Me   H   H   n-Pr   CF 3         Me   H   H   i-Pr   CF 3         Me   H   H   Cl   CF 3         Me   H   H   F   CF 3         Me   H   H   Me   SMe       Me   H   H   Me   OMe       Me   H   H   Me   OEt       Me   H   H   Me   n-C 3 F 7         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   Et       Me   H   H   Me   OCF 2 CHF 2         Me   H   H   Me   SCF 2 CHF 2         Me   H   H   Me   SO 2 Me       Me   H   H   Me   SO 2 CF 3         Me   H   H   CF 3     CF 3         Me   H   H   CF 3     Me       Me   H   H   OMe   CF 3         Me   H   H   H   CF 3         Me   H   H   H   OCHF 2         Me   H   H   H   C 2 F 5         Et   H   H   H   C 2 F 5         Me   H   H   H   OCF 3         Me   H   H   H   OCF 2 CHF 2         Me   H   H   H   SCF 2 CHF 2         Me   H   H   H   n-C 3 F 7         Me   H   H   H   i-C 3 F 7         Me   H   H   H   Br       Me   H   H   H   Cl       Me   H   H   H   SCF 3         Me   H   H   Ph   CF 3         Me   H   H   Ph   Cl       Me   H   H   Ph   Br       Me   H   H   2-pyridyl   CF 3         Me   H   H   2-pyridyl   Cl       Me   H   H   2-ClPh   CF 3         Me   H   H   2-ClPh   OCF 3         Me   H   H   2-ClPh   Br       Me   H   H   2-ClPh   Cl       Me   H   H   2-ClPh   SCHF 2         Me   H   H   2-BrPh   CF 3         Me   H   H   2-MePh   CF 3         Me   H   H   2-CNPh   CF 3         Me   H   H   2-FPh   CF 3         Me   H   H   2,6-F 2 Ph   CF 3         Me   H   H   2,4-F 2 Ph   CF 3         Me   H   H   2,5-F 2 Ph   CF 3         Me   H   H   2-MeOPh   CF 3         Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   H   3-Cl-2-pyridyl   Br       Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   H   3-F-2-pyridyl   CF 3         Me   H   H   3-CF 3 -2-   CF 3                     pyridyl       Me   H   H   3-Me-2-   CF 3                     pyridyl       Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   H   3-Br-2-pyridyl   Br       Me   H   H   3-Br-2-pyridyl   Cl       Me   H   Cl   Et   Br       Me   H   Cl   Me   Cl       Me   H   Cl   Et   Cl       Me   H   Cl   Me   I       Me   H   Cl   Me   CF 3         Me   H   Cl   Me   OCF 3         H   Cl   Me   CF 3         Me   H   Cl   Me   SCF 3         Me   H   Cl   Me   SCHF 2         Me   H   Cl   Me   OCHF 2         n-Pr   H   Cl   Me   CF 3         Me   H   Cl   Me   C 2 F 5         Et   H   Cl   Me   C 2 F 5         Me   H   Cl   Et   CF 3         Me   H   Cl   n-Pr   CF 3         Me   H   Cl   i-Pr   CF 3         Me   H   Cl   Cl   CF 3         Me   H   Cl   F   CF 3         Me   H   Cl   Me   SMe       Me   H   Cl   Me   OMe       Me   H   Cl   Me   OEt       Me   H   Cl   Me   n-C 3 F 7         Me   H   Cl   Me   i-C 3 F 7         Me   H   Cl   Me   Et       Me   H   Cl   Me   OCF 2 CHF 2         Me   H   Cl   Me   SCF 2 CHF 2         Me   H   Cl   Me   SO 2 Me       Me   H   Cl   Me   SO 2 CF 3         Me   H   Cl   CF 3     CF 3         Me   H   Cl   CF 3     Me       Me   H   Cl   OMe   CF 3         Me   H   Cl   H   CF 3         Me   H   Cl   H   OCHF 2         Me   H   Cl   H   C 2 F 5         Et   H   Cl   H   C 2 F 5         Me   H   Cl   H   OCF 3         Me   H   Cl   H   OCF 2 CHF 2         Me   H   Cl   H   SCF 2 CHF 2         Me   H   Cl   H   n-C 3 F 7         Me   H   Cl   H   i-C 3 F 7         Me   H   Cl   H   Br       Me   H   Cl   H   Cl       Me   H   Cl   H   SCF 3         Me   H   Cl   Ph   CF 3         Me   H   Cl   Ph   Cl       Me   H   Cl   Ph   Br       Me   H   Cl   2-pyridyl   CF 3         Me   H   Cl   2-pyridyl   Cl       Me   H   Cl   2-ClPh   CF 3         Me   H   Cl   2-ClPh   OCF 3         Me   H   Cl   2-ClPh   Br       Me   H   Cl   2-ClPh   Cl       Me   H   Cl   2-ClPh   SCHF 2         Me   H   Cl   2-BrPh   CF 3         Me   H   Cl   2-MePh   CF 3         Me   H   Cl   2-CNPh   CF 3         Me   H   Cl   2-FPh   CF 3         Me   H   Cl   2,6-FPh   CF 3         Me   H   Cl   2,4-F 2 Ph   CF 3         Me   H   Cl   2,5-F 2 Ph   CF 3         Me   H   Cl   2-MeOPh   CF 3         Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   H   Cl   3-Cl-2-pyridyl   Br       Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   H   Cl   3-F-2-pyridyl   CF 3         Me   H   Cl   3-CF 3-2-     CF 3                     pyridyl       Me   H   Cl   3-Me-2-   CF 3                     pyridyl       Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   H   Cl   3-Br-2-pyridyl   Br       Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Cl   H   H   OCF 3         Me   Cl   H   H   OCF 2 CHF 2         Me   Cl   H   H   SCF 2 CHF 2         Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   H   Br       Me   Cl   H   H   Cl       Me   Cl   H   H   SCF 3         Me   Cl   H   Ph   CF 3         Me   Cl   H   Ph   Cl       Me   Cl   H   Ph   Br       Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   2-ClPh   OCF 3         Me   Cl   H   2-ClPh   Br       Me   Cl   H   2-ClPh   Cl       Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   2-MePh   CF 3         Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   2-FPh   CF 3         Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   CF 3     CF 3         Me   Cl   H   3-Me-2-   CF 3                     pyridyl       Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   3-Br-2-pyridyl   Cl       Et   Cl   H   H   C 2 F 5                      
     [0161]               TABLE 3                                                                                              R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3         Me   H   Me   H   OCF 3         Et   H   Me   H   OCF 3         Me   H   Me   Me   Br       Me   H   Me   Et   Br       Me   H   Me   Me   Cl       Me   H   Me   Et   Cl       Me   H   Me   Me   I       Me   H   Me   Me   CF 3         Me   H   Me   Me   OCF 3         Et   H   Me   Me   CF 3         Me   H   Me   Me   SCF 3         Me   H   Me   Me   SCHF 2         Me   H   Me   Me   OCHF 2         n-Pr   H   Me   Me   CF 3         Me   H   Me   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5         Me   H   Me   Et   CF 3         Me   H   Me   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3         Me   H   Me   Cl   CF 3         Me   H   Me   F   CF 3         Me   H   Me   Me   SMe       Me   H   Me   Me   OMe       Me   H   Me   Me   OEt       Me   H   Me   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7         Me   H   Me   Me   Et       Me   H   Me   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3         Me   H   Me   CF 3     Me       Me   H   Me   OMe   CF 3         Me   H   Me   H   CF 3         Me   H   Me   H   OCHF 2         Me   H   Me   H   C 2 F 5         Et   H   Me   H   C 2 F 5         Me   H   Me   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7         Me   H   Me   H   Br       Me   H   Me   H   Cl       Me   H   Me   H   SCF 3         Me   H   Me   Ph   CF 3         Me   H   Me   Ph   Cl       Me   H   Me   Ph   Br       Me   H   Me   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br       Me   H   Me   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3                     pyridyl           Me   H   Me   3-Me-2-   CF 3                     pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3         Me   Me   H   H   OCF 3         Et   Me   H   H   OCF 3         Me   Me   H   Me   Br       Me   Me   H   Et   Br       Me   Me   H   Me   Cl       Me   Me   H   Et   Cl       Me   Me   H   Me   I       Me   Me   H   Me   CF 3         Me   Me   H   Me   OCF 3         Et   Me   H   Me   CF 3         Me   Me   H   Me   SCF 3         Me   Me   H   Me   SCHF 2         Me   Me   H   Me   OCHF 2         n-Pr   Me   H   Me   CF 3         Me   Me   H   Me   C 2 F 5         Et   Me   H   Me   C 2 F 5         Me   Me   H   Et   CF 3         Me   Me   H   n-Pr   CF 3         Me   Me   H   i-Pr   CF 3         Me   Me   H   Cl   CF 3         Me   Me   H   F   CF 3         Me   Me   H   Me   SMe       Me   Me   H   Me   OMe       Me   Me   H   Me   OEt       Me   Me   H   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   Et       Me   Me   H   Me   OCF 2 CHF 2         Me   Me   H   Me   SCF 2 CHF 2         Me   Me   H   Me   SO 2 Me       Me   Me   H   Me   SO 2 CF 3         Me   Me   H   CF 3     CF 3         Me   Me   H   CF 3     Me       Me   Me   H   OMe   CF 3         Me   Me   H   H   CF 3         Me   Me   H   H   OCHF 2         Me   Me   H   H   C 2 F 5         Et   Me   H   H   C 2 F 5         Me   Me   H   H   OCF 3         Me   Me   H   H   OCF 2 CHF 2         Me   Me   H   H   SCF 2 CHF 2         Me   Me   H   H   n-C 3 F 7         Me   Me   H   H   i-C 3 F 7         Me   Me   H   H   Br       Me   Me   H   H   Cl       Me   Me   H   H   SCF 3         Me   Me   H   Ph   CF 3         Me   Me   H   Ph   Cl       Me   Me   H   Ph   Br       Me   Me   H   2-pyridyl   CF 3         Me   Me   H   2-pyridyl   Cl       Me   Me   H   2-ClPh   CF 3         Me   Me   H   2-ClPh   OCF 3         Me   Me   H   2-ClPh   Br       Me   Me   H   2-ClPh   Cl       Me   Me   H   2-ClPh   SCHF 2         Me   Me   H   2-BrPh   CF 3         Me   Me   H   2-MePh   CF 3         Me   Me   H   2-CNPh   CF 3         Me   Me   H   2-FPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3         Me   Me   H   2-MeOPh   CF 3         Me   Me   H   3-Cl-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   OCF 3         Me   Me   H   3-CF 3 -2-   CF 3                     pyridyl           Me   Me   H   3-Me-2-   CF 3                     pyridyl           Me   Me   H   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-F-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Br-2-pyridyl   Br       Me   Me   H   3-Br-2-pyridyl   Cl       Me   Cl   H   Me   Br       Me   Cl   H   Et   Br       Me   Cl   H   Me   Cl       Me   Cl   H   Et   Cl       Me   Cl   H   Me   I       Me   Cl   H   Me   CF 3         Me   Cl   H   Me   OCF 3         Et   Cl   H   Me   CF 3         Me   Cl   H   Me   SCF 3         Me   Cl   H   Me   SCHF 2         Me   Cl   H   Me   OCHF 2         n-Pr   Cl   H   Me   CF 3         Me   Cl   H   Me   C 2 F 5         Et   Cl   H   Me   C 2 F 5         Me   Cl   H   Et   CF 3         Me   Cl   H   n-Pr   CF 3         Me   Cl   H   i-Pr   CF 3         Me   Cl   H   Cl   CF 3         Me   Cl   H   F   CF 3         Me   Cl   H   Me   SMe       Me   Cl   H   Me   OMe       Me   Cl   H   Me   OEt       Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   Et       Me   Cl   H   Me   OCF 2 CHF 2         Me   Cl   H   Me   SCF 2 CHF 2         Me   Cl   H   Me   SO 2 Me       Me   Cl   H   Me   SO 2 CF 3         Me   Cl   H   3-CF 3 -2-   CF 3                     pyridyl           Me   Cl   H   CF 3     Me       Me   Cl   H   OMe   CF 3         Me   Cl   H   H   CF 3         Me   Cl   H   H   OCHF 2         Me   Cl   H   H   C 2 F 5         Me   H   H   H   CF 3         Me   H   H   H   OCF 3         Et   H   H   H   OCF 3         Me   H   H   Me   Br       Me   H   H   Et   Br       Me   H   H   Me   Cl       Me   H   H   Et   Cl       Me   H   H   Me   I       Me   H   H   Me   CF 3         Me   H   H   Me   OCF 3         Et   H   H   Me   CF 3         Me   H   H   Me   SCF 3         Me   H   H   Me   SCHF 2         Me   H   H   Me   OCHF 2         n-Pr   H   H   Me   CF 3         Me   H   H   Me   C 2 F 5         Et   H   H   Me   C 2 F 5         Me   H   H   Et   CF 3         Me   H   H   n-Pr   CF 3         Me   H   H   i-Pr   CF 3         Me   H   H   Cl   CF 3         Me   H   H   F   CF 3         Me   H   H   Me   SMe       Me   H   H   Me   OMe       Me   H   H   Me   OEt       Me   H   H   Me   n-C 3 F 7         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   Et       Me   H   H   Me   OCF 2 CHF 2         Me   H   H   Me   SCF 2 CHF 2         Me   H   H   Me   SO 2 Me       Me   H   H   Me   SO 2 CF 3         Me   H   H   CF 3     CF 3         Me   H   H   CF 3     Me       Me   H   H   OMe   CF 3         Me   H   H   H   CF 3         Me   H   H   H   OCHF 2         Me   H   H   H   C 2 F 5         Et   H   H   H   C 2 F 5         Me   H   H   H   OCF 3         Me   H   H   H   OCF 2 CHF 2         Me   H   H   H   SCF 2 CHF 2         Me   H   H   H   n-C 3 F 7         Me   H   H   H   i-C 3 F 7         Me   H   H   H   Br       Me   H   H   H   Cl       Me   H   H   H   SCF 3         Me   H   H   Ph   CF 3         Me   H   H   Ph   Cl       Me   H   H   Ph   Br       Me   H   H   2-pyridyl   CF 3         Me   H   H   2-pyridyl   Cl       Me   H   H   2-ClPh   CF 3         Me   H   H   2-ClPh   OCF 3         Me   H   H   2-ClPh   Br       Me   H   H   2-ClPh   Cl       Me   H   H   2-ClPh   SCHF 2         Me   H   H   2-BrPh   CF 3         Me   H   H   2-MePh   CF 3         Me   H   H   2-CNPh   CF 3         Me   H   H   2-FPh   CF 3         Me   H   H   2,6-F 2 Ph   CF 3         Me   H   H   2,4-F 2 Ph   CF 3         Me   H   H   2,5-F 2 Ph   CF 3         Me   H   H   2-MeOPh   CF 3         Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   H   3-Cl-2-pyridyl   Br       Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   H   3-F-2-pyridyl   CF 3         Me   H   H   3-CF 3 -2-   CF 3                     pyridyl       Me   H   H   3-Me-2-   CF 3                     pyridyl       Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   H   3-Br-2-pyridyl   Br       Me   H   H   3-Br-2-pyridyl   Cl       Me   H   Cl   Et   Br       Me   H   Cl   Me   Cl       Me   H   Cl   Et   Cl       Me   H   Cl   Me   I       Me   H   Cl   Me   CF 3         Me   H   Cl   Me   OCF 3         Et   H   Cl   Me   CF 3         Me   H   Cl   Me   SCF 3         Me   H   Cl   Me   SCHF 2         Me   H   Cl   Me   OCHF 2         n-Pr   H   Cl   Me   CF 3         Me   H   Cl   Me   C 2 F 5         Et   H   Cl   Me   C 2 F 5         Me   H   Cl   Et   CF 3         Me   H   Cl   n-Pr   CF 3         Me   H   Cl   i-Pr   CF 3         Me   H   Cl   Cl   CF 3         Me   H   Cl   F   CF 3         Me   H   Cl   Me   SMe       Me   H   Cl   Me   OMe       Me   H   Cl   Me   OEt       Me   H   Cl   Me   n-C 3 F 7         Me   H   Cl   Me   i-C 3 F 7         Me   H   Cl   Me   Et       Me   H   Cl   Me   OCF 2 CHF 2         Me   H   Cl   Me   SCF 2 CHF 2         Me   H   Cl   Me   SO 2 Me       Me   H   Cl   Me   SO 2 CF 3         Me   H   Cl   CF 3     CF 3         Me   H   Cl   CF 3     Me       Me   H   Cl   OMe   CF 3         Me   H   Cl   H   CF 3         Me   H   Cl   H   OCHF 2         Me   H   Cl   H   C 2 F 5         Et   H   Cl   H   C 2 F 5         Me   H   Cl   H   OCF 3         Me   H   Cl   H   OCF 2 CHF 2         Me   H   Cl   H   SCF 2 CHF 2         Me   H   Cl   H   n-C 3 F 7         Me   H   Cl   H   i-C 3 F 7         Me   H   Cl   H   Br       Me   H   Cl   H   Cl       Me   H   Cl   H   SCF 3         Me   H   Cl   Ph   CF 3         Me   H   Cl   Ph   Cl       Me   H   Cl   Ph   Br       Me   H   Cl   2-pyridyl   CF 3         Me   H   Cl   2-pyridyl   Cl       Me   H   Cl   2-ClPh   CF 3         Me   H   Cl   2-ClPh   OCF 3         Me   H   Cl   2-ClPh   Br       Me   H   Cl   2-ClPh   Cl       Me   H   Cl   2-ClPh   SCHF 2         Me   H   Cl   2-BrPh   CF 3         Me   H   Cl   2-MePh   CF 3         Me   H   Cl   2-CNPh   CF 3         Me   H   Cl   2-FPh   CF 3         Me   H   Cl   2,6-F 2 Ph   CF 3         Me   H   Cl   2,4-F 2 Ph   CF 3         Me   H   Cl   2,5-F 2 Ph   CF 3         Me   H   Cl   2-MeOPh   CF 3         Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   H   Cl   3-Cl-2-pyridyl   Br       Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   H   Cl   3-F-2-pyridyl   CF 3         Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl       Me   H   Cl   3-Me-2-   CF 3                     pyridyl       Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   H   Cl   3-Br-2-pyridyl   Br       Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Cl   H   H   OCF 3         Me   Cl   H   H   OCF 2 CHF 2         Me   Cl   H   H   SCF 2 CHF 2         Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   H   Br       Me   Cl   H   H   Cl       Me   Cl   H   H   SCF 3         Me   Cl   H   Ph   CF 3         Me   Cl   H   Ph   Cl       Me   Cl   H   Ph   Br       Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   2-ClPh   OCF 3         Me   Cl   H   2-ClPh   Br       Me   Cl   H   2-ClPh   Cl       Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   2-MePh   CF 3         Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   2-FPh   CF 3         Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   CF 3     CF 3         Me   Cl   H   3-Me-2-   CF 3                     pyridyl       Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   3-Br-2-pyridyl   Cl       Et   Cl   H   H   C 2 F 5                      
     [0162]               TABLE 4                                                                                              R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3         Me   H   Me   H   OCF 3         Et   H   Me   H   OCF 3         Me   H   Me   Me   Br       Me   H   Me   Et   Br       Me   H   Me   Me   Cl       Me   H   Me   Et   Cl       Me   H   Me   Me   I       Me   H   Me   Me   CF 3         Me   H   Me   Me   OCF 3         Et   H   Me   Me   CF 3         Me   H   Me   Me   SCF 3         Me   H   Me   Me   SCHF 2         Me   H   Me   Me   OCHF 2         n-Pr   H   Me   Me   CF 3         Me   H   Me   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5         Me   H   Me   Et   CF 3         Me   H   Me   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3         Me   H   Mc   i-Pr   OCF 3         Me   H   Me   Me   SMe       Me   H   Me   Me   OMe       Me   H   Me   Me   OEt       Me   H   Me   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7         Me   H   Me   Me   Et       Me   H   Me   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3         Me   H   Me   CHF 2     CF 3         Me   H   Me   CHF 2     Me       Me   H   Me   Ph   CF 3         Me   H   Me   Ph   Cl       Me   H   Me   Ph   Br       Me   H   Me   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br       Me   H   Me   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-CF 3 -2-   CF 3                     pyridyl           Me   H   Me   3-Me-2-   CF 3                     pyridyl           Me   H   Me   3-F-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl       Me   Me   H   Me   Br       Me   Me   H   Et   Br       Me   Me   H   Me   Cl       Me   Me   H   Et   Cl       Me   Me   H   Me   I       Me   Me   H   Me   CF 3         Me   Me   H   Me   OCF 3         Et   Me   H   Me   CF 3         Me   Me   H   Me   SCF 3         Me   Me   H   Me   SCHF 2         Me   Me   H   Me   OCHF 2         n-Pr   Me   H   Me   CF 3         Me   Me   H   Me   C 2 F 5         Et   Me   H   Me   C 2 F 5         Me   Me   H   Et   CF 3         Me   Me   H   n-Pr   CF 3         Me   Me   H   i-Pr   CF 3         Me   Me   H   Me   SMe       Me   Me   H   Me   OMe       Me   Me   H   Me   OEt       Me   Me   H   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   Et       Me   Me   H   Me   OCF 2 CHF 2         Me   Me   H   Me   SCF 2 CHF 2         Me   Me   H   Me   SO 2 Me       Me   Me   H   Me   SO 2 CF 3         Me   Me   H   CF 3     CF 3         Me   Me   H   CF 3     Me       Me   Me   H   Ph   CF 3         Me   Me   H   Ph   Cl       Me   Me   H   Ph   Br       Me   Me   H   2-pyridyl   CF 3         Me   Me   H   2-pyridyl   Cl       Me   Me   H   2-ClPh   CF 3         Me   Me   H   2-ClPh   OCF 3         Me   Me   H   2-ClPh   Br       Me   Me   H   2-ClPh   Cl       Me   Me   H   2-ClPh   SCHF 2         Me   Me   H   2-BrPh   CF 3         Me   Me   H   2-MePh   CF 3         Me   Me   H   2-CNPh   CF 3         Me   Me   H   2-FPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3         Me   Me   H   2-MeOPh   CF 3         Me   Me   H   3-Cl-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   OCF 3         Me   Me   H   3-Cl-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   Cl       Me   Me   H   3-CF 3 -2-   CF 3                     pyridyl           Me   Me   H   3-Me-2-   CF 3                     pyridyl           Me   Me   H   3-Cl-2-pyridyl   SHF 2         Me   Me   H   3-F-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Br-2-pyridyl   Br       Me   Me   H   3-Br-2-pyridyl   Cl       Me   Cl   H   Me   Br       Me   Cl   H   Et   Br       Me   Cl   H   Me   Cl       Me   Cl   H   Et   Cl       Me   Cl   H   Me   I       Me   Cl   H   Me   CF 3         Me   Cl   H   Me   OCF 3         Et   Cl   H   Me   CF 3         Me   Cl   H   Me   SCF 3         Me   Cl   H   Me   SCHF 2         Me   Cl   H   Me   OCHF 2         n-Pr   Cl   H   Me   CF 3         Me   Cl   H   Me   C 2 F 5         Et   Cl   H   Me   C 2 F 5         Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   3-Cl-2-pyridyl   SHF 2         Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   3-CF 3 -2-   CF 3                     pyridyl           Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   3-Br-2-pyridyl   Cl       Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   2-OMe   CF 3         Me   Cl   H   2-ClPh   Br       Me   H   H   H   CF 3         Me   H   H   H   OCF 3         Et   H   H   H   OCF 3         Me   H   H   Me   Br       Me   H   H   Et   Br       Me   H   H   Me   CI       Me   H   H   Et   Cl       Me   H   H   Me   I       Me   H   H   Me   CF 3         Me   H   H   Me   OCF 3         Et   H   H   Me   CF 3         Me   H   H   Me   SCF 3         Me   H   H   Me   SCHF 2         Me   H   H   Me   OCHF 2         n-Pr   H   H   Me   CF 3         Me   H   H   Me   C 2 F 5         Et   H   H   Me   C 2 F 5         Me   H   H   Et   CF 3         Me   H   H   n-Pr   CF 3         Me   H   H   i-Pr   CF 3         Me   H   H   Me   SMe       Me   H   H   Me   OMe       Me   H   H   Me   OEt       Me   H   H   Me   n-C 3 F 7         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   Et       Me   H   H   Me   OCF 2 CHF 2         Me   H   H   Me   SCF 2 CHF 2         Me   H   H   Me   SO 2 Me       Me   H   H   Me   SO 2 CF 3         Me   H   H   CF 3     CF 3         Me   H   H   CF 3     Me       Me   H   H   Ph   CF 3         Me   H   H   Ph   Cl       Me   H   H   Ph   Br       Me   H   H   2-pyridyl   CF 3         Me   H   H   2-pyridyl   Cl       Me   H   H   2-ClPh   CF 3         Me   H   H   2-ClPh   OCF 3         Me   H   H   2-ClPh   Br       Me   H   H   2-ClPh   Cl       Me   H   H   2-ClPh   SCHF 2         Me   H   H   2-BrPh   CF 3         Me   H   H   2-MePh   CF 3         Me   H   H   2-CNPh   CF 3         Me   H   H   2-FPh   CF 3         Me   H   H   2,6-F 2 Ph   CF 3         Me   H   H   2,4-F 2 Ph   CF 3         Me   H   H   2,5-F 2 Ph   CF 3         Me   H   H   2-MeOPh   CF 3         Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   H   3-Cl-2-pyridyl   Br       Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   H   3-F-2-pyridyl   CF 3         Me   H   H   3-CF 3 -2-   CF 3                     pyridyl       Me   H   H   3-Me-2-   CF 3                     pyridyl       Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   H   3-Br-2-pyridyl   Br       Me   H   H   3-Br-2-pyridyl   Cl       Me   H   Cl   Et   Br       Me   H   Cl   Me   Cl       Me   H   Cl   Et   Cl       Me   H   Cl   Me   I       Me   H   Cl   Me   CF 3         Me   H   Cl   Me   OCF 3         Et   H   Cl   Me   CF 3         Me   H   Cl   Me   SCF 3         Me   H   Cl   Me   SCHF 2         Me   H   Cl   Me   OCHF 2         n-Pr   H   Cl   Me   CF 3         Me   H   Cl   Me   C 2 F 5         Et   H   Cl   Me   C 2 F 5         Me   H   Cl   Et   CF 3         Me   H   Cl   n-Pr   CF 3         Me   H   Cl   i-Pr   CF 3         Me   H   Cl   Me   SMe       Me   H   Cl   Me   OMe       Me   H   Cl   Me   OEt       Me   H   Cl   Me   n-C 3 F 7         Me   H   Cl   Me   i-C 3 F 7         Me   H   Cl   Me   Et       Me   H   Cl   Me   OCF 2 CHF 2         Me   H   Cl   Me   SCF 2 CHF 2         Me   H   Cl   Me   SO 2 Me       Me   H   Cl   Me   SO 2 CF 3         Me   H   Cl   CF 3     CF 3         Me   H   Cl   CF 3     Me       Me   H   Cl   Ph   CF 3         Me   H   Cl   Ph   Cl       Me   H   Cl   Ph   Br       Me   H   Cl   2-pyridyl   CF 3         Me   H   Cl   2-pyridyl   Cl       Me   H   Cl   2-ClPh   CF 3         Me   H   Cl   2-ClPh   OCF 3         Me   H   Cl   2-ClPh   Br       Me   H   Cl   2-ClPh   Cl       Me   H   Cl   2-ClPh   SCHF 2         Me   H   Cl   2-BrPh   CF 3         Me   H   Cl   2-MePh   CF 3         Me   H   Cl   2-CNPh   CF 3         Me   H   Cl   2-FPh   CF 3         Me   H   Cl   2,6-F 2 Ph   CF 3         Me   H   Cl   2,4-F 2 Ph   CF 3         Me   H   Cl   2,5-F 2 Ph   CF 3         Me   H   Cl   2-OMe   CF 3         Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   H   Cl   3-Cl-2-pyridyl   Br       Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   H   Cl   3-F-2-pyridyl   CF 3         Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl       Me   H   Cl   3-Me-2-   CF 3                     pyridyl       Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   H   Cl   3-Br-2-pyridyl   Br       Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Cl   H   Et   CF 3         Me   Cl   H   n-Pr   CF 3         Me   Cl   H   i-Pr   CF 3         Me   Cl   H   Me   SMe       Me   Cl   H   Me   OMe       Me   Cl   H   Me   OEt       Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   Et       Me   Cl   H   Me   OCF 2 CHF 2         Me   Cl   H   Me   SCF 2 CHF 2         Me   Cl   H   Me   SO 2 Me       Me   Cl   H   Me   SO 2 CF 3         Me   Cl   H   CF 3     CF 3         Me   Cl   H   CF 3     Me       Me   Cl   H   OMe   CF 3         Me   Cl   H   Ph   CF 3         Me   Cl   H   Ph   Cl       Me   Cl   H   Ph   Br       Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   3-Me-2-   CF 3                     pyridyl       Me   Cl   H   2-ClPh   Cl       Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   2-MePh   CF 3         Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   2-FPh   CF 3         Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   2-ClPh   OCF- 3                      
     [0163]               TABLE 5                                                                                              R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CHF 2         Me   H   Me   H   CH 2 CF 3         Et   H   Me   H   CH 2 CF 3         Me   H   Me   Me   CH 2 CF 3         Me   H   Me   Et   CH 2 CF 3         Me   H   Me   Me   CF 2 CHF 2         Me   H   Me   Et   CHF 2         Me   H   Me   Me   CHF 2         Me   H   Me   Me   CBrF 2         Me   H   Me   Me   CHF 2         Et   H   Me   Me   CH 2 CF 3         Me   H   Me   Me   Et       Me   H   Me   Me   n-Pr       Me   H   Me   Me   CH 2 C 2 F 5         n-Pr   H   Me   Me   CH 2 CF 3         Me   H   Me   Me   CF 3         Et   H   Me   Me   C 2 F 5         Me   H   Me   Et   CHF 2         Me   H   Me   n-Pr   CH 2 CF 3         Me   H   Me   i-Pr   CHF 2         Me   H   Me   Cl   CH 2 CF 3         Me   H   Me   F   CH 2 CF 3         Me   H   Me   Me   CH 2 Cl       Me   H   Me   Me   CClF 2         Me   H   Me   Me   CH 2 CH 2 Cl       Me   H   Me   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7         Me   H   Me   Me   Allyl       Me   H   Me   Et   CF 2 CHF 2         Me   H   Me   Et   i-C 3 F 7         Me   H   Me   i-Pr   CF 2 CHF 2         Me   H   Me   n-Pr   CF 2 CHF 2         Me   H   Me   CF 3     CF 2 CHF 2         Me   H   Me   CF 3     Me       Me   H   Me   OMe   CH 2 CF 3         Me   H   Me   H   CH 2 CF 3         Me   H   Me   H   CH 2 CF 3         Me   H   Me   H   C 2 F 5         Et   H   Me   H   C 2 F 5         Me   H   Me   H   C 2 F 5         Me   H   Me   H   CF 2 CHF 2         Me   H   Me   i-Pr   CH 2 CF 3         Me   H   Me   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7         Me   H   Me   Ph   CH 2 CF 3         Me   H   Me   Ph   CF 2 CHF 2         Me   H   Me   Ph   CHF 2         Me   H   Me   2-pyridyl   CH 2 CF 3         Me   H   Me   2-pyridyl   CF 2 CHF 2         Me   H   Me   2-ClPh   CH 2 CF 3         Me   H   Me   2-ClPh   CF 2 CHF 2         Me   H   Me   2-ClPh   CHF 2         Me   H   Me   2-ClPh   Et       Me   H   Me   2-ClPh   CBrF 2         Me   H   Me   2-BrPh   CH 2 CF 3         Me   H   Me   2-MePh   CH 2 CF 3         Me   H   Me   2-CNPh   CH 2 CF 3         Me   H   Me   2-FPh   CH 2 CF 3         Me   H   Me   2,6-F 2 Ph   CH 2 CF 3         Me   H   Me   2,4-F 2 Ph   CH 2 CF 3         Me   H   Me   2,5-F 2 Ph   CH 2 CF 3         Me   H   Me   2-MeOPh   CH 2 CF 3         Me   H   Me   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 2 CHF 2         Me   H   Me   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   CHF 2         Me   H   Me   3-Cl-2-pyridyl   CBrF 2         Me   H   Me   3-F-2-pyridyl   CH 2 CF 3         Me   H   Me   3-CF 3 -2-   CH 2 CF 3                     pyridyl       Me   H   Me   3-Me-2-   CH 2 CF 3                     pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   CH 2 CF 3         Me   H   Me   3-Br-2-pyridyl   CF 2 CHF 2         Me   H   Me   3-Br-2-pyridyl   CClF 2         Me   Me   H   H   CHF 2         Me   Me   H   H   CH 2 CF 3         Et   Me   H   H   CH 2 CF 3         Me   Me   H   Me   CH 2 CF 3         Me   Me   H   Et   CH 2 CF 3         Me   Me   H   Me   CF 2 CHF 2         Me   Me   H   Et   CHF 2         Me   Me   H   Me   CHF 2         Me   Me   H   Me   CBrF 2         Me   Me   H   Me   CHF 2         Et   Me   H   Me   CH 2 CF 3         Me   Me   H   Me   Et       Me   Me   H   Me   n-Pr       Me   Me   H   Me   CH 2 C 2 F 5         n-Pr   Me   H   Me   CH 2 CF 3         Me   Me   H   Me   CF 3         Et   Me   H   Me   C 2 F 5         Me   Me   H   Et   CHF 2         Me   Me   H   n-Pr   CH 2 CF 3         Me   Me   H   i-Pr   CHF 2         Me   Me   H   Cl   CH 2 CF 3         Me   Me   H   F   CH 2 CF 3         Me   Me   H   Me   CH 2 Cl       Me   Me   H   Me   CClF 2         Me   Me   H   Me   CH 2 CH 2 Cl       Me   Me   H   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   Allyl       Me   Me   H   Me   CF 2 CHF 2         Me   Me   H   Me   i-C 3 F 7         Me   Me   H   Me   CF 2 CHF 2         Me   Me   H   Me   CF 2 CHF 2         Me   Me   H   CF 3     CF 2 CHF 2         Me   Me   H   CF 3     Me       Me   Me   H   OMe   CH 2 CF 3         Me   Me   H   H   CH 2 CF 3         Me   Me   H   H   CH 2 CF 3         Me   Me   H   H   C 2 F 5         Et   Me   H   H   C 2 F 5         Me   Me   H   H   C 2 F 5         Me   Me   H   H   CF 2 CHF 2         Me   Me   H   H   CH 2 CF 3         Me   Me   H   H   n-C 3 F 7         Me   Me   H   H   i-C 3 F 7         Me   Me   H   H   CH 2 CF 3         Me   Me   H   H   CF 2 CHF 2         Me   Me   H   H   CHF 2         Me   Me   H   Ph   CH 2 CF 3         Me   Me   H   Ph   CF 2 CHF 2         Me   Me   H   Ph   CH 2 CF 3         Me   Me   H   2-pyridyl   CF 2 CHF 2         Me   Me   H   2-pyridyl   CHF 2         Me   Me   H   2-ClPh   Et       Me   Me   H   2-ClPh   CBrF 2         Me   Me   H   2-ClPh   CH 2 CF 3         Me   Me   H   2-ClPh   CH 2 CF 3         Me   Me   H   2-ClPh   CH 2 CF 3         Me   Me   H   2-BrPh   CH 2 CF 3         Me   Me   H   2-MePh   CH 2 CF 3         Me   Me   H   2-CNPh   CH 2 CF 3         Me   Me   H   2-FPh   CH 2 CF 3         Me   Me   H   2,6-F 2 Ph   CH 2 CF 3         Me   Me   H   2,4-F 2 Ph   CH 2 CF 3         Me   Me   H   2,5-F 2 Ph   CF 2 CHF 2         Me   Me   H   2-MeOPh   CF 3         Me   Me   H   3-Cl-2-pyridyl   CHF 2         Me   Me   H   3-Cl-2-pyridyl   CBrF 2         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   Me   H   3-F-2-pyridyl   CF 3         Me   Me   H   3-CF 3 -2-   CH 2 CF 3                     pyridyl           Me   Me   H   3-Me-2-   CF 2 CHF 2                     pyridyl           Me   Me   H   3-Br-2-pyridyl   CClF 2         Me   Me   H   3-Br-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   Me   CHF 2         Me   Cl   H   Et   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3         Me   Cl   H   Et   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3         Me   Cl   H   Me   CF 2 CHF 2         Me   Cl   H   Me   CHF 2         Et   Cl   H   Me   CHF 2         Me   Cl   H   Me   CBrF 2         Me   Cl   H   Me   CHF 2         Me   Cl   H   Me   CH 2 CF 3         n-Pr   Cl   H   Me   Et       Me   Cl   H   Me   n-Pr       Et   Cl   H   Me   CH 2 C 2 F 5         Me   Cl   H   Et   CH 2 CF 3         Me   Cl   H   n-Pr   CF 3         Me   Cl   H   i-Pr   C 2 F 5         Me   Cl   H   Cl   CHF 2         Me   Cl   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   Cl   H   3-Cl-2-pyridyl   CF 2 CHF 2         Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   CHF 2         Me   Cl   H   3-Cl-2-pyridyl   CBrF 2         Me   Cl   H   3-F-2-pyridyl   CH 2 CF 3         Me   Cl   H   3-CF 3 -2-   CH 2 CF 3                     pyridyl           Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   3-Br-2-pyridyl   CH 2 CF 3         Me   Cl   H   3-Br-2-pyridyl   CF 2 CHF 2         Me   Cl   H   3-Br-2-pyridyl   CCF 2         Me   Cl   H   2-ClPh   CHF 2         Me   Cl   H   2-ClPh   Et       Me   Cl   H   2-ClPh   CBrF 2         Me   Cl   H   2-BrPh   CH 2 CF 3         Me   Cl   H   2-MePh   CH 2 CF 3         Me   Cl   H   2-CNPh   CH 2 CF 3         Me   Cl   H   2-MeOPh   CH 2 CF 3         Me   Cl   H   2,5-F 2 Ph   CH 2 CF 3         Me   H   H   H   CH 2         Me   H   H   H   CH 2 CF 3         Et   H   H   H   CH 2 CF 3         Me   H   H   Me   CH 2 CF 3         Me   H   H   Et   CH 2 CF 3         Me   H   H   Me   CF 2 CHF 2         Me   H   H   Et   CHF 2         Me   H   H   Me   CHF 2         Me   H   H   Me   CBrF 2         Me   H   H   Me   CHF 2         Et   H   H   Me   CH 2 CF 3         Me   H   H   Me   Et       Me   H   H   Me   n-Pr       Me   H   H   Me   CH 2 C 2 F 5         n-Pr   H   H   Me   CH 2 CF 3         Me   H   H   Me   CF 3         Et   H   H   Me   C 2 F 5         Me   H   H   Et   CHF 2         Me   H   H   n-Pr   CH 2 CF 3         Me   H   H   i-Pr   CHF 2         Me   H   H   Cl   CH 2 CF 3         Me   H   H   F   CH 2 CF 3         Me   H   H   Me   CH 2 Cl       Me   H   H   Me   CClF 2         Me   H   H   Me   CH 2 CH 2 Cl       Me   H   H   Me   n-C 3 F 7         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   Allyl       Me   H   H   Me   CF 2 CHF 2         Me   H   H   Me   i-C 3 F 7         Me   H   H   Me   CF 2 CHF 2         Me   H   H   Me   CF 2 CHF 2         Me   H   H   CF 3     CF 2 CHF 2         Me   H   H   CF 3     Me       Me   H   H   OMe   CH 2 CF 3         Me   H   H   H   CH 2 CF 3         Me   H   H   H   CH 2 CF 3         Me   H   H   H   C 2 F 5         Et   H   H   H   C 2 F 5         Me   H   H   H   C 2 F 5         Me   H   H   H   CF 2 CHF 2         Me   H   H   H   CH 2 CF 3         Me   H   H   H   n-C 3 F 7         Me   H   H   H   i-C 3 F 7         Me   H   H   H   CH 2 CF 3         Me   H   H   H   CF 2 CHF 2         Me   H   H   H   CHF 2         Me   H   H   Ph   CH 2 CF 3         Me   H   H   Ph   CF 2 CHF 2         Me   H   H   Ph   CH 2 CF 3         Me   H   H   2-pyridyl   CF 2 CHF 2         Me   H   H   2-pyridyl   CHF 2         Me   H   H   2-ClPh   Et       Me   H   H   2-ClPh   CBrF 2         Me   H   H   2-ClPh   CH 2 CF 3         Me   H   H   2-ClPh   CH 2 CF 3         Me   H   H   2-ClPh   CH 2 CF 3         Me   H   H   2-BrPh   CH 2 CF 3         Me   H   H   2-MePh   CH 2 CF 3         Me   H   H   2-CNPh   CH 2 CF 3         Me   H   H   2-FPh   CH 2 CF 3         Me   H   H   2,6-F 2 Ph   CH 2 CF 3         Me   H   H   2,4-F 2 Ph   CH 2 CF 3         Me   H   H   2,5-F 2 Ph   CF 2 CHF 2         Me   H   H   2-MeOPh   CF 3         Me   H   H   3-Cl-2-pyridyl   CHF 2         Me   H   H   3-Cl-2-pyridyl   CBrF 2         Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   H   3-CF 3 -2-   CH 2 CF 3                     pyridyl       Me   H   H   3-Me-2-   CF 2 CHF 2                     pyridyl       Me   H   H   3-F-2-pyridyl   CF 3         Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   H   3-Br-2-pyridyl   CClF 2         Me   H   H   3-Br-2-pyridyl   CH 2 CF 3         Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   Cl   Et   CHF 2         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Et   CH 2 CF 3         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   CF 2 CHF 2         Et   H   Cl   Me   CHF 2         Me   H   Cl   Me   CHF 2         Me   H   Cl   Me   CBrF 2         Me   H   Cl   Me   CHF 2         n-Pr   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   Et       Et   H   Cl   Me   n-Pr       Me   H   Cl   Et   CH 2 C 2 F 5         Me   H   Cl   n-Pr   CH 2 CF 3         Me   H   Cl   i-Pr   CF 3         Me   H   Cl   Cl   C 2 F 5         Me   H   Cl   F   CHF 2         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   CHF 2         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   CH 2 CF 3         Me   H   Cl   Me   CH 2 Cl       Me   H   Cl   Me   CClF 2         Me   H   Cl   Me   CH 2 CH 2 Cl       Me   H   Cl   Me   n-C 3 F 7         Me   H   Cl   Me   i-C 3 F 7         Me   H   Cl   Me   Allyl       Me   H   Cl   CF 3     CF 2 CHF 2         Me   H   Cl   CF 3     i-C 3 F 7         Me   H   Cl   OMe   CF 2 CHF 2         Me   H   Cl   H   CF 2 CHF 2         Me   H   Cl   H   CF 2 CHF 2         Me   H   Cl   H   Me       Et   H   Cl   H   CH 2 CF 3         Me   H   Cl   H   CH 2 CF 3         Me   H   Cl   H   CH 2 CF 3         Me   H   Cl   H   C 2 F 5         Me   H   Cl   H   C 2 F 5         Me   H   Cl   H   C 2 F 5         Me   H   Cl   H   CF 2 CHF 2         Me   H   Cl   H   CH 2 CF 3         Me   H   Cl   H   n-C 3 F 7         Me   H   Cl   Ph   i-C 3 F 7         Me   H   Cl   Ph   CH 2 CF 3         Me   H   Cl   Ph   CF 2 CHF 2         Me   H   Cl   2-pyridyl   CHF 2         Me   H   Cl   2-pyridyl   CH 2 CF 3         Me   H   Cl   2-ClPh   CF 2 CHF 2         Me   H   Cl   2-ClPh   CH 2 CF 3         Me   H   Cl   2-ClPh   CF 2 CHF 2         Me   H   Cl   2-ClPh   CHF 2         Me   H   Cl   2-ClPh   Et       Me   H   Cl   2-BrPh   CBrF 2         Me   H   Cl   2-MePh   CH 2 CF 3         Me   H   Cl   2-CNPh   CH 2 CF 3         Me   H   Cl   2-FPh   CH 2 CF 3         Me   H   Cl   2,6-F 2 Ph   CH 2 CF 3         Me   H   Cl   2,4-F 2 Ph   CH 2 CF 3         Me   H   Cl   2,5-F 2 Ph   CH 2 CF 3         Me   H   Cl   2-MeOPh   CH 2 CF 3         Me   H   CL   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Cl   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Cl   3-Cl-2-pyridyl   CF 2 CHF 2         Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   H   Cl   3-Cl-2-pyridyl   CHF 2         Me   H   Cl   3-F-2-pyridyl   CBrF 2         Me   H   CL   3-Br-2-pyridyl   CH 2 CF 3         Me   H   Cl   3-CF 3 -2-   CH 2 CF 3                     pyridyl       Me   H   Cl   3-Me-2-   CH 2 CF 3                     pyridyl       Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   H   Cl   3-Br-2-pyridyl   CH 2 CF 3         Me   H   Cl   3-Br-2-pyridyl   CF 2 CHF 2         Me   Cl   H   F   Cl 2 CF 3         Me   Cl   H   Me   CHF 2         Me   Cl   H   Me   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3         Me   Cl   H   Me   CH 2 Cl       Me   Cl   H   Me   CClF 2         Me   Cl   H   Me   CH 2 CH 2 Cl       Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   Allyl       Me   Cl   H   Me   CF 2 CHF 2         Me   Cl   H   CF 3     i-C 3 F 7         Me   Cl   H   CF 3     CF 2 CHF 2         Me   Cl   H   OMe   CF 2 CHF 2         Me   Cl   H   H   CF 2 CHF 2         Me   Cl   H   H   Me       Me   Cl   H   H   CH 2 CF 3         Et   Cl   H   H   CH 2 CF 3         Me   Cl   H   H   CH 2 CF 3         Me   Cl   H   H   C 2 F 5         Me   Cl   H   H   C 2 F 5         Me   Cl   H   H   C 2 F 5         Me   Cl   H   H   CF 2 CHF 2         Me   Cl   H   H   CH 2 CF 3         Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   3-Me-2-   CH 2 CF 3                     pyridyl       Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   Ph   CH 2 CF 3         Me   Cl   H   Ph   CF 2 CHF 2         Me   Cl   H   Ph   CHF 2         Me   Cl   H   2-pyridyl   CH 2 CF 3         Me   Cl   H   2-pyridyl   CF 2 CHF 2         Me   Cl   H   2-ClPh   CH 2 CF 3         Me   Cl   H   2-ClPh   CF 2 CHF 2         Me   Cl   H   2-FPh   CH 2 CF 3         Me   Cl   H   2,6-F 2 Ph   CH 2 CF 3         Me   Cl   H   2,4-F 2 Ph   CH 2 CF 3                      
     [0164]               TABLE 6                                                                                                                  R 3     R 4a     R 4b     R 5a     R 5b     R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Et   H   Me   H   OCF 3     Et   H   H   H   OCF 3         Me   H   Me   Me   Br   Me   H   H   Me   Br       Me   H   Me   Et   Br   Me   H   H   Et   Br       Me   H   Me   Me   Cl   Me   H   H   Me   Cl       Me   H   Me   Et   Cl   Me   H   H   Et   Cl       Me   H   Me   Me   I   Me   H   H   Me   I       Me   H   Me   Me   CF 3     Me   H   H   Me   CF 3         Me   H   Me   Me   OCF 3     Me   H   H   Me   OCF 3         Et   H   Me   Me   CF 3     Et   H   H   Me   CF 3         Me   H   Me   Me   SCF 3     Me   H   H   Me   SCF 3         Me   H   Me   Me   SCHF 2     Me   H   H   Me   SCHF 2         Me   H   Me   Me   OCHF 2     Me   H   H   Me   OCHF 2         n-Pr   H   Me   Me   CF 3     n-Pr   H   H   Me   CF 3         Me   H   Me   Me   C 2 F 5     Me   H   H   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5     Et   H   H   Me   C 2 F 5         Me   H   Me   Et   CF 3     Me   H   H   Et   CF 3         Me   H   Me   n-Pr   CF 3     Me   H   H   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3     Me   H   H   i-Pr   CF 3         Me   H   Me   Cl   CF 3     Me   H   H   Cl   CF 3         Me   H   Me   F   CF 3     Me   H   H   F   CF 3         Me   H   Me   Me   SMe   Me   H   H   Me   SMe       Me   H   Me   Me   OMe   Me   H   H   Me   OMe       Me   H   Me   Me   OEt   Me   H   H   Me   OEt       Me   H   Me   Me   n-C 3 F 7     Me   H   H   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   Me   Et   Me   H   H   Me   Et       Me   H   Me   Me   OCF 2 CHF 2     Me   H   H   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2     Me   H   H   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me   Me   H   H   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3     Me   H   H   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3     Me   H   H   CF 3     CF 3         Me   H   Me   CF 3     Me   Me   H   H   CF 3     Me       Me   H   Me   OMe   CF 3     Me   H   H   OMe   CF 3         Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCHF 2     Me   H   H   H   OCHF 2         Me   H   Me   H   C 2 F 5     Me   H   H   H   C 2 F 5         Et   H   Me   H   C 2 F 5     Et   H   H   H   C 2 F 5         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2     Me   H   H   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2     Me   H   H   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7     Me   H   H   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7     Me   H   H   H   i-C 3 F 7         Me   H   Me   H   Br   Me   H   H   H   Br       Me   H   Me   H   Cl   Me   H   H   H   Cl       Me   H   Me   H   SCF 3     Me   H   H   H   SCF 3         Me   H   Me   Ph   CF 3     Me   H   H   Ph   CF 3         Me   H   Me   Ph   Cl   Me   H   H   Ph   Cl       Me   H   Me   Ph   Br   Me   H   H   Ph   Br       Me   H   Me   2-pyridyl   CF 3     Me   H   H   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl   Me   H   H   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3     Me   H   H   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3     Me   H   H   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br   Me   H   H   2-ClPh   Br       Me   H   Me   2-ClPh   Cl   Me   H   H   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2     Me   H   H   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3     Me   H   H   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3     Me   H   H   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3     Me   H   H   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3     Me   H   H   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3     Me   H   H   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3     Me   H   H   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3     Me   H   H   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3     Me   H   H   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3     Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3     Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br   Me   H   H   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl   Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2     Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3     Me   H   H   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3     Me   H   H   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Me-2-   CF 3     Me   H   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3     Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br   Me   H   H   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl   Me   H   H   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3     Me   H   Cl   Et   Br       Me   Me   H   H   OCF 3     Me   H   Cl   Me   Cl       Et   Me   H   H   OCF 3     Me   H   Cl   Et   Cl       Me   Me   H   Me   Br   Me   H   Cl   Me   I       Me   Me   H   Et   Br   Me   H   Cl   Me   CF 3         Me   Me   H   Me   Cl   Me   H   Cl   Me   OCF 3         Me   Me   H   Et   Cl   Et   H   Cl   Me   CF 3         Me   Me   H   Me   I   Me   H   Cl   Me   SCF 3         Me   Me   H   Me   CF 3     Me   H   Cl   Me   SCHF 2         Me   Me   H   Me   OCF 3     Me   H   Cl   Me   OCHF 2         Et   Me   H   Me   CF 3     n-Pr   H   Cl   Me   CF 3         Me   Me   H   Me   SCF 3     Me   H   Cl   Me   C 2 F 5         Me   Me   H   Me   SCHF 2     Et   H   Cl   Me   C 2 F 5         Me   Me   H   Me   OCHF 2     Me   H   Cl   Et   CF 3         n-Pr   Me   H   Me   CF 3     Me   H   Cl   n-Pr   CF 3         Me   Me   H   Me   C 2 F 5     Me   H   Cl   i-Pr   CF 3         Et   Me   H   Me   C 2 F 5     Me   H   Cl   Cl   CF 3         Me   Me   H   Et   CF 3     Me   H   Cl   F   CF 3         Me   Me   H   n-Pr   CF 3     Me   H   Cl   Me   SMe       Me   Me   H   i-Pr   CF 3     Me   H   Cl   Me   OMe       Me   Me   H   Cl   CF 3     Me   H   Cl   Me   OEt       Me   Me   H   F   CF 3     Me   H   Cl   Me   n-C 3 F 7         Me   Me   H   Me   SMe   Me   H   Cl   Me   i-C 3 F 7         Me   Me   H   Me   OMe   Me   H   Cl   Me   Et       Me   Me   H   Me   OEt   Me   H   Cl   Me   OCF 2 CHF 2         Me   Me   H   Me   n-C 3 F 7     Me   H   Cl   Me   SCF 2 CHF 2         Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   SO 2 Me       Me   Me   H   Me   Et   Me   H   Cl   Me   SO 2 CF 3         Me   Me   H   Me   OCF 2 CHF 2     Me   H   Cl   CF 3     CF 3         Me   Me   H   Me   SCF 2 CHF 2     Me   H   Cl   CF 3     Me       Me   Me   H   Me   SO 2 Me   Me   H   Cl   OMe   CF 3         Me   Me   H   Me   SO 2 CF 3     Me   H   Cl   H   CF 3         Me   Me   H   CF 3     CF 3     Me   H   Cl   H   OCHF 2         Me   Me   H   CF 3     Me   Me   H   Cl   H   C 2 F 5         Me   Me   H   OMe   CF 3     Et   H   Cl   H   C 2 F 5         Me   Me   H   H   CF 3     Me   H   Cl   H   OCF 3         Me   Me   H   H   OCHF 2     Me   H   Cl   H   OCF 2 CHF 2         Me   Me   H   H   C 2 F 5     Me   H   Cl   H   SCF 2 CHF 2         Et   Me   H   H   C 2 F 5     Me   H   Cl   H   n-C 3 F 7         Me   Me   H   H   OCF 3     Me   H   Cl   H   i-C 3 F 7         Me   Me   H   H   OCF 2 CHF 2     Me   H   Cl   H   Br       Me   Me   H   H   SCF 2 CHF 2     Me   H   Cl   H   Cl       Me   Me   H   H   n-C 3 F 7     Me   H   Cl   H   SCF 3         Me   Me   H   H   i-C 3 F 7     Me   H   Cl   Ph   CF 3         Me   Me   H   H   Br   Me   H   Cl   Ph   Cl       Me   Me   H   H   Cl   Me   H   Cl   Ph   Br       Me   Me   H   H   SCF 3     Me   H   Cl   2-pyridyl   CF 3         Me   Me   H   Ph   CF 3     Me   H   Cl   2-pyridyl   Cl       Me   Me   H   Ph   Cl   Me   H   Cl   2-ClPh   CF 3         Me   Me   H   Ph   Br   Me   H   Cl   2-ClPh   OCF 3         Me   Me   H   2-pyridyl   CF 3     Me   H   Cl   2-ClPh   Br       Me   Me   H   2-pyridyl   Cl   Me   H   Cl   2-ClPh   Cl       Me   Me   H   2-ClPh   CF 3     Me   H   Cl   2-ClPh   SCHF 2         Me   Me   H   2-ClPh   OCF 3     Me   H   Cl   2-BrPh   CF 3         Me   Me   H   2-ClPh   Br   Me   H   Cl   2-MePh   CF 3         Me   Me   H   2-ClPh   Cl   Me   H   Cl   2-CNPh   CF 3         Me   Me   H   2-ClPh   SCHF 2     Me   H   Cl   2-FPh   CF 3         Me   Me   H   2-BrPh   CF 3     Me   H   Cl   2,6-F 2 Ph   CF 3         Me   Me   H   2-MePh   CF 3     Me   H   Cl   2,4-F 2 Ph   CF 3         Me   Me   H   2-CNPh   CF 3     Me   H   Cl   2.5-F 2 Ph   CF 3         Me   Me   H   2-FPh   CF 3     Me   H   Cl   2-MeOPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   Me   H   2,5-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyL   Br       Me   Me   H   2-MeOPh   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Cl-2-pyridyl   CF 3     Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-Cl-2-pyridyl   OCF 3     Me   H   Cl   3-F-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Br   Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Cl   Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Cl-2-pyridyl   SCHF 2     Me   H   Cl   3-Br-2-pyridyl   Br       Me   Me   H   3-F-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Me   H   3-CF 3 -2-   CF 3     Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Me-2-   CF 3     Me   H   Cl   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Br-2-pyridyl   CF 3     Me   Cl   H   H   OCF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3     Me   Cl   H   H   OCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Br   Me   Cl   H   H   SCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Cl   Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   Me   Br   Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   Et   Br   Me   Cl   H   H   Br       Me   Cl   H   Me   Cl   Me   Cl   H   H   Cl       Me   Cl   H   Et   Cl   Me   Cl   H   H   SCF 3         Me   Cl   H   Me   I   Me   Cl   H   Ph   CF 3         Me   Cl   H   Me   CF 3     Me   Cl   H   Ph   Cl       Me   Cl   H   Me   OCF 3     Me   Cl   H   Ph   Br       Et   Cl   H   Me   CF 3     Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   Me   SCF 3     Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   Me   SCHF 2     Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   Me   OCHF 2     Me   Cl   H   2-ClPh   OCF 3         n-Pr   Cl   H   Me   CF 3     Me   Cl   H   2-ClPh   Br       Me   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   Cl       Et   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   Et   CF 3     Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   n-Pr   CF 3     Me   Cl   H   2-MePh   CF 3         Me   Cl   H   i-Pr   CF 3     Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   Cl   CF 3     Me   Cl   H   2-FPh   CF 3         Me   Cl   H   F   CF 3     Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   Me   SMe   Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   Me   OMe   Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   Me   OEt   Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   Me   n-G 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   Me   i-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   Me   Et   Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   Me   OCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   Me   SCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   Me   SO 2 Me   Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   Me   SO 2 CF 3     Me   Cl   H   CF 3     CF 3         Me   Cl   H   3-CF 3 -2-   CF 3     Me   Cl   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Cl   H   CF 3     Me   Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   OMe   CF 3     Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   H   CF 3     Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   H   OCHF 2     Me   Cl   H   3-Br-2-pyridyl   Cl       Me   Cl   H   H   C 2 F 5     Et   Cl   H   H   C 2 F 5                      
     [0165]               TABLE 7                                                                                                                  R 3     R 4a     R 4b     R 5a     R 5b     R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Et   H   Me   H   OCF 3     Et   H   H   H   OCF 3         Me   H   Me   Me   Br   Me   H   H   Me   Br       Me   H   Me   Et   Br   Me   H   H   Et   Br       Me   H   Me   Me   CI   Me   H   H   Me   Cl       Me   H   Me   Et   Cl   Me   H   H   Et   Cl       Me   H   Me   Me   I   Me   H   H   Me   I       Me   H   Me   Me   CF 3     Me   H   H   Me   CF 3         Me   H   Me   Me   OCF 3     Me   H   H   Me   OCF 3         Et   H   Me   Me   CF 3     Et   H   H   Me   CF 3         Me   H   Me   Me   SCF 3     Me   H   H   Me   SCF 3         Me   H   Me   Me   SCHF 2     Me   H   H   Me   SCHF 2         Me   H   Me   Me   OCHF 2     Me   H   H   Me   OCHF 2         n-Pr   H   Me   Me   CF 3     n-Pr   H   H   Me   CF 3         Me   H   Me   Me   C 2 F 5     Me   H   H   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5     Et   H   H   Me   C 2 F 5         Me   H   Me   Et   CF 3     Me   H   H   Et   CF 3         Me   H   Me   n-Pr   CF 3     Me   H   H   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3     Me   H   H   i-Pr   CF 3         Me   H   Me   Cl   CF 3     Me   H   H   Cl   CF 3         Me   H   Me   F   CF 3     Me   H   H   F   CF 3         Me   H   Me   Me   SMe   Me   H   H   Me   SMe       Me   H   Me   Me   OMe   Me   H   H   Me   OMe       Me   H   Me   Me   OEt   Me   H   H   Me   OEt       Me   H   Me   Me   n-C 3 F 7     Me   H   H   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   Me   Et   Me   H   H   Me   Et       Me   H   Me   Me   OCF 2 CHF 2     Me   H   H   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2     Me   H   H   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me   Me   H   H   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3     Me   H   H   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3     Me   H   H   CF 3     CF 3         Me   H   Me   CF 3     Me   Me   H   H   CF 3     Me       Me   H   Me   OMe   CF 3     Me   H   H   OMe   CF 3         Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCHF 2     Me   H   H   H   OCHF 2         Me   H   Me   H   C 2 F 5     Me   H   H   H   C 2 F 5         Et   H   Me   H   C 2 F 5     Et   H   H   H   C 2 F 5         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2     Me   H   H   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2     Me   H   H   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7     Me   H   H   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7     Me   H   H   H   i-C 3 F 7         Me   H   Me   H   Br   Me   H   H   H   Br       Me   H   Me   H   Cl   Me   H   H   H   Cl       Me   H   Me   H   SCF 3     Me   H   H   H   SCF 3         Me   H   Me   Ph   CF 3     Me   H   H   Ph   CF 3         Me   H   Me   Ph   Cl   Me   H   H   Ph   Cl       Me   H   Me   Ph   Br   Me   H   H   Ph   Br       Me   H   Me   2-pyridyl   CF 3     Me   H   H   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl   Me   H   H   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3     Me   H   H   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3     Me   H   H   2-ClPh   OCF 3         Me   H   Me   2-Clph   Br   Me   H   H   2-ClPh   Br       Me   H   Me   2-ClPh   Cl   Me   H   H   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2     Me   H   H   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3     Me   H   H   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3     Me   H   H   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3     Me   H   H   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3     Me   H   H   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3     Me   H   H   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3     Me   H   H   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3     Me   H   H   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3     Me   H   H   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3     Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3     Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br   Me   H   H   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl   Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2     Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3     Me   H   H   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3     Me   H   H   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Me-2-   CF 3     Me   H   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3     Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br   Me   H   H   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl   Me   H   H   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3     Me   H   Cl   Et   Br       Me   Me   H   H   OCF 3     Me   H   Cl   Me   Cl       Et   Me   H   H   OCF 3     Me   H   Cl   Et   Cl       Me   Me   H   Me   Br   Me   H   Cl   Me   I       Me   Me   H   El   Br   Me   H   Cl   Me   CF 3         Me   Me   H   Me   Cl   Me   H   Cl   Me   OCF 3         Me   Me   H   Et   Cl   Et   H   Cl   Me   CF 3         Me   Me   H   Me   I   Me   H   Cl   Me   SCF 3         Me   Me   H   Me   CF 3     Me   H   Cl   Me   SCHF 2         Me   Me   H   Me   OCF 3     Me   H   Cl   Me   OCHF 2         Et   Me   H   Me   CF 3     n-Pr   H   Cl   Me   CF 3         Me   Me   H   Me   SCF 3     Me   H   Cl   Me   C 2 F 5         Me   Me   H   Me   SCHF 2     Et   H   Cl   Me   C 2 F 5         Me   Me   H   Me   OCHF 2     Me   H   Cl   Et   CF 3         n-Pr   Me   H   Me   CF 3     Me   H   Cl   n-Pr   CF 3         Me   Me   H   Me   C 2 F 5     Me   H   Cl   i-Pr   CF 3         Et   Me   H   Me   C 2 F 5     Me   H   Cl   Cl   CF 3         Me   Me   H   Et   CF 3     Me   H   Cl   F   CF 3         Me   Me   H   n-Pr   CF 3     Me   H   Cl   Me   SMe       Me   Me   H   i-Pr   CF 3     Me   H   Cl   Me   OMe       Me   Me   H   Cl   CF 3     Me   H   Cl   Me   OEt       Me   Me   H   F   CF 3     Me   H   Cl   Me   n-C 3 F 7         Me   Me   H   Me   SMe   Me   H   Cl   Me   i-C 3 F 7         Me   Me   H   Me   OMe   Me   H   Cl   Me   Et       Me   Me   H   Me   OEt   Me   H   Cl   Me   OCF 2 CHF 2         Me   Me   H   Me   n-C 3 F 7     Me   H   Cl   Me   SCF 2 CHF 2         Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   SO 2 Me       Me   Me   H   Me   Et   Me   H   Cl   Me   SO 2 CF 3         Me   Me   H   Me   OCF 2 CHF 2     Me   H   Cl   CF 3     CF 3         Me   Me   H   Me   SCF 2 CHF 2     Me   H   Cl   CF 3     Me       Me   Me   H   Me   SO 2 Me   Me   H   Cl   OMe   CF 3         Me   Me   H   Me   SO 2 CF 3     Me   H   Cl   H   CF 3         Me   Me   H   CF 3     CF 3     Me   H   Cl   H   OCHF 2         Me   Me   H   CF 3     Me   Me   H   Cl   H   C 2 F 5         Me   Me   H   OMe   CF 3     Et   H   Cl   H   C 2 F 5         Me   Me   H   H   CF 3     Me   H   Cl   H   OCF 3         Me   Me   H   H   OCHF 2     Me   H   Cl   H   OCF 2 CHF 2         Me   Me   H   H   C 2 F 5     Me   H   Cl   H   SCF 2 CHF 2         Et   Me   H   H   C 2 F 5     Me   H   Cl   H   n-C 3 F 7         Me   Me   H   H   OCF 3     Me   H   Cl   H   i-C 3 F 7         Me   Me   H   H   OCF 2 CHF 2     Me   H   Cl   H   Br       Me   Me   H   H   SCF 2 CHF 2     Me   H   Cl   H   Cl       Me   Me   H   H   n-C 3 F 7     Me   H   Cl   H   SCF 3         Me   Me   H   H   i-C 3 F 7     Me   H   Cl   Ph   CF 3         Me   Me   H   H   Br   Me   H   Cl   Ph   Cl       Me   Me   H   H   Cl   Me   H   Cl   Ph   Br       Me   Me   H   H   SCF 3     Me   H   Cl   2-pyridyl   CF 3         Me   Me   H   Ph   CF 3     Me   H   Cl   2-pyridyl   Cl       Me   Me   H   Ph   Cl   Me   H   Cl   2-ClPh   CF 3         Me   Me   H   Ph   Br   Me   H   Cl   2-ClPh   OCF 3         Me   Me   H   2-pyridyl   CF 3     Me   H   Cl   2-ClPh   Br       Me   Me   H   2-pyridyl   Cl   Me   H   Cl   2-ClPh   Cl       Me   Me   H   2-ClPh   CF 3     Me   H   Cl   2-ClPh   SCHF 2         Me   Me   H   2-ClPh   OCF 3     Me   H   Cl   2-BrPh   CF 3         Me   Me   H   2-ClPh   Br   Me   H   Cl   2-MePh   CF 3         Me   Me   H   2-ClPh   Cl   Me   Et   Cl   2-CNPh   CF 3         Me   Me   H   2-ClPh   SCHF 2     Me   H   Cl   2-FPh   CF 3         Me   Me   H   2-BrPh   CF 3     Me   H   Cl   2,6-F 2 Ph   CF 3         Me   Me   H   2-MePh   CF 3     Me   H   Cl   2,4-F 2 Ph   CF 3         Me   Me   H   2-CNPh   CF 3     Me   H   Cl   2,5-F 2 Ph   CF 3         Me   Me   H   2-FPh   CF 3     Me   H   Cl   2-MeOPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   Me   H   2,5-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Br       Me   Me   H   2-MeOPh   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Cl-2-pyridyl   CF 3     Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-Cl-2-pyridyl   OCF 3     Me   H   Cl   3-F-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   Br   Me   Me   H   3-Cl-2-pyridyl   Cl       Me   H   Cl   3-CF 3 -2-   CF 3     Me   H   Cl   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Cl-2-pyridyl   SCHF 2     Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   Me   H   3-F-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-CF 3 -2-   CF 3     Me   Me   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   H   Cl   3-Br-2-pyridyl   Br   Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   CF 3     Me   Cl   H   H   OCF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3     Me   Cl   H   H   OCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Br   Me   Cl   H   H   SCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Cl   Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   Me   Br   Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   Et   Br   Me   Cl   H   H   Br       Me   Cl   H   Me   Cl   Me   Cl   H   H   Cl       Me   Cl   H   Et   Cl   Me   Cl   H   H   SCF 3         Me   Cl   H   Me   I   Me   Cl   H   Ph   CF 3         Me   Cl   H   Me   CF 3     Me   Cl   H   Ph   Cl       Me   Cl   H   Me   OCF 3     Me   Cl   H   Ph   Br       Et   Cl   H   Me   CF 3     Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   Me   SCF 3     Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   Me   SCHF 2     Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   Me   OCHF 2     Me   Cl   H   2-ClPh   OCF 3         n-Pr   Cl   H   Me   CF 3     Me   Cl   H   2-ClPh   Br       Me   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   Cl       Et   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   Et   CF 3     Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   n-Pr   CF 3     Me   Cl   H   2-MePh   CF 3         Me   Cl   H   i-Pr   CF 3     Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   Cl   CF 3     Me   Cl   H   2-FPh   CF 3         Me   Cl   H   F   CF 3     Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   Me   SMe   Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   Me   OMe   Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   Me   OEt   Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   Me   n-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   Me   i-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   Me   Et   Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   Me   OCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   Me   SCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   Me   SO 2 Me   Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   3-Me-2-   CF 3     Me   Cl   H   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   Cl   H   CF 3     CF 3     Me   Cl   H   Me   SO 2 CF 3         Me   Cl   H   CF 3     Me   Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   OMe   CF 3     Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   H   CF 3     Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   H   OCHF 2     Me   Cl   H   3-Br-2-pyridyl   Cl       Me   Cl   H   H   C 2 F 5     Et   Cl   H   H   C 2 F 5                      
     [0166]               TABLE 8                                                                                                                  R 3     R 4a     R 4b     R 5a     R 5b     R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Et   H   Me   H   OCF 3     Et   H   H   H   OCF 3         Me   H   Me   Me   Br   Me   H   H   Me   Br       Me   H   Me   Et   Br   Me   H   H   Et   Br       Me   H   Me   Me   Cl   Me   H   H   Me   Cl       Me   H   Me   Et   Cl   Me   H   H   Et   Cl       Me   H   Me   Me   I   Me   H   H   Me   I       Me   H   Me   Me   CF 3     Me   H   H   Me   CF 3         Me   H   Me   Me   OCF 3     Me   H   H   Me   OCF 3         Et   H   Me   Me   CF 3     Et   H   H   Me   CF 3         Me   H   Me   Me   SCF 3     Me   H   H   Me   SCF 3         Me   H   Me   Me   SCHF 2     Me   H   H   Me   SCHF 2         Me   H   Me   Me   OCHF 2     Me   H   H   Me   OCHF 2         n-Pr   H   Me   Me   CF 3     n-Pr   H   H   Me   CF 3         Me   H   Me   Me   C 2 F 5     Me   H   H   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5     Et   H   H   Me   C 2 F 5         Me   H   Me   Et   CF 3     Me   H   H   Et   CF 3         Me   H   Me   n-Pr   CF 3     Me   H   H   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3     Me   H   H   i-Pr   CF 3         Me   H   Me   Cl   CF 3     Me   H   H   Cl   CF 3         Me   H   Me   F   CF 3     Me   H   H   F   CF 3         Me   H   Me   Me   SMe   Me   H   H   Me   SMe       Me   H   Me   Me   OMe   Me   H   H   Me   OMe       Me   H   Me   Me   OEt   Me   H   H   Me   OEt       Me   H   Me   Me   n-C 3 F 7     Me   H   H   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   Me   Et   Me   H   H   Me   Et       Me   H   Me   Me   OCF 2 CHF 2     Me   H   H   Me   OCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2     Me   H   H   Me   SCF 2 CHF 2         Me   H   Me   Me   SO 2 Me   Me   H   H   Me   SO 2 Me       Me   H   Me   Me   SO 2 CF 3     Me   H   H   Me   SO 2 CF 3         Me   H   Me   CF 3     CF 3     Me   H   H   CF 3     CF 3         Me   H   Me   CF 3     Me   Me   H   H   CF 3     Me       Me   H   Me   OMe   CF 3     Me   H   H   OMe   CF 3         Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCHF 2     Me   H   H   H   OCHF 2         Me   H   Me   H   C 2 F 5     Me   H   H   H   C 2 F 5         Et   H   Me   H   C 2 F 5     Et   H   H   H   C 2 F 5         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Me   H   Me   H   OCF 2 CHF 2     Me   H   H   H   OCF 2 CHF 2         Me   H   Me   H   SCF 2 CHF 2     Me   H   H   H   SCF 2 CHF 2         Me   H   Me   H   n-C 3 F 7     Me   H   H   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7     Me   H   H   H   i-C 3 F 7         Me   H   Me   H   Br   Me   H   H   H   Br       Me   H   Me   H   Cl   Me   H   H   H   Cl       Me   H   Me   H   SCF 3     Me   H   H   H   SCF 3         Me   H   Me   Ph   CF 3     Me   H   H   Ph   CF 3         Me   H   Me   Ph   Cl   Me   H   H   Ph   Cl       Me   H   Me   Ph   Br   Me   H   H   Ph   Br       Me   H   Me   2-pyridyl   CF 3     Me   H   H   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   Cl   Me   H   H   2-pyridyl   Cl       Me   H   Me   2-ClPh   CF 3     Me   H   H   2-ClPh   CF 3         Me   H   Me   2-ClPh   OCF 3     Me   H   H   2-ClPh   OCF 3         Me   H   Me   2-ClPh   Br   Me   H   H   2-ClPh   Br       Me   H   Me   2-ClPh   Cl   Me   H   H   2-ClPh   Cl       Me   H   Me   2-ClPh   SCHF 2     Me   H   H   2-ClPh   SCHF 2         Me   H   Me   2-BrPh   CF 3     Me   H   H   2-BrPh   CF 3         Me   H   Me   2-MePh   CF 3     Me   H   H   2-MePh   CF 3         Me   H   Me   2-CNPh   CF 3     Me   H   H   2-CNPh   CF 3         Me   H   Me   2-FPh   CF 3     Me   H   H   2-FPh   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3     Me   H   H   2,6-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3     Me   H   H   2,4-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3     Me   H   H   2,5-F 2 Ph   CF 3         Me   H   Me   2-MeOPh   CF 3     Me   H   H   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3     Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyriddyl   OCF 3     Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   Br   Me   H   H   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Cl   Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   SCHF 2     Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-F-2-pyridyl   CF 3     Me   H   H   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3     Me   H   H   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Me-2-   CF 3     Me   H   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3     Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   Br   Me   H   H   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Cl   Me   H   H   3-Br-2-pyridyl   Cl       Me   Me   H   H   CF 3     Me   H   Cl   Et   Br       Me   Me   H   H   OCF 3     Me   H   Cl   Me   Cl       Et   Me   H   H   OCF 3     Me   H   Cl   Et   Cl       Me   Me   H   Me   Br   Me   H   Cl   Me   I       Me   Me   H   Et   Br   Me   H   Cl   Me   CF 3         Me   Me   H   Me   Cl   Me   H   Cl   Me   OCF 3         Me   Me   H   Et   Cl   Et   H   Cl   Me   CF 3         Me   Me   H   Me   I   Me   H   Cl   Me   SCF 3         Me   Me   H   Me   CF 3     Me   H   Cl   Me   SCHF 2         Me   Me   H   Me   OCF 3     Me   H   Cl   Me   OCHF 2         Et   Me   H   Me   CF 3     n-Pr   H   Cl   Me   CF 3         Me   Me   H   Me   SCF 3     Me   H   Cl   Me   C 2 F 5         Me   Me   H   Me   SCHF 2     Et   H   Cl   Me   C 2 F 5         Me   Me   H   Me   OCHF 2     Me   H   Cl   Et   CF 3         n-Pr   Me   H   Me   CF 3     Me   H   Cl   n-Pr   CF 3         Me   Me   H   Me   C 2 F 5     Me   H   Cl   i-Pr   CF 3         Et   Me   H   Me   C 2 F 5     Me   H   Cl   Cl   CF 3         Me   Me   H   Et   CF 3     Me   H   Cl   F   CF 3         Me   Me   H   n-Pr   CF 3     Me   H   Cl   Me   SMe       Me   Me   H   i-Pr   CF 3     Me   H   Cl   Me   OMe       Me   Me   H   Cl   CF 3     Me   H   Cl   Me   OEt       Me   Me   H   F   CF 3     Me   H   Cl   Me   n-C 3 F 7         Me   Me   H   Me   SMe   Me   H   Cl   Me   i-C 3 F 7         Me   Me   H   Me   OMe   Me   H   Cl   Me   Et       Me   Me   H   Me   OEt   Me   H   Cl   Me   OCF 2 CHF 2         Me   Me   H   Me   n-C 3 F 7     Me   H   Cl   Me   SCF 2 CHF 2         Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   SO 2 Me       Me   Me   H   Me   Et   Me   H   Cl   Me   SO 2 CF 3         Me   Me   H   Me   OCF 2 CHF 2     Me   H   Cl   CF 3     CF 3         Me   Me   H   Me   SCF 2 CHF 2     Me   H   Cl   CF 3     Me       Me   Me   H   Me   SO 2 Me   Me   H   Cl   OMe   CF 3         Me   Me   H   Me   SO 2 CF 3     Me   H   Cl   H   CF 3         Me   Me   H   CF 3     CF 3     Me   H   Cl   H   OCHF 2         Me   Me   H   CF 3     Me   Me   H   Cl   H   C 2 F 5         Me   Me   H   OMe   CF 3     Et   H   Cl   H   C 2 F 5         Me   Me   H   H   CF 3     Me   H   Cl   H   OCF 3         Me   Me   H   H   OCHF 2     Me   H   Cl   H   OCF 2 CHF 2         Me   Me   H   H   C 2 F 5     Me   H   Cl   H   SCF 2 CHF 2         Et   Me   H   H   C 2 F 5     Me   H   Cl   H   n-C 3 F 7         Me   Me   H   H   OCF 3     Me   H   Cl   H   i-C 3 F 7         Me   Me   H   H   OCF 2 CHF 2     Me   H   Cl   H   Br       Me   Me   H   H   SCF 2 CHF 2     Me   H   Cl   H   Cl       Me   Me   H   H   n-C 3 F 7     Me   H   Cl   H   SCF 3         Me   Me   H   H   i-C 3 F 7     Me   H   Cl   Ph   CF 3         Me   Me   H   H   Br   Me   H   Cl   Ph   Cl       Me   Me   H   H   Cl   Me   H   Cl   Ph   Br       Me   Me   H   H   SCF 3     Me   H   Cl   2-pyridyl   CF 3         Me   Me   H   Ph   CF 3     Me   H   Cl   2-pyridyl   Cl       Me   Me   H   Ph   Cl   Me   H   Cl   2-ClPh   CF 3         Me   Me   H   Ph   Br   Me   H   Cl   2-ClPh   OCF 3         Me   Me   H   2-pyridyl   CF 3     Me   H   Cl   2-ClPh   Br       Me   Me   H   2-pyridyl   Cl   Me   H   Cl   2-ClPh   Cl       Me   Me   H   2-ClPh   CF 3     Me   H   Cl   2-ClPh   SCHF 2         Me   Me   H   2-ClPh   OCF 3     Me   H   Cl   2-BrPh   CF 3         Me   Me   H   2-ClPh   Br   Me   H   Cl   2-MePh   CF 3         Me   Me   H   2-ClPh   Cl   Me   H   Cl   2-CNPh   CF 3         Me   Me   H   2-ClPh   SCHF 2     Me   H   Cl   2-FPh   CF 3         Me   Me   H   2-BrPh   CF 3     Me   H   Cl   2,6-F 2 Ph   CF 3         Me   Me   H   2-MePh   CF 3     Me   H   Cl   2,4-F 2 Ph   CF 3         Me   Me   H   2-CNPh   CF 3     Me   H   Cl   2,5-F 2 Ph   CF 3         Me   Me   H   2-FPh   CF 3     Me   H   Cl   2-MeOPh   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   Me   H   2,5-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Br       Me   Me   H   2-MeOPh   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Cl-2-pyridyl   CF 3     Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-Cl-2-pyridyl   OCF 3     Me   H   Cl   3-F-2-pyridyl   CF 3         Me   Me   H   3-CF 3 -2-   CF 3     Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Me-2-   CF 3     Me   H   Cl   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Cl-2-pyridyl   SCHF 2     Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   Me   H   3-F-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Cl-2-pyridyl   Br   Me   H   Cl   3-Br-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   Cl   Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   CF 3     Me   Cl   H   H   OCF 3         Me   Me   H   3-Br-2-pyridyl   OCF 3     Me   Cl   H   H   OCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Br   Me   Cl   H   H   SCF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   Cl   Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   Me   Br   Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   Et   Br   Me   Cl   H   H   Br       Me   Cl   H   Me   Cl   Me   Cl   H   H   Cl       Me   Cl   H   Et   Cl   Me   Cl   H   H   SCF 3         Me   Cl   H   Me   1   Me   Cl   H   Ph   CF 3         Me   Cl   H   Me   CF 3     Me   Cl   H   Ph   Cl       Me   Cl   H   Me   OCF 3     Me   Cl   H   Ph   Br       Et   Cl   H   Me   CF 3     Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   Me   SCF 3     Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   Me   SCHF 2     Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   Me   OCHF 2     Me   Cl   H   2-ClPh   OCF 3         n-Pr   Cl   H   Me   CF 3     Me   Cl   H   2-ClPh   Br       Me   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   Cl       Et   Cl   H   Me   C 2 F 5     Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   El   CF 3     Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   n-Pr   CF 3     Me   Cl   H   2-MePh   CF 3         Me   Cl   H   i-Pr   CF 3     Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   Cl   CF 3     Me   Cl   H   2-FPh   CF 3         Me   Cl   H   F   CF 3     Me   Cl   H   2,6-F 2 Ph   CF 3         Me   Cl   H   Me   SMe   Me   Cl   H   2,4-F 2 Ph   CF 3         Me   Cl   H   Me   OMe   Me   Cl   H   2,5-F 2 Ph   CF 3         Me   Cl   H   Me   OEt   Me   Cl   H   2-MeOPh   CF 3         Me   Cl   H   Me   n-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   Me   i-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   OCF 3         Me   Cl   H   Me   Et   Me   Cl   H   3-Cl-2-pyridyl   Br       Me   Cl   H   Me   OCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   Cl       Me   Cl   H   Me   SCF 2 CHF 2     Me   Cl   H   3-Cl-2-pyridyl   SCHF 2         Me   Cl   H   Me   SO 2 Me   Me   Cl   H   3-F-2-pyridyl   CF 3         Me   Cl   H   Me   SO 2 CF 3     Me   Cl   H   CF 3     CF 3         Me   Cl   H   3-CF 3 -2-   CF 3     Me   Cl   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Cl   H   CF 3     Me   Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   OMe   CF 3     Me   Cl   H   3-Br-2-pyridyl   OCF 3         Me   Cl   H   H   CF 3     Me   Cl   H   3-Br-2-pyridyl   Br       Me   Cl   H   H   OCHF 2     Me   Cl   H   3-Br-2-pyridyl   Cl       Me   Cl   H   H   C 2 F 5     Et   Cl   H   H   C 2 F 5                      
     [0167]               TABLE 9                                                                                                                  R 3     R 4a     R 4b     R 5a     R 5b     R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CF 3     Me   H   H   H   CF 3         Me   H   Me   H   OCF 3     Me   H   H   H   OCF 3         Et   H   Me   H   OCF 3     Et   H   H   H   OCF 3         Me   H   Me   Me   Br   Me   H   H   Me   Br       Me   H   Me   Et   Br   Me   H   H   Et   Br       Me   H   Me   Me   Cl   Me   H   H   Me   Cl       Me   H   Me   Et   Cl   Me   H   H   Et   Cl       Me   H   Me   Me   I   Me   H   H   Me   I       Me   H   Me   Me   CF 3     Me   H   H   Me   CF 3         Me   H   Me   Me   OCF 3     Me   H   H   Me   OCF 3         Et   H   Me   Me   CF 3     Et   H   H   Me   CF 3         Me   H   Me   Me   SCF 3     Me   H   H   Me   SCF 3         Me   H   Me   Me   SCHF 2     Me   H   H   Me   SCHF 2         Me   H   Me   Me   OCHF 2     Me   H   H   Me   OCHF 2         n-Pr   H   Me   Me   CF 3     n-Pr   H   H   Me   CF 3         Me   H   Me   Me   C 2 F 5     Me   H   H   Me   C 2 F 5         Et   H   Me   Me   C 2 F 5     Et   H   H   Me   C 2 F 5         Me   H   Me   Et   CF 3     Me   H   H   Et   CF 3         Me   H   Me   n-Pr   CF 3     Me   H   H   n-Pr   CF 3         Me   H   Me   i-Pr   CF 3     Me   H   H   i-Pr   CF 3         Me   H   Me   i-Pr   OCF 3     Me   H   H   Me   SMe       Me   H   Me   Me   SMe   Me   H   H   Me   OMe       Me   H   Me   Me   OMe   Me   H   H   Me   OEt       Me   H   Me   Me   OEt   Me   H   H   Me   n-C 3 F 7         Me   H   Me   Me   n-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   Me   i-C 3 F 7     Me   H   H   Me   Et       Me   H   Me   Me   Et   Me   H   H   Me   OCF 2 CHF 2         Me   H   Me   Me   OCF 2 CHF 2     Me   H   H   Me   SCF 2 CHF 2         Me   H   Me   Me   SCF 2 CHF 2     Me   H   H   Me   SO 2 Me       Me   H   Me   Me   SO 2 Me   Me   H   H   Me   SO 2 CF 3         Me   H   Me   Me   SO 2 CF 3     Me   H   H   CF 3     CF 3         Me   H   Me   CHF 2     CF 3     Me   H   H   CF 3     Me       Me   H   Me   CHF 2     Me   Me   H   H   Ph   CF 3         Me   H   Me   Ph   CF 3     Me   H   H   Ph   Cl       Me   H   Me   Ph   Cl   Me   H   H   Ph   Br       Me   H   Me   Ph   Br   Me   H   H   2-pyridyl   CF 3         Me   H   Me   2-pyridyl   CF 3     Me   H   H   2-pyridyl   Cl       Me   H   Me   2-pyridyl   Cl   Me   H   H   2-ClPh   CF 3         Me   H   Me   2-ClPh   CF 3     Me   H   H   2-ClPh   OCF 3         Me   H   Me   2-ClPh   OCF 3     Me   H   H   2-ClPh   Br       Me   H   Me   2-ClPh   Br   Me   H   H   2-ClPh   Cl       Me   H   Me   2-ClPh   Cl   Me   H   H   2-ClPh   SCHF 2         Me   H   Me   2-ClPh   SCHF,   Me   H   H   2-BrPh   CF 3         Me   H   Me   2-BrPh   CF 3     Me   H   H   2-MePh   CF 3         Me   H   Me   2-MePh   CF 3     Me   H   H   2-CNPh   CF 3         Me   H   Me   2-CNPh   CF 3     Me   H   H   2-FPh   CF 3         Me   H   Me   2-FPh   CF 3     Me   H   H   2,6-F 2 Ph   CF 3         Me   H   Me   2,6-F 2 Ph   CF 3     Me   H   H   2,4-F 2 Ph   CF 3         Me   H   Me   2,4-F 2 Ph   CF 3     Me   H   H   2,5-F 2 Ph   CF 3         Me   H   Me   2,5-F 2 Ph   CF 3     Me   H   H   2-MeOPh   CF 3         Me   H   Me   2-MeOPh   CF 3     Me   H   H   3-Cl-2-pyridyl   CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 3     Me   H   H   3-Cl-2-pyridyl   OCF 3         Me   H   Me   3-Cl-2-pyridyl   OCF 3     Me   H   H   3-Cl-2-pyridyl   Br       Me   H   Me   3-Cl-2-pyridyl   Br   Me   H   H   3-Cl-2-pyridyl   Cl       Me   H   Me   3-Cl-2-pyridyl   Cl   Me   H   H   3-Cl-2-pyridyl   SCHF 2         Me   H   Me   3-Cl-2-pyridyl   SCHF 2     Me   H   H   3-F-2-pyridyl   CF 3         Me   H   Me   3-CF 3 -2-   CF 3     Me   H   H   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Me-2-   CF 3     Me   H   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   H   Me   3-F-2-pyridyl   CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   CF 3     Me   H   H   3-Br-2-pyridyl   OCF 3         Me   H   Me   3-Br-2-pyridyl   OCF 3     Me   H   H   3-Br-2-pyridyl   Br       Me   H   Me   3-Br-2-pyridyl   Br   Me   H   H   3-Br-2-pyridyl   Cl       Me   H   Me   3-Br-2-pyridyl   Cl   Me   H   Cl   Et   Br       Me   Me   H   Me   Br   Me   H   Cl   Me   Cl       Me   Me   H   Et   Br   Me   H   Cl   Et   Cl       Me   Me   H   Me   Cl   Me   H   Cl   Me   I       Me   Me   H   Et   Cl   Me   H   Cl   Me   CF 3         Me   Me   H   Me   I   Me   H   Cl   Me   OCF 3         Me   Me   H   Me   CF 3     Et   H   Cl   Me   CF 3         Me   Me   H   Me   OCF 3     Me   H   Cl   Me   SCF 3         Et   Me   H   Me   CF 3     Me   H   Cl   Me   SCHF 2         Me   Me   H   Me   SCF 3     Me   H   Cl   Me   OCHF 2         Me   Me   H   Me   SCHF 2     n-Pr   H   Cl   Me   CF 3         Me   Me   H   Me   OCHF 2     Me   H   Cl   Me   C 2 F 5         n-Pr   Me   H   Me   CF 3     Et   H   Cl   Me   C 2 F 5         Me   Me   H   Me   C 2 F 5     Me   H   Cl   Et   CF 3         Et   Me   H   Me   C 2 F 5     Me   H   Cl   n-Pr   CF 3         Me   Me   H   Et   CF 3     Me   H   Cl   i-Pr   CF 3         Me   Me   H   n-Pr   CF 3     Me   H   Cl   Me   SMe       Me   Me   H   i-Pr   CF 3     Me   H   Cl   Me   OMe       Me   Me   H   Me   SMe   Me   H   Cl   Me   OEt       Me   Me   H   Me   OMe   Me   H   Cl   Me   n-C 3 F 7         Me   Me   H   Me   OEt   Me   H   Cl   Me   i-C 3 F 7         Me   Me   H   Me   n-C 3 F 7     Me   H   Cl   Me   Et       Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   OCF 2 CHF 2         Me   Me   H   Me   Et   Me   H   Cl   Me   SCF 2 CHF 2         Me   Me   H   Me   OCF 2 CHF 2     Me   H   Cl   Me   SO 2 Me       Me   Me   H   Me   SCF 2 CHF 2     Me   H   Cl   Me   SO 2 CF 3         Me   Me   H   Me   SO 2 Me   Me   H   Cl   CF 3     CF 3         Me   Me   H   Me   SO 2 CF 3     Me   H   Cl   CF 3     Me       Me   Me   H   CF 3     CF 3     Me   H   Cl   Ph   CF 3         Me   Me   H   CF 3     Me   Me   H   Cl   Ph   Cl       Me   Me   H   Ph   CF 3     Me   H   Cl   Ph   Br       Me   Me   H   Ph   Cl   Me   H   Cl   2-pyridyl   CF 3         Me   Me   H   Ph   Br   Me   H   Cl   2-pyridyl   Cl       Me   Me   H   2-pyridyl   CF 3     Me   H   Cl   2-ClPh   CF 3         Me   Me   H   2-pyridyl   Cl   Me   H   Cl   2-ClPh   OCF 3         Me   Me   H   2-ClPh   CF 3     Me   H   Cl   2-ClPh   Br       Me   Me   H   2-ClPh   OCF 3     Me   H   Cl   2-ClPh   Cl       Me   Me   H   2-ClPh   Br   Me   H   Cl   2-ClPh   SCHF 2         Me   Me   H   2-ClPh   Cl   Me   H   Cl   2-BrPh   CF 3         Me   Me   H   2-ClPh   SCHF 2     Me   H   Cl   2-MePh   CF 3         Me   Me   H   2-BrPh   CF 3     Me   H   Cl   2-CNPh   CF 3         Me   Me   H   2-MePh   CF 3     Me   H   Cl   2-FPh   CF 3         Me   Me   H   2-CNPh   CF 3     Me   H   Cl   2,6-F 2 Ph   CF 3         Me   Me   H   2-FPh   CF 3     Me   H   Cl   2,4-F 2 Ph   CF 3         Me   Me   H   2,6-F 2 Ph   CF 3     Me   H   Cl   2,5-F 2 Ph   CF 3         Me   Me   H   2,4-F 2 Ph   CF 3     Me   H   Cl   2-OMe   CF 3         Me   Me   H   2,5-F 2 Ph   CF 3     Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   Me   H   2-MeOPh   CF 3     Me   H   Cl   3-Cl-2-pyridyl   OCF 3         Me   Me   H   3-Cl-2-pyridyl   CF 3     Me   H   Cl   3-Cl-2-pyridyl   Br       Me   Me   H   3-Cl-2-pyridyl   OCF 3     Me   H   Cl   3-Cl-2-pyridyl   Cl       Me   Me   H   3-Cl-2-pyridyl   Br   Me   H   Cl   3-Cl-2-pyridyl   SCHF 2         Me   Me   H   3-Cl-2-pyridyl   Cl   Me   H   Cl   3-F-2-pyridyl   CF 3         Me   Me   H   3-CF 3 -2-   CF 3     Me   H   Cl   3-CF 3 -2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Me-2-   CF 3     Me   H   Cl   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Me   H   3-Cl-2-pyridyl   SCHF 2     Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   Me   H   3-F-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   OCF 3         Me   Me   H   3-Br-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   Br       Me   Me   H   3-Br-2-pyridyl   OCF 3     Me   H   Cl   3-Br-2-pyridyl   Cl       Me   Me   H   3-Br-2-pyridyl   Br   Me   Cl   H   Et   CF 3         Me   Me   H   3-Br-2-pyridyl   Cl   Me   Cl   H   n-Pr   CF 3         Me   Cl   H   Me   Br   Me   Cl   H   i-Pr   CF 3         Me   Cl   H   Et   Br   Me   Cl   H   Me   SMe       Me   Cl   H   Me   Cl   Me   Cl   H   Me   OMe       Me   Cl   H   Et   Cl   Me   Cl   H   Me   OEt       Me   Cl   H   Me   I   Me   Cl   H   Me   n-C 3 F 7         Me   Cl   H   Me   CF 3     Me   Cl   H   Me   i-C 3 F 7         Me   Cl   H   Me   OCF 3     Me   Cl   H   Me   Et       Et   Cl   H   Me   CF 3     Me   Cl   H   Me   OCF 2 CHF 2         Me   Cl   H   Me   SCF 3     Me   Cl   H   Me   SCF 2 CHF 2         Me   Cl   H   Me   SCHF 2     Me   Cl   H   Me   SO 2 Me       Me   Cl   H   Me   OCHF 2     Me   Cl   H   Me   SO 2 CF 3         n-Pr   Cl   H   Me   CF 3     Me   Cl   H   CF 3     CF 3         Me   Cl   H   Me   C 2 F 5     Me   Cl   H   CF 3     Me       Et   Cl   H   Me   C 2 F 5     Me   Cl   H   OMe   CF 3         Me   Cl   H   3-Cl-2-pyridyl   CF 3     Me   Cl   H   Ph   CF 3         Me   Cl   H   3-Cl-2-pyridyl   OCF 3     Me   Cl   H   Ph   Cl       Me   Cl   H   3-Cl-2-pyridyl   Br   Me   Cl   H   Ph   Br       Me   Cl   H   3-Cl-2-pyridyl   Cl   Me   Cl   H   2-pyridyl   CF 3         Me   Cl   H   3-Cl-2-pyridyl   SCHF 2     Me   Cl   H   2-pyridyl   Cl       Me   Cl   H   3-F-2-pyridyl   CF 3     Me   Cl   H   2-ClPh   CF 3         Me   Cl   H   3-CF 3 -2-   CF 3     Me   Cl   H   3-Me-2-   CF 3                     pyridyl                   pyridyl       Me   Cl   H   3-Br-2-pyridyl   CF 3     Me   Cl   H   2-ClPh   Br       Me   Cl   H   3-Br-2-pyridyl   OCF 3     Me   Cl   H   2-ClPh   Cl       Me   Cl   H   3-Br-2-pyridyl   Br   Me   Cl   H   2-ClPh   SCHF 2         Me   Cl   H   3-Br-2-pyridyl   Cl   Me   Cl   H   2-BrPh   CF 3         Me   Cl   H   2,4-F 2 Ph   CF 3     Me   Cl   H   2-MePh   CF 3         Me   Cl   H   2,5-F 2 Ph   CF 3     Me   Cl   H   2-CNPh   CF 3         Me   Cl   H   2-OMe   CF 3     Me   Cl   H   2-FPh   CF 3         Me   Cl   H   2-ClPh   OCF 3     Me   Cl   H   2,6-F 2 Ph   CF 3                      
     [0168]               TABLE 10                                                                                                                  R 3     R 4a     R 4b     R 5a     R 5b     R 3     R 4a     R 4b     R 5a     R 5b                 Me   H   Me   H   CHF 2     Me   H   H   H   CHF 2         Me   H   Me   H   CH 2 CF 3     Me   H   H   H   CH 2 CF 3         Et   H   Me   H   CH 2 CF 3     Et   H   H   H   CH 2 CF 3         Me   H   Me   Me   CH 2 CF 3     Me   H   H   Me   CH 2 CF 3         Me   H   Me   Et   CH 2 CF 3     Me   H   H   Et   CH 2 CF 3         Me   H   Me   Me   CF 2 CHF 2     Me   H   H   Me   CF 2 CHF 2         Me   H   Me   Et   CHF 2     Me   H   H   Et   CHF 2         Me   H   Me   Me   CHF 2     Me   H   H   Me   CHF 2         Me   H   Me   Me   CBrF 2     Me   H   H   Me   CBrF 2         Me   H   Me   Me   CHF 2     Me   H   H   Me   CHF 2         Et   H   Me   Me   CH 2 CF 3     Et   H   H   Me   CH 2 CF 3         Me   H   Me   Me   Et   Me   H   H   Me   Et       Me   H   Me   Me   n-Pr   Me   H   H   Me   n-Pr       Me   H   Me   Me   CH 2 C 2 F 5     Me   H   H   Me   CH 2 C 2 F 5         n-Pr   H   Me   Me   CH 2 CF 3     n-Pr   H   H   Me   CH 2 CF 3         Me   H   Me   Me   CF 3     Me   H   H   Me   CF 3         Et   H   Me   Me   C 2 F 5     Et   H   H   Me   C 2 F 5         Me   H   Me   Et   CHF 2     Me   H   H   Et   CHF 2         Me   H   Me   n-Pr   CH 2 CF 3     Me   H   H   n-Pr   CH 2 CF 3         Me   H   Me   i-Pr   CHF 2     Me   H   H   i-Pr   CHF 2         Me   H   Me   Cl   CH 2 CF 3     Me   H   H   Cl   CH 2 CF 3         Me   H   Me   F   CH 2 CF 3     Me   H   H   F   CH 2 CF 3         Me   H   Me   Me   CH 2 Cl   Me   H   H   Me   CH 2 Cl       Me   H   Me   Me   CClF 2     Me   H   H   Me   CClF 2         Me   H   Me   Me   CH 2 CH 2 Cl   Me   H   H   Me   CH 2 CH 2 C1       Me   H   Me   Me   n-C 3 F 7     Me   H   H   Me   n-C 3 F 7         Me   H   Me   Me   i-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   Me   Allyl   Me   H   H   Me   Allyl       Me   H   Me   Et   CF 2 CHF 2     Me   H   H   Me   CF 2 CHF 2         Me   H   Me   Et   i-C 3 F 7     Me   H   H   Me   i-C 3 F 7         Me   H   Me   i-Pr   CF 2 CHF 2     Me   H   H   Me   CF 2 CHF 2         Me   H   Me   n-Pr   CF 2 CHF 2     Me   H   H   Me   CF 2 CHF 2         Me   H   Me   CF 3     CF 2 CHF 2     Me   H   H   CF 3     CF 2 CHF 2         Me   H   Me   CF 3     Me   Me   H   H   CF 3     Me       Me   H   Me   OMe   CH 2 CF 3     Me   H   H   OMe   CH 2 CF 3         Me   H   Me   H   CH 2 CF 3     Me   H   H   H   CH 2 CF 3         Me   H   Me   H   CH 2 CF 3     Me   H   H   H   CH 2 CF 3         Me   H   Me   H   C 2 F 5     Me   H   H   H   C 2 F 5         Et   H   Me   H   C 2 F 5     Et   H   H   H   C 2 F 5         Me   H   Me   H   C 2 F 5     Me   H   H   H   C 2 F 5         Me   H   Me   H   CF 2 CHF 2     Me   H   H   H   CF 2 CHF 2         Me   H   Me   i-Pr   CH 2 CF 3     Me   H   H   H   CH 2 CF 3         Me   H   Me   H   n-C 3 F 7     Me   H   H   H   n-C 3 F 7         Me   H   Me   H   i-C 3 F 7     Me   H   H   H   i-C 3 F 7         Me   H   Me   Ph   CH 2 CF 3     Me   H   H   H   CH 2 CF 3         Me   H   Me   Ph   CF 2 CHF 2     Me   H   H   H   CF 2 CHF 2         Me   H   Me   Ph   CHF 2     Me   H   H   H   CHF 2         Me   H   Me   2-pyridyl   CH 2 CF 3     Me   H   H   Ph   CH 2 CF 3         Me   H   Me   2-pyridyl   CF 2 CHF 2     Me   H   H   Ph   CF 2 CHF 2         Me   H   Me   2-ClPh   CH 2 CF 3     Me   H   H   Ph   CH 2 CF 3         Me   H   Me   2-ClPh   CF 2 CHF 2     Me   H   H   2-pyridyl   CF 2 CHF 2         Me   H   Me   2-ClPh   CHF 2     Me   H   H   2-pyridyl   CHF 2         Me   H   Me   2-ClPh   Et   Me   H   H   2-ClPh   Et       Me   H   Me   2-ClPh   CBrF 2     Me   H   H   2-ClPh   CBrF 2         Me   H   Me   2-BrPh   CH 2 CF 3     Me   H   H   2-ClPh   CH 2 CF 3         Me   H   Me   2-MePh   CH 2 CF 3     Me   H   H   2-ClPh   CH 2 CF 3         Me   H   Me   2-CNPh   CH 2 CF 3     Me   H   H   2-ClPh   CH 2 CF 3         Me   H   Me   2-FPh   CH 2 CF 3     Me   H   H   2-BrPh   CH 2 CF 3         Me   H   Me   2,6-F 2 Ph   CH 2 CF 3     Me   H   H   2-MePh   CH 2 CF 3         Me   H   Me   2,4-F 2 Ph   CH 2 CF 3     Me   H   H   2-CNPh   CH 2 CF 3         Me   H   Me   2,5-F 2 Ph   CH 2 CF 3     Me   H   H   2-FPh   CH 2 CF 3         Me   H   Me   2-MeOPh   CH 2 CF 3     Me   H   H   2,6-F 2 Ph   CH 2 CF 3         Me   H   Me   3-Cl-2-pyridyl   CH 2 CF 3     Me   H   H   2,4-F 2 Ph   CH 2 CF 3         Me   H   Me   3-Cl-2-pyridyl   CF 2 CHF 2     Me   H   H   2,5-F- 2 Ph   CF 2 CHF 2         Me   H   Me   3-Cl-2-pyridyl   CF 3     Me   H   H   2-MeOPh   CF 3         Me   H   Me   3-Cl-2-pyridyl   CHF 2     Me   H   H   3-Cl-2-pyridyl   CHF 2         Me   H   Me   3-Cl-2-pyridyl   CBrF 2     Me   H   H   3-Cl-2-pyridyl   CBrF 2         Me   H   Me   3-F-2-pyridyl   CH 2 CF 3     Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Me   3-CF 3 -2-   CH 2 CF 3     Me   H   H   3-CF 3 -2-   CH 2 CF 3                     pyridyl                   pyridyl       Me   H   Me   3-Me-2-   CH 2 CF 3     Me   H   H   3-Me-2-   CF 2 CHF 2                     pyridyl                   pyridyl       Me   H   Me   3-Br-2-pyridyl   CF 3     Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Me   3-Br-2-pyridyl   CH 2 CF 3     Me   H   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   H   Me   3-Br-2-pyridyl   CF 2 CHF 2     Me   H   H   3-F-2-pyridyl   CF 3         Me   H   Me   3-Br-2-pyridyl   CClF 2     Me   H   H   3-Br-2-pyridyl   CClF 2         Me   Me   H   H   CHF 2     Me   H   H   3-Br-2-pyridyl   CH 2 CF 3         Me   Me   H   H   CH 2 CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Et   Me   H   H   CH 2 CF 3     Me   H   H   3-Br-2-pyridyl   CF 3         Me   Me   H   Me   CH 2 CF 3     Me   H   Cl   Et   CHF 2         Me   Me   H   Et   CH 2 CF 3     Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   CF 2 CHF 2     Me   H   Cl   Et   CH 2 CF 3         Me   Me   H   Et   CHF 2     Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   CHF 2     Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   CBrF 2     Me   H   Cl   Me   CF 2 CHF 2         Me   Me   H   Me   CHF 2     Et   H   Cl   Me   CHF 2         Et   Me   H   Me   CH 2 CF 3     Me   H   Cl   Me   CHF 2         Me   Me   H   Me   Et   Me   H   Cl   Me   CBrF 2         Me   Me   H   Me   n-Pr   Me   H   Cl   Me   CHF 2         Me   Me   H   Me   CH 2 C 2 F 5     n-Pr   H   Cl   Me   CH 2 CF 3         n-Pr   Me   H   Me   CH 2 CF 3     Me   H   Cl   Me   Et       Me   Me   H   Me   CF 3     Et   H   Cl   Me   n-Pr       Et   Me   H   Me   C 2 F 5     Me   H   Cl   Et   CH 2 C 2 F 5         Me   Me   H   Et   CHF 2     Me   H   Cl   n-Pr   CH 2 CF 3         Me   Me   H   n-Pr   CH 2 CF 3     Me   H   Cl   i-Pr   CF 3         Me   Me   H   i-Pr   CHF 2     Me   H   Cl   Cl   C 2 F 5         Me   Me   H   Cl   CH 2 CF 3     Me   H   Cl   F   CHF 2         Me   Me   H   F   CH 2 CF 3     Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   CH 2 Cl   Me   H   Cl   Me   CHF 2         Me   Me   H   Me   CClF 2     Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   CH 2 CH 2 Cl   Me   H   Cl   Me   CH 2 CF 3         Me   Me   H   Me   n-C 3 F 7     Me   H   Cl   Me   CH 2 Cl       Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   CClF 2         Me   Me   H   Me   Allyl   Me   H   Cl   Me   CH 2 CH 2 Cl       Me   Me   H   Me   CF 2 CHF 2     Me   H   Cl   Me   n-C 3 F 7         Me   Me   H   Me   i-C 3 F 7     Me   H   Cl   Me   i-C 3 F 7         Me   Me   H   Me   CF 2 CHF 2     Me   H   Cl   Me   Allyl       Me   Me   H   Me   CF 2 CHF 2     Me   H   Cl   CF 3     CF 2 CHF 2         Me   Me   H   CF 3     CF 2 CHF 2     Me   H   Cl   CF 3     i-C 3 F 7         Me   Me   H   CF 3     Me   Me   H   Cl   OMe   CF 2 CHF 2         Me   Me   H   OMe   CH 2 CF 3     Me   H   Cl   H   CF 2 CHF 2         Me   Me   H   H   CH 2 CF 3     Me   H   Cl   H   CF 2 CHF 2         Me   Me   H   H   CH 2 CF 3     Me   H   Cl   H   Me       Me   Me   H   H   C 2 F 5     Et   H   Cl   H   CH 2 CF 3         Et   Me   H   H   C 2 F 5     Me   H   Cl   H   CH 2 CF 3         Me   Me   H   H   C 2 F 5     Me   H   Cl   H   CH 2 CF 3         Me   Me   H   H   CF 2 CHF 2     Me   H   Cl   H   C 2 F 5         Me   Me   H   H   CH 2 CF 3     Me   H   Cl   H   C 2 F 5         Me   Me   H   H   n-C 3 F 7     Me   H   Cl   H   C 2 F 5         Me   Me   H   H   i-C 3 F 7     Me   H   Cl   H   CF 2 CHF 2         Me   Me   H   H   CH 2 CF 3     Me   H   Cl   H   CH 2 CF 3         Me   Me   H   H   CF 2 CHF 2     Me   H   Cl   H   n-C 3 F 7         Me   Me   H   H   CHF 2     Me   H   Cl   Ph   i-C 3 F 7         Me   Me   H   Ph   CH 2 CF 3     Me   H   Cl   Ph   CH 2 CF 3         Me   Me   H   Ph   CF 2 CHF 2     Me   H   Cl   Ph   CF 2 CHF 2         Me   Me   H   Ph   CH 2 CF 3     Me   H   Cl   2-pyridyl   CHF 2         Me   Me   H   2-pyridyl   CF 2 CHF 2     Me   H   Cl   2-pyridyl   CH 2 CF 3         Me   Me   H   2-pyridyl   CHF 2     Me   H   Cl   2-ClPh   CF 2 CHF 2         Me   Me   H   2-ClPh   Et   Me   H   Cl   2-ClPh   CH 2 CF 3         Me   Me   H   2-ClPh   CBrF 2     Me   H   Cl   2-ClPh   CF 2 CHF 2         Me   Me   H   2-ClPh   CH 2 CF 3     Me   H   Cl   2-ClPh   CHF 2         Me   Me   H   2-ClPh   CH 2 CF 3     Me   H   Cl   2-ClPh   Et       Me   Me   H   2-ClPh   CH 2 CF 3     Me   H   Cl   2-BrPh   CBrF 2         Me   Me   H   2-BrPh   CH 2 CF 3     Me   H   Cl   2-MePh   CH 2 CF 3         Me   Me   H   2-MePh   CH 2 CF 3     Me   H   Cl   2-CNPh   CH 2 CF 3         Me   Me   H   2-CNPh   CH 2 CF 3     Me   H   Cl   2-FPh   CH 2 CF 3         Me   Me   H   2-FPh   CH 2 CF 3     Me   H   Cl   2,6-F 2 Ph   CH 2 CF 3         Me   Me   H   2,6-F 2 Ph   CH 2 CF 3     Me   H   Cl   2,4-F 2 Ph   CH 2 CF 3         Me   Me   H   2,4-F 2 Ph   CH 2 CF 3     Me   H   Cl   2,5-F 2 Ph   CH 2 CF 3         Me   Me   H   2,5-F 2 Ph   CF 2 CHF 2     Me   H   Cl   2-MeOPh   CH 2 CF 3         Me   Me   H   2-MeOPh   CF 3     Me   H   Cl   3-Cl-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Cl-2-pyridyl   CHF 2     Me   H   Cl   3-Cl-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Cl-2-pyridyl   CBrF 2     Me   H   Cl   3-Cl-2-pyridyl   CF 2 CHF 2         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3     Me   H   Cl   3-Cl-2-pyridyl   CF 3         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3     Me   H   Cl   3-Cl-2-pyridyl   CHF 2         Me   Me   H   3-Cl-2-pyridyl   CH 2 CF 3     Me   H   Cl   3-F-2-pyridyl   CBrF 2         Me   Me   H   3-CF 3 -2-   CH 2 CF 3     Me   H   Cl   3-CF 3 -2-   CH 2 CF 3                     pyridyl   pyridyl       Me   Me   H   3-Me-2-   CF 2 CHF 2     Me   H   Cl   3-Me-2-   CH 2 CF 3                     pyridyl                   pyridyl       Me   Me   H   3-F-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Br-2-pyridyl   CClF 2     Me   H   Cl   3-Br-2-pyridyl   CF 3         Me   Me   H   3-Br-2-pyridyl   CH 2 CF 3     Me   H   Cl   3-Br-2-pyridyl   CH 2 CF 3         Me   Me   H   3-Br-2-pyridyl   CF 3     Me   H   Cl   3-Br-2-pyridyl   CF 2 CHF 2         Me   Me   H   3-Br-2-pyridyl   CF 3     Me   Cl   H   H   CF 2 CHF 2         Me   Cl   H   Me   CHF 2     Me   Cl   H   H   CH 2 CF 3         Me   Cl   H   Et   CH 2 CF 3     Me   Cl   H   H   n-C 3 F 7         Me   Cl   H   Me   CH 2 CF 3     Me   Cl   H   H   i-C 3 F 7         Me   Cl   H   Et   CH 2 CF 3     Me   Cl   H   Ph   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3     Me   Cl   H   Ph   CF 2 CHF 2         Me   Cl   H   Me   CF 2 CHF 2     Me   Cl   H   Ph   CHF 2         Me   Cl   H   Me   CHF 2     Me   Cl   H   2-pyridyl   CH 2 CF 3         Et   Cl   H   Me   CHF 2     Me   Cl   H   2-pyridyl   CF 2 CHF 2         Me   Cl   H   Me   CBrF 2     Me   Cl   H   2-ClPh   CH 2 CF 3         Me   Cl   H   Me   CHF 2     Me   Cl   H   2-ClPh   CF 2 CHF 2         Me   Cl   H   Me   CH 2 CF 3     Me   Cl   H   2-ClPh   CHF 2         n-Pr   Cl   H   Me   Et   Me   Cl   H   2-ClPh   Et       Me   Cl   H   Me   n-Pr   Me   Cl   H   2-ClPh   CBrF 2         Et   Cl   H   Me   CH 2 C 2 F 5     Me   Cl   H   2-BrPh   CH 2 CF 3         Me   Cl   H   Et   CH 2 CF 3     Me   Cl   H   2-MePh   CH 2 CF 3         Me   Cl   H   n-Pr   CF 3     Me   Cl   H   2-CNPh   CH 2 CF 3         Me   Cl   H   i-Pr   C 2 F 5     Me   Cl   H   2-FPh   CH 2 CF 3         Me   Cl   H   Cl   CHF 2     Me   Cl   H   2,6-F 2 Ph   CH 2 CF 3         Me   Cl   H   F   CH 2 CF 3     Me   Cl   H   2,4-F 2 Ph   CH 2 CF 3         Me   Cl   H   Me   CHF 2     Me   Cl   H   2,5-F 2 Ph   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3     Me   Cl   H   2-MeOPh   CH 2 CF 3         Me   Cl   H   Me   CH 2 CF 3     Me   Cl   H   3-Cl-2-pyridyl   CH 2 CF 3         Me   Cl   H   Me   CH 2 Cl   Me   Cl   H   3-Cl-2-pyridyl   CF 2 CHF 2         Me   Cl   H   Me   CClF 2     Me   Cl   H   3-Cl-2-pyridyl   CF 3         Me   Cl   H   Me   CH 2 CH 2 Cl   Me   Cl   H   3-Cl-2-pyridyl   CHF 2         Me   Cl   H   Me   n-C 3 F 7     Me   Cl   H   3-Cl-2-pyridyl   CBrF 2         Me   Cl   H   Me   i-C 3 F 7     Me   Cl   H   3-F-2-pyridyl   CH 2 CF 3         Me   Cl   H   3-Me-2-   CH 2 CF 3     Me   Cl   H   3-CF 3 -2-   CH 2 CF 3                     pyridyl               pyridyl       Me   Cl   H   Me   CF 2 CHF 2     Me   Cl   H   3-Br-2-pyridyl   CF 3         Me   Cl   H   CF 3     i-C 3 F 7     Me   Cl   H   3-Br-2-pyridyl   CH 2 CF 3         Me   Cl   H   CF 3     CF 2 CHF 2     Me   Cl   H   3-Br-2-pyridyl   CF 2 CHF 2         Me   Cl   H   OMe   CF 2 CHF 2     Me   Cl   H   3-Br-2-pyridyl   CClF 2         Me   Cl   H   H   CF 2 CHF 2     Me   Cl   H   H   C 2 F 5         Me   Cl   H   H   Me   Me   Cl   H   H   C 2 F 5         Me   Cl   H   H   CH 2 CF 3     Me   Cl   H   H   C 2 F 5         Et   Cl   H   H   CH 2 CF 3     Me   Cl   H   Me   Allyl       Me   Cl   H   H   CH 2 CF 3                      
     [0169] Formulation/Utility  
     [0170] Compounds of this invention will generally be used as a formulation or composition with an agriculturally suitable carrier comprising at least one of a liquid diluent, a solid diluent or a surfactant. The formulation or composition ingredients are selected to be consistent with the physical properties of the active ingredient, mode of application and environmental factors such as soil type, moisture and temperature. Useful formulations include liquids such as solutions (including emulsifiable concentrates), suspensions, emulsions (including microemulsions and/or suspoemulsions) and the like which optionally can be thickened into gels. Useful formulations further include solids such as dusts, powders, granules, pellets, tablets, films, and the like which can be water-dispersible (“wettable”) or water-soluble. Active ingredient can be (micro)encapsulated and further formed into a suspension or solid formulation; alternatively the entire formulation of active ingredient can be encapsulated (or “overcoated”). Encapsulation can control or delay release of the active ingredient. Sprayable formulations can be extended in suitable media and used at spray volumes from about one to several hundred liters per hectare. High-strength compositions are primarily used as intermediates for further formulation.  
     [0171] The formulations will typically contain effective amounts of active ingredient, diluent and Surfactant within the following approximate ranges that add up to 100 percent by weight.  
                                              Weight Percent                                 Active                   Ingredient   Diluent   Surfactant                                         Water-Dispersible and Water-soluble   5-90    0-94   1-15       Granules, Tablets and Powders.       Suspensions, Emulsions, Solutions   5-50   40-95   0-15       (including Emulsifiable       Concentrates)       Dusts   1-25   70-99   0-5       Granules and Pellets   0.01-   5-    0-15           99   99.99       High Strength Compositions   90-99     0-10   0-2                  
 
     [0172] Typical solid diluents are described in Watkins, et al.,  Handbook of Insecticide Dust Diluents and Carriers,  2nd Ed., Dorland Books, Caldwell, N.J. Typical liquid diluents are described in Marsden,  Solvents Guide,  2nd Ed., Interscience, New York, 1950.  McCutcheon&#39;s Detergents and Emulsifiers Annual , Allured Publ. Corp., Ridgewood, N.J., as well as Sisely and Wood,  Encyclopedia of Surface Active Agents , Chemical Publ. Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foam, caking, corrosion, microbiological growth and the like, or thickeners to increase viscosity.  
     [0173] Surfactants include, for example, polyethoxylated alcohols, polyethoxylated alkylphenols, polyethoxylated sorbitan fatty acid esters, dialkyl sulfosuccinates, alkyl sulfates, alkylbenzene sulfonates, organosilicones, N,N-dialkyltaurates, lignin sulfonates, naphthalene sulfonate formaldehyde condensates, polycarboxylates, and polyoxyethylene/polyoxypropylene block copolymers. Solid diluents include, for example, clays such as bentonite, montmorillonite, attapulgite and kaolin, starch, sugar, silica, talc, diatomaceous earth, urea, calcium carbonate, sodium carbonate and bicarbonate, and sodium sulfate. Liquid diluents include, for example, water, N,N-dimethylformamide, dimethyl sulfoxide, N-alkylpyrrolidone, ethylene glycol, polypropylene glycol, paraffins, alkylbenzenes, alkylnaphthalenes, oils of olive, castor, linseed, tung, sesame, corn, peanut, cotton-seed, soybean, rape-seed and coconut, fatty acid esters, ketones such as cyclohexanone, 2-heptanone, isophorone and 4-hydroxy-4-methyl-2-pentanone, and alcohols such as methanol, cyclohexanol, decanol and tetrahydrofurfuryl alcohol.  
     [0174] Solutions, including emulsifiable concentrates, can be prepared by simply mixing the ingredients. Dusts and powders can be prepared by blending and, usually, grinding as in a hammer mill or fluid-energy mill. Suspensions are usually prepared by wet-milling; see, for example, U.S. Pat. No. 3,060,084. Granules and pellets can be prepared by spraying the active material upon preformed granular carriers or by agglomeration techniques. See Browning, “Agglomeration”,  Chemical Engineering  Dec. 4, 1967, pp 147-48 , Perry&#39;s Chemical Engineer&#39;s Handbook,  4th Ed., McGraw-Hill, New York, 1963, pages 8-57 and following, and PCT Publication WO 91/13546. Pellets can be prepared as described in U.S. Pat. No. 4,172,714. Water-dispersible and water-soluble granules can be prepared as taught in U.S. Pat. No. 4,144,050, U.S. Pat. No. 3,920,442 and DE 3,246,493. Tablets can be prepared as taught in U.S. Pat. No. 5,180,587, U.S. Pat. No. 5,232,701 and U.S. Pat. No. 5,208,030. Films can be prepared as taught in GB 2,095,558 and U.S. Pat. No. 3,299,566.  
     [0175] For further information regarding the art of formulation, see T. S. Woods, “The Formulator&#39;s Toolbox—Product Forms for Modern Agriculture” in Pesticide Chemistry and Bioscienice, The Food- Environment Challenge , T. Brooks and T. R. Roberts, Eds., Proceedings of the 9th International Congress on Pesticide Chemistry, The Royal Society of Chemistry, Cambridge, 1999, pp. 120-133. See also U.S. Pat. No. 3,235,361, Col. 6, line 16 through Col. 7, line 19 and Examples 10-41; U.S. Pat. No. 3,309,192, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167 and 169-182; U.S. Pat. No. 2,891,855, Col. 3, line 66 through Col. 5, line 17 and Examples 14; Klingman,  Weed Control as a Science , John Wiley and Sons, Inc., New York, 1961, pp 81-96; and Hance et al.,  Weed Control Handbook,  8th Ed., Blackwell Scientific Publications, Oxford, 1989.  
     [0176] In the following Examples, all percentages are by weight and all formulations are prepared in conventional ways. Compound numbers refer to compounds in Index Table A.  
     EXAMPLE A  
     [0177]                               Wettable Powder                                                Compound 1    65.0%           dodecylphenol polyethylene glycol ether     2.0%           sodium ligninsulfonate     4.0%           sodium silicoaluminate     6.0%           montmorillonite (calcined)   23.0%.                        
     EXAMPLE B  
     [0178]                               Granule                                                Compound 7   10.0%            attapulgite granules (low volatile matter,           0.71/0.30 mm; U.S.S. No. 25-50 sieves)   90.0%.                        
     EXAMPLE C  
     [0179]                               Extruded Pellet                                                Compound 1    25.0%           anhydrous sodium sulfate    10.0%           crude calcium ligninsulfonate     5.0%           sodium alkylnaphthalenesulfonate     1.0%           calcium/magnesium bentonite    59.0%.                        
     EXAMPLE D  
     [0180]                               Emulsifiable Concentrate                                                Compound 7    20.0%           blend of oil soluble sulfonates           and polyoxyethylene ethers    10.0%           isophorone   70.0%.                        
     EXAMPLE E  
     [0181]                               Granule                                                Compound 1     0.5%           cellulose     2.5%           lactose     4.0%           cornmeal   93.0%.                        
     [0182] Compounds of this invention are characterized by favorable metabolic and/or soil residual patterns and exhibit activity controlling a spectrum of agronomic and non-agronomic invertebrate pests. (In the context of this disclosure “invertebrate pest control” means inhibition of invertebrate pest development (including mortality) that causes significant reduction in feeding or other injury or damage caused by the pest; related expressions are defined analogously.) As referred to in this disclosure, the term “invertebrate pest” includes arthropods, gastropods and nematodes of economic importance as pests. The term “arthropod” includes insects, mites, spiders, scorpions, centipedes, millipedes, pill bugs and symphylans. The term “gastropod” includes snails, slugs and other Stylommatophora. The term “nematode” includes all of the helminths, such as: roundworms, heartworms, and phytophagous nematodes (Nematoda), flukes (Tematoda), Acanthocephala, and tapeworms (Cestoda). Those skilled in the art will recognize that not all compounds are equally effective against all pests. Compounds of this invention display activity against economically important agronomic, forest, greenhouse, nursery, ornamentals, food and fiber, public and animal health, domestic and commercial structure, household, and stored product pests. These include larvae of the order Lepidoptera, such as armyworms, cutworms, loopers, and heliothines in the family Noctuidae (e.g., fall armyworm ( Spodoptera fugiperda  J. E. Smith), beet armyworm ( Spodoptera exigua  Hübner), black cutworm ( Agrotis ipsilon  Hufnagel), cabbage looper ( Trichoplusia ni  Hübner), tobacco budworm ( Heliothis virescens  Fabricius)); borers, casebearers, webworms, coneworms, cabbageworms and skeletonizers from the family Pyralidae (e.g., European corn borer ( Ostrina nubilalis  Hübner), navel orangeworm ( Amyelois tracisilella  Walker), corn root webworm ( Crambus caliginosellus  Clemens), sod webworm ( Herpetogramma licarsisalis  Walker)); leafrollers, budworms, seed worms, and fruit worms in the family Tortricidae (e.g., codling moth ( Cydia pomonella  Linnaeus) grape berry moth ( Endopiza viteana  Clemens), oriental fruit moth ( Grapholita molesta  Busck)); and many other economically important lepidoptera (e.g., diamondback moth ( Plutella xylostella  Linnaeus), pink bollworm ( Pectinophora gossypiella  Saunders), gypsy moth (Lymantria dispar Linnaeus)); nymphs and adults of the order Blattodea including cockroaches from the families Blattellidae and Blattidae (e.g., oriental cockroach ( Blatta orientalis  Linnaeus), Asian cockroach ( Blatella asahinai  Mizukubo), German cockroach ( Blatella germianica  Linnaeus), brownbanded cockroach ( Supella lonigipalpa  Fabricius), American cockroach ( Periplanieta americana  Linnaeus), brown cockroach ( Periplaneta brunnea  Burmeister), Madeira cockroach ( Leticophaea maderae  Fabricius)); foliar feeding larvae and adults of the order Coleoptera including weevils from the families Anthribidae, Bruchidae, and Curculionidae (e.g., boll weevil ( Anthonomus gratidis  Boheman), rice water weevil ( Lissorhoptrus oryzophiltus  Kuschel), granary weevil ( Sitophilus granarios  Linnaeus), rice weevil ( Sitophilius oryzae  Linnaeus)); flea beetles, cucumber beetles, rootworms, leaf beetles, potato beetles, and leafminers in the family Chrysomelidae (e.g., Colorado potato beetle ( Leptinotarsa decemlineata  Say), western corn rootworm ( Diabrotica virgifera virgifera  LeConte)); chafers and other beetles from the family Scaribaeidae (e.g., Japanese beetle ( Popillia japonica  Newman) and European chafer ( Rhizotrogus majalis  Razoumowsky)); carpet beetles from the family Dermestidae; wireworms from the family Elateridae; bark beetles from the family Scolytidae and flour beetles from the family Tenebrionidae. In addition it includes: adults and larvae of the order Dermaptera including earwigs from the family Forficulidae (e.g., European earwig ( Forficula auricularia  Linnaeus), black earwig ( Clhelisoches monio  Fabricius)); adults and nymphs of the orders Hemiptera and Homoptera such as, plant bugs from the family Miridae, cicadas from the family Cicadidae, leafhoppers (e.g. Empoasca spp.) from the family Cicadellidae, planthoppers from the families Fulgoroidae and Delphacidae, treehoppers from the family Membracidae, psyllids from the family Psyllidae, whiteflies from the family Aleyrodidae, aphids from the family Aphididae, phylloxera from the family Phylloxeridae, mealybugs from the family Pseudococcidae, scales from the families Coccidae, Diaspididae and Margarodidae, lace bugs from the family Tingidae, stink bugs from the family Pentatomidae, cinch bugs (e.g., Blisszis spp.) and other seed bugs from the family Lygaeidae, spittlebugs from the family Cercopidae squash bugs from the family Coreidae, and red bugs and cotton stainers from the family Pyrrhocoridae. Also included are adults and larvae of the order Acari (mites) such as spider mites and red mites in the family Tetranychidae (e.g., European red mite ( Panonychus ulmi  Koch), two spotted spider mite ( Tetranychus urticae  Koch), McDaniel mite ( Tetranychus mcdanieli  McGregor)), flat mites in the family Tenuipalpidae (e.g., citrus flat mite ( Brevipalpus lewisi  McGregor)), rust and bud mites in the family Eriophyidae and other foliar feeding mites and mites important in human and animal health, i.e. dust mites in the family Epidermoptidae, follicle mites in the family Demodicidae, grain mites in the family Glycyphagidae, ticks in the order Ixodidae (e.g., deer tick ( Ixodes scapularis  Say), Australian paralysis tick ( Ixodes holocyclus  Neumann), American dog tick ( Dermacentor variabilis  Say), lone star tick ( Amblyomma americanum  Linnaeus) and scab and itch mites in the families Psoroptidae, Pyemotidae, and Sarcoptidae; adults and immatures of the order Orthoptera including grasshoppers, locusts and crickets (e.g., migratory grasshoppers (e.g.,  Melanoplus sanguinipes  Fabricius,  M. differetialis  Thomas), American grasshoppers (e.g.,  Schistocerca americania  Drury), desert locust ( Schistocerca gregaria  Forskal), migratory locust ( Locusta migratoria  Linnaeus), house cricket ( Acheta domesticus  Linnaeus), mole crickets (Gryllotalpa spp.)); adults and immatures of the order Diptera including leafminers, midges, fruit flies (Tephritidae), frit flies (e.g., Oscinella frit Linnaeus), soil maggots, house flies (e.g.,  Musca domestica  Linnaeus), lesser house flies (e.g.,  Fannia caninularis  Linnaeus,  F. femoralis  Stein), stable flies (e.g.,  Stomoxys calcitrans  Linnaeus), face flies, horn flies, blow flies (e.g., Chrysomya spp., Phormia spp.), and other muscoid fly pests, horse flies (e.g., Tabanus spp.), bot flies (e.g., Gastrophilus spp., Oestrus spp.), cattle grubs (e.g., Hypoderma spp.), deer flies (e.g., Chrysops spp.), keds (e.g.,  Melophagus ovinus  Linnaeus) and other Brachycera, mosquitoes (e.g., Aedes spp., Anopheles spp., Culex spp.), black flies (e.g., Prosimulium spp., Simulium spp.), biting midges, sand flies, sciarids, and other Nematocera; adults and immatures of the order Thysanoptera including onion thrips (Thrips tabaci Lindeman) and other foliar feeding thrips; insect pests of the order Hymenoptera including ants (e.g., red carpenter ant ( Camponotus ferrugineus  Fabricius), black carpenter ant ( Camponotus pennnsylvanicus  DE Geer), Pharaoh ant ( Monomorium pharaonis  Linnaeus), little fire ant ( Wasmannia auropunctata  Roger), fire ant ( Solenopsis geminata  Fabricius), red imported fire ant (Solenopsis invicta Buren), Argentine ant ( Iridomyrmex humilis  Mayr), crazy ant ( Paratrechina longicornis  Latreille), pavement ant ( Tetramorium caespitum  Linnaeus), cornfield ant ( Lasius alienus  Förster), odorous house ant ( Tapinoma sessile  Say)), bees (including carpenter bees), hornets, yellow jackets and wasps; insect pests of the order Isoptera including the eastern subterranean termite ( Reticulitermes herperus  Kollar), western subterranean termite ( Rericulitermes hesperus  Banks), Formosan subterranean termite ( Coptotermes formosanus  Shiraki), West Indian drywood termite ( Incisitermes immigrans  Snyder) and other termites of economic importance; insect pests of the order Thysanura such as silverfish ( Lepisma saccharina  Linnaeus) and firebrat ( Thermobia domestica  Packard); insect pests of the order Mallophaga and including the head louse ( Pediculus humanus capitis  De Geer), body louse ( Pediculus humanus humanus  Linnaeus), chicken body louse ( Menacacthus stramineus  Nitszch), dog biting louse ( Trichodectes canis  De Geer), fluff louse ( Goniocotes gallinae  De Geer), sheep body louse ( Bovicola ovis  Schrank), short-nosed cattle louse ( Haematopinus eurysternus  Nitzsch), long-nosed cattle louse ( Linognathus vituli  Linnaeus) and other sucking and chewing parasitic lice that attack man and animals; insect pests of the order Siphonoptera including the oriental rat flea ( Xellopsylla cheopis  Rothschild), cat flea ( Ctenocephalides felis  Bouche), dog flea ( Ctenocephalides canis  Curtis), hen flea ( Ceratophyllus gallinae  Schrank), sticktight flea ( Echidnophaga gallinacea  Westwood), human flea ( Pulex irritans  Linnaeus) and other fleas afflicting mammals and birds. Additional arthropod pests covered include: spiders in the order Araneae such as the brown recluse spider ( Loxosceles reclusa  Gertsch &amp; Mulaik) and the black widow spider ( Latrodectus mactans  Fabricius), and centipedes in the order Scutigeromorpha such as the house centipede ( Scutigera coleoptrata  Linnaeus). Activity also includes members of the Classes Nematoda, Cestoda, Trematoda, and Acanthocephala including economically important members of the orders Strongylida, Ascaridida, Oxyurida, Rhabditida, Spirurida, and Enoplida such as but not limited to economically important agricultural pests (i.e. root knot nematodes in the genus Meloidogyne, lesion nematodes in the genus Pratylenchus, stubby root nematodes in the genus Trichodorus, etc.) and animal and human health pests (i.e. all economically important flukes, tapeworms, and roundworms, such as  Strongtlus vulgaris  in horses,  Toxocara canis  in dogs,  Haemonchus contortus  in sheep,  Dirofilaria immitis  Leidy in dogs,  Anoplocephala perfoliata  in horses,  Fasciola hepatica  Linnaeus in ruminants, etc.).  
     [0183] Compounds of the invention show particularly high activity against pests in the order Lepidoptera (e.g.,  Alabama argillacea  Hübner (cotton leaf worm),  Archips argyrospila  Walker (fruit tree leaf roller),  A. rosana  Linnaeus (European leaf roller) and other Archips species,  Chilo suppressalis  Walker (rice stem borer),  Cnaphalocrosis medinalis  Guenee (rice leaf roller),  Crambus caliginiosellus  Clemens (corn root webworm),  Crambus teterrellus  Zincken (bluegrass webworm),  Cydia pomonella  Linnaeus (codling moth),  Earias insulana  Boisduval (spiny bollworm),  Earias vittella  Fabricius (spotted bollworm),  Helicoverpa armigera  Hübner (American bollworm),  Helicoverpa zea  Boddie (corn earworm),  Heliothis virescens  Fabricius (tobacco budworm),  Herpetogramma licarsisalis  Walker (sod webworm), Lobesia botrana Denis &amp; Schiffermüller (grape berry moth),  Pectinophora gossypiella  Saunders (pink bollworm),  Phyllocnistis citrella  Stainton (citrus leafminer),  Pieris brassicae  Linnaeus (large white butterfly),  Pieris rapae  Linnaeus (small white butterfly),  Plutella xylostella  Linnaeus (diamondback moth),  Spodoptera exigita  Hübner (beet armyworm),  Spodoptera litura  Fabricius (tobacco cutworm, cluster caterpillar),  Spodoptera frugiperda  J. E. Smith (fall armyworm),  Trichoplusia ni  Hübner (cabbage looper) and  Tuta absoluta  Meyrick (tomato leafminer)). Compounds of the invention also have commercially significant activity on members from the order Homoptera including:  Acyrthisiphon pisum  Harris (pea aphid),  Aphis craccivora  Koch (cowpea aphid),  Aphis fabae  Scopoli (black bean aphid),  Aphis gossypii  Glover (cotton aphid, melon aphid),  Aphis pomi  De Geer (apple aphid),  Aphis spirarcola  Patch (spirea aphid),  Aulacorthum solani  Kaltenbach (foxglove aphid),  Chaetosiphon fragarfolii  Cockerell (strawberry aphid),  Diuraphis noxia  Kurdjumov/Mordvilko (Russian wheat aphid),  Dysaphis plantaginea  Paaserini (rosy apple aphid),  Eriosoma lanigerum  Hausmann (woolly apple aphid),  Hyalopterus pruni  Geoffroy (mealy plum aphid),  Lipaphis erysimi  Kaltenbach (turnip -aphid),  Metopolophium dirrhodum  Walker (cereal aphid),  Macrosipum euphorbiae  Thomas (potato aphid),  Myzus persicae  Sulzer (peach-potato aphid, green peach aphid),  Nasonovia ribisnigri  Mosley (lettuce aphid), Pemphigus spp. (root aphids and gall aphids),  Rhopalosiphum maidis  Fitch (corn leaf aphid),  Rhopalosiphum padi  Linnaeus (bird cherry-oat aphid),  Schizaphis graiminim  Rondani (greenbug),  Sitobion avenae  Fabricius (English grain aphid),  Therioaphis mactulata  Buckton (spotted alfalfa aphid),  Toxoptera aurantii  Boyer de Fonscolombe (black citrus aphid), and  Toxoptera citricida  Kirkaldy (brown citrus aphid); Adelges spp. (adelgids);  Phylloxera devastatrix  Pergande (pecan phylloxera);  Bemisia tabaci  Gennadius (tobacco whitefly, sweetpotato whitefly),  Bemisia argentifolii  Bellows &amp; Perring (silverleaf whitefly),  Dialeurodes citri  Ashmead (citrus whitefly) and  Trialeurodes vaporarioirum  Westwood (greenhouse whitefly);  Empoasca fabae  Harris (potato leafhopper),  Laodelphax striatellus  Fallen (smaller brown planthopper),  Macrolestes quadrilineatus  Forbes (aster leafhopper),  Nephotettix cinticeps  Uhler (green leafhopper),  Nephotettix nigropictus  Stal (rice leafhopper),  Nilaparvata lugents  Stål (brown planthopper),  Peregrinus maidis  Ashmead (corn planthopper),  Sogatella furcifera Horvath (white-backed planthopper),    Sogatodes orizicola  Muir (rice delphacid),  Typhlocyba pomaria  McAtee white apple leafhopper, Erythroneoura spp. (grape leafhoppers);  Magicidada septenzclecim  Linnaeus (periodical cicada);  Icerya purchasi  Maskell (cottony cushion scale),  Quadraspidiotus perniciosus  Comstock (San Jose scale);  Planiococcus citri  Risso (citrus mealybug); Pseudococus spp. (other mealybug complex);  Cacopsylla pyricola  Foerster (pear psylla),  Trioza diospyri  Ashmead (persimmon psylla). These compounds also have activity on members from the order Hemiptera including:  Acrosternum hilare  Say (green stink bug),  Anasa tristis  De Geer (squash bug),  Blissus leucopterus leucopterus  Say (chinch bug),  Corythutca gossypii  Fabricius (cotton lace bug),  Cyrtopeltis modesta  Distant (tomato bug),  Dysdercus suturellus  Herrich-Schäffer (cotton stainer),  Eutchistus servus  Say (brown stink bug),  Euchistus variolarius  Palisot de Beauvois (one-spotted stink bug), Graptosthetus spp. (complex of seed bugs),  Leptoglossus corculus  Say (leaf-footed pine seed bug),  Lygus lineolaris  Palisot de Beauvois (tarnished plant bug),  Nezara virdula  Linnaeus (southern green stink bug),  Oebalus pugnax  Fabricius (rice stink bug),  Oncopeltus fasciatus  Dallas (large milkweed bug),  Pseudatomoscelis seriatus  Reuter (cotton fleahopper). Other insect orders controlled by compounds of the invention include Thysanoptera (e.g.,  Frankliniella occidenitalis  Pergande (western flower thrip),  Scirthothrops citri  Moulton (citrus thrip),  Sericothrips variabilis  Beach (soybean thrip), and  Thrips tabaci  Lindeman (onion thrip); and the order Coleoptera (e.g.,  Leptinotarsa decemlineata  Say (Colorado potato beetle),  Epilachna varivestis  Mulsant (Mexican bean beetle) and wireworms of the genera  Agriotes, Atlous  or Limonius).  
     [0184] Compounds of this invention can also be mixed with one or more other biologically active compounds or agents including insecticides, fungicides, nematocides, bactericides, acaricides, growth regulators such as rooting stimulants, chemosterilants, semiochemicals, repellents, attractants, pheromones, feeding stimulants, other biologically active compounds or entomopathogenic bacteria, virus or fungi to form a multi-component pesticide giving an even broader spectrum of agricultural utility. Thus compositions of the present invention can further comprise a biologically effective amount of at least one additional biologically active compound or agent. Examples of such biologically active compounds or agents with which compounds of this invention can be formulated are: insecticides such as abamectin, acephate, acetamiprid, avermectin, azadirachtin, azinphos-methyl, bifenthrin, binfenazate, buprofezin, carbofuran, chlorfenapyr, chlorfluazuron, chlorpyrifos, chlorpyrifos-methyl, chromafenozide, clothianidin, cyfluthrin, beta-cyfluthrin, cyhalothrin, lambda-cyhalothrin, cypermethrin, cyromazine, deltamethrin, diafenthiuron, diazinon, diflubenzuron, dimethoate, diofenolan, emamectin, endosulfan, esfenvalerate, ethiprole, fenothicarb, fenoxycarb, fenpropathrin, fenproximate, fenvalerate, fipronil, flonicamid, flucythrinate, tau-fluvalinate, flufenoxuron, fonophos, halofenozide, hexaflumuron, imidacloprid, indoxacarb, isofenphos, lufenuron, malathion, metaldehyde, methamidophos, methidathion, methomyl, methoprene, methoxychlor, monocrotophos, methoxyfenozide, nithiazin, novaluron, oxamyl, parathion, parathion-methyl, permethrin, phorate, phosalone, phosmet, phosphamidon, pirimicarb, profenofos, pymetrozine, pyridalyl, pyriproxyfen, rotenone, spinosad, sulprofos, tebufenozide, teflubenzuron, tefluthrin, terbufos, tetrachlorvinphos, thiacloprid, thiamethoxam, thiodicarb, thiosultap-sodium, tralomethrin, trichlorfon and triflumuron; fungicides such as acibenzolar, azoxystrobin, benomyl, blasticidin, Bordeaux mixture (tribasic copper sulfate), bromuconazole, carpropamid, captafol, captan, carbendazim, chloroneb, chlorothalonil, copper oxychloride, copper salts, cyflufenamid, cymoxanil, cyproconazole, cyprodinil, (S)-3,5-dichloro-N-(3-chloro-1-ethyl-1-methyl-2-oxopropyl)-4-methylbenzamide (RH 7281), diclocymet (S-2900), diclomezine, dicloran, difenoconazole, (5)-3,5-dihydro-5-methyl-2-(methylthio)-5-phenyl-3-(phenylamino)-4H-imidazol-4-one (RP 407213), dimethomorph, dimoxystrobin, diniconazole, diniconazole-M, dodine, edifenphos, epoxiconazole, famoxadone, fenamidone, fenarimol, fenbuconazole, fencaramid (SZX0722), fenpiclonil, fenpropidin, fenpropimorph, fentin acetate, fentin hydroxide, fluazinam, fludioxonil, flumetover (RPA 403397), fluquinconazole, flusilazole, flutolanil, flutriafol, folpet, fosetyl-aluminum, furalaxyl, furametapyr (S-82658), hexaconazole, ipconazole, iprobenfos, iprodione, isoprothiolane, kasugamycin, kresoxim-methyl, mancozeb, maneb, mefenoxam, mepronil, metalaxyl, metconazole, metomino-strobin/fenominostrobin (SSF-126), myclobutanil, neo-asozin (ferric methanearsonate), oxadixyl, penconazole, pencycuron, probenazole, prochloraz, propamocarb, propiconazole, pyrifenox, pyraclostrobin, pyrimethanil, pyroquilon, quinoxyfen, spiroxamine, sulfur, tebuconazole, tetraconazole, thiabendazole, thifluzamide, thioplhanate-methyl, thiram, tiadinil, triadimefon, triadimenol, tricyclazole, trifloxystrobin, triticonazole, validamycin and vinclozolin; nematocides such as aldicarb, oxamyl and fenamiphos; bactericides such as streptomycin; acaricides such as amitraz, chinomethionat, chlorobenzilate, cyhexatin, dicofol, dienochlor, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenpyroximate, hexythiazox, propargite, pyridaben and tebufenpyrad; and biological agents such as Bacillizs thutritigietisis including ssp. aizaivai and kzirstaki, Bacillus thuiriiigieiisis delta endotoxin, baculovirus, and entomopathogenic bacteria, virus and fungi.  
     [0185] A general reference for these agricultural protectants is  The Pesticide Manual,  12th Edition, C. D. S. Tomlin, Ed., British Crop Protection Council, Farnham, Surrey, U.K., 2000.  
     [0186] Preferred insecticides and acaricides for mixing with compounds of this invention include pyrethroids such as cypermethrin, cyhalothrin, cyfluthrin, beta-cyfluthrin, esfenvalerate, fenvalerate and tralomethrin; carbamates such as fenothicarb, methomyl, oxamyl and thiodicarb; neonicotinoids such as clothianidin, imidacloprid and thiacloprid; neuronal sodium channel blockers such as indoxacarb; insecticidal macrocyclic lactones such as spinosad, abamectin, avenrnectin and emamectin; γ-aminobutyric acid (GABA) antagonists such as endosulfan, ethiprole and fipronil; insecticidal ureas such as flufenoxuron and triflumuron; juvenile hormone mimics such as diofenolan and pyriproxyfen; pymetrozine; and amitraz. Preferred biological agents for mixing with compounds of this invention include  Bacillus thuringiensis  and  Bacillus thuringiensis  delta endotoxin as well as naturally occurring and genetically modified viral insecticides including members of the family Baculoviridae as well as entomophagous fungi.  
     [0187] Most preferred mixtures include a mixture of a compound of this invention with cyhalothrin; a mixture of a compound of this invention with cyfluthrin; a mixture of a compound of this invention with beta-cyfluthrin; a mixture of a compound of this invention with esfenvalerate; a mixture of a compound of this invention with methomyl; a mixture of a compound of this invention with imidacloprid; a mixture of a compound of this invention with thiacloprid; a mixture of a compound of this invention with indoxacarb; a mixture of a compound of this invention with abamectin; a mixture of a compound of this invention with endosulfan; a mixture of a compound of this invention with ethiprole; a mixture of a compound of this invention with fipronil; a mixture of a compound of this invention with flufenoxuron; a mixture of a compound of this invention with pyriproxyfen; a mixture of a compound of this invention with pymetrozine; a mixture of a compound of this invention with amitrax; a mixture of a compound of this invention with Bacillus thuringiensis and a mixture of a compound of this invention with  Bacillus thuringiensis  delta endotoxin.  
     [0188] In certain instances, combinations with other invertebrate pest control compounds or agents having a similar spectrum of control but a different mode of action will be particularly advantageous for resistance management. Thus, compositions of the present invention can further comprise an biologically effective amount of at least one additional invertebrate pest control compounds or agents having a similar spectrum of control but a different mode of action. Contacting a plant genetically modified to express a plant protection compound (e.g., protein) or the locus of the plant with a biologically effective amount of a compound of invention can also provide a broader spectrum of plant protection and be advantageous for resistance management.  
     [0189] Invertebrate pests are controlled and protection of agronomic, horticultural and specialty crops, animal and human health is achieved by applying one or more of the compounds of this invention, in an effective amount, to the environment of the pests including the agronomic and/or nonagronomic locus of infestation, to the area to be protected, or directly on the pests to be controlled. Thus, the present invention further comprises a method for the control of foliar- and soil-inhabiting invertebrates and protection of agronomic and/or nonagronomic crops, comprising contacting the invertebrates or their environment with a biologically effective amount of one or more of the compounds of the invention, or with a composition comprising at least one such compound or a composition comprising at least one such compound and an effective amount of at least one additional biologically active compound or agent. A preferred method of contact is by spraying. Alternatively, a granular composition comprising a compound of the invention can be applied to the plant foliage or the soil. Compounds of this invention are effective in delivery through plant uptake by contacting the plant with a composition comprising a compound of this invention applied as a soil drench of a liquid formulation, a granular formulation to the soil, a nursery box treatment or a dip of transplants. Other methods of contact include application of a compound or a composition of the invention by direct and residual sprays, aerial sprays, seed coats, microencapsulations, systemic uptake, baits, eartags, boluses, floggers, fumigants, aerosols, dusts and many others.  
     [0190] The compounds of this invention can be incorporated into baits that are consumed by the invertebrates or within devices such as traps and the like. Granules or baits comprising between 0.01-5% active ingredient, 0.05-10% moisture retaining agent(s) and 40-99% vegetable flour are effective in controlling soil insects at very low application rates, particularly at doses of active ingredient that are lethal by ingestion rather than by direct contact.  
     [0191] The compounds of this invention can be applied in their pure state, but most often application will be of a formulation comprising one or more compounds with suitable carriers, diluents, and surfactants and possibly in combination with a food depending on the contemplated end use. A preferred method of application involves spraying a water dispersion or refined oil solution of the compounds. Combinations with spray oils, spray oil concentrations, spreader stickers, adjuvants, other solvents, and synergists such as piperonyl butoxide often enhance compound efficacy.  
     [0192] The rate of application required for effective control (i.e. “biologically effective amount”) will depend on such factors as the species of invertebrate to be controlled, the pest&#39;s life cycle, life stage, its size, location, time of year, host crop or animal, feeding behavior, mating behavior, ambient moisture, temperature, and the like. Under normal circumstances, application rates of about 0.01 to 2 kg of active ingredient per hectare are sufficient to control pests in agronomic ecosystems, but as little as 0.0001 kg/hectare may be sufficient or as much as 8 kg/hectare may be required. For nonagronomic applications, effective use rates will range from about 1.0 to 50 mg/square meter but as little as 0.1 mg/square meter may be sufficient or as much as 150 mg/square meter may be required.  
     [0193] One skilled in the art can easily determine the biologically effective amount necessary for the desired level of invertebrate pest control. The following Tests in the Biological Examples of the Invention demonstrate the control efficacy of compounds of this invention on specific pests. “Control efficacy” represents inhibition of arthropod development (including mortality) that causes significantly reduced feeding. The pest control protection afforded by the compounds is not limited, however, to these species. See Index Tables A-E for compound descriptions. The following abbreviations are used in the Index Tables that follow: t is tertiary, si is normal, i is iso, s is secondary, Me is methyl, Et is ethyl, Pr is propyl and Bu is butyl; accordingly i-Pr is isopropyl, s-Bu is secondary butyl, etc. Ac is COCH 3 . The abbreviation “Ex.” stands for “Example” and is followed by a number indicating in which example the compound is prepared.  
               INDEX TABLE A                                                                                                      Com-                       m.p.       pound   R 2     R 3     R 4     m   R 5     ° C.                                                 1 (Ex. 1)   Me   H   H   2   2-Me-4-F   249       2    i-Pr   H   H   2   2-Me-4-Cl   &gt;250       3    n-Pr   H   H   2   2-Me-4-Cl   212       4    i-Bu   H   H   2   2-Me-4-Cl   ***       5    Me   Me   H   2   2-Me-4-Cl   ***       6    Et   H   H   2   2-Me-4-Cl   ***       7    Me   H   H   2   2-Me-4-Cl   244       8    allyl   H   H   2   2,4-di-Me   243       9    cyclo-Pr   H   H   2   2-Me-4-Cl   246       10   H   H   H   2   2-Me-4-Cl   ***       11   Me   H   H   2   2-Me-4-OCF 3     &gt;250       12   Me   H   H   1   4-OCF 3     &gt;250       13   Me   H   H   2   2,4-di-Cl   &gt;250       14   Me   H   H   2   2-Me-5-Cl   241       15   Me   H   H   2   2-Me-3-Cl   &gt;250       16   Me   H   H   1   2-Me   236       17   Me   H   H   2   2-Me-4-Br   234       18   Me   H   H   1   4-i-Pr   &gt;250       19   Me   H   H   1   4-NHAc   224       20   Me   H   H   1   2-Br   210       21   Me   H   H   1   2-OPh   193       22   Me   H   H   1   4-OMe   188       23   Me   H   H   1   4-   246                           (morpholin-4-yl)       24   Me   H   H   1   2-F   177       25   Me   H   H   1   4-I   235       26   Me   H   H   2   2-Me-4-NO 2     242       27   Me   H   H   1   3-CF 3     235       28   Me   H   H   1   3-I   216       29   Me   H   H   2   2-Me-4-OMe   205       30   Me   H   H   1   3-Br   230       31   Me   H   H   1   4-Ac   226       32   Me   H   H   1   4-Br   220       33   Me   H   H   1   4-CN   216       34   Me   H   H   1   3-NO 2     242       35   Me   H   H   1   4-Cl   197       36   Me   H   H   1   3-CH 3     220       37   Me   H   H   1   3-Cl   209       38   Me   H   H   2   2,5-di-Me   204       39   Me   H   H   2   2-Me-6-OMe   223       40   Me   H   H   2   2,3-di-Me   187       41   Me   H   H   1   2-OMe   192       42   Me   H   H   1   4-CO 2 Et   202       43   Me   H   H   1   4-NMeAc   210       44   Me   H   H   2   2,6-di-Me   &gt;250       45   Me   H   H   1   2-(pyrrol-1-yl)   208       46   Me   H   H   1   4-NO 2     224       47   Me   H   H   1   3-OCH 2 Ph   214       48   Me   H   H   2   2,4-di-Me   213       49   Me   H   H   1   3-CN   200       50   Me   H   H   1   3-OCF 3     &gt;250       51   Me   H   H   2   2-Me-3-NO 2     233       52   Me   H   H   1   2-OEt   224       53   Me   H   H   1   4-(4-ClPhO)   224       54   Me   H   H   1   4-CH 3     248       55   Me   H   H   1   4-O-i-Pr   183       56   Me   H   H   1   4-F   247       57   Me   H   H   1   2-SMe   204       58   Me   H   H   1   2-t-Bu   248       59   Me   H   H   1   3-SMe   218       60   Me   H   H   1   4-OEt   195       61   Me   H   H   1   2-CH 2 CN   191       62   Me   H   H   1   2-Et   200       63   i-Pr   H   4-NO2/   2   2-Me-4-Cl   ***                   5-NO2                   (1/1 mixture)       64   Me   H   4-Br/   2   2-Me-4-Cl   ***                   5-Br                   (1/1 mixture)       65   Me   H   H   1   2-CONH(i-Pr)-   248                           6-Me        66*   Me   H   H   2   2-Me-4-Cl   ***        67*   Me   H   H   2   2-Me-4-OCF 3     ***       68   Me   H   H   2   2-Me-S-NO 2     242       69   Me   H   H   2   2-Me-4-CF 3     250       70   Me   H   H   1   4-CF 3     246       71   Me   H   H   1   2-Ph   163       72   Me   H   H   2   2-(1-Me-tetrazol-   202                           5-yl)-6-Me       73   Me   H   H   1   2-CONHMe   235       74   Me   H   H   2   2-Me-6-Cl   231       75   Me   H   H   2   3-NO 2 -4-Me   223       76   Me   H   H   3   2-F-4-Cl-5-NO 2     250       77   Me   H   H   2   2-Br-4-Me   198       78   Me   H   H   3   2-Br-4,6-di-F   197       79   Me   H   H   2   2,5-di-NO 2     223       80   Me   H   H   2   2-F-4-Cl   250       81   Me   H   H   2   2-Me-3-F   242       82   Me   H   H   2   2-Br-4-F   126.5       83   Me   H   H   1   2-   193                           (morpholin-4-yl)       84   Me   H   H   2   3-NO 2 -4-F   248       85   Me   H   H   2   3,4-di-F   110       86   Me   H   H   2   2-Cl-4-F   250       87   Me   H   H   1   2-CF 3     217       88   Me   H   H   2   2-CN-4-Cl   250       89   Me   H   H   1   2-Ac   237       90   Me   H   H   1   2-OCF 3     209       91   Me   H   H   1   2-SCF 3     211       92   Me   H   H   2   2-CF 3 -4-Br   250                                  
 
     [0194]               INDEX TABLE B                                                                                                  Compound   R 2     R 3     R 4     J   m.p. ° C.                                                                         93   Me   H   H                         199               94   Me   H   H                         175               95   Me   H   H                         126.5               96   Me   H   H                         217               97   Me   H   H                         171                    
     [0195]               INDEX TABLE C                                                                                                      Compound   R 2     R 3     R 4     m   R 5     m.p. ° C.                                                 98 (Ex. 2)   i-Pr   H   H   2   3,4-di-F   227        99   i-Pr   H   H   2   2,3-di-Me   242       100   i-Pr   H   H   2   2,4-di-F   204       101   i-Pr   H   H   1   4-OCF 3     186       102   i-Pr   H   H   1   4-Cl   218       103   i-Pr   H   H   1   4-Et   206       104   i-Pr   H   H   1   4-CF 3     165       105   Me   H   H   2   3,4-di-F   250       106   Me   H   H   2   2,3-di-Me   184.5       107   Me   H   H   2   2,4-di-F   207       108   Me   H   H   1   4-Cl   250       109   Me   H   H   1   4-Et   250       110   Me   H   H   1   4-CF 3     208       111   Me   H   H   1   4-OCF 3     144       112   Me   H   H   1   2-Me   173.5       113   i-Pr   H   H   1   2-Me   176.5       114   i-Pr   H   H   2   2-Me-4-O-CF 3     173.5       115   i-Pr   H   H   2   2-Me-4-CF 3     194.5       116   Me   H   H   2   2-Me-4-OCF 3     173.5       117   Me   H   H   2   2-Me-4-CF 3     204.5                    
     [0196]               INDEX TABLE D                                                                                                  Com-                           pound   R 2     R 3     R 4     J   m.p. ° C.                                             118   i-Pr   H   H   1-naphthyl   210       119   i-Pr   H   H   2-thienyl   208       120   Me   H   H   2-thienyl   215       (Ex. 3)       121   Me   H   H   1-naphthyl   214               121   i-Pr   H   H                         210               123   Me   H   H                         210               124   Me   H   H                         215.5               125   i-Pr   H   H                         186                    
     [0197]                              INDEX TABLE E                     Cmpd No.     1 H NMR Data (CDCl 3  solution unless indicated otherwise) a                               4   (DMSO-d6) δ: 0.9 (m, 6H), 2.37 (s, 3H), 3.01 (m, 1H), 3.96           (d, 2H), 7.27-8.48 (m, 10H), 9.84 (br s, 1H).       5   (DMSO-d6) δ: 2.36 (s, 3H), 2.88 (s, 3H), 2.94 (s, 3H),           7.28-8.08 (m, 10H), 9.99 (s, 1H).       6   (DMSO-d6) δ: 1.07 (t, 3H), 2.37 (s, 3H), 3.22 (m, 2H),           7.30-8.06 (m, 9H), 8.40 (t, 1H), 9.86 (s, 1H).       10   (DMSO-d6) δ: 2.36 (s, 3K), 7.25-8.08 (m, 11H), 9.88           (s, 1H).       63   (DMSO-d6) δ: 1.09 (d, 6H), 2.36 (s, 3H), 4.03 (m, 1H),           7.27-8.52 (m, 9H), 10.04 (s, 1H).       64   (DMSO-d6) δ: 2.36 (s, 3H), 2.69 (d, 3H), 7.33-8.84           (m, 8H), 8.45 (br q, 1H), 9,98 (s, 1H).       66   (DMSO-d6) δ: 2.37 (s, 3H), 2.71 (d, 3H), 7.27-8.10           (m, 9H), 8.34 (br q, 1H), 9.88 (s, 1H).       67   (DMSO-d6) δ: 2.41 (s, 3H), 2.72 (d, 3H), 7.26-8.08 (m,           9H), 8.36 (br q, 1H), 9.95 (s, 1H).                            
     BIOLOGICAL EXAMPLES OF THE INVENTION  
     Test A  
     [0198] For evaluating control of fall armyworm ( Spodoptera frugiperda ) the test unit consisted of a small open container with a 45-day-old corn (maize) plant inside. This was pre-infested with 10-15 1-day-old larvae on a piece of insect diet by use of a core sampler to remove a plug from a sheet of hardened insect diet having many larvae growing on it and transfer the plug containing larvae and diet to the test unit. The larvae moved onto the test plant as the diet plug dried out.  
     [0199] Test compounds were formulated using a solution containing 10% acetone, 90% water and 300 ppm X-770 Spreader Lo-Foam Formula non-ionic surfactant containing alkylarylpolyoxyethylene, free fatty acids, glycols and isopropanol (Loveland Industries, Inc.), unless otherwise indicated. The formulated compounds were applied in 1 mL of liquid through a SUJ2 atomizer nozzle with 1/8 JJ custom body (Spraying Systems Co,) positioned 1.27 cm (0.5 inches) above the top of each test unit. All experimental compounds in this screen were sprayed at 250 ppm and replicated three times. After spraying of the formulated test compound, each test unit was allowed to dry for 1 hour and then a black, screened cap was placed on top. The test units were held for 6 days in a growth chamber at 25° C. and 70% relative humidity. Plant feeding damage was then visually assessed.  
     [0200] Of the compounds tested, the following provided excellent levels of plant protection (10% or less feeding damage): 1, 7, 11, 16, 48, 66 and 67.  
     Test B  
     [0201] For evaluating control of tobacco budworm ( Heliothis virescens ) the test unit consisted of a small open container with a 67 day old cotton plant inside. This was pre-infested with 82-day-old larvae on a piece of insect diet by use of a core sampler as described for Test A.  
     [0202] Test compounds were formulated and sprayed at 250 ppm as described for Test A. The applications were replicated three times. After spraying, the test units were maintained in a growth chamber and then visually rated as described for Test A.  
     [0203] Of the compounds tested, the following provided excellent levels of plant protection (10% or less feeding damage): 1, 7 and 16.  
     Test C  
     [0204] For evaluating control of diamondback moth ( Plutella xylostella ) the test unit consisted of a small open container with a 12-14-day-old radish plant inside. This was pre-infested with 10-15 neonate larvae on a piece of insect diet by use of a core sampler as described for Test A.  
     [0205] Test compounds were formulated and sprayed at 250 ppm as described for Test A. The applications were replicated three times. After spraying, the test units were maintained in a growth chamber and then visually rated as described for Test A.  
     [0206] Of the compounds tested, the following provided excellent levels of plant protection (10% or less feeding damage): 1, 7, 11, 12, 14, 16, 20, 24, 37, 48, 51, 54, 55, 56, 61, 66, 67, 69, 70, 72, 75, 81, 85, 86, 89, 90, 91, 93 and 97.  
     Test D  
     [0207] For evaluating control of beet armyworm ( Spodoptera exigua ) the test unit consisted of a small open container with a 4-5-day-old corn plant inside. This was pre-infested with 10-15 1-day-old larvae on a piece of insect diet by use of a core sampler as described for Test A.  
     [0208] Test compounds were formulated and sprayed at 250 ppm as described for Test A. The applications were replicated three times. After spraying, the test units were maintained in a growth chamber and then visually rated as described for Test A.  
     [0209] Of the compounds tested, the following provided excellent levels of plant protection (10% or less feeding damage): 1, 40 and 54.