(AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS

Abstract: The present application describes 6-membered aromatics of formula (I) or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.

Description: TITLE (AMIDIN0)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS FIELD OF THE INVENTION This invention relates generally to novel 6-membered aromatics which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders. BACKGROUND OF THE INVENTION WO 96/28427 describes benzamidine anticoagulants of the formula: wherein Z 1 and Z 2 are O, N(R) , S or OCH 2 and the central ring may be phenyl or a variety of heterocycles . The presently claimed compounds do not contain the Z 1 linker or the substitution pattern of the above compounds. WO 95/18111 addresses fibrinogen receptor antagonists, containing basic and acidic termini, of the formula: wherein R 1 represents the basic termini, U is an alkylene or heteroatom linker, V may be a heterocycle, and the right hand portion of the molecule represents the acidic termini . The presently claimed compounds do not contain the acidic termini of WO 95/18111. Activated factor Xa, whose major practical role is the generation of thrombin by the limited proteolysis of prothrombin, holds a central position that links the intrinsic and extrinsic activation mechanisms in the final common pathway of blood coagulation. The generation of thrombin, the final serine protease in the pathway to generate a fibrin clot, from its precursor is amplified by formation of prothrombinase complex (factor Xa, factor V, Ca 2+ and phospholipid) . Since it is calculated that one molecule of factor Xa can generate 138 molecules of thrombin (Elodi, S., Varadi, K. : Optimization of condi tions for the catalytic effect of the factor IXa- factor VIII Complex: Probable role of the complex in the amplification of blood coagulation . Thromb. Res . 1979, 15, 617-629), inhibition of factor Xa may be more efficient than inactivation of thrombin in interrupting the blood coagulation system. Therefore, efficacious and specific inhibitors of factor Xa are needed as potentially valuable therapeutic agents for the treatment of thromboembolic disorders . It is thus desirable to discover new factor Xa inhibitors. SUMMARY OF THE INVENTION Accordingly, one object of the present invention is to provide novel 6-membered aromatics which are useful as factor Xa inhibitors or pharmaceutically acceptable salts or prodrugs thereof . It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt or prodrug form thereof . It is another object of the present invention to provide a method for treating thromboembolic disorders comprising administering to a host in need of such treatment a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt or prodrug form thereof . These and other objects, which will become apparent during the following detailed description, have been achieved by the inventors' discovery that compounds of formula (I): I or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, D, E, M, R la , R lb , and Z are defined below, are effective factor Xa inhibitors. DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS [1] Thus, in a first embodiment, the present invention provides novel compounds of formula I : I or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein; ring M contains from 0-4 N atoms; D is selected from CN, C (=NR 7 ) NR 8 R 9 , NHC (=NR 7 ) R 8 R 9 , NR 8 CH(=NR 7 ), C(0)NR 8 R 9 , and (CR 8 R 9 ) t NR 8 R 9 ; E is selected from phenyl, 2-pyridyl, 4-pyridyl, pyrimidyl, and piperidinyl substituted with 1 R; R is selected from H, F, Cl, Br, I, OR 3 , SR 3 , CO 2 R 3 , NO 2 , and CH 2 OR 3 , and (CR 8 R 9 ) t NR 8 R 9 ; alternatively, E and R combine to form methylenedioxy or ethylenedioxy; Z is selected from a bond, Cι_ 4 alkylene, (CH 2 ) r O (CH 2 ) r ( CH 2 ) rNR 3( CH 2 )r, ( CH 2 ) r C ( 0 ) (CH 2 ) r , ( CH 2 ) r C ( 0 ) 0 ( CH 2 ) r , (CH 2 ) r 0C(0) (CH 2 )r/ (CH 2 ) r C (0) NR 3 (CH 2 ) r , (CH 2 ) r NR 3 C(0) (CH 2 ) r , (CH 2 ) r 0C (0) 0 (CH 2 ) r , (CH 2 )rOC(0)NR 3 (CH 2 )r, (CH 2 ) r NR 3 C (0) 0 ( CH 2 ) r , ( CH 2 )rNR 3 C(0)NR 3 (CH 2 )r, (CH 2 ) r S (O) p ( CH 2 ) r , ( CH2) r S0 2 NR 3 (CH 2 )r, (CH 2 ) r NR 3 S0 2 (CH 2 ) r . and (CH2) r NR 3 S02NR 3 (CH2)r/ provided that Z does not form a N- N, N-O, N-S, NCH 2 N, NCH 2 0, or NCH 2 S bond with ring M or group A; R la and R lb are independently absent or selected from -(CH2) r -R 1' / -CH=CH-R 1# , NCH2R 1" , OCH2R 1" , SCH2R 1 ", NH ( CH 2 )2(CH 2 ) t R 1 ', 0(CH 2 )2(CH 2 )tR 1' , and S (CH 2 ) 2 (CH 2 ) tR 1 ' ; alternatively, R la and R lb , when attached to adjacent carbon atoms, together with the atoms to which they are attached form a 5-8 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R 4 and which contains from 0-2 heteroatoms selected from the group consisting of N, 0, and S; alternatively, when Z is C(0)NH and R la is attached to a ring carbon adjacent to Z, then R la is a C(0) which replaces the amide hydrogen of Z to form a cyclic imide; R 1 ' is selected from H, C 1 - 3 alkyl, F, Cl, Br, I, -CN, -CHO, (CF 2 )rCF 3 , (CH 2 ) r OR 2 , NR 2 R 2a , C(0)R 2c , 0C(0)R 2 , (CF 2 ) r Cθ 2 R 2c , S(0) p R 2b , NR 2 (CH 2 ) r 0R 2 , CH (=NR 2c )NR 2 R 2a , NR 2 C(0)R 2b , NR 2 C(0)NHR 2b , NR 2 C(0) 2 R 2a , OC (0)NR 2 R 2b , C(0)NR 2 R 2a , C(0)NR 2 (CH 2 ) r OR 2 , S0 2 NR 2 R 2a , NR 2 S0 2 R 2b , C 3 _ 6 carbocyclic residue substituted with 0-2 R 4 , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with C-2 R 4 ; R 1 " is selected from H, CH(CH 2 OR 2 ) , C(0)R 2c , C(0)NR 2 R 2a , S(0)R 2b , S(0) R 2b , and S0NR 2 R 2a ; R 2 , at each occurrence, is selected from H, CF 3 , Cι_ 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with ϋ-2 R 4b ; R 2a , at each occurrence, is selected from H, CF 3 , Cχ_ 6 alkyl, benzyl, phenethyl, C 3 - 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R b ; R 2b , at each occurrence, is selected from CF , C 1 -. 4 alkoxy, Cι- 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R 4b ; R c , at each occurrence, is selected from CF 3 , OH, C 1 - 4 alkoxy, Cχ_ 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R b ; alternatively, R 2 and R a , together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R b and containing from 0-1 additional heteroatoms selected from the group consisting of N, 0, and S; R 3 , at each occurrence, is selected from H, C 1 - 4 alkyl, and phenyl ; R 3a , at each occurrence, is selected from H, C 1 - 4 alkyl, and phenyl ; R 3b , at each occurrence, is selected from H, Cι_ 4 alkyl, and phenyl ; R 3c , at each occurrence, is selected from C 1 - 4 alkyl, and phenyl ,- A is selected from: C 3 _ιo carbocyclic residue substituted with 0-2 R , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4 ; B is selected from: H, Y, and X-Y; X is selected from Cι_ alkylene, -CR 2 (CR 2 R 2b ) (CH 2 ) t ~ , -C(O)-, -C(=NR 1 ")-, -CR 2 (NR 1 "R 2 )-, -CR 2 (OR 2 )-, -CR 2 (SR 2 )-, -C(0)CR 2 R 2a -, -CR 2 R 2a C(0), -S(0) p -, -S (0) p CR 2 R 2a - , -CR 2 R 2a S(0) p -, -S(0) 2 NR 2 -, -NR 2 S(0} 2 -, -NR 2 S (0) 2 CR 2 R 2a - , -CR 2 R 2a S(0) 2 NR 2 -, -NR 2 S(0) 2 NR 2 -, -C(0)NR 2 -, -NR 2 C(0)-, -C(0)NR 2 CR 2 R 2a -, -NR 2 C (0) CR 2 R 2a - , -CR 2 R 2a C (O)NR 2 - , -CR 2 R 2a NR 2 C(0)-, -NR 2 C(0)0-, -0C(0)NR 2 -, -NR 2 C (0) NR 2 - , -NR 2 -, -NR 2 CR 2 R 2a -, -CR 2 R 2a NR 2 -, 0, -CR 2 R 2a O-, and -OCR 2 R 2a -; Y is selected from: (CH 2 ) r NR 2 R 2a , provided that X-Y do not form a N-N, O-N, or S-N bond, C 3 _ιo carbocyclic residue substituted with 0-2 R a , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R a ; R 4 , at each occurrence, is selected from H, =0, (CH 2 ) r OR 2 F, Cl, Br, I, Cι_ 4 alkyl, -CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(0)R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , NR 2 C (0) NR 2 R 2 , CH(=NR 2 )NR 2 R 2a , CH(=NS(0) 2 R 5 )NR 2 R 2a , NHC (=NR 2 ) NR 2 R 2a , C(0)NHC(=NR 2 )NR 2 R 2a , S0 2 NR 2 R 2a , NR 2 S0 2 NR 2 R 2a , NR 2 S0 2 -Ci- alkyl, NR 2 S0 2 R 5 , S(0) p R 5 , (CF 2 ) r CF 3 , NCH2R 1 ", OCH 2 R 1 ", SCH2R 1 " , N ( CH 2 ) 2 ( CH 2 ) t R 1 \ 0 ( CH 2 ) 2 ( CH 2 ) tR 1 ' , and S ( CH 2 ) 2 ( CH 2 ) tR 1 ' ; alternatively, one R 4 is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S; R a , at each occurrence, is selected from H, =0, (CH 2 ) r OR 2 , (CH 2 ) r -F, (CH 2 ) r -Br, (CH 2 ) r -Cl, I, Cι_ 4 alkyl, -CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r NR 2 R 2b , (CH 2 ) r C (0) R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , C(0)NH(CH 2 ) 2 NR 2 R 2a , NR 2 C (0) NR 2 R 2a , CH(=NR 2 )NR 2 R 2a , NHC(=NR 2 )NR 2 R 2a , S0 2 NR 2 R 2a , NR 2 S0 2 NR 2 R 2a , NR 2 S0 2 -Cι_ 4 alkyl, C (0)NHS0 2 -Cι_ 4 alkyl, NR 2 S0 2 R 5 , S(0) p R 5 , and (CF 2 ) r CF 3 ; alternatively, one R a is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S and substituted with 0-1 R 5 ; R 4b , at each occurrence, is selected from H, =0, (CH 2 ) r OR 3 , F, Cl, Br, I, Ci- 4 alkyl, -CN, N0 2 , (CH 2 ) r NR 3 R 3a , (CH 2 ) r C(0)R 3 , (CH 2 ) r C(0)0R 3c , NR 3 C(0)R 3a , C(0)NR 3 R 3a , NR 3 C(0)NRR 3a , CH(=NR 3 )NR 3 R 3a , NH 3 C (=NR 3 ) NR 3 R 3a , S0 2 NR 3 R 3a , NR 3 S0 2 NR 3 R 3a , NR 3 S0 2 -Cι_ 4 alkyl, NR 3 S0 2 CF 3 , NR 3 S0 2 -phenyl , S(0) p CF 3 , S(0) p -Cι_ 4 alkyl, S (0) p -phenyl , and (CF 2 ) r CF 3 ; R 5 , at each occurrence, is selected from CF 3 , Cι_ 6 alkyl, phenyl substituted with 0-2 R 6 , and benzyl substituted with 0-2 R 6 ; R 6 , at each occurrence, is selected from H, OH, (CH 2 ) r OR 2 F» Cl, Br, I, Ci- 4 alkyl, CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(0)R 2b , NR 2 C(0)R 2b , NR 2 C (0)NR 2 R 2a , CH(=NH)NH 2 - NHC(=NH)NH 2 , S0NR 2 R 2a , NR 2 S0 2 NR 2 R 2a , and NR 2 S0 2 Ci- alkyl; R 7 , at each occurrence, is selected from H, OH, C±-β alkyl, Cι- 6 alkylcarbonyl , C 1 - 6 alkoxy, Cι_ 4 alkoxycarbonyl , (CH 2 ) n -phenyl, C 6 -ιo aryloxy, C 6 -ιo aryloxycarbonyl, C 6 -ιo aryl ethylcarbonyl , Cι_ 4 alkylcarbonyloxy C _ 4 alkoxycarbonyl , Cβ-io arylcarbonyloxy C 1 - 4 alkoxycarbonyl , Cι- 6 alkylaminocarbonyl , phenylaminocarbonyl , and phenyl-Cι- 4 alkoxycarbonyl; R 8 , at each occurrence, is selected from H, Cι_ 6 alkyl and (CH 2 ) n-pheny1 ; alternatively, R 7 and R 8 combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, 0, and S; R 9 , at each occurrence, is selected from H, C 1 - 6 alkyl and (CH 2 ) n -phenyl; n is selected from 0, 1, 2, and 3; m is selected from 0, 1, and 2; p is selected from 0, 1, and 2 ,- r is selected from 0, 1, 2, and 3; s is selected from 0, 1, and 2; and, t is selected from 0 and 1. [2] In a preferred embodiment, the present invention provides novel compounds of formulae Ia-Io: wherein .- Z is selected from a bond, CH 2 0, OCH 2 , CH 2 NH, NHCH 2 , CH 2 C(0) , C(0)CH 2 , C(0)NH, C(0)NH, CH 2 S(0) 2 , S(0) 2 (CH 2 ) , S0 2 NH, and S0 2 NH; B is selected from: Y, X-Y, and NR 2 R 2a ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R 4a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3-oxadiazole, 1,2,4- oxadiazole, 1, 2 , 5-oxadiazole, 1, 3 , 4-oxadiazole, 1,2,3- thiadiazole, 1, 2 , 4-thiadiazole, 1, 2, 5-thiadiazole, 1,3,4- thiadiazole, 1, 2, 3-triazole, 1, 2 , 4-triazole, 1,2,5- triazole, 1, 3 , 4-triazole, benzofuran, benzothiofuran, indole, benzimidazole, benzoxazole, benzthiazole, indazole, benzisoxazole, benzisothiazole, and isoindazole; Y may also be selected from the following bicyclic heteroaryl ring systems : K is selected from 0, S, NH, and N. [3] In a more preferred embodiment, the present invention provides novel compounds of formulae: wherein: D is selected from C(=NR 7 )NR 8 R 9 and (CR 8 R 9 ) t NR 8 R 9 ; R is selected from H, F, Cl, OR 3 , CH 2 OR 3 , CH 2 NH 2 ; A is selected from: piperidinyl , piperazinyl, 5 - 6 carbocyclic residue substituted with 0-2 R 4 , and 5-6 membered heteroaryl containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4 ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R 4a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl , oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3 -oxadiazole, 1, 2 , 4-oxadiazole, 1, 2 , 5-oxadiazole, 1 , 3 , 4-oxadiazole, 1, 2 , 3 -thiadiazole, 1, 2 , 4-thiadiazole, 1, 2 , 5-thiadiazole, 1, 3 , 4-thiadiazole, 1, 2 , 3-triazole, 1, 2 , 4-triazole, 1,2,5- triazole, and 1, 3 , 4-triazole. [4] In an even more preferred embodiment, the present invention provides novel compounds wherein: E is phenyl; D is selected from C(=NH)NH 2 and CH 2 NH 2 R is selected from H, F, Cl, and Br; A is selected from: C 5 _ 6 carbocyclic residue substituted with 0-2 R 4 , and 5-6 membered heteroaryl containing from 1-3 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4 ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3 -oxadiazole, 1, 2 , 4-oxadiazole, 1, 2 , 5-oxadiazole, 1, 3 , 4-oxadiazole, 1,2 , 3 -thiadiazole, 1, 2 , 4-thiadiazole, 1, 2 , 5-thiadiazole, 1, 3 , 4-thiadiazole, 1, 2 , 3-triazole, 1, 2 , 4-triazole, 1,2,5- triazole, and 1, 3 , 4-triazole; R , at each occurrence, is selected from H, CF 3 , Cι_ 6 alkyl, benzyl, C 5 - 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2a , at each occurrence, is selected from H, CF 3 , Cι_ 6 alkyl, benzyl, phenethyl, C 5 - 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R b ; R 2b , at each occurrence, is selected from CF 3 , C _ 4 alkoxy, Cι- 6 alkyl, benzyl, Cs_ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2c , at each occurrence, is selected from CF 3 , OH, Cι_ 4 alkoxy, Cι_ 6 alkyl, benzyl, Cs_ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R b ; alternatively, R 2 and R 2a , together with the atom to which they are attached, combine to form a ring selected from imidazolyl, morpholino, piperazinyl, pyridyl, and pyrrolidinyl, substituted with 0-2 R 4b ; R 4 , at each occurrence, is selected from H, =0, OR 2 , CH 2 OR 2 , F, Cl, Ci- 4 alkyl, NR 2 R 2a , CH 2 NR 2 R 2 , C(0)R 2c , CH 2 C(0)R 2c , C(0)NR 2 R 2a , CH(=NR 2 )NR 2 R 2a , CH (=NS (0) 2 R 5 ) NR 2 R 2a , S0 2 NR 2 R 2a , NR 2 S0 2 -Cι_ 4 alkyl, S(0) 2 R 5 , and CF 3 provided that if B is H, then R 4 is other than tetrazole, C(0)-alkoxy, and C(0)NR 2 R 2a ; R a , at each occurrence, is selected from H, =0, (CH 2 ) r OR 2 , F, Cl, Ci- 4 alkyl, NR 2 R 2a , CH 2 NR 2 R 2a , NR 2 R 2b , CH 2 NR 2 R 2b , (CH 2 ) r C(0)R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , C (0) NH (CH 2 ) 2 NR 2 R a , NR 2 C(0)NR 2 R 2a , S0 2 NR 2 R 2a , S(0) 2 R 5 , and CF 3 ; and, R b , at each occurrence, is selected from H, =0, (CH 2 ) r OR 3 , F, Cl, Ci- 4 alkyl, NR 3 R 3a , CH 2 NR 3 R 3a , C(0)R 3 , CH 2 C(0)R 3 , C(0)0R 3c , C(0)NR 3 R 3a , CH(=NR 3 )NR 3 R 3a , S0 2 NR 3 R 3a , NR 3 S0 -Cι_ 4 alkyl, NR 3 S0 2 CF 3 , NR 3 S0 2 -phenyl , S(0) 2 CF 3 , S(0) 2 -Ci_ 4 alkyl, S (0) 2 -phenyl , and CF 3 . [5] In a further preferred embodiment, the present invention provides novel compounds selected from: N-(2'-Aminosulfonyl-[l,l' ]biphen-4-yl) -2- (3'- amidinophenyl) nicotinamide; N- [5- (2-aminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - amidinophenyl ) nicotinamide; N- [5- (2-t-butylaminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - amidinophenyl) nicotinamide; and, N- [5- (2-aminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - carboxamidophenyl) nicotinamide; or a pharmaceutically acceptable salt thereof. In a second embodiment, the present invention provides novel pharmaceutical compositions, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt form thereof . In a third embodiment, the present invention provides a novel method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt form thereof . DEFINITIONS The compounds herein described may have asymmetric centers. Compounds of the present invention containing an asymmetrically substituted atom may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis from optically active starting materials. Many geometric isomers of olefins, C=N double bonds , and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. Cis and trans geometric isomers of the compounds of the present invention are described and may be isolated as a mixture of isomers or as separated isomeric forms. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomeric form is specifically indicated. The term "substituted, " as used herein, means that any one or more hydrogens on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substitent is keto (i.e., =0), then 2 hydrogens on the atom are replaced. Keto substituents are not present on aromatic moieties. The present invention is intended to include all isotopes of atoms occurring in the present compounds. Isotopes include those atoms having the same atomic number but different mass numbers. By way of general example and without limitation, isotopes of hydrogen include tritium and deuterium. Isotopes of carbon include C-13 and C-14. When any variable (e.g., R^) occurs more than one time in any constituent or formula for a compound, its definition at each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-2 R 6 , then said group may optionally be substituted with up to two R 6 groups and R 6 at each occurrence is selected independently from the definition of R 6 . Also, combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. When a bond to a substituent is shown to cross a bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of a given formula, then such substituent may be bonded via any atom in such substituent. Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds . As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms . Examples of alkyl include, but are not limited to, methyl, ethyl, n-propyl, i-propyl, n-butyl, s-butyl, t-butyl, n-pentyl, and s-pentyl. "Haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example -C V F W where v = 1 to 3 and w = 1 to (2v+l) ) . Examples of haloalkyl include, but are not limited to, trifluoromethyl, trichloromethyl, pentafluoroethyl, and pentachloroethyl . "Alkoxy" represents an alkyl group as defined above with the indicated number of carbon atoms attached through an oxygen bridge. Examples of alkoxy include, but are not limited to, methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, t-butoxy, n-pentoxy, and s-pentoxy. "Cycloalkyl" is intended to include saturated ring groups, such as cyclopropyl, cyclobutyl, or cyclopentyl. Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon-carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl and the like. "Alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like. "Halo" or "halogen" as used herein refers to fluoro, chloro, bromo, and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate, and the like. As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 7-membered monocyclic or bicyclic or 7- to 13 -membered bicyclic or tricyclic, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocycles include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl, cyclooctyl, [3.3. OJbicyclooctane, [4.3.0]bicyclononane, [4.4. OJbicyclodecane, [2.2.2]bicyclooctane, fluorenyl, phenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl . As used herein, the term "heterocycle" or "heterocyclic system" is intended to mean a stable 5-to 7-membered monocyclic or bicyclic or 7-to 10-membered bicyclic heterocyclic ring which is saturated partially unsaturated or unsaturated (aromatic) , and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, 0 and S and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The nitrogen and sulfur heteroatoms may optionally be oxidized. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. If specifically noted, a nitrogen in the heterocycle may optionally be quaternized. It is preferred that when the total number of S and 0 atoms in the heterocycle exceeds 1, then these heteroatoms are not adjacent to one another. It is preferred that the total number of S and 0 atoms in the heterocycle is not more than 1. As used herein, the term "aromatic heterocyclic system" is intended to mean a stable 5-to 7- membered monocyclic or bicyclic or 7-to 10-membered bicyclic heterocyclic aromatic ring which consists of carbon atoms and from 1 to 4 heterotams independently selected from the group consisting of N, 0 and S. It is preferred that the total number of S and 0 atoms in the aromatic heterocycle is not more than 1. Examples of heterocycles include, but are not limited to, acridinyl, azocinyl, benzimidazolyl, benzofuranyl, benzothiofuranyl , benzothiophenyl, benzoxazolyl , benzthiazolyl, benztriazolyl, benztetrazolyl , benzisoxazolyl, benzisothiazolyl, benzimidazolinyl , carbazolyl, 4aH-carbazolyl, carbolinyl, chromanyl, chromenyl, cinnolinyl, decahydroquinolinyl, 2H, 6H-1 , 5 , 2-dithiazinyl , dihydrofuro [2 , 3 -b] tetrahydrofuran, furanyl, furazanyl, imidazolidinyl, imidazolinyl , imidazolyl, lJ-indazolyl, indolenyl, indolinyl, indolizinyl, indolyl, 3H-indolyl, isobenzofuranyl, isochromanyl, isoindazolyl, isoindolinyl, isoindolyl, isoquinolinyl, isothiazolyl, isoxazolyl, morpholinyl, naphthyridinyl , octahydroisoquinolinyl, oxadiazolyl, 1, 2 , 3-oxadiazolyl, 1, 2 , 4-oxadiazolyl, 1,2,5- oxadiazolyl, 1, 3 , 4-oxadiazolyl, oxazolidinyl , oxazolyl, oxazolidinyl, pyrimidinyl, phenanthridinyl , phenanthroliny1 , phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phthalazinyl, piperazinyl, piperidinyl, pteridinyl , purinyl, pyranyl, pyrazinyl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridooxazole, pyridoimidazole, pyridothiazole, pyridinyl, pyridyl, pyrimidinyl, pyrrolidinyl, pyrrolinyl, 2H-pyrrolyl, pyrrolyl, quinazolinyl, quinolinyl, 4H-quinolizinyl, quinoxalinyl, quinuclidinyl, tetrahydrofuranyl , tetrahydroisoquinolinyl , tetrahydroquinolinyl, 6H-1, 2 , 5-thiadiazinyl, 1,2,3- thiadiazolyl, 1, 2 , 4-thiadiazolyl, 1, 2 , 5-thiadiazolyl, 1,3,4- thiadiazolyl, thianthrenyl , thiazolyl, thienyl, thienothiazolyl, thienooxazolyl, thienoimidazolyl, thiophenyl, triazinyl, 1, 2 , 3-triazolyl, 1, 2 , 4-triazolyl, 1, 2 , 5-triazolyl, 1, 3 , 4-triazolyl, and xanthenyl . Preferred heterocycles include, but are not limited to, pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, pyrrolidinyl, imidazolyl, indolyl, benzimidazolyl, lH-indazolyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl . Also included are fused ring and spiro compounds containing, for example, the above heterocycles. The phrase "pharmaceutically acceptable" is employed herein to refer to those compounds, materials, compositions, and/or dosage forms which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio. As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound is modified by making acid or base salts thereof. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like. The pharmaceutically acceptable salts include the conventional non-toxic salts or the quaternary ammonium salts of the parent compound formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like. The pharmaceutically acceptable salts of the present invention can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington ' s Pharmaceutical Sciences, 17th ed. , Mack Publishing Company, Easton, PA, 1985, p. 1418, the disclosure of which is hereby incorporated by reference. "Prodrugs" are intended to include any covalently bonded carriers which release the active parent drug according to formula (I) in vivo when such prodrug is administered to a mammalian subject. Prodrugs of a compound of formula (I) are prepared by modifying functional groups present in the compound in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compound. Prodrugs include compounds of formula (I) wherein a hydroxy, amino, or sulfhydryl group is bonded to any group that, when the prodrug or compound of formula (I) is administered to a mammalian subject, cleaves to form a free hydroxyl, free amino, or free sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate and benzoate derivatives of alcohol and amine functional groups in the compounds of formula (I), and the like. Preferred prodrugs are amidine prodrugs wherein D is C(=NR 7 )NH and R 7 is selected from OH, C 1 - 4 alkoxy, C 6 - 10 aryloxy, Cι_ 4 alkoxycarbonyl, Cg-io aryloxycarbonyl, Cβ-io arylmethylcarbonyl , Cι_ 4 alkylcarbonyloxy Cι_ 4 alkoxycarbonyl, and C 6 _ιo arylcarbonyloxy C 1 - 4 alkoxycarbonyl. More preferred prodrugs are where R 7 is OH, methoxy, ethoxy, benzyloxycarbonyl, methoxycarbonyl , and methylcarbonyloxymethoxycarbonyl . "Stable compound" and "stable structure" are meant to indicate a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent . "Substituted" is intended to indicate that one or more hydrogens on the atom indicated in the expression using "substituted" is replaced with a selection from the indicated group (s), provided that the indicated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., =0) group, then 2 hydrogens on the atom are replaced. "Therapeutically effective amount" is intended to include an amount of a compound of the present invention or an amount of the combination of compounds claimed effective to inhibit HIV infection or treat the symptoms of HIV infection in a host. The combination of compounds is preferably a synergistic combination. Synergy, as described for example by Chou and Talalay, Adv. Enzyme Regul . 22:27-55 (1984), occurs when the effect (in this case, inhibition of HIV replication) of the compounds when administered in combination is greater than the additive effect of the compounds when administered alone as a single agent In general, a synergistic effect is most clearly demonstrated at suboptimal concentrations of the compounds. Synergy can be in terms of lower cytotoxicity, increased antiviral effect, or some other beneficial effect of the combination compared with the individual components . SYNTHESIS The compounds of the present invention can be prepared in a number of ways known to one skilled in the art of organic synthesis . The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those described below. The reactions are performed in a solvent appropriate to the reagents and materials employed and suitable for the transformations being effected. It will sometimes require a judgment to modify the order of synthetic steps or to select one particular process scheme over another in order to obtain a desired compound of the invention. It will also be recognized that another major consideration in the planning of any synthetic route in this field is the judicious choice of the protecting group used for the protection of the reactive functional groups present in the compounds described in this invention. An authoritative account describing the many alternatives to the trained practitioner is Greene and Wuts ( Protective Groups in Organic Chemistry, Wiley and Sons, 1991) . All references cited herein are hereby incorporated in their entirety herein by reference. Compounds of this invention where B is either a carbocyclic or heterocyclic residue as defined in Formula 1 are coupled to A as shown generically and by specific example in Schemes 1 and 2, respectively. Either or both of A and B may be substituted with 0-2 R . W is defined as a suitable protected nitrogen, such as N0 2 or NHBOC; a protected sulfur, such as S-tBu or SMOM; or a methyl ester. Halogen-metal exchange of the bromine in bromo-B with n-butyl lithium, quenching with triisopropyl borate and acidic hydrolysis gives the required boronic acid, B-B(OH) 2 . The W-A-Br subunit may be already linked to ring M before the Suzuki coupling reaction. Deprotection provides the complete subunit. Scheme 1 B—Br 1) n-BuLi 2) (iPrO) 3 B 3) HCl B-B(0H) 2 I A - W-A— B I Br Pd(0) Scheme 2 describes a typical example of how the A-B subunit is prepared for attachment to ring M. 4-Bromoaniline is protected as Boc-derivative and the coupled to 2-(t- butylamino) sulfonylphenylboronic acid under Suzuki conditions. 2- (t-Butylamino) sulfonylphenylboronic acid is prepared by the method described by Rivero (Bioorg. Med. Chem . Lett . 1994, 189) . Deprotection with TFA can provide the aminobiphenyl compound. The aminobiphenyl is then coupled to the core ring structures as described below. Scheme 2 When B is defined as X-Y, the following description applies. Groups A and B are available either through commercial sources, known in the literature or readily synthesized by the adaptation of standard procedures known to practitioners skilled in the art of organic synthesis . the required reactive functional groups appended to analogs of A and B are also available either through commercial sources, known in the literature or readily synthesized by the adaptation of standard procedures known to practitioners skilled in the art of synthesis . In the tables that follow the chemistry required to effect the coupling of A to B is outlined. Table A: Preparation of Amide Ester, Urea, Sulfonamide and Sulfamide Linkages Between A and B. If A contains: then the reactive to give the following substituent of Y is: product A-X-Y: A-NHR as a C1C(0)-Y A-NR 2 -C(0)-Y substituent a secondary NH C1C(0)-Y A-C(0)-Y as part of a ring or chain A-OH as a C1C(0)-Y A-0-C(0)-Y substituent A-NHR 2 as a ClC(0)-CR 2 R 2a - • Y A-NR 2 -C (0) -CR 2 R a -Y substituent a secondary NH C1C(0) -CR 2 R 2a -Y A-C(0)-CR 2 R 2a - as part of a ring or chain A-OH as a C1C (0)-CR 2 R 2a -Y A-O-C(O) -CR 2 R 2a -Y substituent A-NHR 2 as a C1C(0)-CNR -Y A-NR -C(0) -CNR -Y substituent a secondary NH C1C(0)-CNR -Y A-C(0)-CNR -Y as part of a ring or chain A-OH as a C1C(0)-CNR -Y A-0-C(0)-CNR -Y substituent A-NHR 2 as a ClSO -Y A-NR -SO,-Y substituent a secondary NH C1S0 2 -Y A-S0 2 -Y as part of a ring or chain A-NHR 2 as a ClS0,-CR 2 R 2a -Y A-NR -SO, -CR 2 R 2a - substituent a secondary NH ClS0,-CR 2 R 2a -Y A-S0 2 -CR 2 R a -Y as part of a ring or chain A-NHR 2 as a CISO 2 - R -Y A-NR 2 -S0 2 -NR 2 -Y substituent a secondary NH CISO 2 -NR -Y A-SO 2 -NR -Y as part of a ring or chain A-C(0)C1 HO-Y as a substituent A-C(0)-0-Y A-C(0)C1 NHR 2 -Y as a A-C(0)-NR 2 -Y substituent A-C(0)C1 a secondary NH as A-C(0)-Y part of a ring or chain A-CR 2 R 2a C(0)Cl HO-Y as a substituent A-CR 2 R 2a C(0)-0-Y A-CR 2 R 2a C(0)Cl NHR 2 -Y as a A-CR 2 R 2a C(0)-NR 2 -Y substituent A-CR 2 R a C (0) Cl a secondary NH as A-CR 2 R 2a C (O) -Y part of a ring or chain A-S0 2 C1 NHR 2 -Y as a A-S0 2 -NR 2 -Y substituent A-S0 2 C1 secondary NH as A-S0 2 -Y part of a ring or chain A-CR 2 R 2a S0 2 Cl NHR 2 -Y as a A-CR 2 R 2a S0 2 -NR 2 -Y substituent A-CR 2 R 2a S0 2 Cl a secondary NH as A-CR 2 R 2a S0 2 -Y part of a ring or chain The chemistry of Table A can be carried out in aprotic solvents such as a chlorocarbon, pyridine, benzene or toluene, at temperatures ranging from -20°C to the reflux point of the solvent and with or without a trialkylamine base. Table B: Preparation of Ketone Linkages between A and B. If A contains: then the reactive to give the following substituent of Y is: product A-X-Y: A-C(0)C1 BrMg-Y A-C(0)-Y A-CR 2 R 2a C (0) Cl BrMg-Y A-CR 2 R 2a C (0) -Y A-C(0)C1 BrMgCR 2 R 2a -Y A-C (0) CR 2 R 2a -Y A-CR 2 R 2a C (0) Cl BrMgCR 2 R 2a -Y A-CR 2 R 2a C (0) CR 2 R 2a -Y The coupling chemistry of table B can be carried out by a variety of methods. The Grignard reagent required for Y is prepared from a halogen analog of Y in dry ether, dimethoxyethane or tetrahydrofuran at 0°C to the reflux point of the solvent. This Grignard reagent can reacted directly under very controlled conditions, that is low temperature (-20°C or lower) and with a large excess of acid chloride or with catalytic or stoichiometric copper bromide*dimethyl sulfide complex in dimethyl sulfide as a solvent or with a variant thereof. Other methods available include transforming the Grignard reagent to the cadmium reagent and coupling according to the procedure of Carson and Prout (Org. Syn. Col Vol. 3 (1955) 601) or a coupling mediated by Fe(acac)3 according to Fiandanese et al.(Tetr. Lett . 1984, 4805), or a coupling mediated by manganese (II) catalysis (Cahiez and aboue, Tetr . Lett . 1992, 33 (31 ) , 4437). Table C: Preparation of Ether and Thioether linkages between A and B. If A contains: then the reactive to give the following substituent of Y is: product A-X-Y: A-OH Br-Y A-O-Y A-CR 2 R 2a -0H Br-Y A-CR 2 R 2a 0-Y A-OH Br-CR 2 R 2a -Y A-0CR 2 R 2a -Y A-SH Br-Y A-S-Y A-CR 2 R 2a -SH Br-Y A-CR 2 R 2a S-Y A-SH Br-CR 2 R 2a -Y A-SCR 2 R 2a -Y The ether and thioether linkages of Table C can be prepared by reacting the two components in a polar aprotic solvent such as acetone, dimethylformamide or dimethylsulfoxide in the presence of a base such as potassium carbonate, sodium hydride or potassium t-butoxide at a temperature ranging from ambient to the reflux point of the solvent used. Table D: Preparation of -SO- and -S0- linkages from thioether of Table C. If the starting then it is oxidized then it is oxidized material is : with wet with m- Alumina/Oxone to chloroperbenzoic acid give: to give : A-S-Y A-S(0)-Y A-S0 2 -Y A-CR 2 R 2a S-Y A-CR 2 R 2a S(0)-Y A-CR 2 R 2a S0 2 -Y A-SCR 2 R 2a -Y A-S(0)CR 2 R 2a -Y A-S0 2 CR 2 R 2a -Y The thioethers of Table C serve as a convenient starting material for the preparation of the sulfoxide and sulfone analogs of Table D. A combination of wet alumina and Oxone can provide a reliable reagents for the oxidation of the thioether to the sulfoxide as shown by Greenhalgh ( Syn . Lett . 1992, 235) . The sulfone can be prepared according to the method of Satoh ( Chem . Lett . 1992, 381) using m- chloroperbenzoic acid. Scheme 3 describes the synthesis of compounds wherein M is a benzene ring and Q is a protected precursor of group D of Formula I and V is a nitro, protected sulfonamide or ester group and precursor of group Z of Formula I. The V group is placed on an appropriately substituted phenol either via nitration as shown by Poirier et al . ( Tetrahedron 1989, 45 (5) , 1415) , sulfonylation as shown by Kuznetsov (Akad. Nauk SSSR Ser . Khim 1990, 8, 1888) or carboxylation by Sartori et al . (Synthesis 1988, 10, 763) . Bromination with triphenylphosphine and bromine (J " . Am . Chem . Soc . 1964, 86, 964) gives the desired bromide. Suzuki coupling with the appropriate boronic acid provides the desired substituted pyridine . Scheme 3 Schemes 4, 5, 6, and 7 describe the synthesis of compounds wherein M is pyridine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyridine ring. In Scheme 4, a suitably protected aldehyde is subjected to base-catalyzed condensation with an activated ester to give after deprotection the desired aldehyde. Refluxing with ammonium chloride as shown by Dornow and Ische ( Chem . Ber. 1956, 89, 876) provides the pyridinol which is brominated with POBr 3 (Tjeenk et al . Rec . Trav. Chi . 1948, 67, 380) to give the desired 2-bromopyridine. Suzuki coupling with the appropriate boronic acid provides the desired substituted pyridine. Scheme 4 Treatment of an appropriately substituted 5-ethoxyoxazole with an alkene as shown by Kondrat ' eva et al . Dokl . Akad. Nauk SSSR 1965, 164 , 816) provides a pyridine with the V substituent at the para position. Bromination at the 3- position as shown by van der Does and Hertog (Rec . Trav. Khim . Pays-Bas 1965, 84 , 951) followed by palladium-catalyzed boronic acid coupling provides the desired substituted pyridine . Scheme 5 Scheme 6 describes a synthesis of a third substitution pattern on a pyridine ring. The appropriate tricarbonyl compound which can be prepared by methods described in Scheme 4 is treated with ammonium chloride to form the pyridinol which is subsequently brominated. Palladium-catalyzed coupling provides the desired substituted pyridine. Scheme 6 Scheme 7 takes a suitably substituted dicarbonyl compound and by chemistry illustrated in Schemes 4 and 6, reacts it with ammonium chloride. Bromination gives the 3 -bromopyridine which upon palladium-catalyzed coupling provides the desired substituted pyridine. Scheme 7 Schemes 8, 9, and 10 describe the synthesis of compounds wherein M is pyridazine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyridine ring. In Scheme 8 an activated ester is reacted with an appropriately substituted α-keto aldehyde and hydrazine as shown by Schmidt and Druey (Helv. Chim. Acta 1954, 37, 134 and 1467) . Conversion of the pyridazinone to the bromide using POBr 3 and palladium- catalyzed coupling provides the desired substituted pyridazine. Scheme 8 In Scheme 9, glyoxal can react under basic conditions with an activated ketone and subsequently brominated/dehydro- brominated to give the desired ketoaldehyde . Alternatively, a protected ketone can react with an activated aldehyde, undergo bromination/dehydrobromination, be deprotected and oxidized to give the regioisomeric ketoaldehyde. Cyclization as shown by Sprio and Madonia (Ann. Chim . 1958, 48, 1316) with hydrazine followed by palladium-catalyzed coupling provides the desired substituted pyridazine. Scheme 9 By analogy to Scheme 9, in Scheme 10 a aldehyde can be reacted with an activated ketone, brominated, de ydro- brominated and deprotected to give the desired diketone. Alternatively, a regioisomeric ketone can be placed through the same reaction sequence to produce an isomeric keto aldehyde. Reaction with hydrazine followed by palladium- catalyzed coupling provides the desired substituted pyridazine . Scheme 10 Schemes 11, and 12 describe the synthesis of compounds wherein M is pyrimidine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyrimidine ring. In Scheme 11, a condensation with an appropriately substituted acid chloride and an activated ester followed by conjugate reduction by tin hydride (Moriya et al . J. Org. Chem. 1986, 51 , 4708) gives the desired 1,4 dicarbonyl compound. Cyclization with formamidine or a substituted amidine followed by bromination gives the desired regioisomeric pyrimidine. Palladium-catalyzed coupling provides the desired substituted pyrimidine. Scheme 11 Using similar chemistry, Scheme 12 shows how an amidine can be condensed with a 1, 3-dicarbonyl compound and subsequently brominated in the 5-position (J " . Het. Chem . 1973, 10, 153) to give a specific regioisomeric bromopyrimidine . Palladium-catalyzed coupling provides the desired substituted pyrimidine. Scheme 12 Using the same ketoaldehyde from Scheme 12, cyclization with an appropriately substituted 1,2-diamine ( Chimia 1967, 21 , 510) followed by aromatization (Helv. Chim. Acta 1967, 50, 1754) provides a regioisomeric mixture of pyrazines as illustrated in Scheme 13. Bromination of the hydrobromide salt (U.S. Patent No. 2,403,710) yields the intermediate for the palladium-catalyzed coupling step which occurs as shown above . Scheme 13 OH Schemes 14 and 15 describe the synthesis of compounds wherein M is a 1, 2 , 3-triazine and Q is a protected precursor of group D of Formula I. In Scheme 14, a vinyl bromide is palladium coupled to a molecule containing the substituent R . Allylic bromination followed by azide displacement provide the cyclization precursor. Triphenylphosphine- mediated cyclization (J. Org. Chem . 1990, 55, 4724) give the 1-aminopyrazole which is subsequently brominated with N- bromosuccimide. Lead tetraacetate mediated rearrangement as shown by Neunhoeffer et al . (Ann . 1985, 1732) provides the desired regioisomeric 1, 2 , 3-triazine. Palladium-catalyzed coupling provides the substituted triazine. Scheme 14 1) R lb CH 2 Br In Scheme 15, an alkene is allylically brominated and the bromide is displaced to give a regioisomer of the azide in Scheme 14. Following the same reaction sequence as shown above, cyclization provides the 1-aminopyrazole. Bromination followed by lead tetraacetate mediated rearrangement give the 1 , 2 , 3 -triazine . Palladium-catalyzed coupling provides the other desired triazine . Scheme 15 Schemes 16 and 17 describe the synthesis of compounds wherein M is a 1, 2 , 4-triazine and Q is a protected precursor of group D of Formula I. In Scheme 16, a nitrile is converted using hydrazine to give the amidrazone which is condensed with a α-ketoester to give the triazinone as shown by Paudler and Lee ( M Org. Chem . 1971, 36, 3921) . Bromination as shown by Rykowski and van der Plas ( J. Org. Chem . 1987, 52, 71) followed by palladium-catalyzed coupling provides the desired 1, 2, 4-triazine. Scheme 16 R ιb c In Scheme 16, to achieve the opposite regioisomer the reaction scheme shown above is modify by the substituting a protect α-ketoester. This allows the most nucleophilic nitrogen to attack the ester functionality setting up the opposite regiochemistry. Deprotection and thermal cyclization gives the triazinone which is brominated as shown above. Palladium-catalyzed coupling provides the other desired 1,2,4- triazine. Scheme 17 b R lb CN 4 ) POBr 3 Scheme 18 describes the synthesis of compounds wherein M is a 1, 2 , 3 , 4-tetrazine and Q is a protected precursor of group D of Formula I. Lithiation of a vinyl bromide, transmetallation with tin, palladium catalyzed carbonylation and hydrazone formation provides a diene for a subsequent Diels-Alder reaction as shown by Carboni and Lindsey ( J. Am. Chem. Soc . 1959, 81 , 4342) . Reaction with dibenzyl azodicarboxylate followed by catalytic hydrogenation to debenzylate and decarboxylate should give after bromination the desired 1, 2 , 3 , 4-tetrazine . Palladium-catalyzed coupling provides the desired substitution. Scheme 18 C0 2 Bn 1 ) nBuLi i ) ^ Br 2 ) (nBu) 3 SnCl Bn ^^ =< V 3) Pd(0), CO \ 2 ) H 2 , Pd 4) BnNHNH 2 v 3) NBS Other features of the invention will become apparent in the course of the following descriptions of exemplary embodiments which are given for illustration fo the invention and are not intended to be limiting thereof. EXAMPLES Example 1 N- (2 ' -Aminosulfonyl- [1, 1' ]biphen-4-yi) -2- (3 ' - amidinophenyl) nicotinamide, trifluoroacetic acid salt Part A. Preparation of 2-bromonicotinic acid. Potassium permanganate (18.4 g, 116 mmol) was dissolved in water (400 mL) and added to 2-bromo-3-methylpyridine (10.0 g, 58 mmol) and refluxed for 16 hours. After cooling to room temperature, the slurry was filtered through a celite plug and rinsed with water and chloroform. The entire filtrate was transferred to a separatory funnel and the layers were separated. The aqueous layer was extracted again with CHC1 3 and acidified with 6N HCl to pH 1. A white solid was obtained on standing (2.08 g of product) . The pH of the remaining aqueous was adjusted to pH 4 with 2M NaOH and 2M HCl, then concentrated to <100mL. A white precipitate was filtered. The pH was adjusted to 4 and the mixture filtered again, combining the isolated solids for a total of 3.88 g of product. The filtrate was concentrated again to <100mL and adjusted to pH 1.5 and an additional quanitity of white solid was obtained (1.80 g) , for a combined yield of 3 crops, (8.76 g, 66%). hi NMR (DMSO-d 6 ) : δ 13.76 (bs, IH) , 8.46 (m, IH) , 8.09 (dd, IH, J = 7.7, J' = 2.2), 7.51 (m, IH) . Part B. Preparation of methyl 2-bromonicotinate. 2-Bromonicotinic acid (7.33 g, 36 mmol) was suspended in dry Et 2 0 (40 L) , and MeOH (2.3 mL) and diethyl azodicarboxylate (5.8 mL, 37 mmol) were added. Triphenylphosphine (9.61 g in 40mL Et 2 0, 37 mmol) was added dropwise over 2.5 hours . After stirring an additional two hours, the reaction was filtered and evaporated. The resulting clear liquid was chromatographed on silica gel (10- 40% EtOAc/ exanes) to yield a clear oil (8.63 g, 100%). 1 H NMR (CDC1 3 ) : δ 8.49 (dd, IH, J = 4.8, J' = 2.2), 8.09 (dd, IH, J = 7.7, J' = 1.8), 7.36 (m, IH) , 3.97 (s, 3H) . Part C. Preparation of 3-cyanophenylboronic acid. 3-Bromobenzonitrile (10.0 g, 55 mmol) was dissolved in dry THF (100 mL) and cooled to -100°C (Et 2 0/N 2 ) . n- Butyllithium (24.2 mL, 2.5 M in hexane) was added over 30 minutes, maintaining the internal temp under -90°. After 20 minutes, triisopropylborate (18.0 mL) was added over 15 minutes, again maintaining the internal temperature. After the addition was complete, the reaction was allowed to warm slowly to room temperature over 1.5 hours. The reaction was stirred at room temp for 16 hours, then cooled to 15°C, after which 6 M HCl (25 mL) was added. After stirring vigorously for 3.5 hours, the reaction was partitioned between water and EtOAc . After extracting a second time with EtOAc, the combined organics were washed with 2 M NaOH. The aqueous extract was neutralized with 6 M HCl. The white precipitate was filtered, yielding the desired product (4.80 g, 60%). 1 H NMR (DMSO-d 6 ) : δ 8.37 (s, 2H) , 8.10 (s, IH) , 8.03 (dt, IH, J = 7.3, J' = 1.1), 7.83 (dt, IH, J = 7.6, J' = 1.4), 7.53 (t, IH, J = 7.7) . Part D. Preparation of methyl 2- (3 ' -cyanophenyl) nicotinate . Methyl 2-bromonicotinate (2.0 g, 9.3 mmol) and 3- cyanophenylboronic acid (2.7 g, 18.4 mmol) were combined in 190 mL benzene. Sodium carbonate (19 mL of a 2 M aqueous solution), tetrabutylammonium bromide (152 mg, 0.5 mmol), and bis (triphenylphosphine) palladium (II) chloride (325 mg, 0.5 mmol) were added. The entire mixture was evacuated to remove dissolved gasses, then placed under argon. The reaction was refluxed for 14 hours, diluted with water and EtOAc, separated, dried over Na 2 S0 4 , filtered, and evaporated. The resulting yellow solid was chromatographed on silica gel (30% EtOAc/hexanes) to yield a light yellow solid (1.70 g, 77%). X H NMR (CDCI 3 ) : δ 8.81 (dd, IH, J = 4.8, J' = 1.8) , 8.23 (dd, IH, J = 8.0, J' =1.9) , 7.85 (s, IH) , 7.73 (m, 2H) , 7.55 (t, IH, J = 7.7) , 7.43 (m, IH) , 3.76 (s, 3H) . Part E. Preparation of 2- ( t-butylaminosulfonyl ) phenylboronic acid. To a solution of 206.5 g (0.968 mol) of benzene- (N-t- butyl) sulfonamide in 2500 mL of THF under N 2 was added 790 mL (1.98 mol) of 2.5M n-butyllithium in hexane over 35 minutes, keeping the temperature between 0-5°C. The reaction mixture was allowed to warm to 10°C, at which time a thick precipitate formed. Triisopropylborate (305 mL, 1.32 mol) was added keeping the temperature below 35°C. After 1 hour, the reaction mixture was cooled, IN HCl (1570 mL) was added, and the mixture was stirred overnight. The mixture was extracted with 400 mL of ether three times, and the combined organic extracts were extracted with 500 mL of IN NaOH three times. The aqueous extracts were acidified to pH 1 with 6N HCl, and then extracted with 500 mL ether three times. The combined ether extracts were dried over MgS0 4 , and the solvents evaporated in vacuo until the volume was 700 mL. Hexane (150 mL) was added and overnight, a white precipitate formed. The solid was collected and washed with 10% ether/hexane (250 mL) , then dried in vacuo to give 216.3 g (87%) of the desired compound as white crystals. m.p. 118-119°C; X H NMR (CDC1 3 ): δ 8.00 (d, IH) ; 7.82 (d, IH) ; 7.53 (m, 2H) ; 6.29 (br s, 2H) ; 5.13 (s, IH) ; 1.18 (s, 9H) . Part F. Preparation of 4-amino-2 ' -t-butylaminosulfonyl- [1,1'] biphenyl . A mixture of 3.44 g (20 mmol) of 4-bromoaniline and 5.14 g (20 mmol) of 2- (t-butylaminosulfonyl) phenylboronic acid, 1.16 g of tetrakis ( triphenylphosphine) palladium(O) (1 mmol), 0.32 g of tetrabutylammonium bromide (1 mmol) and 20 mL of 2M aqueous sodium carbonate were refluxed with 180 mL of benzene under N 2 for 5.5 hours. After cooling, the mixture was diluted with methylene chloride and water. The two phases were separated and the organic phase was washed with water, dried with MgS0 4 and concentrated in vacuo . The resulting thick oil was chromatographed on silica with 30% EtOAc/hexane to afford 2.52 g (41%) of the aniline. X H NMR (CDC1 3 ): δ 8.14 (d, IH) ; 7.53 (t, IH) ; 7.43 (t, IH) ; 7.33 (d, 2H) ; 7.27 (d, IH) ; 6.76 (d, 2H) ; 3.7 (br s, IH) ; 0.99 (s, 9H) . Part G. Preparation of N- (2 ' -t-butylaminosulfonyl- [1,1' ]biphen-4-yl) -2- (3 ' -cyanophenyl) nicotinamide. Methyl 2- (3 ' -cyanophenyl) nicotinate (300 mg, 1.3 mmol) was combined with of 4-amino-2 ' -t-butylaminosulfonyl- [1 , 1 ' ] biphenyl (383 mg, 1.3 mmol) in 12 mL dry CH 2 C1 2 . A solution of trimethylaluminum (3.8 mL, 2.0 M in heptane) was added, and an exothermic reaction immediately occurred and the mixture darkened. The resulting solution was stirred at room temperature under argon for 3 days and then quenched carefully with a few drops of 1 M HCl. An emulsion was obtained on dilution with EtOAc and water. The layers were separated, and the organic was extracted again with water and brine, dried over Na 2 S0 , filtered, and evaporated. A small amount of additional material was obtained from the aqueous extract by adjusting the pH to 8 with sat. NaHC0 3 and extracting with EtOAc. This material was dried over Na 2 S0 4 , filtered, evaporated, and combined with the previous extract for chromatography on silica gel (50-60% EtOAc/hexanes) to yield the desired product (190 mg, 30%). X H NMR (CDC1 3 ): δ 8.86 (dd, IH, J = 4.7, J' = 1.9), 8.14 (m, 3H) , 8.00 (d, IH, J = 7.7), 7.73 (d, IH, J = 8.1), 7.50 (m, 9H) , 7.29 (dd, IH, J = 7.4, J' = 1.1), 3.60 (s, IH) , 1.02 (s, 9H) . Part H. Preparation of N- (2 ' -aminosulfonyl- [1, 1' ]biphen-4- yl) -2- (3 ' -amidinophenyl) nicotinamide, trifluoroacetic acid salt. N- (2 ' -t-butylaminosulfonyl- [1, 1 ' ]biphen-4-yl) -2- (3 ' - cyanophenyl) nicotinamide (190 mg, 0.37 mmol) was dissolved in dry MeOH (10 mL) and cooled to 0°C. HCl (g) was generated by the addition of concentrated H 2 S0 4 (60 mL) to NaCl (240 g) over 40 minutes and was bubbled into the reaction mixture. The gas was permitted to continue bubbling through the reaction for 3 hours after the H 2 S0 4 addition was complete. At this point, the HCl generator and ice bath were removed, and the reaction stirred under argon for 19 hours. This solution was then evaporated, placed under high vacuum, and redissolved in dry MeOH (10 mL) . Ammonium carbonate (200 mg) was added, stirred for 24 hours under argon, and evaporated. The product was purified by preparative HPLC on a C-18 reverse phase column (10-70% MeCN/H 2 O/0.05% TFA), yielding a white powder (140 mg, 54%). X H NMR (DMSO-d 6 ) : δ 10.65 (s, IH) , 9.38 (s, 2H) , 8.92 (s, 2H) , 8.81 (dd, IH, J = 4.4, J' = 1.4), 8.10 (m, 2H) , 7.97 (m, 2H) , 7.76 (m, IH) , 7.67 (t, IH, J = 8.0), 7.57 ( , 5H) , 7.29 (m, 5H) . HRMS calc . for C 25 H 22 N 5 0 3 S: m/z 472.1443; found, 472.1457. Examples 2, 3 and 4 N- [5- (2- minosulfonyl) henylpyrid-2-yl] -2- (3 ' - amidinophenyl)nicotinamide, trifluoroacetic acid salt (Exastple 2) , N- [5- (2-t-butylaminosulfonyl)phenylpyrid-2-yl] -2- (3'- amidinophenyl) nicotinamide, trifluoroacetic acid salt (Example 3), and N- [5- (2-aminosulfonyl)phenylpyrid-2-yl] -2- (3'- carboxamidophenyl)nicotinamide, trifluoroacetic acid salt (Example 4) Part A. Preparation of 2- (3 ' -cyanophenyl) nicotinic acid. Methyl 2- (3 ' -cyanophenyl) nicotinate (1.21 g, 5.1 mmol) was partially dissolved in MeOH (40 mL) , and lithium hydroxide monohydrate (234 mg dissolved in 6 mL H0, 5.6 mmol) was added. After 20 hours, the resulting solution was diluted with water and extracted with CHC1 3 . The aqueous was acidified to pK 4 with 1 M HCl and extracted several times with CHC1 3 . Solid sodium chloride was added to the aqueous solution and the solution was extracted with 5-10% MeOH/CHCl 3 . The organic extracts were combined, dried over Na 2 S0 , filtered, and evaporated to yield a white solid (1.06 g, 93%) . X H NMR (CDC1 3 ) : δ 8.85 (dd, IH, J = 5.1, J' = 1.5) , 8.35 (dd, IH, J = 7.6, J' = 1.4), 7.84 (s, IH) , 7.75 (m, 2H) , 7.55 (t, IH, J = 7.7) , 7.47 (m, IH) . Part B. Preparation of 2-amino-5- (2-t-butylamino- sulfonyl) phenylpyridine . A mixture of 1.55 g (9.0 mmol) of 2-amino-5-bromopyridine and 2.3 g (9.0 mmol) of 2- (t-butylaminosulfonyl) phenylboronic acid, 0.52 g of tetrakis ( triphenylphosphine) palladium(O) (0.45 mmol), 0.15 g of tetrabutylammonium bromide (0.45 mmol) and 9 mL of 2M aqueous sodium carbonate were refluxed with 80 mL of benzene under Ar for 5 hours. After cooling, the mixture was diluted with 25 mL of methylene chloride and 25 mL of water. The two phases were separated and the organic phase was washed with water, dried with MgS0 4 and concentrated in vacuo . The resulting thick oil was chromatographed on silica with 50% EtOAc/hexane to afford 1.34 g (49%) of the aniline. 1 H NMR (CDCI 3 ): δ 8.18 (d, IH) ; 8.07 (m, IH) ; 7.70 (dd, IH) ; 7.58 (dt, IH) ; 7.48 (dt, IH) ; 7.28 (d, IH) ; 6.56 (d, IH) ; 4.62 (br s, 2H) ; 3.88 (br s, IH) ; 1.06 (s, 9H) . Part C. Preparation of N-[5-(2-t- butylaminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - cyanophenyl ) nicotinamide . 2- (3 ' -cyanophenyl) nicotinic acid (300 mg, 1.3 mmol) was suspended in 5 mL dry CH 2 C1 2 , and oxalyl chloride (175 μl, 2.0 mmol) was added, followed by 2 drops of dry DMF. The reaction stirred at room temperature under argon for 2 hours and then evaporated. This solid was redissolved in 8 mL dry CH 2 C1 2 , and dimethylaminopyridine (490 mg, 4.0 mmol) was added, followed by 2-amino-5- (2-t-butylaminosulfonyl)phenylpyridine (410 mg, 1.3 mmol) . The reaction was stirred 3 days at room temperature, diluted with CH 2 C1 2 , extracted with saturated NaHC0 3 , dried over Na 2 S0 4 , filtered, and evaporated. The resulting material was chromatographed on silica gel (50-75% EtOAc / hexanes) to yield the desired product (423 mg, 62%) . X H NMR (CDC1 3 ) : δ 8.83 (dd, IH, J = 4.8, J' = 1.5) , 8.40 (bs, IH) , 8.29 (bd, IH, J = 8.4), 8.17 (dd, IH) , J = 8.0, J' = 1.1), 8.09 (m, 3H) , 7.97 (d, IH, J = 7.7), 7.79 (d, IH, J = 8.4), 7.69 (d, IH, J = 7.7), 7.54 (m, 4H) , 7.25 (m, IH) , 4.19 (bs, IH) , 1.08 (s, 9H) . Part D. Preparation of N- [5- (2-aminosulfonyl)phenylpyrid-2- yl] -2- (3 ' -amidinophenyl) nicotinamide, trifluoroacetic acid salt (Example 2), N- [5- (2-t-butylaminosulfonyl) phenylpyrid-2- yl] -2- (3 ' -amidinophenyl) nicotinamide, trifluoroacetic acid salt (Example 3), and N- [5- (2-aminosulfonyl) phenylpyrid-2-yl] - 2- (3 ' -carboxamidophenyl) nicotinamide, trifluoroacetic acid salt (Example 4) . N- [5- (2-t-butylaminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - cyanophenyl) nicotinamide (410 mg, 1.03) was dissolved in a mixture of dry MeOH (5mL) and dry CHC1 3 (15mL) and cooled to 0°C . HCl(g) was generated by the addition of concentrated H 2 S0 4 (45 mL) to NaCl (220 g) over 55 min and was bubbled into the reaction mixture. The HCl generator and ice bath were removed, and the reaction was stirred under argon for 16 hours and evaporated. The resulting solid was redissolved in dry MeOH (15 mL) , and ammonium carbonate (385 mg) was added. The reaction was stirred 19 hours at room temperature under argon and evaporated. The resulting solid was purified by preparative HPLC on a C-18 reverse phase column (5-70% MeCN / H20 / 0.05% TFA) to yield N- [5- (2-aminosulfonyl) phenylpyrid-2- yl] -2- (3 ' -amidinophenyl) nicotinamide, trifluoroacetic acid salt (Example 2), (250 mg, 45%). X H NMR (DMS0-d 6 ) : δ 11.27 (s, IH) , 9.43 (s, 2H) , 8.98 (s, 2H) , 8.83 (dd, IH, J = 4.8, J' = 1.9), 8.32 (s, IH) , 8.13 (m, 2H) , 8.05 (m, 2H) , 7.96 (d, IH, J = 7.3), 7.81 (d, 2H, J = 8.4), 7.65 (m, 4H) , 7.47 (s, 2H) , 7.37 (m, IH) . HRMS calc . for C 24 H 21 N 6 0 3 S: m/z 473.1396; found, 473.1397. A second product, N- [5- (2-t-butylaminosulfonyl) - phenylpyrid-2-yl] -2- (3 ' -amidinophenyl) nicotinamide, trifluoroacetic acid salt (Example 3), was also obtained (58 mg, 10%). λ K NMR (DMSO-d 6 ) : δ 9.7 (s, IH) , 9.41 (s, 2H) , 8.95 (s, 2H) , 8.82 (m, IH) , 8.28 (s, IH) , 8.09 (m, 4H) , 7.95 (d, IH, J = 7.7), 7.79 (m, 2H) , 7.63 (m, 4H) , 7.34 (d, IH, J = 7.7), 7.18 (s, IH) , 1.04 (s, 9H) . HRMS calc . for C 28 H 29 N 6 0 3 S: 529.2022; found, 529.2050. A third product, N-[5-(2- aminosulfonyl) phenylpyrid-2-yl] -2- (3 ' - carboxamidophenyl) nicotinamide, trifluoroacetic acid sale (Example 4) was isolated and chromatographed on silica gel (10-20% MeOH/CHCl 3 ) to yield a white solid (77 mg, 20%) . X H NMR (DMSO-d 6 ) : δ 11.13 (s, IH) , 8.75 (dd, IH, J = 4.8, J' = 1.9), 8.26 (m, 2H) , 8.02 (m, 4H) , 7.84 (d, IH, J = 7.7), 7.74 (m, 2H) , 7.59 (m, 2H) , 7.47 (m, 2H) , 7.36 (m, 4H) . Table 1 The following table contains representative examples of the present invention. Each entry in the table is intended to be paired with each formulae at the start of the table. For example, example 1 in Table 2 is intended to be paired with each of formulae ~ss 4 . Table 2 a 1 R=F, D=NH 2 b! R=F, D=NH 2 c 1 R=F, D=NH 2 a 2 R=H, D=NH 2 b 2 R=H, D=NH 2 c 2 R=H, D=NH 2 a 3 R=F, D=CH 2 NH 2 b 3 R=F, D=CH 2 NH 2 c 3 R=F, D=CH 2 NH 2 a 4 R=H, D=CH 2 NH 2 b 4 R=H, D=CH 2 NH 2 c 4 R=H, D=CH 2 NH 2 a 5 R=F, D=C(=NH)NH 2 b 5 R=F, D=C(=NH)NH 2 c 5 R=F, D=C(=NH)NH 2 a 6 R=H, D=C(=NH)NH 2 b 6 R=H, D=C(=NH)NH 2 c 6 R=H, D=C(=NH)NH 2 a 7 R=F, D=C(0)NH 2 b 7 R=F, D=C(0)NH 2 c 7 R=F, D=C(0)NH 2 a 8 R=H, D=C(0)NH 2 b 8 R=H, D=C(0)NH 2 c 8 R=H, D=C(0)NH 2 d! R=F, D=NH 2 θ! R=F, D=NH 2 f^ R=F, D=NH 2 d 2 R=H, D=NH 2 e 2 R=H, D=NH 2 f 2 R=H, D=NH 2 d 3 R=F, D=CH 2 NH 2 e 3 R=F, D=CH 2 NH 2 f 3 R=F, D=CH 2 NH 2 d 4 R=H, D=CH 2 NH 2 e 4 R=H, D=CH 2 NH 2 f 4 R=H, D=CH 2 NH 2 d 5 R=F, D=C(=NH)NH 2 e 5 R=F, D=C(=NH)NH 2 f 5 R=F, D=C(=NH)NH 2 d 6 R=H, D=C(=NH)NH 2 e 6 R=H, D=C(=NH)NH 2 f 6 R=H, D=C(=NH)NH 2 d 7 R=F, D=C(0)NH 2 e 7 R=F, D=C(0)NH 2 f 7 R=F, D=C(0)NH 2 d 8 R=H, D=C(0)NH 2 e 8 R=H, D=C(0)NH 2 f 8 R=H, D=C(0)NH 2 g! R=F, D=NH 2 hi R=F, D=NH 2 R=F, D=NH 2 g 2 R=H, D=NH 2 h R=H, D=NH 2 i 2 R=H, D=NH 2 g 3 R=F, D=CH 2 NH 2 h 3 R=F, D=CH 2 NH 2 i 3 R=F, D=CH 2 NH 2 g 4 R=H, D=CH 2 NH 2 h 4 R=H, D=CH 2 NH 2 i 4 R=H, D=CH 2 NH 2 g 5 R=F, D=C(=NH)NH 2 h 5 R=F, D=C(=NH)NH 2 i 5 R=F, D=C(=NH)NH 2 g 6 R=H, D=C(=NH)NH 2 h 6 R=H, D=C(=NH)NH 2 i 6 R=H, D=C(=NH)NH 2 g 7 R=F, D=C(0)NH 2 h 7 R=F, D=C(0)NH 2 i 7 R=F, D=C(0)NH 2 g 8 R=H, D=C(0)NH 2 h 8 R=H, D=C(0)NH 2 i 8 R=H, D=C(0)NH 2 U R=F, D=NH 2 ^ R=F, D=NH 2 h R=F, D=NH 2 J2 R=H, D=NH 2 k 2 R=H, D=NH 2 1 2 R=H, D=NH 2 j 3 R=F, D=CH 2 NH 2 k 3 R=F, D=CH 2 NH 2 1 3 R=F, D=CH 2 NH 2 j 4 R=H, D=CH 2 NH 2 l^ R=H, D=CH 2 NH 2 1 4 R=H, D=CH 2 NH 2 j 5 R=F, D=C(=NH)NH 2 k 5 R=F, D=C(=NH)NH 2 1 5 R=F, D=C(=NH)NH 2 J6 R=H, D=C(=NH)NH 2 k 6 R=H, D=C(=NH)NH 2 1 6 R=H, D=C(=NH)NH 2 j 7 R=F, D=C(0)NH 2 k 7 R=F, D=C(0)NH 2 1 7 R=F, D=C(0)NH 2 j 8 R=H, D=C(Q)NH 2 k 8 R=H, D=C(0)NH 2 1 8 R=H, D=C(0)NH 2 n^ R=F, D=NH 2 ri! R=F, D=NH 2 0 1 R=F, D=NH 2 m 2 R=H, D=NH 2 n 2 R=H, D=NH 2 0 2 R=H, D=NH 2 m 3 R=F, D=CH 2 NH 2 n 3 R=F, D=CH 2 NH 2 0 3 R=F, D=CH 2 NH 2 m 4 R=H, D=CH 2 NH 2 n 4 R=H, D=CH 2 NH 2 0 4 R=H, D=CH 2 NH 2 m 5 R=F, D=C(=NH)NH 2 n 5 R=F, D=C(=NH)NH 2 0 5 R=F, D=C(=NH)NH 2 m 6 R=H, D=C(=NH)NH 2 n 6 R=H, D=C(=NH)NH 2 0 6 R=H, D=C(=NH)NH 2 m 7 R=F, D=C(0)NH 2 n 7 R=F, D=C(0)NH 2 0 7 R=F, D=C(0)NH 2 m 8 R=H, D=C(0)NH 2 n 8 R=H, D=C(0)NH 2 0 8 R=H, D=C(0)NH 2 P! R=F, D=NH 2 qi R=F, D=NH 2 R=F, D=NH 2 p 2 R=CI, D=NH 2 q 2 R=CI, D=NH 2 R=CI, D=NH 2 p 3 R=OMe, D=NH 2 q 3 R=OMe, D=NH 2 R=OMe, D=NH 2 p 4 R=F, D=CH 2 NH 2 q 4 R=F, D=CH 2 NH 2 R=F, D=CH 2 NH 2 p 5 R=CI, D=CH 2 NH 2 q 5 R=CI, D=CH 2 NH 2 R=CI, D=CH 2 NH 2 p 6 R=OMe, D=CH 2 NH 2 q 6 R=OMe, D=CH 2 NH2 R=OMe, D=CH 2 NH 2 p 7 R=F, D=C(=NH)NH 2 q 7 R=F, D=C(=NH)NH 2 R=F, D=C(=NH)NH 2 p 8 R=CI, D=C(=NH)NH 2 q 8 R=CI, D=C(=NH)NH 2 8 R=CI, D=C(=NH)NH 2 P9 R=OMe, D=C(=NH)NH 2 q 9 R=OMe, D=C(=NH)NH 2 9 R=OMe, D=C(=NH)NH 2 P10 R=F, D=C(0)NH 2 q 10 R=F, D=C(0)NH 2 10 R=F, D=C(0)NH 2 Pn R=CI, D=C(0)NH 2 qn R=CI, D=C(0)NH 2 n R=CI, D=C(0)NH 2 p 12 R=OMe, D=C(0)NH 2 q 12 R=OMe, D=C(0)NH 2 12 R=OMe, D=C(0)NH 2 Si s 2 s 3 s 4 s 5 s 6 s s 8 s s 1 S Sι v 1 R=F, D=NH 2 W! v 2 R=CI, D=NH 2 w 2 v 3 R=OMe, D=NH 2 w 3 v 4 R=F, D=CH 2 NH 2 w 4 v 5 R=CI, D=CH 2 NH 2 w 5 v 6 R=OMe, D=CH 2 NH 2 w 6 v 7 R=F, D=C(=NH)NH w 7 v 8 R=CI, D=C(=NH)NH 2 w 8 v 9 R=OMe, D=C(=NH)NH 2 w g 2 v 10 R=F, D=C(0)NH 2 w 10 n R=CI, D=C(0)NH 2 W11 v 12 R=OMe, D=C(0)NH 2 w-| yi R=F, D=NH 2 Zi R=F, D=NH 2 aai R=F, D=NH 2 y 2 R=CI, D=NH 2 z 2 R=CI, D=NH 2 aa 2 R=CI, D=NH 2 y 3 R=OMe, D=NH 2 z 3 R=OMe, D=NH 2 aa 3 R=OMe, D=NH 2 y 4 R=F, D=CH 2 NH 2 z 4 R=F, D=CH 2 NH 2 aa 4 R=F, D=CH 2 NH 2 y 5 R=CI, D=CH 2 NH 2 z 5 R=CI, D=CH 2 NH 2 aa 5 R=CI, D=CH 2 NH 2 y 6 R=OMe, D=CH 2 NH 2 z 6 R=OMe, D=CH 2 NH 2 aa 6 R=OMe, D=CH 2 NH 2 y 7 R=F, D=C(=NH)NH 2 z 7 R=F, D=C(=NH)NH 2 aa 7 R=F, D=C(=NH)NH 2 y 8 R=CI, D=C(=NH)NH 2 z 8 R=CI, D=C(=NH)NH 2 aa 8 R=CI, D=C(=NH)NH 2 y 9 R=OMe, D=C(=NH)NH 2 z 9 R=OMe, D=C(=NH)NH 2 aa 9 R=OMe, D=C(=NH)NH 2 y 10 R=F, D=C(0)NH 2 z 10 R=F, D=C(0)NH 2 aa 10 R=F, D=C(0)NH 2 yn R=CI, D=C(0)NH 2 Z11 R=CI, D=C(0)NH 2 aan R=CI, D=C(0)NH 2 y 12 R=OMe, D=C(0)NH 2 z 12 R=OMe, D=C(0)NH 2 aa 12 R=OMe, D=C(0)NH 2 bbi R=F, D= NH 2 cci R=F, D= NH 2 ddi R=F, D=NH 2 bb 2 R=CI, D :NH 2 cc 2 R=CI, D= NH 2 dd 2 R=CI, D=NH 2 bb 3 R=OMe D=NH 2 cc 3 R=OMe, D=NH 2 dd 3 R=OMe, D=NH 2 bb 4 R=F, D=< CH 2 NH 2 cc 4 R=F, D= CH 2 NH 2 dd 4 R=F, D=CH 2 NH 2 bb 5 R=CI, D= =CH 2 NH 2 cc 5 R=CI, D: =CH 2 NH 2 dd 5 R=CI, D=CH 2 NH 2 bb 6 R=OMe, D=CH 2 NH 2 cc 6 R=OMe, D=CH 2 NH 2 dd 8 R=OMe, D=CH 2 NH 2 bb 7 R=F, D= C(=NH)NH 2 cc R=F, D= C(=NH)NH 2 dd 7 R=F, D=C(=NH)NH 2 bb 8 R=CI, D= C(=NH)NH 2 cc 8 R=CI, D= C(=NH)NH 2 dd 8 R=CI, D=C(=NH)NH 2 bbg R=OMe, D=C(=NH)NH 2 ccg R=OMe, D=C(=NH)NH 2 dd 9 R=OMe, D=C(=NH)NH 2 bb 10 R=F, D =C(0)NH 2 cc 10 R=F, D =C(0)NH 2 dd 10 R=F, D=C(0)NH 2 bbn R=CI, D =C(0)NH 2 ecu R=CI, D C(0)NH 2 ddn R=CI, D=C(0)NH 2 bb 12 R=OMe , D=C(0)NH 2 cc-t2 R=OMe D=C(0)NH 2 dd 12 R=OMe, D=C(0)NH 2 ee 1 R=F, D=CH 2 NH 2 f-i R=F, D=CH 2 NH 2 ggi R=F, D=CH 2 NH 2 ee 2 R=CI, D=CH 2 NH 2 f 2 R=CI, D=CH 2 NH 2 gg 2 R=CI, D=CH 2 NH 2 ee 3 R=OMe, D=CH 2 NH 2 ff 3 R=OMe, D=CH 2 NH 2 gg 3 R=OMe, D=CH 2 NH 2 ee 4 R=CH 2 NH 2 , ff 4 R=CH 2 NH 2l gg 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH NH 2 D=CH 2 NH 2 hhi R=F, D=CH 2 NH 2 ii R=F, D=CH 2 NH 2 jji R=F, D=CH 2 NH 2 hh 2 R=CI, D=CH 2 NH 2 i 2 R=CI, D=CH 2 NH 2 jJ2 R=CI, D=CH 2 NH 2 hh 3 R=OMe, D=CH 2 NH 2 i 3 R=OMe, D=CH 2 NH 2 jJ3 R=OMe, D=CH 2 NH 2 hh 4 R=CH 2 NH 2 , i 4 R=CH 2 NH 2 , jj 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 kki R=F, D=CH 2 NH 2 Hi R=F, D=CH 2 NH 2 mmι R=F, D=CH 2 NH 2 kk 2 R=CI, D=CH 2 NH 2 11 2 R=CI, D=CH 2 NH 2 mm 2 R=CI, D=CH 2 NH 2 kk 3 R=OMe, D=CH 2 NH 2 11 3 R=OMe, D=CH 2 NH 2 mm 3 R=OMe, D=CH 2 NH 2 kk 4 R=CH 2 NH 2 , 11 4 R=CH 2 NH 2> mm 4 R=CH 2 NH 2> D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 nnι R=F, D=CH 2 NH 2 ∞< \ R=F, D=CH 2 NH 2 PP1 R=F, D=CH NH 2 nn 2 R=CI, D=CH 2 NH 2 00 2 R=CI, D=CH 2 NH 2 PP2 R=CI, D=CH 2 NH 2 nn 3 R=OMe, D=CH 2 NH 2 00 3 R=OMe, D=CH 2 NH 2 PP3 R=OMe, D=CH 2 NH 2 nn 4 R=CH 2 NH 2 , 00 4 R=CH 2 NH 2 , pp 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 qqi R=F, D=CH 2 NH 2 rr-i R=F, D=CH 2 NH 2 ss 1 R=F, D=CH 2 NH2 qq 2 R=CI, D=CH 2 NH 2 rr 2 R=CI, D=CH 2 NH 2 ss 2 R=CI, D=CH 2 NH 2 qq 3 R=OMe, D=CH 2 NH 2 rr 3 R=OMe, D=CH 2 NH2 ss 3 R=OMe, D=CH 2 NH 2 qq 4 R=CH 2 NH 2 , rr 4 R=CH 2 NH 2 , ss 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 Ex # R lb 1 H phenyl 2- (aminosulfonyl) phenyl 2 H phenyl 2- (methylaminosulfonyl) phenyl 3 H phenyl 1-pyrrolidinocarbonyl 4 H phenyl 2- (me hylsulfonyl) phenyl 5 H phenyl 4-morpholino 6 H phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl 7 H phenyl 4-morpholinocarbonyl 8 H 2-pyridyl 2- (aminosulfonyl) phenyl 9 H 2-pyridyl 2- (methylaminosulfonyl) phenyl 10 H 2-pyridyl 1-pyrro1idinocarbony1 11 H 2-pyridyl 2- (me hylsulfonyl)phenyl 12 H 2-pyridyl 4-morpholino 13 H 2-pyridyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl H 2-pyridyl 4-morpholinocarbonyl H 3 -pyridyl 2- ( aminosulfonyl ) phenyl H 3 -pyridyl 2- (methylaminosulfonyl) phenyl H 3-pyridyl 1-pyrrolidinocarbonyl H 3-pyridyl 2- (methylsulfonyl) phenyl H 3-pyridyl 4-morpholino H 3-pyridyl 2- (1' -CF3-tetrazol-2-yl) phenyl H 3-pyridyl 4-morpholinocarbonyl H 2-pyrimidyl 2- (aminosulfonyl) phenyl H 2-pyrimidyl 2- (methylaminosulfonyl) phenyl H 2-pyrimidyl 1-pyrrolidinocarbonyl H 2-pyrimidyl 2- (methylsulfonyl) phenyl H 2-pyrimidyl 4-morpholino H 2-pyrimidyl 2-(l'-CF3-tetrazol-2-yl)phenyl H 2-pyrimidyl 4-morpholinocarbony1 H 5-pyrimidyl 2- (aminosulfonyl) phenyl H 5-pyrimidyl 2- (methylaminosulfonyl) phenyl H 5-pyrimidyl 1-pyrro1idinocarbony1 H 5-pyrimidyl 2- (methylsulfonyl) phenyl H 5-pyrimidyl 4-morpholino H 5-pyrimidyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl H 5-pyrimidyl 4-morpholinocarbonyl H 2-Cl-phenyl 2- (aminosulfonyl ) phenyl H 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl H 2-C1-phenyl 1-pyrrolidinocarbonyl H 2-Cl-phenyl 2- (methylsulfonyl) phenyl H 2-Cl-phenyl 4-morpholino H 2-C1-phenyl 2- (1' -CF3-tetrazol-2-yl)phenyl H 2-Cl-phenyl 4-morpholinocarbonyl H 2-F-phenyl 2- (aminosulfonyl) phenyl H 2-F-phenyl 2- (methylaminosulfonyl) phenyl H 2-F-phenyl 1-pyrro1idinocarbony1 H 2-F-phenyl 2- (methylsulfonyl) phenyl H 2-F-phenyl 4-morpholino H 2-F-phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl H 2-F-phenyl 4-morpholinocarbonyl H 2 , 5-diF-phenyl 2- (aminosulfonyl) phenyl H 2, 5-diF-phenyl 2- (methylaminosulfonyl) phenyl H 2, 5-diF-phenyl 1-pyrrolidinocarbony1 H 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl H 2, 5-diF-phenyl 4-morpholino H 2, 5-diF-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl H 2, 5-diF-phenyl 4-morpholinocarbonyl H phenyl 2- (N-pyrrolidinyl-methyl)phenyl H phenyl 2- (N-piperidinyl-methyl ) phenyl H phenyl 2- (N-morpholino-methyl) phenyl H phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl H phenyl 2- (N-pyridinium-methyl) phenyl H phenyl 2-(N-4- (N, N' -dimethylamino)- pyridinium-methyl ) phenyl H phenyl 2- (N-azatanyl-methyl) phenyl H phenyl 2- (N-azetidinyl-methyl) phenyl H phenyl 2- (N-piperazinyl-methyl) phenyl H phenyl 2- (N,N' -BOC-piperazinyl- methyl) phenyl H phenyl 2- (N-imidazolyl-methyl) phenyl H phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl H phenyl 2- (N-pyridonyl-methyl ) phenyl H phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl H phenyl 2- (amidiny1 ) henyl H phenyl 2- (N-guanidinyl ) phenyl H phenyl 2- ( imidazolyl ) phenyl H phenyl 2- (imidazolidinyl) phenyl H phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl H phenyl 2- (2-pyrrolidinyl) phenyl H phenyl 2- (2-piperidinyl) phenyl H phenyl 2- (amidinyl-methyl ) phenyl H phenyl 2- (2-imidazolidinyl- methyl ) phenyl H phenyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl H phenyl 2-dimethylaminoimidazol-l-yl H phenyl 2- (3-aminophenyl ) H phenyl 2- (3-pyrrolidinylcarbonyl) H phenyl 2-glycinoyl H phenyl 2- imidazol-1-ylacetyl) H 2-pyridyl 2- N-pyrrolidinyl-methyl ) phenyl H 2-pyridyl 2- N-piperidinyl-methyl) phenyl H 2-pyridyl 2- N-morpholino-methyl ) phenyl H 2-pyridyl 2- N,N' -methylmorpholinium- methyl ) phenyl H 2-pyridyl 2- N-pyridinium-methyl) henyl H 2-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl H 2-pyridyl 2- N-azatanyl-methyl) phenyl H 2-pyridyl 2- N-azetidinyl-methyl) phenyl H 2-pyridyl 2- N-piperazinyl-methyl ) phenyl H 2-pyridyl 2- N,N' -BOC-piperazinyl- methyl) phenyl H 2-pyridyl 2- N-imidazolyl-methyl ) phenyl H 2-pyridyl 2- N-methoxy-N-methylamino- methyl) phenyl H 2-pyridyl 2- N-pyridonyl-methyl ) phenyl H 2-pyridyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl) phenyl H 2-pyridyl 2- amidinyl) phenyl H 2-pyridyl 2- N-guanidinyl) phenyl H 2-pyridyl 2- imidazolyl ) phenyl H 2-pyridyl 2- imidazolidinyl) phenyl H 2-pyridyl 2- 2-imidazolidinyl- sulfonyl) phenyl H 2-pyridyl 2- 2-pyrrolidinyl) phenyl H 2-pyridyl 2- 2-piperidinyl) phenyl H 2-pyridyl 2- amidinyl-methyl) phenyl H 2-pyridyl 2- 2-imidazolidinyl- methyl) phenyl H 2-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 110 H 2-pyridyl 2-dimethylaminoimidazol-l-yl 111 H 2-pyridyl 2- 3-aminophenyl) 112 H 2 -pyridyl 2- 3 -pyrrolidinylcarbonyl ] 113 H 2-pyridyl 2-glycinoyl 114 H 2-pyridyl imidazol-1-ylacetyl ) 115 H 3 -pyridyl (N-pyrrolidinyl-methyl ) henyl 116 H 3 -pyridyl (N-piperidinyl-methyl) phenyl 117 H 3 -pyridyl (N-morpholino-methyl ) phenyl 118 H 3 -pyridyl (N, N ' -methylmorpholinium- methyl ) phenyl 119 H 3 -pyridyl (N-pyridinium-methyl ) phenyl 120 H 3 -pyridyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 121 H 3 -pyridyl (N-azatanyl-methyl) phenyl 122 H 3 -pyridyl (N-azetidiny1-methyl ) phenyl 123 H 3 -pyridyl (N-piperazinyl-methyl) phenyl 124 H 3 -pyridyl (N, N ' -BOC-piperazinyl- methyl ) phenyl 125 H 3 -pyridyl (N-imidazolyl-methyl) phenyl 126 H 3 -pyridyl (N-methoxy-N-methylamino- methyl ) phenyl 127 H 3 -pyridyl (N-pyridonyl-methyl ) phenyl 128 H 3 -pyridyl (N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 129 H 3 -pyridyl [amidinyl ) phenyl 130 H 3 -pyridyl (N-guanidinyl ) phenyl 131 H 3 -pyridyl imidazolyl ) phenyl 132 H 3-pyridyl imidazolidinyl ) phenyl 133 H 3-pyridyl [2 -imidazolidiny1- sulfonyl ) phenyl 134 H 3-pyridyl [ 2 -pyrrolidinyl ) phenyl 135 H 3 -pyridyl [ 2 -piperidinyl ) phenyl 136 H 3-pyridyl [ amidinyl-methyl ) phenyl 137 H 3 -pyridyl [2-imidazolidinyl- methyl ) phenyl 138 H 3 -pyridyl (N- (2 -aminoimidazolyl) - methyl ) phenyl 139 H 3 -pyridyl -dimethylaminoimidazol-1-yl 140 H 3 -pyridyl 3 -aminophenyl ) 141 H 3 -pyridyl [ 3 -pyrrolidinylcarbonyl ) 142 H 3-pyridyl 2-glycinoyl 143 H 3 -pyridyl 2- imidazol-1-ylacetyl ) 144 H 2-pyrimidyl 2- N-pyrrolidinyl-methyl ) phenyl 145 H 2-pyrimidyl 2- N-piperidinyl-methyl ) phenyl 146 H 2-pyrimidyl 2- N-morpholino-methyl ) phenyl 147 H 2-pyrimidyl 2- N, N ' -methylmorpholinium- methyl ) phenyl 148 H 2-pyrimidyl 2- N-pyridinium-methyl ) phenyl 149 H 2-pyrimidyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 150 H 2-pyrimidyl 2- N-azatanyl-methyl ) phenyl 151 H 2-pyrimidyl 2- N-azetidinyl-methyl ) phenyl 152 H 2-pyrimidyl 2- N-piperazinyl-methyl ) phenyl 153 H 2-pyrimidyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 154 H 2-pyrimidyl 2- N-imidazolyl-methyl) phenyl 155 H 2-pyrimidyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 156 H 2-pyrimidyl 2- (N-pyridonyl-methyl) phenyl 157 H 2-pyrimidyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 158 H 2-pyrimidyl 2- (amidinyl ) phenyl 159 H 2-pyrimidyl 2- (N-guanidinyl) phenyl 160 H 2-pyrimidyl 2- ( imidazolyl ) phenyl 161 H 2-pyrimidyl 2- (imidazolidinyl) phenyl 162 H 2-pyrimidyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 163 H 2-pyrimidyl 2- (2-pyrrolidinyl) phenyl 164 H 2-pyrimidyl 2- ( 2-piperidinyl ) phenyl 165 H 2-pyrimidyl 2- (amidinyl-methyl ) phenyl 166 H 2-pyrimidyl 2- (2-imidazolidinyl- methyl ) phenyl 167 H 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 168 H 2-pyrimidyl 2-dimethylaminoimidazol-1-yl 169 H 2-pyrimidyl 2- ( 3 -aminophenyl ) 170 H 2-pyrimidyl 2- (3-pyrrolidinylcarbonyl) 171 H 2-pyrimidyl 2-glycinoyl 172 H 2-pyrimidyl 2- ( imidazol-1-ylacetyl) 173 H 2-Cl-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 174 H 2-Cl-phenyl 2- (N-piperidinyl-methyl) phenyl 175 H 2-Cl-phenyl 2- (N-morpholino-methyl) phenyl 176 H 2-Cl-phenyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 177 H 2-Cl-phenyl 2- (N-pyridinium-methyl) phenyl 178 H 2-Cl-phenyl 2- (N-4- (N, N ' -dimethylamino) - pyridinium-methyl) phenyl 179 H 2-Cl-phenyl 2- (N-azatanyl-methyl) phenyl 180 H 2-Cl-phenyl 2- (N-azetidinyl-methyl) phenyl 181 H 2-Cl-phenyl 2- (N-piperazinyl-methyl) phenyl 182 H 2-Cl-phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 183 H 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 184 H 2-Cl-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 185 H 2-Cl-phenyl 2- (N-pyridonyl-methyl ) phenyl 186 H 2-Cl-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 187 H 2-Cl-phenyl 2- (amidinyl) phenyl 188 H 2-C1-phenyl 2- (N-guanidinyl ) phenyl 189 H 2-Cl-phenyl 2- ( imidazolyl) phenyl 190 H 2-Cl-phenyl 2- (imidazolidinyl) phenyl 191 H 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 192 H 2-C1-phenyl 2- ( 2-pyrrolidinyl) phenyl 193 H 2-Cl-phenyl 2- (2-piperidinyl) phenyl 194 H 2-Cl-phenyl 2- (amidinyl-methyl ) phenyl 195 H 2-Cl-phenyl 2- (2-imidazolidinyl- methyl) phenyl 196 H 2-Cl-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 197 H 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl 198 H 2-Cl-phenyl 2- 3 -aminophenyl ) 199 H 2-Cl-phenyl 2- 3 -pyrrolidinylcarbonyl ) 200 H 2-Cl-phenyl 2-glycinoyl 201 H 2-Cl-phenyl 2- imidazol-1-ylacetyl) 202 H 2-F-phenyl 2- N-pyrrolidinyl-methyl) phenyl 203 H 2-F-phenyl 2- N-piperidinyl-methyl ) phenyl 204 H 2-F-phenyl 2- N-morpholino-methyl) phenyl 205 H 2-F-phenyl 2- N, N ' -mathylmorpholinium- methyl) phenyl 206 H 2-F-phenyl 2- N-pyridinium-methyl ) phenyl 207 H 2-F-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 208 H 2-F-phenyl 2- N-azatanyl-methyl ) phenyl 209 H 2-F-phenyl 2- N-azetidinyl-methyl ) phenyl 210 H 2-F-phenyl 2- N-piperazinyl-methyl) phenyl 211 H 2-F-phenyl 2- N, N ' -BOC-piperazinyl- methyl ) phenyl 212 H 2-F-phenyl 2- N-imidazolyl-methyl) phenyl 213 H 2-F-phenyl 2- N-methoxy-N-methylamino- methyl ) henyl 214 H 2-F-phenyl 2- N-pyridonyl-methyl ) phenyl 215 H 2-F-phenyl 2- N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 216 H 2-F-phenyl 2- amidinyl) phenyl 217 H 2-F-phenyl 2- N-guanidinyl ) phenyl 218 H 2-F-phenyl 2- imidazolyl) phenyl 219 H 2-F-phenyl 2- imidazolidinyl) phenyl 220 H 2-F-phenyl 2- 2-imidazolidinyl- sulfonyl ) phenyl 221 H 2-F-phenyl 2- 2-pyrrolidiny1) phenyl 222 H 2-F-phenyl 2- 2-piperidinyl) phenyl 223 H 2-F-phenyl 2- amidinyl-methyl ) phenyl 224 H 2-F-phenyl 2- 2-imidazolidiny1- methyl ) phenyl 225 H 2-F-phenyl 2- N- (2-aminoimidazolyl) - methyl ) phenyl 226 H 2-F-phenyl 2- dimethylaminoimidazol-1-yl 227 H 2-F-phenyl 2- 3 -aminophenyl ) 228 H 2-F-phenyl 2- 3-pyrrolidinylcarbonyl) 229 H 2-F-phenyl 2- glycinoyl 230 H 2-F-phenyl 2- imidazol-1-ylacetyl ) 231 H 2, 5-diF-phenyl 2- N-pyrrolidinyl-methyl) phenyl 232 H 2, 5-diF-phenyl 2- N-piperidinyl-methyl) phenyl 233 H 2, 5-diF-phenyl 2- N-morpholino-methyl) phenyl 234 H 2, 5-diF-phenyl 2- N, ' -methylmorpholinium- methyl) phenyl 235 H 2, 5-diF-phenyl 2- N-pyridinium-methyl) phenyl 236 H 2, 5-diF-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 237 H 2, 5-diF-phenyl 2- N-azatanyl-methyl) phenyl 238 H 2, 5-diF-phenyl 2- N-azetidinyl-methyl) phenyl 239 H 2, 5-diF-phenyl 2- N-piperazinyl-methyl) phenyl 240 H 2, 5-diF-phenyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 241 H 2, 5-diF-phenyl 2- N-imidazolyl-methyl) phenyl 242 H 2, 5-diF-phenyl 2- N-methoxy-N-methylamino- methyl ) phenyl 243 H 2, 5-diF-phenyl 2- (N-pyridonyl-methyl ) phenyl 244 H 2, 5-diF-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 245 H 2, 5-diF-phenyl 2- (amidinyl ) phenyl 246 H 2, 5-diF-phenyl 2- (N-guanidinyl) phenyl 247 H 2, 5-diF-phenyl 2- ( imidazolyl) phenyl 248 H 2, 5-diF-phenyl 2- (imidazolidinyl) phenyl 249 H 2, 5-diF-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 250 H 2, 5-diF-phenyl 2- ( 2-pyrrolidinyl) phenyl 251 H 2 , 5-diF-phenyl 2- (2-piperidinyl) phenyl 252 H 2, 5-diF-phenyl 2- (amidinyl-methyl ) phenyl 253 H 2, 5-diF-phenyl 2- (2-imidazolidinyl- methyl) phenyl 254 H 2, 5-diF-phenyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 255 H 2 , 5-diF-phenyl 2-dimethylaminoimidazol-l-yl 256 H 2, 5-diF-phenyl 2- (3 -aminophenyl ) 257 H 2, 5-diF-phenyl 2- (3-pyrrolidinylcarbonyl) 258 H 2, 5-diF-phenyl 2-glycinoyl 259 H 2, 5-diF-phenyl 2- ( imidazol-1-ylacetyl) 260 -CN phenyl 2- (aminosulfonyl) phenyl 261 -CN phenyl 2- (methylaminosulfonyl) phenyl 262 -CN phenyl 1-pyrro1idinocarbony1 263 -CN phenyl 2- (methylsulfonyl) phenyl 264 -CN phenyl 4-morpholino 265 -CN phenyl 2- (l'-CF3-tetrazol-2-yl)phenyl 266 -CN phenyl 4-morpholinocarbonyl 267 -CN 2-pyridyl 2- (aminosulfonyl ) phenyl 268 -CN 2-pyridyl 2- (methylaminosulfonyl) phenyl 269 -CN 2-pyridyl 1-pyrro1idinocarbony1 270 -CN 2-pyridyl 2- (methylsulfonyl) phenyl 271 -CN 2-pyridyl 4-morpholino 272 -CN 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 273 -CN 2-pyridyl 4-morpholinocarbonyl 274 -CN 3 -pyridyl 2- (aminosulfonyl) phenyl 275 -CN 3 -pyridyl 2- (methylaminosulfonyl ) phenyl 276 -CN 3-pyridyl 1-pyrrolidinocarbonyl 277 -CN 3-pyridyl 2- (methylsulfonyl) phenyl 278 -CN 3-pyridyl 4-morpholino 279 -CN 3-pyridyl 2-(l'-CF3-tetrazol-2-yl)phenyl 280 -CN 3-pyridyl 4-morpholinocarbonyl 281 -CN 2-pyrimidyl 2- (aminosulfonyl ) phenyl 282 -CN 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 283 -CN 2-pyrimidyl 1-pyrrolidinocarbonyl 284 -CN 2-pyrimidyl 2- (methylsulfonyl) phenyl 285 -CN 2-pyrimidyl 4-morpholino 286 -CN 2-pyrimidyl 2- (l'-CF3-tetrazol-2-yl) phenyl 287 -CN 2-pyrimidyl 4-morpholinocarbonyl 288 -CN 5-pyrimidyl 2- (aminosulfonyl) henyl 289 -CN 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 290 -CN 5-pyrimidyl 1-pyrrolidinocarbonyl 291 -CN 5-pyrimidyl 2- (methylsulfonyl) phenyl 292 -CN 5-pyrimidyl 4-morpho1ino 293 -CN 5-pyrimidyl 2- (1' -CF3-tetrazol-2-yl) phenyl 294 -CN 5-pyrimidyl 4-morpho1inocarbony1 295 -CN 2-Cl-phenyl 2- aminosulfonyl ) phenyl 296 -CN 2-Cl-phenyl 2- methylaminosulfonyl ) phenyl 297 -CN 2-Cl-phenyl 1-pyrrolidinocarbonyl 298 -CN 2-Cl-phenyl 2- methylsulfonyl ) phenyl 299 -CN 2-Cl-phenyl 4-morpholino 300 -CN 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 301 -CN 2-Cl-phenyl 4-morpholinocarbonyl 302 -CN 2-F-phenyl 2 - aminosulfonyl ) phenyl 303 -CN 2-F-phenyl 2 - methylaminosulfony1) phenyl 304 -CN 2-F-phenyl 1-pyrro1idinocarbony1 305 -CN 2-F-phenyl 2- methylsulfonyl ) phenyl 306 -CN 2-F-phenyl 4-morpholino 307 -CN 2-F-phenyl 2- 1 ' -CF3 -tetrazol-2-yl ) phenyl 308 -CN 2-F-phenyl 4-morpholinocarbonyl 309 -CN 2 , 5-diF-phenyl 2- aminosulfonyl ) henyl 310 -CN 2, 5-diF-phenyl 2- methylaminosulfonyl ) phenyl 311 -CN 2, 5-diF-phenyl 1-pyrrolidinocarbonyl 312 -CN 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 313 -CN 2 , 5-diF-phenyl 4-morpholino 314 -CN 2, 5-diF-phenyl 2- 1 ' -CF3 -tetrazol-2-yl ) phenyl 315 -CN 2 , 5-diF-phenyl 4-morpholinocarbonyl 316 -CN phenyl 2- N-pyrrolidinyl-methyl ) phenyl 317 -CN phenyl 2- N-piperidinyl-methyl ) phenyl 318 -CN phenyl 2- N-morpholino-methyl) phenyl 319 -CN phenyl 2- N, N ' -methylmorpholinium- methyl) phenyl 320 -CN phenyl 2- (N-pyridinium-methyl) phenyl 321 -CN phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 322 -CN phenyl 2- (N-azatanyl-methyl) phenyl 323 -CN phenyl 2- (N-azetidinyl-methyl) phenyl 324 -CN phenyl 2- (N-piperazinyl-methyl) phenyl 325 -CN phenyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 326 -CN phenyl 2- (N-imidazolyl-methyl) phenyl 327 -CN phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 328 -CN phenyl 2- (N-pyridonyl-methyl ) phenyl 329 -CN phenyl 2- (N- (N 1 ,N' -dimethylhydrazinyl- methyl) phenyl 330 -CN phenyl 2- (amidinyl) phenyl 331 -CN phenyl 2- (N-guanidinyl ) phenyl 332 -CN phenyl 2- ( imidazolyl) phenyl 333 -CN phenyl 2- (imidazolidinyl) phenyl 334 -CN phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 335 -CN phenyl 2- (2-pyrrolidinyl) phenyl 336 -CN phenyl 2- (2-piperidinyl) phenyl 337 -CN phenyl 2- (amidinyl-methyl ) phenyl 338 -CN phenyl 2- (2-imidazolidinyl- methyl) phenyl 339 -CN phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 340 -CN phenyl 2-dimethylaminoimidazol-1-yl 341 -CN phenyl 2- (3-aminophenyl ) 342 -CN phenyl 2- (3 -pyrrolidinylcarbonyl) 343 -CN phenyl 2-glycinoyl 344 -CN phenyl 2- (imidazol-1-ylacetyl) 345 -CN 2-pyridyl 2- (N-pyrrolidinyl-methyl) phenyl 346 -CN 2-pyridyl 2- (N-piperidinyl-methyl) phenyl 347 -CN 2-pyridyl 2- (N-morpholino-methyl) phenyl 348 -CN 2-pyridyl 2- (N,N T -methylmorpholinium- methyl ) phenyl 349 -CN 2-pyridyl 2- (N-pyridinium-methyl ) phenyl 350 -CN 2-pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 351 -CN 2-pyridyl 2- (N-azatanyl-methyl) phenyl 352 -CN 2-pyridyl 2- (N-azetidinyl-methyl) phenyl 353 -CN 2-pyridyl 2 - (N-piperazinyl-methyl) phenyl 354 -CN 2-pyridyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 355 -CN 2-pyridyl 2- (N-imidazolyl-methyl) phenyl 356 -CN 2-pyridyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 357 -CN 2-pyridyl 2- (N-pyridonyl-methyl ) phenyl 358 -CN 2-pyridyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl ) phenyl 359 -CN 2-pyridyl 2- (amidinyl ) phenyl 360 -CN 2-pyridyl 2- (N-guanidinyl ) phenyl 361 -CN 2-pyridyl 2- ( imidazolyl ) phenyl 362 -CN 2-pyridyl 2- (imidazolidinyl) phenyl 363 -CN 2-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 364 -CN 2-pyridyl 2- (2-pyrrolidinyl) phenyl 365 -CN 2-pyridyl 2- (2-piperidinyl) phenyl 366 -CN 2-pyridyl 2- (amidinyl-methyl) henyl 367 -CN 2-pyridyl 2- (2-imidazolidinyl- methyl) phenyl 368 -CN 2-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 369 -CN 2-pyridyl 2-dimethylaminoimidazol-l-yl 370 -CN 2-pyridyl 2- (3 -aminophenyl ) 371 -CN 2-pyridyl 2- (3-pyrrolidinylcarbonyl) 372 -CN 2-pyridyl 2-glycinoyl 373 -CN 2-pyridyl 2- (imidazol-1-ylacetyl) 374 -CN 3-pyridyl 2- (N-pyrrolidinyl-methyl ) phenyl 375 -CN 3-pyridyl 2- (N-piperidinyl-methyl) phenyl 376 -CN 3-pyridyl 2- (N-morpholino-methyl) phenyl 377 -CN 3-pyridyl 2- (N,N' -methylmorpholinium- methyl) phenyl 378 -CN 3-pyridyl 2- (N-pyridinium-methyl) phenyl 379 -CN 3-pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 380 -CN 3-pyridyl 2- (N-azatanyl-methyl) phenyl 381 -CN 3-pyridyl 2- (N-azetidinyl-methyl) phenyl 382 -CN 3-pyridyl 2- (N-piperazinyl-methyl) phenyl 383 -CN 3-pyridyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 384 -CN 3-pyridyl 2- (N-imidazolyl-methyl) phenyl 385 -CN 3-pyridyl 2- (N-methoxy-N-methylamino- methyl) phenyl 386 -CN 3-pyridyl 2- (N-pyridonyl-methyl) phenyl 387 -CN 3 -pyridyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl ) phenyl 388 -CN 3 -pyridyl 2- (amidinyl ) phenyl 389 -CN 3 -pyridyl 2- (N-guanidinyl ) phenyl 390 -CN 3 -pyridyl 2- ( imidazolyl ) phenyl 391 -CN 3 -pyridyl 2- (imidazolidinyl) phenyl 392 -CN 3 -pyridyl 2- (2 -imidazolidinyl - sulfonyl ) phenyl 393 -CN 3 -pyridyl 2- (2-pyrrolidinyl) phenyl 394 -CN 3-pyridyl 2- (2-piperidinyl ) phenyl 395 -CN 3-pyridyl 2- (amidinyl-methyl) phenyl 396 -CN 3 -pyridyl 2- (2 -imidazolidinyl- methyl ) phenyl 397 -CN 3-pyridyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 398 -CN 3-pyridyl 2-dimethylaminoimidazol-l-yl 399 -CN 3-pyridyl 2- ( 3 -aminophenyl ) 400 -CN 3-pyridyl 2- (3 -pyrrolidinylcarbonyl) 401 -CN 3-pyridyl 2-glycinoyl 402 -CN 3-pyridyl 2- (imidazol-1-ylacetyl) 403 -CN 2-pyrimidyl 2- (N-pyrrolidinyl-methyl) phenyl 404 -CN 2-pyrimidyl 2- (N-piperidinyl-methyl) phenyl 405 -CN 2-pyrimidyl 2- (N-morpholino-methyl) phenyl 406 -CN 2-pyrimidyl 2- (N,N' -methylmorpholinium- methyl) phenyl 407 -CN 2-pyrimidyl 2- (N-pyridinium-methyl) phenyl 408 -CN 2-pyrimidyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 409 -CN 2-pyrimidyl 2- (N-azatanyl-methyl) phenyl 410 -CN 2-pyrimidyl 2- (N-azetidinyl-methyl) phenyl 411 -CN 2-pyrimidyl 2- (N-piperazinyl-methyl) phenyl 412 -CN 2-pyrimidyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 413 -CN 2-pyrimidyl 2- (N-imidazolyl-methyl) phenyl 414 -CN 2-pyrimidyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 415 -CN 2-pyrimidyl 2- (N-pyridonyl-methyl) phenyl 416 -CN 2-pyrimidyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 417 -CN 2-pyrimidyl 2- (amidinyl ) phenyl 418 -CN 2-pyrimidyl 2- (N-guanidinyl) henyl 419 -CN 2-pyrimidyl 2- (imidazolyl) phenyl 420 -CN 2-pyrimidyl 2- (imidazolidinyl) phenyl 421 -CN 2-pyrimidyl 2- (2-imidazolidinyl- sulfonyl) phenyl 422 -CN 2-pyrimidyl 2- (2-pyrrolidiny1) phenyl 423 -CN 2-pyrimidyl 2- (2-piperidinyl) phenyl 424 -CN 2-pyrimidyl 2- (amidinyl-methyl)phenyl 425 -CN 2-pyrimidyl 2- (2-imidazolidinyl- methyl ) phenyl 426 -CN 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 427 -CN 2-pyrimidyl 2-dimethylaminoimidazol-1-yl 428 -CN 2-pyrimidyl 2- (3 -aminophenyl ) 429 -CN 2-pyrimidyl 2- (3-pyrrolidinylcarbonyl) 430 -CN 2-pyrimidyl 2-glycinoyl 431 -CN 2-pyrimidyl 2- (imidazol-1-ylacetyl) 432 -CN 2-Cl-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 433 -CN 2-Cl-phenyl 2- (N-piperidinyl-methyl) phenyl 434 -CN 2-Cl-phenyl 2- (N-morpholino-methyl) phenyl 435 -CN 2-Cl-phenyl 2- (N, N ' -methylmorpholinium- methyl ) phenyl 436 -CN 2-Cl-phenyl 2- (N-pyridinium-methyl ) phenyl 437 -CN 2-Cl-phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 438 -CN 2-Cl-phenyl 2- (N-azatanyl-methyl) phenyl 439 -CN 2-Cl-phenyl 2- (N-azetidinyl-methyl) phenyl 440 -CN 2-Cl-phenyl 2- (N-piperazinyl-methyl) phenyl 441 -CN 2-Cl-phenyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 442 -CN 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 443 -CN 2-Cl-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 444 -CN 2-Cl-phenyl 2- (N-pyridonyl-methyl ) phenyl 445 -CN 2-Cl-phenyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl) phenyl 446 -CN 2-Cl-phenyl 2- (amidinyl ) phenyl 447 -CN 2-Cl-phenyl 2- (N-guanidinyl ) phenyl 448 -CN 2-Cl-phenyl 2- ( imidazolyl) phenyl 449 -CN 2-Cl-phenyl 2- (imidazolidinyl) phenyl 450 -CN 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 451 -CN 2-Cl-phenyl 2- (2-pyrrolidinyl) phenyl 452 -CN 2-Cl-phenyl 2- (2-piperidinyl) phenyl 453 -CN 2-Cl-phenyl 2- (amidinyl-methyl) phenyl 454 -CN 2-Cl-phenyl 2- (2-imidazolidiny1- methyl) phenyl 455 -CN 2-Cl-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 456 -CN 2-Cl-phenyl 2-dimethylaminoimidazol-l-yl 457 -CN 2-Cl-phenyl 2- (3 -aminophenyl ) 458 -CN 2-Cl-phenyl 2- (3 -pyrrolidinylcarbonyl) 459 -CN 2-Cl-phenyl 2-glycinoyl 460 -CN 2-Cl-phenyl 2- ( imidazol-1-ylacetyl) 461 -CN 2-F-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 462 -CN 2-F-phenyl 2- (N-piperidinyl-methyl ) phenyl 463 -CN 2-F-phenyl 2- (N-morpholino-methyl ) phenyl 464 -CN 2-F-phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl 465 -CN 2-F-phenyl 2- (N-pyridinium-methyl ) phenyl 466 -CN 2-F-phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 467 -CN 2-F-phenyl 2- (N-azatanyl-methyl) phenyl 468 -CN 2-F-phenyl 2- (N-azetidinyl-methyl) phenyl 469 -CN 2-F-phenyl 2- (N-piperazinyl-methyl) phenyl 470 -CN 2-F-phenyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 471 -CN 2-F-phenyl 2- (N-imidazolyl-methyl) phenyl 472 -CN 2-F-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 473 -CN 2-F-phenyl 2- (N-pyridonyl-methyl ) henyl 474 -CN 2 -F-phenyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl ) phenyl 475 -CN 2 -F-phenyl 2- [amidinyl ) phenyl 476 -CN 2 -F-phenyl 2- (N-guanidinyl ) phenyl 477 -CN 2 -F-phenyl 2- imidazolyl ) phenyl 478 -CN 2 -F-phenyl 2- [ imidazolidinyl) phenyl 479 -CN 2 -F-phenyl 2- 2 -imidazolidinyl- sulfonyl ) phenyl 480 -CN 2 -F-phenyl 2- ;2-pyrrolidiny1 ) phenyl 481 -CN 2 -F-phenyl 2- ;2-piperidinyl) phenyl 482 -CN 2 -F-phenyl 2- (amidinyl-methyl ) phenyl 483 -CN 2 -F-phenyl 2- [ 2-imidazolidiny1- methyl ) phenyl 484 -CN 2 -F-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 485 -CN 2-F-phenyl 2 dimethylaminoimidazol-1-y1 486 -CN 2-F-phenyl 2- ;3 -aminophenyl) 487 -CN 2-F-phenyl 2- 3 -pyrrolidinylcarbonyl ) 488 -CN 2-F-phenyl 2 glycinoyl 489 -CN 2-F-phenyl 2- imidazol-1-ylacetyl ) 490 -CN 2, 5-diF-phenyl 2- (N-pyrrolidinyl-methyl ) phenyl 491 -CN 5-diF-phenyl 2- (N-piperidinyl-methyl ) phenyl 492 -CN 5-diF-phenyl 2- (N-morpholino-methyl) phenyl 493 -CN 5-diF-phenyl 2- (N, N ' -methylmorpholinium- methyl) phenyl 494 -CN 5-diF-phenyl 2- (N-pyridinium-methyl ) phenyl 495 -CN 5-diF-phenyl 2- (N-4- (N,N' -dimethyiamino) - pyridinium-methyl ) phenyl 496 -CN 5-diF-pheny1 2- (N-azatanyl-methyl) phenyl 497 -CN 5-diF-phenyl 2- (N-azetidinyl-methyl) phenyl 498 -CN 5-diF-phenyl 2- (N-piperazinyl-methyl) phenyl 499 -CN 5-diF-phenyl 2- (N, N ' -BOC-piperazinyl- methyl) phenyl 500 -CN 5-diF-phenyl 2- (N-imidazolyl-methyl ) phenyl 501 -CN 5-diF-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 502 -CN 5-diF-phenyl 2- (N-pyridonyl-methyl ) phenyl 503 -CN 5-diF-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 504 -CN 5-diF-phenyl 2- (amidinyl ) phenyl 505 -CN 5-diF-phenyl 2- (N-guanidinyl ) phenyl 506 -CN 5-diF-phenyl 2- [ imidazolyl) phenyl 507 -CN 5-diF-phenyl 2- [ imidazolidinyl ) phenyl 508 -CN 5-diF-phenyl 2- [2-imidazolidinyl- sulfonyl ) phenyl 509 -CN 5-diF-phenyl 2- [2-pyrrolidinyl ) phenyl 510 -CN 5-diF-phenyl 2- ;2-piperidinyl) phenyl 511 -CN 5-diF-phenyl 2- (amidinyl-methyl) phenyl 512 -CN 5-diF-phenyl 2- [2-imidazolidinyl- methyl) phenyl 513 -CN 5-diF-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 514 -CN 5-diF-phenyl 2-dimethylaminoimidazol-1-yl 515 -CN 5-diF-phenyl 2- (3-aminophenyl ) 516 -CN 5-diF-phenyl 2- (3-pyrrolidinylcarbonyl) 517 -CN 5-diF-phenyl 2-glycinoyl 518 -CN 2 , 5-diF-phenyl 2- (imidazol-1-ylacetyl) 519 CF 3 phenyl 2- (aminosulfonyl ) phenyl 520 CF 3 phenyl 2- (methylaminosulfonyl) phenyl 521 CF 3 phenyl 1-pyrrolidinocarbonyl 522 CF 3 phenyl 2- (methylsulfonyl) phenyl 523 CF 3 phenyl 4-morpholino 524 CF 3 phenyl 2 - ( l ' -CF 3 - tetrazol-2 -yD phenyl 525 CF 3 phenyl 4-morpholinocarbony1 526 CF 3 2-pyridyl 2- (aminosulfonyl)phenyl 527 CF 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 528 CF 3 2-pyridyl 1-pyrro1idinocarbony1 529 CF 3 2-pyridyl 2- (methylsulfonyl) phenyl 530 CF 3 2-pyridyl 4-morpholino 531 CF 3 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 532 CF 3 2-pyridyl 4-morpholinocarbonyl 533 CF 3 3 -pyridyl 2- (aminosulfonyl) phenyl 534 CF 3 3-pyridyl 2- (methylaminosulfonyl) phenyl 535 CF 3 3-pyridyl 1-pyrrolidinocarbonyl 536 CF 3 3-pyridyl 2- (methylsulfonyl) phenyl 537 CF 3 3-pyridyl 4-morpholino 538 CF 3 3-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 539 CF 3 3 -pyridyl 4-morpholinocarbonyl 540 CF 3 2-pyrimidyl 2- (aminosulfonyl) phenyl 541 CF 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 542 CF 3 2-pyrimidyl 1-pyrrolidinocarbonyl 543 CF 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 544 CF 3 2-pyrimidyl 4-morpholino 545 CF 3 2-pyrimidyl 2-(l'-CF3-tetrazol-2-yl)phenyl 546 CF 3 2-pyrimidyl 4-morpholinocarbonyl 547 CF 3 5-pyrimidyl 2- (aminosulfonyl) phenyl 548 CF 3 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 549 CF 3 5-pyrimidyl 1-pyrro1idinocarbony1 550 CF 3 5-pyrimidyl 2- (methylsulfonyl) henyl 551 CF 3 5-pyrimidyl 4-morpho1ino 552 CF 3 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 553 CF 3 5-pyrimidyl 4-morpholinocarbonyl 554 CF 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 555 CF 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 556 CF 3 2-Cl-phenyl 1-pyrro1idinocarbony1 557 CF 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 558 CF 3 2-Cl-phenyl 4-morpholino 559 CF 3 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 560 CF 3 2-Cl-phenyl 4-morpholinocarbonyl 561 CF 3 2-F-phenyl 2- (aminosulfonyl) henyl 562 CF 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 563 CF 3 2-F-phenyl 1-pyrro1idinocarbony1 564 CF 3 2-F-phenyl 2- (methylsulfonyl) phenyl 565 CF 3 2-F-phenyl 4-morpholino 566 CF 3 2-F-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 567 CF 3 2-F-phenyl 4-morpholinocarbonyl 568 CF 3 2 , 5-diF-phenyl 2- (aminosulfonyl) phenyl 569 CF 3 2 , 5-diF-phenyl 2- (methylaminosulfonyl) phenyl 570 CF 3 2,5-diF -phenyl 1-pyrrolidinocarbonyl 571 CF 3 2,5-diF -phenyl 2- (methylsulfonyl) phenyl 572 CF 3 2,5-diF'-phenyl 4-morpholino 573 CF 3 2,5-diF'-phenyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 574 CF 3 2,5-diF -phenyl 4-morpholinocarbonyl 575 CF 3 phenyl (N-pyrrolidinyl-methyl ) phenyl 576 CF 3 phenyl (N-piperidinyl-methyl) phenyl 577 CF 3 phenyl (N-morpholino-methyl) phenyl 578 CF 3 phenyl (N,N' -methylmorpholinium- methyl ) phenyl 579 CF 3 phenyl (N-pyridinium-methyl ) phenyl 580 CF 3 phenyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 581 CF 3 phenyl (N-azatanyl-methyl) phenyl 582 CF 3 phenyl (N-azetidinyl-methyl ) phenyl 583 CF 3 phenyl (N-piperazinyl-methyl) phenyl 584 CF 3 phenyl (N,N' -BOC-piperazinyl- methyl ) phenyl 585 CF 3 phenyl (N-imidazolyl-methyl ) phenyl 586 CF 3 phenyl (N-methoxy-N-methylamino- methyl ) phenyl 587 CF 3 phenyl (N-pyridonyl-methyl ) phenyl 588 CF 3 phenyl (N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 589 CF 3 phenyl (amidinyl ) phenyl 590 CF 3 phenyl (N-guanidinyl ) phenyl 591 CF 3 phenyl ( imidazolyl ) phenyl 592 CF 3 phenyl (imidazolidinyl) phenyl 593 CF 3 phenyl (2-imidazolidiny1- sulfonyl ) phenyl 594 CF 3 phenyl (2-pyrrolidinyl) phenyl 595 CF 3 phenyl (2-piperidinyl) phenyl 596 CF 3 phenyl (amidinyl-methyl ) phenyl 597 CF 3 phenyl - (2-imidazolidinyl- methyl ) henyl 598 CF 3 phenyl - (N- (2-aminoimidazolyl) - methyl ) phenyl 599 CF 3 phenyl -dimethylaminoimidazol-1-yl 600 CF 3 phenyl - (3-aminophenyl ) 601 CF 3 phenyl - (3-pyrrolidinylcarbonyl) 602 CF 3 phenyl 2-glycinoyl 603 CF 3 phenyl 2- imidazol-1-ylacetyl) 604 CF 3 2-pyridyl 2- N-pyrrolidinyl-methyl) phenyl 605 CF 3 2-pyridyl 2- N-piperidinyl-methyl) phenyl 606 CF 3 2-pyridyl 2- N-morpholino-methyl) phenyl 607 CF 3 2-pyridyl 2- N, N ' -methylmorpholinium- methyl ) phenyl 608 CF 3 2-pyridyl 2- N-pyridinium-methyl)phenyl 609 CF 3 2-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 610 CF 3 2-pyridyl 2- N-azatanyl-methyl) phenyl 611 CF 3 2-pyridyl 2- N-azetidinyl-methyl ) phenyl 612 CF 3 2-pyridyl 2- N-piperazinyl-methyl ) phenyl 613 CF 3 2-pyridyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 614 CF 3 2-pyridyl 2- (N-imidazolyl-methyl) phenyl 615 CF 3 2-pyridyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 616 CF 3 2-pyridyl 2- (N-pyridonyl-methyl ) phenyl 617 CF 3 2-pyridyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 618 CF 3 2-pyridyl 2- (amidinyl ) phenyl 619 CF 3 2-pyridyl 2- ( -guanidinyl ) phenyl 620 CF 3 2-pyridyl 2- ( imidazolyl ) phenyl 621 CF 3 2-pyridyl 2- (imidazolidinyl) phenyl 622 CF 3 2-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 623 CF 3 2-pyridyl 2- (2-pyrrolidinyl ) phenyl 624 CF 3 2-pyridyl 2- (2-piperidinyl) phenyl 625 CF 3 2-pyridyl 2- (amidinyl-methyl ) phenyl 626 CF 3 2-pyridyl 2- (2-imidazolidinyl- methyl ) phenyl 627 CF 3 2-pyridyl N- (2-aminoimidazolyl) - methyl ) phenyl 628 CF 3 2-pyridyl 2-dimethylaminoimidazol-l-yl 629 CF 3 2-pyridyl 2- (3 -aminophenyl) 630 CF 3 2-pyridyl 2- (3-pyrrolidinylcarbonyl) 631 CF 3 2-pyridyl 2-glycinoyl 632 CF 3 2-pyridyl 2- imidazol-1-ylacetyl) 633 CF 3 3-pyridyl 2- N-pyrrolidinyl-methyl ) phenyl 634 CF 3 3-pyridyl 2- N-piperidinyl-methyl ) phenyl 635 CF 3 3-pyridyl 2- N-morpholino-methyl) phenyl 636 CF 3 3-pyridyl 2- N, N ' -methylmorpholinium- methyl) phenyl 637 CF 3 3-pyridyl 2- N-pyridinium-methyl ) phenyl 638 CF 3 3-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 639 CF 3 3-pyridyl 2- N-azatanyl-methyl) phenyl 640 CF 3 3-pyridyl 2- N-azetidinyl-methyl) phenyl 641 CF 3 3-pyridyl 2- N-piperazinyl-methyl) phenyl 642 CF 3 3-pyridyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 643 CF 3 3-pyridyl 2- N-imidazolyl-methyl) phenyl 644 CF 3 3-pyridyl 2- N-methoxy-N-methylamino- methyl)phenyl 645 CF 3 3-pyridyl 2- N-pyridonyl-methyl) phenyl 646 CF 3 3-pyridyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl) phenyl 647 CF 3 3-pyridyl 2- amidinyl) phenyl 648 CF 3 3-pyridyl 2- N-guanidinyl) phenyl 649 CF 3 3-pyridyl 2- imidazolyl ) phenyl 650 CF 3 3-pyridyl 2- imidazolidinyl) phenyl 651 CF 3 3-pyridyl 2- 2-imidazolidiny1- sulfonyl ) phenyl 652 CF 3 3-pyridyl 2- 2-pyrrolidinyl) phenyl 653 CF 3 3-pyridyl 2- 2-piperidinyl) phenyl 654 CF 3 3-pyridyl 2- (amidinyl-methyl ) phenyl ~~ 655 CF 3 3 -pyridyl 2- (2-imidazolidinyl- methyl) phenyl 656 CF 3 3-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 657 CF 3 3-pyridyl 2-dimethylaminoimidazol-1-yl 658 CF 3 3 -pyridyl (3 -aminophenyl ) 659 CF 3 3 -pyridyl - ( 3-pyrrolidinylcarbonyl ) 660 CF 3 3-pyridyl -glycinoyl 661 CF 3 3-pyridyl - (imidazol-1-ylacetyl) 662 CF 3 2-pyrimidyl - (N-pyrrolidinyl-methyl) phenyl 663 CF 3 2-pyrimidyl (N-piperidinyl-methyl ) phenyl 664 CF 3 2-pyrimidyl (N-morpholino-methyl ) henyl 665 CF 3 2-pyrimidyl (N,N' -methylmorpholinium- methyl ) phenyl 666 CF 3 2-pyrimidyl (N-pyridinium-methyl ) phenyl 667 CF 3 2-pyrimidyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 668 CF 3 2-pyrimidyl (N-azatanyl-methyl) phenyl 669 CF 3 2-pyrimidyl (N-azetidinyl-methyl) phenyl 670 CF 3 2-pyrimidyl (N-piperazinyl-methyl ) phenyl 671 CF 3 2-pyrimidyl (N,N' -BOC-piperazinyl- methyl ) phenyl 672 CF 3 2-pyrimidyl (N-imidazolyl-methyl ) phenyl 673 CF 3 2-pyrimidyl (N-methoxy-N-methylamino- methyl) phenyl 674 CF 3 2-pyrimidyl (N-pyridonyl-methyl ) phenyl 675 CF 3 2-pyrimidyl (N- (N ' ,N ' -dimethylhydrazinyl- methyl) phenyl 676 CF 3 2-pyrimidyl (amidinyl) phenyl 677 CF 3 2-pyrimidyl (N-guanidinyl ) phenyl 678 CF 3 2-pyrimidyl (imidazolyl) phenyl 679 CF 3 2-pyrimidyl ( imidazolidiny1) phenyl 680 CF 3 2-pyrimidyl (2-imidazolidiny1- sulfonyl ) phenyl 681 CF 3 2-pyrimidyl (2-pyrrolidiny1 ) phenyl 682 CF 3 2-pyrimidyl (2-piperidinyl ) phenyl 683 CF 3 2-pyrimidyl (amidinyl-methyl ) phenyl 684 CF 3 2-pyrimidyl (2-imidazolidinyl- methyl) phenyl 685 CF 3 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 686 CF 3 2-pyrimidyl 2-dimethylaminoimidazol-l-yl 687 CF 3 2-pyrimidyl 2- (3-aminophenyl) 688 CF 3 2-pyrimidyl 2- (3-pyrrolidinylcarbonyl) 689 CF 3 2-pyrimidyl 2-glycinoyl 690 CF 3 2-pyrimidyl 2- imidazol-1-ylacetyl) 691 CF 3 2-Cl-phenyl 2- N-pyrrolidinyl-methyl) phenyl 692 CF 3 2-Cl-phenyl 2- N-piperidinyl-methyl ) phenyl 693 CF 3 2-Cl-phenyl 2- N-morpholino-methyl) phenyl 694 CF 3 2-Cl-phenyl 2- N, N ' -methylmorpholinium- methyl) phenyl 695 CF 3 2-Cl-phenyl (N-pyridinium-methyl) phenyl 696 CF 3 2-Cl-phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 697 CF 3 2-Cl-phenyl 2- (N-azatanyl-methyl) phenyl 698 CF 3 2-Cl-phenyl 2- (N-azetidinyl-methyl) phenyl 699 CF 3 2-Cl-phenyl 2- (N-piperazinyl-methyl) phenyl 700 CF 3 2-Cl-phenyl 2- (N,N T -BOC-piperazinyl- methyl ) phenyl 701 CF 3 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 702 CF 3 2-Cl-phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 703 CF 3 2-Cl-phenyl 2- (N-pyridonyl-methyl) phenyl 704 CF 3 2-Cl-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 705 CF 3 2-Cl-phenyl 2- (amidinyl ) phenyl 706 CF 3 2-Cl-phenyl 2- (N-guanidinyl ) phenyl 707 CF 3 2-Cl-phenyl 2- ( imidazolyl) phenyl 708 CF 3 2-Cl-phenyl 2- (imidazolidinyl) phenyl 709 CF 3 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 710 CF 3 2-Cl-phenyl 2- (2-pyrrolidinyl) phenyl 711 CF 3 2-Cl-phenyl 2- ( 2-piperidinyl ) henyl 712 CF 3 2-Cl-phenyl 2- (amidinyl-methyl ) phenyl 713 CF 3 2-Cl-phenyl 2- (2-imidazolidinyl- methyl ) phenyl 714 CF 3 2-Cl-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 715 CF 3 2-Cl-phenyl 2-dimethylaminoimidazol-l-yl 716 CF 3 2-Cl-phenyl 2- (3-aminophenyl) 717 CF 3 2-Cl-phenyl 2- ( 3-pyrrolidinylcarbonyl ) 718 CF 3 2-Cl-phenyl 2-glycinoyl 719 CF 3 2-Cl-phenyl 2- (imidazol-1-ylacetyl) 720 CF 3 2-F-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 721 CF 3 2-F-phenyl 2- (N-piperidinyl-methyl) phenyl 722 CF 3 2-F-phenyl 2- (N-morpholino-methyl) phenyl 723 CF 3 2-F-phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl 724 CF 3 2-F-phenyl 2- (N-pyridinium-methyl ) phenyl 725 CF 3 2-F-phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 726 CF 3 2-F-phenyl 2- (N-azatanyl-methyl) phenyl 727 CF 3 2-F-phenyl 2- (N-azetidinyl-methyl) phenyl 728 CF 3 2-F-phenyl 2- (N-piperazinyl-methyl) phenyl 729 CF 3 2-F-phenyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 730 CF 3 2-F-phenyl 2- (N-imidazolyl-methyl) phenyl 731 CF 3 2-F-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 732 CF 3 2-F-phenyl 2- (N-pyridonyl-methyl ) phenyl 733 CF 3 2-F-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 734 CF 3 2-F-phenyl 2- (amidinyl) phenyl 735 CF 3 2-F-phenyl 2- (N-guanidinyl ) phenyl 736 CF 3 2-F-phenyl 2- ( imidazolyl) phenyl 737 CF 3 2-F-phenyl 2- (imidazolidinyl) phenyl 738 CF 3 2-F-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 739 CF 3 2-F-phenyl 2- (2-pyrrolidinyl) phenyl 740 CF 3 2-F-phenyl 2- (2-piperidinyl ) phenyl 741 CF 3 2-F-phenyl 2- (amidinyl-methyl) phenyl 742 CF 3 2-F-phenyl 2- (2-imidazolidinyl- methyl ) henyl 743 CF 3 2-F-phenyl 2- (N- ( 2 -aminoimidazolyl ) - methyl ) phenyl 744 CF 3 2-F-phenyl 2-dimethylaminoimidazol-l-yl 745 CF 3 2-F-phenyl 2- (3 -aminophenyl ) 746 CF 3 2-F-phenyl 2- (3-pyrrolidinylcarbonyl) 747 CF 3 2-F-phenyl 2-glycinoyl 748 CF 3 2-F-phenyl 2- ( imidazol-1-ylacetyl) 749 CF 3 2, 5-diF-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 750 CF 3 2, 5-diF-phenyl 2- (N-piperidinyl-methyl) phenyl 751 CF 3 2, 5-diF-phenyl 2- (N-morpholino-methyl) phenyl 752 CF 3 2, 5-diF-phenyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 753 CF 3 2, 5-diF-phenyl 2- (N-pyridinium-methyl) phenyl 754 CF 3 2, 5-diF-phenyl 2- (N-4- (N, N' -dimethylamino) - pyridinium-methyl ) phenyl 755 CF 3 2, 5-diF-phenyl 2- (N-azatanyl-methyl) phenyl 756 CF 3 2, 5-diF-phenyl 2- (N-azetidinyl-methyl) phenyl 757 CF 3 2, 5-diF-phenyl 2- (N-piperazinyl-methyl) phenyl 758 CF 3 2, 5-diF-phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 759 CF 3 2, 5-diF-phenyl 2- (N-imidazolyl-methyl) phenyl 760 CF 3 2, 5-diF-phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 761 CF 3 2, 5-diF-phenyl 2- (N-pyridonyl-methyl) phenyl 762 CF 3 2, 5-diF-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 763 CF 3 2, 5-diF-phenyl 2- (amidinyl ) phenyl 764 CF 3 2, 5-diF-phenyl 2- (N-guanidinyl ) phenyl 765 CF 3 2, 5-diF-phenyl 2- (imidazolyl) phenyl 766 CF 3 2, 5-diF-phenyl 2- (imidazolidinyl) phenyl 767 CF 3 2, 5-diF-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 768 CF 3 2, 5-diF-phenyl 2- (2-pyrrolidinyl) henyl 769 CF 3 2, 5-diF-phenyl 2- (2-piperidinyl) phenyl 770 CF 3 2, 5-diF-phenyl 2- (amidinyl-methyl ) phenyl 771 CF 3 2, 5-diF-phenyl 2- (2-imidazolidinyl- methyl) phenyl 772 CF 3 2, 5-diF-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 773 CF 3 2, 5-diF-phenyl 2-dimethylaminoimidazol-1-yl 774 CF 3 2, 5-diF-phenyl 2- (3 -aminophenyl ) 775 CF 3 2, 5-diF-phenyl 2- (3-pyrrolidinylcarbonyl) 776 CF 3 2, 5-diF-phenyl 2-glycinoyl 777 CF 3 2, 5-diF-phenyl 2- ( imidazol-1-ylacetyl) 778 CONH 2 phenyl 2- (aminosulfonyl) phenyl 779 CONH 2 phenyl 2- (methylaminosulfonyl) phenyl 780 CONH 2 phenyl 1-pyrrolidinocarbony1 781 C0NH 2 phenyl 2- (methylsulfonyl) phenyl 782 CONH 2 phenyl 4-morpholino 783 C0NH 2 phenyl 2-(l'-CF3-tetrazol-2-yl)phenyl 784 C0NH 2 phenyl 4-morpholinocarbonyl 785 C0NH 2 2-pyridyl 2- (aminosulfonyl) phenyl 786 CONH 2 2-pyridyl 2- (methylaminosulfonyl) phenyl 787 CONH 2 2-pyridyl 1-pyrrolidinocarbonyl 788 CONH 2 2-pyridyl 2- (methylsulfonyl) phenyl 789 CONH 2 2-pyridyl 4-morpholino 790 C0NH 2 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 791 C0NH 2 2-pyridyl 4-morpho1inocarbony1 792 CONH 2 3-pyridyl 2- (aminosulfonyl) phenyl 793 CONH 2 3-pyridyl 2- (methylaminosulfonyl) phenyl 794 CONH 2 3-pyridyl 1-pyrrolidinocarbonyl 795 CONH 2 3-pyridyl 2- (methylsulfonyl) phenyl 796 CONH 2 3-pyridyl 4-morpholino 797 CONH 2 3-pyridyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl 798 CONH 2 3-pyridyl 4-morpholinocarbonyl 799 CONH 2 2-pyrimidyl 2- (aminosulfonyl ) phenyl 800 CONH 2 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 801 CONH 2 2-pyrimidyl 1-pyrro1idinocarbony1 802 CONH 2 2-pyrimidyl 2- (methylsulfonyl) phenyl 803 CONH 2 2-pyrimidyl 4-morpholino 804 CONH 2 2-pyrimidyl 2- (1' -CF3-tetrazol-2-yl) phenyl 805 CONH 2 2-pyrimidyl 4-morpholinocarbonyl 806 CONH 2 5-pyrimidyl 2- (aminosulfonyl) phenyl 807 CONH 2 5-pyrimidyl 2- (methylaminosulfonyl ) phenyl 808 CONH 2 5-pyrimidyl 1-pyrro1idinocarbony1 809 CONH 5-pyrimidyl 2- (methylsulfonyl) phenyl 810 CONH 2 5-pyrimidyl 4-morpholino 811 C0NH 2 5-pyrimidyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 812 C0NH 2 5-pyrimidyl 4-morpholinocarbonyl 813 CONH 2 2-Cl-phenyl 2- (aminosulfonyl) phenyl 814 CONH 2 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 815 C0NH 2 2-Cl-phenyl 1-pyrrolidinocarbonyl 816 C0NH 2 2-Cl-phenyl 2- (methylsulfonyl) phenyl 817 C0NH 2 2-Cl-phenyl 4-morpholino 818 C0NH 2 2-Cl-phenyl 2- (1 ' -CF3-tetrazol-2-yl)phenyl 819 C0NH 2 2-Cl-phenyl 4-morpholinocarbonyl 820 C0NH 2 2-F-phenyl 2- (aminosulfonyl) phenyl 821 CONH 2 2-F-phenyl 2- (methylaminosulfonyl) phenyl 822 CONH 2 2-F-phenyl 1-pyrro1idinocarbony1 823 C0NH 2 2-F-phenyl 2- (methylsulfonyl ) phenyl 824 CONH2 2-F-phenyl 4-morpholino 825 C0NH 2 2-F-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 826 CONH 2 2-F-phenyl 4-morpho1inocarbony1 827 CONH 2 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 828 C0NH 2 2, 5-diF-phenyl 2- (methylaminosulfonyl) phenyl 829 C0NH 2 2, 5-diF-phenyl 1-pyrro1idinocarbony1 830 C0NH 2 2, 5-diF-phenyl 2- (methylsulfonyl ) phenyl 831 C0NH 2 2 , 5-diF-phenyl 4-morpholino 832 C0NH 2 2, 5-diF-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 833 C0NH 2 2, 5-diF-phenyl 4-morpholinocarbonyl 834 C0NH 2 phenyl 2- (N-pyrrolidinyl-methyl) phenyl 835 C0NH 2 phenyl 2- (N-piperidinyl-methyl) phenyl 836 C0NH 2 phenyl 2- (N-morpholino-methyl) phenyl 837 C0NH 2 phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl 838 C0NH 2 phenyl 2- (N-pyridinium-methyl) phenyl 839 CONH 2 phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 840 CONH 2 phenyl 2- (N-azatanyl-methyl) phenyl 841 CONH 2 phenyl 2- (N-azetidinyl-methyl) phenyl 842 CONH 2 phenyl 2- (N-piperazinyl-methyl) phenyl 843 CONH 2 phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 844 CONH 2 phenyl 2- (N-imidazolyl-methyl) phenyl 845 CONH 2 phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 846 CONH 2 phenyl 2- (N-pyridonyl-methyl ) phenyl 847 CONH 2 phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 848 CONH 2 phenyl 2- (amidinyl) phenyl 849 CONH 2 phenyl 2- (N-guanidinyl ) phenyl 850 CONH 2 phenyl 2- ( imidazolyl ) phenyl 851 CONH 2 phenyl 2- (imidazolidinyl) phenyl 852 CONH 2 phenyl 2- (2-imidazolidinyl- sulfonyl) henyl 853 CONH 2 phenyl 2- (2-pyrrolidinyl) phenyl 854 CONH 2 phenyl 2- (2-piperidinyl) phenyl 855 CONH 2 phenyl 2- (amidinyl-methyl) phenyl 856 CONH 2 phenyl 2- (2-imidazolidinyl- methyl) phenyl 8 85577 CCOONNHH 22 phenyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 858 CONH 2 phenyl 2-dimethylaminoimidazol-l-yl 859 CONH 2 phenyl 2- (3 -aminophenyl ) 860 CONH 2 phenyl 2- (3-pyrrolidinylcarbonyl) 861 CONH 2 phenyl 2-glycinoyl 862 CONH 2 phenyl 2- imidazol-1-ylacetyl) 863 CONH 2 2-pyridyl 2- N-pyrrolidinyl-methyl) phenyl 864 CONH 2 2-pyridyl 2- N-piperidinyl-methyl ) phenyl 865 CONH 2 2-pyridyl 2- N-morpholino-methyl) phenyl 866 CONH 2 2-pyridyl 2- N, N ' -methylmorpholinium- methyl) phenyl 867 CONH 2 2-pyridyl 2- N-pyridinium-methyl) phenyl 868 CONH 2 2-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 869 CONH 2 2-pyridyl 2- N-azatanyl-methyl) phenyl 870 CONH 2 2-pyridyl 2- N-azetidinyl-methyl ) phenyl 871 CONH 2 2-pyridyl 2- N-piperazinyl-methyl) phenyl 872 CONH 2 2-pyridyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 873 CONH 2 2-pyridyl 2- N-imidazolyl-methyl) phenyl 874 CONH 2 2-pyridyl 2- N-methoxy-N-methylamino- methyl) phenyl 875 CONH 2 2-pyridyl 2- N-pyridonyl-methyl ) phenyl 876 CONH 2 2-pyridyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 877 CONH 2 2-pyridyl 2- amidinyl ) phenyl 878 CONH 2 2-pyridyl 2- N-guanidinyl ) phenyl 879 CONH 2 2-pyridyl 2- imidazolyl) phenyl 880 CONH 2 2-pyridyl 2- imidazolidinyl ) phenyl 881 CONH 2 2-pyridyl 2- 2-imidazolidiny1- sulfonyl ) phenyl 882 CONH 2 2-pyridyl 2- 2-pyrrolidinyl ) phenyl 883 CONH 2 2-pyridyl 2- 2-piperidinyl ) phenyl 884 CONH 2 2-pyridyl 2- amidinyl-methyl ) phenyl 885 CONH 2 2-pyridyl 2- 2-imidazolidinyl- methyl) phenyl 886 CONH 2 2-pyridyl 2 N- (2-aminoimidazolyl) - methyl ) phenyl 887 CONH 2 2-pyridyl 2 dimethylaminoimidazol-1-yl 888 CONH 2 2-pyridyl 2 3 -aminophenyl ) 889 CONH 2 2-pyridyl 2 3 -pyrrolidinylcarbonyl ) 890 CONH 2 2-pyridyl 2 glycinoyl 891 CONH 2 2-pyridyl 2 imidazol-1-ylacetyl) 892 CONH 2 3-pyridyl 2 N-pyrrolidinyl-methyl ) phenyl 893 CONH 2 3-pyridyl 2 N-piperidinyl-methyl ) phenyl 894 CONH 3-pyridyl 2 N-morpholino-methyl) phenyl 895 CONH 2 3-pyridyl 2 N, N ' -methylmorpholinium- methyl) phenyl 896 CONH 2 3-pyridyl 2 N-pyridinium-methyl) phenyl 897 CONH 2 3-pyridyl 2 N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 898 CONH 2 3-pyridyl 2 N-azatanyl-methyl) phenyl 899 CONH 2 3-pyridyl 2 N-azetidinyl-methyl) phenyl 900 CONH 2 3-pyridyl 2 N-piperazinyl-methyl) phenyl 901 CONH 2 3-pyridyl 2 N,N' -BOC-piperazinyl- methyl ) phenyl 902 CONH 2 3-pyridyl 2 N-imidazolyl-methyl) phenyl 903 CONH 2 3-pyridyl 2 N-methoxy-N-methylamino- methyl ) phenyl 904 CONH 2 3-pyridyl 2 N-pyridonyl-methyl ) phenyl 905 CONH 2 3-pyridyl 2 N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 906 CONH 2 3-pyridyl 2 amidinyl) phenyl 907 CONH 2 3-pyridyl 2 N-guanidinyl) phenyl 908 CONH 2 3-pyridyl 2 imidazolyl) phenyl 909 CONH 2 3-pyridyl 2 imidazolidinyl) phenyl 910 CONH 2 3-pyridyl 2 2-imidazolidiny1- sulfonyl) phenyl 911 CONH 2 3-pyridyl 2 2-pyrrolidinyl) phenyl 912 CONH 2 3-pyridyl 2 2-piperidinyl) phenyl 913 CONH 2 3-pyridyl 2 amidinyl-methyl ) phenyl 914 CONH 2 3-pyridyl 2 2-imidazolidinyl- methyl ) phenyl 915 CONH 3-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 916 CONH 2 3-pyridyl 2-dimethylaminoimidazol-1- yi 917 CONH 2 3 -pyridyl ; 3 -aminophenyl ) 918 CONH 2 3 -pyridyl ; 3-pyrrolidinylcarbonyl ) 919 CONH 2 3-pyridyl -glycinoyl 920 CONH 2 3-pyridyl - ( . ιmidazol-1-ylacetyl) 921 CONH 2 2-pyrimidyl - (N-pyrrolidinyl-methyl ) phenyl 922 CONH 2 2-pyrimidyl - (N-piperidinyl-methyl) phenyl 923 CONH 2 2-pyrimidyl - (N-morpholino-methyl) phenyl 924 CONH2 2-pyrimidyl - (N, N ' -methylmorpholinium- methyl ) phenyl 925 CONH 2 2-pyrimidyl - (N-pyridinium-methyl) phenyl 926 CONH 2 2-pyrimidyl - (N-4- (N,N ? -dimethylamino) - pyridinium-methyl ) phenyl 927 CONH 2 2-pyrimidyl - (N-azatanyl-methyl) phenyl 928 CONH 2 2-pyrimidyl - (N-azetidinyl-methyl) phenyl 929 CONH 2 2-pyrimidyl - (N-piperazinyl-methyl ) phenyl 930 CONH 2 2-pyrimidyl (N,N' -BOC-piperazinyl- methyl ) phenyl 931 CONH 2 2-pyrimidyl (N-imidazolyl-methyl) phenyl 932 CONH 2 2-pyrimidyl (N-methoxy-N-methylamino- methyl ) phenyl 933 CONH 2 2-pyrimidyl (N-pyridonyl-methyl ) phenyl 934 CONH 2 2-pyrimidyl (N- (N ' , N ' -dimethylhydrazinyl- methyl) phenyl 935 CONH 2 2-pyrimidyl (amidinyl ) phenyl 936 CONH 2 2-pyrimidyl (N-guanidinyl ) phenyl 937 CONH 2 2-pyrimidyl ( imidazolyl) phenyl 938 CONH 2 2-pyrimidyl ( imidazolidinyl) phenyl 939 CONH 2 2-pyrimidyl (2-imidazolidinyl- sulfonyl ) phenyl 940 CONH 2 2-pyrimidyl (2-pyrrolidinyl) phenyl 941 CONH 2 2-pyrimidyl (2-piperidinyl) phenyl 942 CONH 2 2-pyrimidyl (amidinyl-methyl) phenyl 943 CONH 2 2-pyrimidyl (2-imidazolidinyl- methyl ) phenyl 944 CONH 2 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 945 CONH 2 2-pyrimidyl 2-dimethylaminoimidazol-l-yl 946 CONH 2 2-pyrimidyl 2- (3-aminophenyl) 947 CONH 2 2-pyrimidyl 2- (3-pyrrolidinylcarbonyl) 948 CONH2 2-pyrimidyl 2-glycinoyl 949 CONH 2 2-pyrimidyl 2- imidazol-1-ylacetyl) 950 CONH 2 2-Cl-phenyl 2- N-pyrrolidinyl-methyl ) phenyl 951 CONH2 2-Cl-phenyl 2- N-piperidinyl-methyl) phenyl 952 CONH2 2-Cl-phenyl 2- N-morpholino-methyl) phenyl 953 CONH 2 2-Cl-phenyl 2- N,N' -methylmorpholinium- methyl) phenyl 954 CONH 2 2-Cl-phenyl 2- N-pyridinium-methyl) phenyl 955 CONH 2 2-Cl-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) henyl 956 CONH 2 2-Cl-phenyl 2 (N-azatanyl-methyl) phenyl 957 CONH 2 2-Cl-phenyl 2 (N-azetidinyl-methyl) phenyl 958 CONH 2 2-Cl-phenyl 2 (N-piperazinyl-methyl) phenyl 959 CONH 2 2-Cl-phenyl 2 (N,N' -BOC-piperazinyl- methyl ) phenyl 960 CONH 2 2-Cl-phenyl 2 (N-imidazolyl-methyl) phenyl 961 CONH 2 2-Cl-phenyl 2 (N-methoxy-N-methylamino- methyl) phenyl 962 CONH2 2-Cl-phenyl 2 (N-pyridonyl-methyl ) phenyl 963 CONH 2 2-Cl-phenyl 2 (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 964 CONH 2 2-Cl-phenyl 2 (amidinyl) phenyl 965 CONH2 2-Cl-phenyl 2 (N-guanidinyl ) phenyl 966 CONH 2 2-Cl-phenyl 2 ( imidazolyl ) phenyl 967 CONH 2 2-Cl-phenyl 2 ( imidazolidinyl ) phenyl 968 CONH 2 2-Cl-phenyl 2 (2-imidazolidinyl- sulfonyl ) phenyl 969 CONH 2 2-Cl-phenyl 2 ( 2-pyrrolidinyl ) phenyl 970 CONH 2 2-Cl-phenyl 2 (2-piperidinyl) phenyl 971 CONH 2 2-Cl-phenyl 2 (amidinyl-methyl ) phenyl 972 CONH 2 2-Cl-phenyl 2 (2-imidazolidinyl- methyl) phenyl 973 CONH 2 2-Cl-phenyl (N- (2-aminoimidazolyl) - methyl) phenyl 974 CONH2 2-Cl-phenyl 2 dimethylaminoimidazol-1-yl 975 CONH2 2-Cl-phenyl 2 (3-aminophenyl ) 976 CONH 2 2-Cl-phenyl 2 ( 3-pyrrolidinylcarbonyl) 977 CONH 2 2-Cl-phenyl 2 glycinoyl 978 CONH 2 2-Cl-phenyl 2 (imidazol-1-ylacetyl) 979 CONH 2 2-F-phenyl 2 (N-pyrrolidinyl-methyl)phenyl 980 CONH 2 2-F-phenyl 2 (N-piperidinyl-methyl) phenyl 981 CONH 2 2-F-phenyl 2 (N-morpho1ino-methyl) phenyl 982 CONH 2 2-F-phenyl 2 (N, N ' -methylmorpholinium- methyl) phenyl 983 CONH 2 2-F-phenyl 2 (N-pyridinium-methyl) phenyl 984 CONH 2 2-F-phenyl 2 (N-4- (N,N' -dimethylamino) - pyridinium-methyl) henyl 985 CONH 2 2-F-phenyl 2 (N-azatanyl-methyl) phenyl 986 CONH 2 2-F-phenyl 2 (N-azetidinyl-methyl ) phenyl 987 CONH 2 2-F-phenyl 2 (N-piperazinyl-methyl) phenyl 988 CONH 2 2-F-phenyl 2 (N,N' -BOC-piperazinyl- methyl) phenyl 989 C0NH 2 2-F-phenyl 2 (N-imidazolyl-methyl ) phenyl 990 CONH 2 2-F-phenyl 2 (N-methoxy-N-methy1amino- methyl) phenyl 991 CONH 2 2-F-phenyl 2- (N-pyridonyl-methyl ) phenyl 992 CONH2 2-F-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 993 CONH 2 2-F-phenyl 2- (amidinyl) phenyl 994 CONH 2 2-F-phenyl 2- (N-guanidinyl ) phenyl 995 CONH 2 2-F-phenyl 2- (imidazolyl ) phenyl 996 CONH 2 2-F-phenyl 2- ( imidazolidinyl) phenyl 997 CONH 2 2-F-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 998 CONH 2 2-F-phenyl 2- 2-pyrrolidinyl ) phenyl 999 CONH 2 2-F-phenyl 2- 2-piperidinyl ) phenyl 1000 CONH 2 2-F-phenyl 2- amidinyl-methyl ) phenyl 1001 CONH 2 2-F-phenyl 2- 2-imidazolidinyl- methyl) phenyl 1002 CONH 2 2-F-phenyl N- (2-aminoimidazolyl) - methyl ) phenyl 1003 CONH 2 2-F-phenyl 2- dimethylaminoimidazol-1-yl 1004 CONH 2 2-F-phenyl 2- 3-aminophenyl ) 1005 CONH 2 2-F-phenyl 2- 3 -pyrrolidinylcarbonyl) 1006 CONH 2 2-F-phenyl 2-glycinoyl 1007 CONH 2 2-F-phenyl (imidazol-1-ylacetyl) 1008 CONH 2 2, 5-diF-phenyl (N-pyrrolidinyl-methyl) phenyl 1009 CONH 2 2 5-diF-phenyl (N-piperidinyl-methyl) henyl 1010 CONH 2 2 5-diF-phenyl (N-morpholino-methyl ) phenyl 1011 CONH 2 2 5-diF-phenyl (N, N ' -methylmorpholinium- methyl) phenyl 1012 CONH 2 5-diF-phenyl (N-pyridinium-methyl ) phenyl 1013 CONH2 5-diF-phenyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1014 CONH 2 5-diF-phenyl (N-azatanyl-methyl) phenyl 1015 CONH 2 5-diF-phenyl (N-azetidinyl-methyl) phenyl 1016 CONH 2 5-diF-phenyl (N-piperazinyl-methyl) phenyl 1017 CONH 2 5-diF-phenyl (N,N' -BOC-piperazinyl- ethyl)phenyl 1018 CONH 2 5-diF-phenyl (N-imidazolyl-methyl ) phenyl 1019 CONH 2 5-diF-phenyl (N-methoxy-N-methylamino- methyl) phenyl 1020 CONH 2 5-diF-phenyl (N-pyridonyl-methyl ) phenyl 1021 CONH 2 5-diF-phenyl (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 1022 CONH2 5-diF-phenyl (amidinyl ) phenyl 1023 CONH 2 5-diF-phenyl (N-guanidinyl ) phenyl 1024 CONH 2 5-diF-phenyl (imidazolyl ) phenyl 1025 C0NH 2 5-diF-phenyl (imidazolidinyl) phenyl 1026 CONH 2 5-diF-phenyl (2-imidazolidinyl- sulfonyl ) phenyl 1027 CONH 2 5-diF-phenyl (2-pyrrolidinyl) phenyl 1028 CONH 2 5-diF-phenyl (2-piperidinyl) phenyl 1029 CONH 2 5-diF-phenyl (amidinyl-methyl) phenyl 1030 CONH 2 5-diF-phenyl (2-imidazolidinyl- methyl) phenyl 1031 CONH 2 5-diF-phenyl 2 N- (2-aminoimidazolyl) - methyl) phenyl 1032 CONH 2 5-diF- ■ phenyl 2-dimethylaminoimidazol-l-yl 1033 CONH 2 5-diF- ■ phenyl 2- (3-aminophenyl) 1034 CONH 2 5-diF- • phenyl 2- (3-pyrrolidinylcarbonyl) 1035 CONH 2 5-diF- • phenyl 2-glycinoyl 1036 CONH 2 5-diF- • phenyl 2- imidazol-1-ylacetyl ) 1037 SCH 3 phenyl 2- aminosulfonyl)phenyl 1038 SCH 3 phenyl 2- methylaminosulfonyl) phenyl 1039 SCH 3 phenyl 1-pyrrolidinocarbonyl 1040 SCH 3 phenyl 2- (methylsulfonyl) phenyl 1041 SCH 3 phenyl 4-morpholino 1042 SCH 3 phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 1043 SCH 3 phenyl 4-morpholinocarbonyl 1044 SCH 3 2-pyridyl 2- (aminosulfony1) phenyl 1045 SCH 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 1046 SCH 3 2-pyridyl 1-pyrro1idinocarbony1 1047 SCH 3 2-pyridyl 2- (methylsulfonyl) phenyl 1048 ΞCH 3 2-pyridyl 4-morpholino 1049 SCH 3 2-pyridyl 2- (1' -CF3-tetrazol-2-yl) phenyl 1050 SCH 3 2-pyridyl 4-morpholinocarbonyl 1051 SCH 3 3-pyridyl 2- (aminosulfonyl ) phenyl 1052 SCH 3 3-pyridyl 2- (methylaminosulfonyl ) phenyl 1053 SCH 3 3-pyridyl 1-pyrro1idinocarbonyl 1054 SCH 3 3-pyridyl 2- (methylsulfonyl) phenyl 1055 SCH 3 3-pyridyl 4-morpholino 1056 SCH 3 3 -pyridyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl 1057 SCH 3 3-pyridyl 4-morpholinocarbonyl 1058 SCH 3 2-pyrimidyl 2- (aminosulfonyl) phenyl 1059 SCH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 1060 SCH 3 2-pyrimidyl 1-pyrro1idinocarbonyl 1061 SCH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 1062 SCH 3 2-pyrimidyl 4-morpholino 1063 SCH 3 2-pyrimidyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 1064 SCH 3 2-pyrimidyl 4-morpholinocarbonyl 1065 SCH 3 5-pyrimidyl 2- (aminosulfonyl ) phenyl 1066 SCH 3 5-pyrimidyl 2- (methylaminosulfonyl ) phenyl 1067 SCH 3 5-pyrimidyl 1-pyrro1idinocarbony1 1068 SCH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 1069 SCH 3 5-pyrimidyl 4-morpholino 1070 SCH 3 5-pyrimidyl 2- (l'-CF3-tetrazol-2-yl)phenyl 1071 SCH 3 5-pyrimidyl 4-morpholinocarbonyl 1072 SCH 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 1073 SCH 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 1074 SCH 3 2-Cl-phenyl 1-pyrrolidinocarbonyl 1075 SCH 3 2-Cl-phenyl 2- (methylsulfonyl ) phenyl 1076 SCH 3 2-Cl-phenyl 4-morpholino 1077 SCH 3 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 1078 SCH 2-Cl-phenyl 4-morpholinocarbonyl 1079 SCH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 1080 SCH 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 1081 SCH 3 2-F-phenyl 1-pyrrolidinocarbonyl 1082 SCH 3 2-F-phenyl 2- (methylsulfonyl) phenyl 1083 SCH 3 2-F-phenyl 4-morpholino 1084 SCH 3 2-F-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl 1085 SCH 3 2-F-phenyl 4-morpholinocarbonyl 1086 SCH 3 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 1087 SCH 3 2, 5-diF-phenyl 2- (methylaminosulfonyl) henyl 1088 SCH 3 2, 5-diF-phenyl 1-pyrrolidinocarbonyl 1089 SCH 3 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 1090 SCH 3 2, 5-diF-phenyl 4-morpholino 1091 SCH 3 2, 5-diF-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl 1092 SCH 3 2, 5-diF-phenyl -morpholinocarbonyl 1093 SCH 3 phenyl - (N-pyrrolidinyl-methyl ) phenyl 1094 SCH 3 phenyl - (N-piperidinyl-methyl) phenyl 1095 SCH 3 phenyl - (N-morpholino-methyl) phenyl 1096 SCH 3 phenyl - (N, ' -methylmorpholinium- methyl) phenyl 1097 SCH 3 phenyl - (N-pyridinium-methyl) phenyl 1098 SCH 3 phenyl - (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1099 SCH 3 phenyl - (N-azatanyl-methyl) phenyl 1100 SCH 3 phenyl - (N-azetidinyl-methyl) phenyl 1101 SCH 3 phenyl - (N-piperazinyl-methyl) phenyl 1102 SCH 3 phenyl (N,N' -BOC-piperazinyl- methyl) henyl 1103 SCH 3 phenyl (N-imidazolyl-methyl) phenyl 1104 SCH 3 phenyl (N-methoxy-N-methylamino- methyl ) phenyl 1105 SCH 3 phenyl (N-pyridonyl-methyl ) phenyl 1106 SCH 3 phenyl (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 1107 SCH 3 phenyl (amidinyl ) phenyl 1108 SCH 3 phenyl • (N-guanidinyl ) phenyl 1109 SCH 3 phenyl • ( imidazolyl ) phenyl 1110 SCH 3 phenyl ( imidazolidinyl ) phenyl 1111 SCH 3 phenyl (2-imidazolidinyl- sulfonyl ) phenyl 1112 SCH 3 phenyl (2-pyrrolidinyl) phenyl 1113 SCH 3 phenyl (2-piperidinyl ) phenyl 1114 SCH 3 phenyl (amidinyl-methyl) phenyl 1115 SCH 3 phenyl (2-imidazolidinyl- methyl ) phenyl 1116 SCH phenyl N- (2-aminoimidazolyl) - methyl ) phenyl 1117 SCH 3 phenyl 2-dimethylaminoimidazol-l-yl 1118 SCH 3 phenyl 2- ( 3 -aminophenyl ) 1119 SCH 3 phenyl 2- (3-pyrrolidinylcarbonyl) 1120 SCH 3 phenyl 2-glycinoyl 1121 SCH 3 phenyl 2- imidazol-1-ylacetyl) 1122 SCH 3 2-pyridyl 2- N-pyrrolidinyl-methyl) phenyl 1123 SCH 3 2-pyridyl 2- N-piperidinyl-methyl) phenyl 1124 SCH 3 2-pyridyl 2- N-morpholino-methyl) phenyl 1125 SCH 3 2-pyridyl 2- N,N' -methylmorpholinium- methyl) phenyl 1126 SCH 3 2-pyridyl 2- N-pyridinium-methyl) phenyl 1127 SCH 3 2-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1128 SCH 3 2-pyridyl 2- N-azatanyl-methyl) phenyl 1129 SCH 3 2-pyridyl 2- N-azetidinyl-methyl) phenyl 1130 SCH 3 2-pyridyl 2- N-piperazinyl-methyl) phenyl 1131 SCH 3 2-pyridyl 2- N,N' -BOC-piperazinyl- methyl)phenyl 1132 SCH 3 2-pyridyl 2- N-imidazolyl-methyl)phenyl 1133 SCH 3 2-pyridyl 2- N-methoxy-N-methylamino- methyl ) phenyl 1134 SCH 3 2-pyridyl 2- (N-pyridonyl-methyl) phenyl 1135 SCH 3 2-pyridyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 1136 SCH 3 2-pyridyl 2- (amidinyl) phenyl 1137 SCH 3 2-pyridyl 2- (N-guanidinyl ) phenyl 1138 SCH 3 2-pyridyl 2- ( imidazolyl) phenyl 1139 SCH 3 2-pyridyl 2- ( imidazolidiny1 ) phenyl 1140 SCH 3 2-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1141 SCH 3 2-pyridyl 2- (2-pyrrolidinyl) phenyl 1142 SCH 3 2-pyridyl 2- (2-piperidinyl) phenyl 1143 SCH 3 2-pyridyl 2- (amidinyl-methyl ) phenyl 1144 SCH 3 2-pyridyl 2- (2-imidazolidinyl- methyl ) phenyl 1145 SCH 3 2-pyridyl 2- (N- (2-aminoimidazolyl ) - methyl) phenyl 1146 SCH 3 2-pyridyl 2-dimethylaminoimidazol-1-yl 1147 SCH 3 2-pyridyl 2- (3 -aminophenyl ) 1148 SCH 3 2-pyridyl 2- (3-pyrrolidinylcarbonyl) 1149 SCH 3 2-pyridyl 2-glycinoyl 1150 SCH 3 2-pyridyl 2- (imidazol-1-ylacetyl) 1151 SCH 3 3-pyridyl 2- (N-pyrrolidinyl-methyl ) phenyl 1152 SCH 3 3-pyridyl 2- (N-piperidinyl-methyl ) phenyl 1153 SCH 3 3 -pyridyl 2- (N-morpholino-methyl) phenyl 1154 SCH 3 3-pyridyl 2- (N,N' -methylmorpholinium- methyl) phenyl 1155 SCH 3 3-pyridyl 2- (N-pyridinium-methyl) phenyl 1156 SCH 3 3-pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1157 SCH 3 3-pyridyl 2- (N-azatanyl-methyl) phenyl 1158 SCH 3 3-pyridyl 2- (N-azetidinyl-methyl) phenyl 1159 SCH 3 3-pyridyl 2- (N-piperazinyl-methyl) phenyl 1160 SCH 3 3-pyridyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 1161 SCH 3 3-pyridyl 2- (N-imidazolyl-methyl) phenyl 1162 SCH 3 3-pyridyl 2- (N-methoxy-N-methylamino- methyl) phenyl 1163 SCH 3 3-pyridyl 2- (N-pyridonyl-methyl ) phenyl 1164 SCH 3 3-pyridyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 1165 SCH 3 3-pyridyl 2- (amidinyl)phenyl 1166 SCH 3 3-pyridyl 2- (N-guanidinyl) phenyl 1167 SCH 3 3-pyridyl 2- ( imidazolyl) phenyl 1168 SCH 3 3-pyridyl 2- ( imidazolidinyl) phenyl 1169 SCH 3 3-pyridyl 2- (2-imidazolidinyl- sulfonyl) phenyl 1170 SCH 3 3-pyridyl 2- (2-pyrrolidinyl) phenyl 1171 SCH 3 3-pyridyl 2- (2-piperidin 1) phenyl 1172 SCH 3 3-pyridyl 2- (amidinyl-methyl) phenyl 1173 SCH 3 3-pyridyl 2- (2-imidazolidinyl- methyl) phenyl 1174 SCH 3 3-pyridyl 2- (N- (2-aminoimidazolyl ) - methyl ) phenyl 1175 SCH 3 3 -pyridyl 2-dimethylaminoimidazol-l-yl 1176 SCH 3 3 -pyridyl 2- 3 -aminophenyl ) 1177 SCH 3 3 -pyridyl 2- 3 -pyrrolidinylcarbonyl ) 1178 SCH 3 3-pyridyl 2-glycinoyl 1179 SCH 3 3-pyridyl 2- (imidazol-1-ylacetyl) 1180 SCH 3 2-pyrimidyl 2- (N-pyrrolidiny1 -methyl ) phenyl 1181 SCH 3 2-pyrimidyl 2- (N-piperidinyl-methyl) phenyl 1182 SCH 3 2-pyrimidyl 2- (N-morpholino-methyl) phenyl 1183 SCH 3 2-pyrimidyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 1184 SCH 3 2-pyrimidyl 2- (N-pyridinium-methyl) phenyl 1185 SCH 3 2-pyrimidyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1186 SCH 3 2-pyrimidyl 2- (N-azatanyl-methyl) phenyl 1187 SCH 3 2-pyrimidyl 2- (N-azetidinyl-methyl) phenyl 1188 SCH 3 2-pyrimidyl 2- (N-piperaziny1-methyl ) phenyl 1189 SCH 3 2-pyrimidyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 1190 SCH 3 2-pyrimidyl 2- (N-imidazolyl-methyl) phenyl 1191 SCH 3 2-pyrimidyl 2- (N-methoxy-N-methylamino- rnethyl ) phenyl 1192 SCH 3 2-pyrimidyl 2- (N-pyridonyl-methyl) phenyl 1193 SCH 3 2-pyrimidyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) henyl 1 1119944 S SCCHH 33 2-pyrimidyl 2- (amidinyl) phenyl 1 1119955 S SCCHH 33 2-pyrimidyl 2- (N-guanidinyl) phenyl 1 1119966 S SCCHH 33 2-pyrimidyl 2- (imidazolyl) phenyl 1 1119977 S SCCHH 33 2-pyrimidyl 2- (imidazolidinyl) phenyl 1 1119988 S SCCHH 33 2-pyrimidyl 2- (2-imidazolidinyl- sulfonyl) phenyl 1199 SCH 3 2-pyrimidyl 2- (2-pyrrolidinyl) phenyl 1200 SCH 3 2-pyrimidyl 2- (2-piperidinyl ) phenyl 1201 SCH 3 2-pyrimidyl 2- (amidinyl-methyl) phenyl 1202 SCH 3 2-pyrimidyl 2- (2-imidazolidinyl- methyl) phenyl 1 1220033 SSCCHH 33 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 1204 SCH 3 2-pyrimidyl 2-dimethylaminoimidazol-l-yl 1205 SCH 3 2-pyrimidyl 2- (3-aminophenyl ) 1206 SCH 3 2-pyrimidyl 2- (3-pyrrolidinylcarbonyl) 1207 SCH 3 2-pyrimidyl 2-glycinoyl 1208 SCH 3 2-pyrimidyl 2- imidazol-1-ylacetyl) 1209 SCH 3 2-Cl-phenyl 2- N-pyrrolidinyl-methyl)phenyl 1210 SCH 3 2-Cl-phenyl 2- N-piperidinyl-methyl) phenyl 1211 SCH 3 2-Cl-phenyl 2- N-morpholino-methyl) phenyl 1212 SCH 3 2-Cl-phenyl 2- N, N ' -methylmorpholinium- methyl) phenyl 1213 SCH 3 2-Cl-phenyl 2- N-pyridinium-methyl) phenyl 1214 SCH 3 2-Cl-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1215 SCH 3 2-Cl-phenyl 2- N-azatanyl-methyl) phenyl 1216 SCH 3 2-Cl-phenyl 2- N-azetidinyl-methyl) phenyl 1217 SCH 3 2-Cl-phenyl 2- (N-piperazinyl-methyl) phenyl 1218 SCH 3 2-Cl-phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 1219 SCH 3 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 1220 SCH 3 2-Cl-phenyl 2- (N-methoxy-N-methylamino- ethyl) phenyl 1221 SCH 3 2-Cl-phenyl 2- (N-pyridonyl-methyl) phenyl 1222 SCH 3 2-Cl-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 1223 SCH 3 2-Cl-phenyl 2- (amidinyl) phenyl 1224 SCH 3 2-Cl-phenyl 2- (N-guanidinyl ) phenyl 1225 SCH 3 2-Cl-phenyl 2- (imidazolyl)phenyl 1226 SCH 3 2-Cl-phenyl 2- ( imidazolidinyl ) phenyl 1227 SCH 3 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1228 SCH 3 2-Cl-phenyl 2- (2-pyrrolidinyl) phenyl 1229 SCH 3 2-Cl-phenyl 2- (2-piperidinyl ) phenyl 1230 SCH 3 2-Cl-phenyl 2- (amidinyl-methyl ) phenyl 1231 SCH 3 2-Cl-phenyl 2- (2-imidazolidinyl- methyl) phenyl 1232 SCH 3 2-Cl-phenyl N- (2-aminoimidazolyl) - methyl) phenyl 1233 SCH 3 2-Cl-phenyl 2-dimethylaminoimidazol-l-yl 1234 SCH 3 2-Cl-phenyl 2- (3-aminophenyl ) 1235 SCH 3 2-Cl-phenyl 2- (3-pyrrolidinylcarbonyl) 1236 SCH 3 2-Cl-phenyl 2-glycinoyl 1237 SCH 3 2-Cl-phenyl 2- imidazol-1-ylacetyl) 1238 SCH 3 2-F-phenyl 2- N-pyrrolidinyl-methyl ) phenyl 1239 SCH 3 2-F-phenyl 2- N-piperidinyl-methyl) phenyl 1240 SCH 3 2-F-phenyl 2- N-morpholino-methyl) phenyl 1241 SCH 3 2-F-phenyl 2- N,N' -methylmorpholinium- methyl) phenyl 1242 SCH 3 2-F-phenyl 2- N-pyridinium-methyl) phenyl 1243 SCH 3 2-F-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1244 SCH 3 2-F-phenyl 2- N-azatanyl-methyl ) phenyl 1245 SCK 3 2-F-phenyl 2- N-azetidinyl-methyl) phenyl 1246 SCH 3 2-F-phenyl 2- N-piperazinyl-methyl) phenyl 1247 SCH 3 2-F-phenyl 2- N, N ' -BOC-piperazinyl- methyl) phenyl 1248 SCH 3 2-F-phenyl 2- N-imidazolyl-methyl) phenyl 1249 SCH 3 2-F-phenyl 2- N-methoxy-N-methylamino- methyl) phenyl 1250 SCH 3 2-F-phenyl 2- N-pyridonyl-methyl) phenyl 1251 SCH 3 2-F-phenyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl)phenyl 1252 SCH 3 2-F-phenyl 2- amidinyl) phenyl 1253 SCH 3 2-F-phenyl 2- N-guanidinyl) phenyl 1254 SCH 3 2-F-phenyl 2- imidazolyl)phenyl 1255 SCH 2-F-phenyl 2- imidazolidinyl) phenyl 1256 SCH 3 2-F-phenyl 2- 2-imidazolidinyl- sulfonyl ) phenyl 1257 SCH 3 2-F-phenyl (2-pyrrolidinyl) phenyl 1258 SCH 3 2-F-phenyl 2- (2-piperidinyl ) phenyl 1259 SCH 3 2-F-phenyl 2- (amidinyl-methyl ) phenyl 1260 SCH 3 2-F-phenyl 2- (2-imidazolidinyl- me hyl) henyl 1261 SCH 3 2-F-phenyl 2- (N- (2-aminoimidazolyl) - methyl ) henyl 1262 SCH 3 2-F-phenyl 2-dimethylaminoimidazol-1-yl 1263 SCH 3 2-F-phenyi 2- (3-aminophenyl) 1264 SCH 3 2-F-phenyl 2- (3-pyrrolidinylcarbonyl) 1265 SCH 3 2-F-phenyl 2-glycinoyl 1266 SCH 3 2-F-phenyl 2- (imidazol-1-ylacetyl) 1267 SCH 3 2, 5-diF-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 1268 SCH 3 2, 5-diF-phenyl 2- (N-piperidinyl-methyl) phenyl 1269 SCH 3 2, 5-diF-phenyl 2- (N-morpholino-methyl) phenyl 1270 SCH 3 2, 5-diF-phenyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 1271 SCH 3 2, 5-diF-phenyl 2- (N-pyridinium-methyl) phenyl 1272 SCH 3 2, 5-diF-phenyl 2- (N-4- (N, N' -dimethylamino)- pyridinium-methyl) phenyl 1273 SCH 3 2, 5-diF-phenyl 2- (N-azatanyl-methyl) phenyl 1274 SCH 3 2, 5-diF-phenyl 2- (N-azetidinyl-methyl) phenyl 1275 SCH 3 2, 5-diF-phenyl 2- (N-piperazinyl-methyl) phenyl 1276 SCH 3 2 , 5-diF-phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 1277 SCH 3 2, 5-diF-phenyl 2- (N-imidazolyl-methyl) phenyl 1278 SCH 3 2 , 5-diF-phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 1279 SCH 3 2 , 5-diF-phenyl 2- (N-pyridonyl-methyl)phenyl 1280 SCH 3 2, 5-diF-phenyl 2- (N- (N 1 ,N' -dimethylhydrazinyl- methyl) henyl 1281 SCH 3 2, 5-diF-phenyl 2- (amidinyl) henyl 1282 SCH 3 2, 5-diF-phenyl 2- (N-guanidinyl ) phenyl 1283 SCH 3 2, 5-diF-phenyl 2- ( imidazolyl ) phenyl 1284 SCH 3 2, 5-diF-phenyl 2- (imidazolidinyl) phenyl 1285 SCH 3 2, 5-diF-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1286 SCH 3 2, 5-diF-phenyl 2- (2-pyrrolidinyl) phenyl 1287 SCH 3 2, 5-diF-phenyl 2- (2-piperidinyl ) phenyl 1288 SCH 3 2, 5-diF-phenyl 2- (amidinyl-methyl ) phenyl 1289 SCH 3 2, 5-diF-phenyl 2- (2-imidazolidinyl- methyl) phenyl 1290 SCH 3 2, 5-diF-phenyl 2- (N- (2-aminoimidazolyl) - methyl) henyl 1291 SCH 3 2, 5-diF-phenyl 2-dimethylaminoimidazol-l-yl 1292 SCH 3 2, 5-diF-phenyl 2- (3-aminophenyl) 1293 SCH 3 2, 5-diF-phenyl 2- (3-pyrrolidinylcarbonyl) 1294 SCH 3 2, 5-diF-phenyl 2-glycinoyl 1295 SCH 3 2, 5-diF-phenyl 2- (imidazol-1-ylacetyl) 1296 S0 2 CH 3 phenyl 2- (aminosulfonyl) phenyl 1297 Sθ 2 CH 3 phenyl 2- (methylaminosulfonyl) phenyl 1298 S0 2 CH 3 phenyl 1-pyrro1idinocarbonyl 1299 S0 2 CH 3 phenyl 2- (methylsulfonyl) henyl 1300 S0 2 CH 3 phenyl 4-morpholino 1301 S0 2 CH 3 phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 1302 S0 2 CH 3 phenyl 4-morpholinocarbonyl 1303 S0CH 3 2-pyridyl 2- (aminosulfonyl ) phenyl 1304 S0 2 CH 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 1305 S0 2 CH 3 2-pyridyl 1-pyrrolidinocarbonyl 1306 S0 2 CH 3 2-pyridyl 2- (methylsulfonyl) phenyl 1307 S0CH 3 2-pyridyl 4-morpholino 1308 S0 2 CH 3 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 1309 S0 2 CH 3 2-pyridyl 4-morpholinocarbonyl 1310 S0 2 CH 3 3-pyridyl 2- (aminosulfonyl) phenyl 1311 S0 2 CH 3 3-pyridyl 2- (methylaminosulfonyl) phenyl 1312 S0 2 CH 3 3-pyridyl 1-pyrro1idinocarbonyl 1313 S0 2 CH 3 3-pyridyl 2- (methylsulfonyl) phenyl 1314 S0 2 CH 3 3-pyridyl 4-morpholino 1315 S0 2 CH 3 3-pyridyl 2-(l'-CF3-tetrazol-2-yl)phenyl 1316 S0 2 CH 3 3-pyridyl 4-morpholinocarbonyl 1317 S0 2 CH 3 2-pyrimidyl 2- (aminosulfonyl) henyl 1318 S0 2 CH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 1319 S0 2 CH 3 2-pyrimidyl 1-pyrro1idinocarbonyl 1320 S0 2 CH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 1321 S0 2 CH 3 2-pyrimidyl 4-morpholino 1322 S0CH 3 2-pyrimidyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 1323 S0 2 CH 3 2-pyrimidyl 4-morpholinocarbonyl 1324 S0 2 CH 3 5-pyrimidyl 2- (aminosulfonyl ) phenyl 1325 S0 2 CH 3 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 1326 S0 2 CH 3 5-pyrimidyl 1-pyrro1idinocarbonyl 1327 S0 2 CH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 1328 S0 2 CH 3 5-pyrimidyl 4-morpholino 1329 S0 2 CH 3 5-pyrimidyl 2- (1 ' -CF3-tetrazol-2-yl)phenyl 1330 S0 2 CH 3 5-pyrimidyl 4-morpho1inocarbony1 1331 S0 2 CH 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 1332 S0 2 CH 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 1333 S0 2 CH 3 2-Cl-phenyl 1-pyrro1idinocarbonyl 1334 S0 2 CH 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 1335 S0 2 CH 3 2-Cl-phenyl 4-morpho1ino 1336 S0 2 CH 3 2-Cl-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 1337 S0 2 CH 3 2-Cl-phenyl 4-morpholinocarbonyl 1338 S0 2 CH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 1339 S0 2 CH 3 2-F-phenyl 2- (methylaminosulfonyl ) phenyl 1340 S0 2 CH 3 2-F-phenyl 1-pyrrolidinocarbonyl 1341 S0 2 CH 3 2-F-phenyl 2- (methylsulfonyl) phenyl 1342 S0 2 CH 3 2-F-phenyl 4-morpholino 1343 Sθ 2 CH 3 2-F-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 1344 S0 2 CH 3 2-F-phenyl 4-morpholinocarbonyl 1345 S0 2 CH 3 2,5-diF-phenyl 2- ( minosulfonyl)phenyl 1346 S0 2 CH 3 2, 5-diF-phenyl 2- (methylaminosulfonyl) phenyl 1347 S0 2 CH 3 2, 5-diF-phenyl 1-pyrrolidinocarbonyl 1348 S0 2 CH 3 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 1349 S0 2 CH 3 2,5-diF-phenyl 4-morpholino 1350 S0 2 CH 3 2, 5-diF-phenyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl 1351 S0 2 CH 3 2,5-diF-phenyl 4-morpholinocarbonyl 1352 S0 2 CH 3 phenyl 2- (N-pyrrolidinyl-methyl) phenyl 1353 S0 2 CH 3 phenyl 2- (N-piperidinyl-methyl) phenyl 1354 S0 2 CH 3 phenyl 2- (N-morpholino-methyl) phenyl 1355 S0 2 CH 3 phenyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 1356 S0 CH 3 phenyl 2- (N-pyridinium-methyl ) phenyl 1357 S0 2 CH 3 phenyl 2- (N-4- (N,N T -dimethylamino) - pyridinium-methyl) henyl i358 S0 2 CH 3 phenyl 2- (N-azatanyl-methyl) phenyl 1359 S0 CH 3 phenyl 2- (N-azetidinyl-methyl) phenyl 1360 S0 2 CH 3 phenyl 2- ( -piperazinyl-methyl ) phenyl 1361 S0 2 CH 3 phenyl 2- (N,N' -BOC-piperazinyl- methyl ) phenyl 1362 S0 2 CH 3 phenyl 2- (N-imidazolyl-methyl) phenyl 1363 S0 2 CH 3 phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 1364 S0 2 CH 3 phenyl 2- (N-pyridonyl-methyl )phenyl 1365 S0 2 CH 3 phenyl 2- (N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 1366 S0 2 CH 3 phenyl 2- (amidinyl ) phenyl 1367 S0 2 CH 3 phenyl 2- (N-guanidinyl ) phenyl 1368 S0 2 CH 3 phenyl 2- ( imidazolyl ) phenyl 1369 S0 2 CH 3 phenyl 2- ( imidazolidinyl ) phenyl 1370 S0 2 CH 3 phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1371 S0 2 CH 3 phenyl 2- (2-pyrrolidinyl) phenyl 1372 S0 2 CH 3 phenyl 2- (2-piperidinyl) phenyl 1373 S0 2 CH 3 phenyl 2- (amidinyl-methyl ) phenyl 1374 S0 2 CH 3 phenyl 2- (2-imidazolidinyl- methyl ) phenyl 1375 S0 2 CH 3 phenyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 1376 S0 2 CH 3 phenyl 2-dimethylaminoimidazol-l-yl 1377 S0 2 CH 3 phenyl 2- ( 3 -aminophenyl) 1378 S0 CH 3 phenyl 2- ( 3 -pyrrolidinylcarbonyl) 1379 S0 2 CH 3 phenyl 2-glycinoyl 1380 S0 2 CH 3 phenyl 2- (imidazol-1-ylacetyl) 1381 S0 2 CH 3 2-pyridyl 2- (N-pyrrolidinyl-methyl) phenyl 1382 S0 2 CH 3 2-pyridyl 2- (N-piperidinyl-methyl) phenyl 1383 S0 2 CH 3 2-pyridyl 2- (N-morpholino-methyl ) phenyl 1384 S0 2 CH 3 2-pyridyl 2- (N,N' -methylmorpholinium- methyl) phenyl 1385 S0 2 CH 3 2-pyridyl 2- (N-pyridinium-methyl ) phenyl 1386 S0CH 3 2-pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1387 S0 2 CH 3 2-pyridyl 2- (N-azatanyl-methyl) phenyl 1388 S0 2 CH 3 2-pyridyl 2- (N-azetidinyl-methyl) phenyl 1389 S0 2 CH 3 2-pyridyl 2- (N-piperazinyl-methyl) phenyl 1390 S0 2 CH 3 2-pyridyl 2- (N,N' -BOC-piperazinyl- methyl)phenyl 1391 S0 2 CH 3 2-pyridyl 2- (N-imidazolyl-methyl) phenyl 1392 S0 2 CH 3 2-pyridyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 1393 S0 2 CH 3 2-pyridyl 2- (N-pyridonyl-methyl ) phenyl 1394 S0 2 CH 3 2-pyridyl 2- (N- ( ' , N ' -dimethylhydrazinyl- methyl ) phenyl 1395 S0 2 CH 3 2-pyridyl 2- (amidinyl ) phenyl 1396 S0 2 CH 3 2-pyridyl 2- (N-guanidinyl) phenyl 1397 S0 2 CH 3 2-pyridyl 2- ( imidazolyl ) phenyl 1398 S0 2 CH 3 2-pyridyl 2- (imidazolidinyl) phenyl 1399 S0 2 CH 3 2-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1400 S0 2 CH 3 2-pyridyl 2- (2-pyrrolidinyl) henyl 1401 S0 2 CH 3 2-pyridyl 2- (2-piperidinyl) phenyl 1402 S0 2 CH 3 2-pyridyl 2- (amidinyl-methyl ) phenyl 1403 S0 2 CH 3 2-pyridyl 2- (2-imidazolidinyl- methyl ) phenyl 1404 S0 2 CH 3 2-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 1405 S0 2 CH 3 2-pyridyl 2-dimethylaminoimidazol-l-yl 1406 S0 2 CH 3 2-pyridyl 2- (3 -aminophenyl ) 1407 S0 2 CH 3 2-pyridyl 2- (3-pyrrolidinylcarbonyl) 1408 S0 2 CH 3 2-pyridyl 2-glycinoyl 1409 S0 2 CH 3 2-pyridyl 2- ( imidazol-1-ylacetyl ) 1410 S0 2 CH 3 3-pyridyl 2- (N-pyrrolidinyl-methyl) phenyl 1411 S0 2 CH 3 3-pyridyl 2- (N-piperidinyl-methyl) phenyl 1412 S0CH 3 3 -pyridyl 2- (N-morpholino-methyl) phenyl 1413 S0 2 CH 3 3-pyridyl 2- (N,N' -methylmorpholinium- methyl ) phenyl 1414 S0 2 CH 3 3-pyridyl 2- (N-pyridinium-methyl) phenyl 1415 S0 2 CH 3 3-pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1416 S0 2 CH 3 3-pyridyl 2- (N-azatanyl-methyl) phenyl 1417 S0 2 CH 3 3-pyridyl 2- (N-azetidinyl-methyl) phenyl 1418 S0 2 CH 3 3-pyridyl 2- (N-piperazinyl-methyl) phenyl 1419 S0 2 CH 3 3-pyridyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 1420 S0 2 CH 3 3-pyridyl 2- (N-imidazolyl-methyl) phenyl 1421 S0 2 CH 3 3-pyridyl 2- (N-methoxy-N-methylamino- me hyl) phenyl 1422 S0 2 CH 3 3-pyridyl 2- (N-pyridonyl-methyl ) phenyl 1423 S0 2 CH 3 3-pyridyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl)phenyl 1424 S0CH 3 3-pyridyl 2- (amidinyl) phenyl 1425 S0 2 CH 3 3-pyridyl 2- (N-guanidinyl) phenyl 1426 S0 2 CH 3 3-pyridyl 2- (imidazolyl) phenyl 1427 S0 2 CH 3 3-pyridyl 2- (imidazolidinyl)phenyl 1428 S0 2 CH 3 3-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1429 S0 2 CH 3 3-pyridyl 2- (2-pyrrolidinyl) phenyl 1430 S0 2 CH 3 3-pyridyl 2- (2-piperidinyl)phenyl 1431 S0 2 CH 3 3-pyridyl 2- (amidinyl-methyl ) phenyl 1432 S0 2 CH 3 3-pyridyl 2- (2-imidazolidinyl- methyl) phenyl 1433 S0CH 3 3-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 1434 S0 2 CH 3 3-pyridyl 2-dimethylaminoimidazol-1-yl 1435 S0 2 CH 3 3-pyridyl 2-(3 -aminophenyl ) 1436 S0 2 CH 3 3-pyridyl 2-( 3 -pyrrolidinylcarbonyl ) 1437 S0 2 CH 3 3-pyridyl 2-gglycinoyl 1438 S0 2 CH 3 3-pyridyl 2-( imidazol-1-ylacetyl) 1439 S0CH 3 2-pyrimidyl 2-0N-pyrrolidinyl-methyl ) phenyl 1440 S0 2 CH 3 2-pyrimidyl 2-0N-piperidinyl-methyl ) phenyl 1441 S0 2 CH 3 2-pyrimidyl 2-0N-mcrpholino-methyl ) phenyl 1442 S0 2 CH 3 2-pyrimidyl 2-0N,N' -methylmorpholinium- methyl ) phenyl 1443 S0 2 CH 3 2-pyrimidyl 2-0N-pyridinium-methyl ) phenyl 1444 S0 2 CH 3 2-pyrimidyl 2-0N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1445 S0 2 CH 3 2-pyrimidyl 2-(lN-azatanyl-methyl) phenyl 1446 S0 2 CH 3 2-pyrimidyl 2-(N-azetidinyl-methyl) phenyl 1447 S0 2 CH 3 2-pyrimidyl 2-(N-piperazinyl-methyl ) phenyl 1448 S0CH 3 2-pyrimidyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 1449 S0 2 CH 3 2-pyrimidyl 2-(N-imidazolyl-methyl ) phenyl 1450 S0CH 3 2-pyrimidyl 2-(N-methoxy-N-methylamino- methyl ) phenyl 1451 S0 2 CH 3 2-pyrimidyl 2-(N-pyridonyl-methyl ) phenyl 1452 S0 2 CH 3 2-pyrimidyl 2-(N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 1453 S0 2 CH 3 2-pyrimidyl 2-(amidinyl ) phenyl 1454 S0 2 CH 3 2-pyrimidyl 2- (N-guanidinyl ) phenyl 1455 S0 2 CH 3 2-pyrimidyl 2-( imidazolyl ) phenyl 1456 S0 2 CH 3 2-pyrimidyl 2-( imidazolidinyl ) phenyl 1457 S0 2 CH 3 2-pyrimidyl 2-(2 -imidazolidinyl- sulfonyl ) phenyl 1458 S0 2 CH 3 2-pyrimidyl 2-(2-pyrrolidinyl ) phenyl 1459 S0 2 CH 3 2-pyrimidyl 2-(2-piperidinyl ) phenyl 1460 S0 2 CH 3 2-pyrimidyl 2-(amidinyl-methyl ) phenyl 1461 S0CH 3 2-pyrimidyl 2-(2-imidazolidinyl- methyl ) phenyl 1462 S0 2 CH 3 2-pyrimidyl 2-(N- (2-aminoimidazolyl) - methyl ) phenyl 1463 S0 2 CH 3 2-pyrimidyl 2-ddimethylaminoimidazol-1-yl 1464 S0 2 CH 3 2-pyrimidyl 2 - ( 3 -aminophenyl ) 1465 S0 2 CH 3 2-pyrimidyl 2-(3 -pyrrolidinylcarbonyl) 1466 S0CH 3 2-pyrimidyl 2-gglycinoyl 1467 S0 2 CH 3 2-pyrimidyl 2-( imidazol-1-ylacetyl) 1468 S0 2 CH 3 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl ) phenyl 1469 S0 2 CH 3 2-Cl-phenyl 2-(N-piperidinyl-methyl ) phenyl 1470 S0CH 3 2-Cl-phenyl 2-(N-morpholino-methyl ) phenyl 1471 S0 2 CH 3 2-Cl-phenyl 2-(N, N ' -methylmorpholinium- methyl ) phenyl 1472 S0 2 CH 3 2-Cl-phenyl 2-(N-pyridinium-methyl ) phenyl 1473 S0 2 CH 3 2-Cl-phenyl 2-(N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1474 S0 2 CH 3 2-Cl-phenyl 2-(N-azatanyl-methyl ) phenyl 1475 S0 2 CH 3 2-Cl-phenyl 2-(N-azetidinyl-methyl ) phenyl 1476 S0 2 CH 3 2-Cl-phenyl 2-(N-piperazinyl-methyl ) phenyl 1477 S0 2 CH 3 2-Cl-phenyl 2-(N,N' -BOC-piperazinyl- methyl ) henyl 1478 S0 2 CH 3 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 1479 S0 CH 3 2-Cl-phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 1480 S0 2 CH 3 2-Cl-phenyl 2- (N-pyridonyl-methyl ) phenyl 1481 S0 2 CH 3 2-Cl-phenyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl ) phenyl 1482 S0 2 CH 3 2-Cl-phenyl 2- (amidinyl ) phenyl 1483 S0 2 CH 3 2-Cl-phenyl 2- (N-guanidinyl ) phenyl 1484 S0 2 CH 3 2-Cl-phenyl 2- (imidazolyl) henyl 1485 Sθ 2 CH 3 2-Cl-phenyl 2- (imidazolidinyl) phenyl 1486 S0 2 CH 3 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1487 S0 2 CH 3 2-Cl-phenyl 2- (2-pyrrolidinyl) phenyl 1488 S0 2 CH 3 2-Cl-phenyl 2- ( 2-piperidinyl) phenyl 1489 S0 2 CH 3 2-Cl-phenyl 2- (amidinyl-methyl) phenyl 1490 S0 2 CH 3 2-Cl-phenyl 2- (2-imidazolidinyl- methyl) phenyl 1491 S0 2 CH 3 2-Cl-phenyl N- (2-aminoimidazolyl) - methyl ) phenyl 1492 S0 2 CH 3 2-Cl-phenyl 2-dimethylaminoimidazol-l-yl 1493 S0 2 CH 3 2-Cl-phenyl 2- (3 -aminophenyl ) 1494 S0 2 CH 3 2-Cl-phenyl 2- (3 -pyrrolidinylcarbonyl) 1495 S0 2 CH 3 2-Cl-phenyl 2-glycinoyl 1496 S0 2 CH 3 2-Cl-phenyl 2- imidazol-1-ylacetyl ) 1497 S0CH 3 2-F-phenyl 2- N-pyrrolidinyl-methyl ) phenyl 1498 Sθ 2 CH 3 2-F-phenyl 2- N-piperidinyl-methyl) henyl 1499 S0 2 CH 3 2-F-phenyl 2- N-morpholino-methyl) phenyl 1500 S0 2 CH 3 2-F-phenyl 2- N, N ' -methylmorpholinium- methyl) phenyl 1501 S0 2 CH 3 2-F-phenyl 2- N-pyridinium-methyl ) phenyl 1502 S0 2 CH 3 2-F-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1503 S0 2 CH 3 2-F-phenyl 2- N-azatanyl-methyl) phenyl 1504 S0 2 CH 3 2-F-phenyl 2- N-azetidinyl-methyl) phenyl 1505 S0 2 CH 3 2-F-phenyl 2- N-piperazinyl-methyl ) phenyl 1506 S0 2 CH 3 2-F-phenyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 1507 S0 2 CH 3 2-F-phenyl 2- N-imidazolyl-methyl) phenyl 1508 S0 2 CH 3 2-F-phenyl 2- N-methoxy-N-methylamino- methyl) phenyl 1509 S0 2 CH 3 2-F-phenyl 2- N-pyridonyl-methyl ) phenyl 1510 S0 2 CH 3 2-F-phenyl 2- N- (N' , N ' -dimethylhydrazinyl- methyl) phenyl 1511 S0 2 CH 3 2-F-phenyl 2- amidinyl) phenyl 1512 S0 2 CH 3 2-F-phenyl 2- N-guanidinyl ) phenyl 1513 Sθ2CH 3 2-F-phenyl 2- imidazolyl)phenyl 1514 Sθ2CH 3 2-F-phenyl 2- imidazolidinyl) phenyl 1515 S0 2 CH 3 2-F-phenyl 2- 2-imidazolidinyl- sulfonyl ) phenyl 1516 S02CH 3 2-F-phenyl 2- 2-pyrrolidinyl) phenyl 1517 Sθ2CH 3 2-F-phenyl 2- 2-piperidinyl ) phenyl 1518 S0 2 CH 3 2-F-phenyl 2- amidinyl-methyl ) phenyl 1519 S0 2 CH 3 2-F-phenyl - (2-imidazolidinyl- methyl ) phenyl 1520 S0 2 CH 3 2-F-phenyl - (N- (2-aminoimidazolyl) - methyl ) phenyl 1521 S0 2 CH 3 2-F-phenyl -dimethylaminoimidazol-1-yl 1522 S0 2 CH 3 2-F-phenyl - ( 3 -aminophenyl ) 1523 S0 2 CH 3 2-F-phenyl - ( 3 -pyrrolidinylcarbonyl ) 1524 S0 2 CH 3 2-F-phenyl -glycinoyl 1525 S0 2 CH 3 2-F-phenyl ( imidazol-1-ylacetyl) 1526 S0 2 CH 3 2, 5-diF-phenyl (N-pyrrolidinyl-methyl ) phenyl 1527 S0 2 CH 3 5-diF-phenyl (N-piperidinyl-methyl) phenyl 1528 S0 2 CH 3 5-diF-phenyl (N-morpholino-methyl) phenyl 1529 S0 2 CH 3 5-diF-phenyl (N, N ' -methylmorpholinium- methyl ) phenyl 1530 S0 2 CH 3 5-diF-phenyl (N-pyridinium-methyl) phenyl 1531 S0 2 CH 3 5-diF-phenyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1532 S0 2 CH 3 5-diF-phenyl (N-azatanyl-methyl) phenyl 1533 S0 2 CH 3 5-diF-phenyl (N-azetidinyl-methyl) phenyl 1534 Sθ 2 CH 3 5-diF-phenyl (N-piperazinyl-methyl) phenyl 1535 S0 2 CH 3 5-diF-phenyl (N,N' -BOC-piperazinyl- methyl ) phenyl 1536 S0 2 CH 3 5-diF-phenyl (N-imidazolyl-methyl ) phenyl 1537 S0 2 CH 3 5-diF-phenyl (N-methoxy-N-methylamino- methyl ) phenyl 1538 S0CH 3 5-diF-phenyl (N-pyridonyl-methyl ) phenyl 1539 S0 2 CH 3 5-diF-phenyl (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 1540 S0 2 CH 3 5-diF-phenyl (amidinyl ) phenyl 1541 S0 2 CH 3 5-diF-phenyl (N-guanidinyl) phenyl 1542 S0 2 CH 3 5-diF-phenyl ( imidazolyl ) phenyl 1543 S0 2 CH 3 5-diF-phenyl ( imidazolidinyl) phenyl 1544 S0 2 CH 3 5-diF-phenyl (2-imidazolidinyl- sulfonyl ) phenyl 1545 S0 2 CH 3 5-diF-phenyl (2-pyrrolidinyl) phenyl 1546 S0 2 CH 3 5-diF-phenyl (2-piperidinyl) phenyl 1547 S0 2 CH 3 5-diF-phenyl (amidinyl-methyl ) phenyl 1548 S0 2 CH 3 5-diF-phenyl (2-imidazolidinyl- methyl) phenyl 1549 S0 2 CH 3 5-diF-phenyl 2- N- (2-aminoimidazolyl) - methyl) phenyl 1550 S0 2 CH 3 5-diF-phenyl 2-dimethylaminoimidazol-1-yl 1551 S0 2 CH 3 5-diF--phenyl 2- (3-aminophenyl ) 1552 S0 2 CH 3 5-diF- • phenyl 2- ( 3 -pyrrolidinylcarbonyl ) 1553 S0 2 CH 3 5-diF--phenyl 2-glycinoyl 1554 S0 2 CH 3 5-diF- • phenyl 2- imidazol-1-ylacetyl) 1555 NHS0 2 CH 3 phenyl 2- aminosulfonyl) phenyl 1556 NHS0 2 CH 3 phenyl 2- methylaminosulfonyl) phenyl 1557 NHS0 2 CH 3 phenyl -pyrrolidinocarbonyl 1558 NHS0 2 CH 3 phenyl 2- methylsulfonyl) phenyl 1559 NHS0 2 CH 3 phenyl 4-morpholino 1560 NHS0 2 CH 3 phenyl 2- 1 ' -CF3 -tetrazol-2 -yD phenyl 1561 NHS0CH 3 phenyl 4-morpholinocarbonyl 1562 NHS0 2 CH 3 2-pyridyl 2- (aminosulfonyl) phenyl 1563 NHS0 2 CH 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 1564 NHS0 2 CH 3 2-pyridyl 1-pyrro1idinocarbonyl 1565 NHS0 2 CH 3 2-pyridyl 2- (methylsulfonyl) phenyl 1566 NHS0 2 CH 3 2-pyridyl 4-morpholino 1567 NHS0 2 CH 3 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 1568 NHS0 2 CH 3 2-pyridyl 4-morpholinocarbonyl 1569 NHS0 2 CH 3 3-pyridyl 2- (aminosulfonyl ) phenyl 1570 NHS0 2 CH 3 3-pyridyl 2- (methylaminosulfonyl) phenyl 1571 NHS0 2 CH 3 3-pyridyl 1-pyrrolidinocarbonyl 1572 NHS0 2 CH 3 3 -pyridyl 2- (methylsulfonyl) phenyl 1573 NHS0 2 CH 3 3-pyridyl 4-morpholino 1574 NHS0 2 CH 3 3 -pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 1575 NHS0 2 CH 3 3-pyridyl 4-morpholinocarbonyl 1576 NHS0 2 CH 3 2-pyrimidyl 2- (aminosulfonyl) phenyl 1577 NHS0CH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 1578 NHS0 2 CH 3 2-pyrimidyl 1-pyrrolidinocarbonyl 1579 NHS0 2 CH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 1580 NHS0 2 CH 3 2-pyrimidyl 4-morpholino 1581 NHS0 2 CH 3 2-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 1582 NHS0 2 CH 3 2-pyrimidyl 4-morpholinocarbonyl 1583 NHS0 2 CH 3 5-pyrimidyl 2- (aminosulfonyl) phenyl 1584 NHS0 2 CH 3 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 1585 NHS0 2 CH 3 5-pyrimidyl 1-pyrrolidinocarbonyl 1586 NHS0 2 CH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 1587 NHS0 2 CH 3 5-pyrimidyl 4-morpholino 1588 NHS0 2 CH 3 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 1589 NHS0CH 3 5-pyrimidyl 4-morpholinocarbonyl 1590 NHS0 2 CH 3 2-Cl-phenyl 2- (aminosulfonyl ) phenyl 1591 NHS0 2 CH 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 1592 NHS0 2 CH 3 2-Cl-phenyl 1-pyrro1idinocarbonyl 1593 NHS0 2 CH 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 1594 NHS0 2 CH 3 2-Cl-phenyl 4-morpholino 1595 NHS0 2 CH 3 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 1596 NHS0 2 CH 3 2-Cl-phenyl 4-morpholinocarbonyl 1597 NHS0 2 CH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 1598 NHS0 2 CH 3 2-F-phenyl 2- (methylaminosulfonyl) henyl 1599 NHS0 2 CH 3 2-F-phenyl 1-pyrrolidinocarbonyl 1600 NHS0 2 CH 3 2-F-phenyl 2- (me hylsulfonyl) phenyl 1601 NHS0 2 CH 3 2-F-phenyl 4-morpholino 1602 NHS0 2 CH 3 2-F-phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 1603 NHS0 2 CH 3 2-F-phenyl 4-morpholinocarbonyl 1604 NHS0 2 CH 3 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 1605 NHS0 2 CH 3 2,5-diF-phenyl 2- (methylaminosulfonyl) phenyl 1606 NHS0 2 CH 3 2,5-diF-phenyl 1-pyrro1idinocarbony1 1607 NHS0 2 CH 3 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 1608 NHS0 2 CH 3 2, 5-diF-phenyl 4-morpholino 1609 NHS0 2 CH 3 2,5-diF-phenyl 2-(l'-CF3-tetrazol-2-yl)phenyl 1610 NHS0 2 CH 3 2, 5-diF-phenyl 4-morpholinocarbonyl 1611 NHS0 2 CH 3 phenyl 2- (N-pyrrolidinyl-methyl) phenyl 1612 NHS0 2 CH 3 phenyl 2- (N-piperidinyl-methyl ) phenyl 1613 NHS0 2 CH 3 phenyl 2- (N-morpholino-methyl) phenyl 1614 NHS0 2 CH 3 phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl 1615 NHS0 2 CH 3 phenyl 2- (N-pyridinium-methyl ) phenyl 1616 NHS0 2 CH 3 phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1617 NHS0 2 CH 3 phenyl 2- (N-azatanyl-methyl) phenyl 1618 NHS0 2 CH 3 phenyl 2- (N-azetidinyl-methyl) phenyl 1619 NHS0 2 CH 3 phenyl 2- (N-piperazinyl-methyl) pnenyl 1620 NHS0 2 CH 3 phenyl 2-(N,N' -BOC-piperazinyl- methyl ) phenyl 1621 NHS0 2 CH 3 phenyl 2- (N-imidazolyl-methyl) phenyl 1622 NHS0CH 3 phenyl 2- (N-methoxy-N-methylamino- methyl) phenyl 1623 NHS0 2 CH 3 phenyl 2- (N-pyridonyl-methyl ) phenyl 1624 NHS0 2 CH 3 phenyl 2-(N-(N' ^'-dimethylhydrazinyl- methyl) phenyl 1625 NHS0 2 CH 3 phenyl 2- (amidinyl ) phenyl 1626 NHS0 2 CH 3 phenyl 2- (N-guanidinyl) phenyl 1627 NHS0 2 CH 3 phenyl 2- ( imidazolyl ) phenyl 1628 NHS0 2 CH 3 phenyl 2- ( imidazolidinyl ) phenyl 1629 NHS0 2 CH 3 phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1630 NHS0 2 CH 3 phenyl 2- (2-pyrrolidinyl) phenyl 1631 NHS0 2 CH 3 phenyl 2- (2-piperidinyl ) phenyl 1632 NHS0 2 CH 3 phenyl 2- (amidinyl-methy ) phenyl 1633 NHS0 2 CH 3 phenyl 2- (2-imidazolidinyl- methyl) phenyl 1634 NHS0 2 CH 3 phenyl N- (2-aminoimidazolyl) - methyl ) phenyl 1635 NHS0 2 CH 3 phenyl 2-dimethylaminoimidazol-1-yl 1636 NHS0 2 CH 3 phenyl 2- (3 -aminophenyl ) 1637 NHS0 2 CH 3 phenyl 2- ( 3-pyrrolidinylcarbonyl ) 1638 NHS0 2 CH 3 phenyl 2-glycinoyl 1639 NHS0 2 CH 3 phenyl 2- imidazol-1-ylacetyl) 1640 NHS0 2 CH 3 2-pyridyl 2- N-pyrrolidinyl-methyl) phenyl 1641 NHS0 2 CH 3 2-pyridyl 2- N-piperidinyl-methyl) phenyl 1642 NHS0 2 CH 3 2-pyridyl 2- N-morpholino-methyl ) phenyl 1643 NHS0 2 CH 3 2-pyridyl 2- N,N' -methylmorpholinium- methyl) phenyl 1644 NHS0 2 CH 3 2-pyridyl 2- N-pyridinium-methyl) phenyl 1645 NHS0 2 CH 3 2-pyridyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1646 NHS0 2 CH 3 2-pyridyl 2- N-azatanyl-methyl ) phenyl 1647 NHS0CH 3 2-pyridyl 2- N-azetidinyl-methyl) phenyl 1648 NHS0 2 CH 3 2-pyridyl 2- N-piperazinyl-methyl) phenyl 1649 NHS0 2 CH 3 2-pyridyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 1650 NHS0 2 CH 3 2-pyridyl 2- N-imidazolyl-methyl) phenyl 1651 NHSO 2 CH 3 2-pyridyl 2- N-methoxy-N-methylamino- methyl) phenyl 1652 NHS0 2 CH 3 2-pyridyl 2- N-pyridonyl-methyl ) phenyl 1653 NHS0 2 CH 3 2-pyridyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl) phenyl 1654 NHS0CH 3 2-pyridyl 2- (amidinyl) phenyl 1655 NHS0CH 3 2-pyridyl 2- (N-guanidinyl) phenyl 1656 NHS0 2 CH 3 2-pyridyl 2- ( imidazolyl ) phenyl 1657 NHS0 2 CH 3 2-pyridyl 2- (imidazolidinyl) phenyl 1658 NHS0 2 CH 3 2-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1659 NHS0 2 CH 3 2-pyridyl 2- (2-pyrrolidinyl) phenyl 1660 NHS0 2 CH 3 2-pyridyl 2- (2-piperidinyl ) phenyl 1661 NHS0 2 CH 3 2-pyridyl 2- (amidinyl-methyl) phenyl 1662 NHS0 2 CH 3 2-pyridyl 2- (2-imidazolidinyl- methyl ) phenyl 1663 NHS0 2 CH 3 2-pyridyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 1664 NHS0 2 CH 3 2-pyridyl 2-dimethylaminoimidazol-l-yl 1665 NHS0 2 CH 3 2-pyridyl 2- (3 -aminophenyl ) 1666 NHS0 2 CH 3 2-pyridyl 2- (3-pyrrolidinylcarbonyl) 1667 NHS0 2 CH 3 2-pyridyl 2-glycinoyl 1668 NHS0 2 CH 3 2-pyridyl 2- (imidazol-1-ylacetyl) 1669 NHS0 CH 3 3 -pyridyl 2- (N-pyrrolidinyl-methyl) phenyl 1670 NHS0 2 CH 3 3 -pyridyl 2- (N-piperidinyl-methyl) phenyl 1671 NHS0 2 CH 3 3-pyridyl 2- (N-morpholino-methyl) phenyl 1672 NHS0 2 CH 3 3-pyridyl 2- (N,N' -methylmorpholinium- methyl) phenyl 1673 NHS0 2 CH 3 3-pyridyl 2- (N-pyridinium-methyl) phenyl 1674 NHS0 2 CH 3 3 -pyridyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl ) phenyl 1675 NHS0 2 CH 3 3-pyridyl 2- (N-azatanyl-methyl) phenyl 1676 NHS0 2 CH 3 3-pyridyl 2- (N-azetidinyl-methyl) phenyl 1677 NHS0 2 CH 3 3-pyridyl 2- (N-piperazinyl-methyl) phenyl 1678 NHS0CH 3 3-pyridyl 2- (N,N' -BOC-piperazinyl- methyl) phenyl 1679 NHS0 2 CH 3 3-pyridyl 2- (N-imidazolyl-methyl) phenyl 1680 NHS0 2 CH 3 3-pyridyl 2- (N-methoxy-N-methylamino- methyl) phenyl 1681 NHS0 2 CH 3 3-pyridyl 2- (N-pyridonyl-methyl ) phenyl 1682 NHS0 2 CH 3 3-pyridyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl) phenyl 1683 NHS0 2 CH 3 3-pyridyl 2- (amidinyl ) phenyl 1684 NHS0 2 CH 3 3-pyridyl 2- (N-guanidinyl ) phenyl 1685 NHS0 2 CH 3 3-pyridyl 2- (imidazolyl) phenyl 1686 NHS0 2 CH 3 3-pyridyl 2- ( imidazolidinyl) phenyl 1687 NHS0 2 CH 3 3-pyridyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1688 NHS0 2 CH 3 3-pyridyl 2- (2-pyrrolidinyl) phenyl 1689 NHS0 2 CH 3 3-pyridyl 2- (2-piperidinyl ) phenyl 1690 NHS0 2 CH 3 3-pyridyl 2- (amidinyl-methyl ) phenyl 1691 NHS0 2 CH 3 3-pyridyl 2- (2-imidazolidinyl- methyl)phenyl 1692 NHS0 2 CH 3 3-pyridyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 1693 NHS0 2 CH 3 3-pyridyl 2-dimethylaminoimidazol-l-yl 1694 NHS0 2 CH 3 3-pyridyl 2- (3-aminophenyl ) 1695 NHS0 2 CH 3 3-pyridyl 2- (3 -pyrrolidinylcarbonyl) 1696 NHS0 2 CH 3 3-pyridyl 2-glycinoyl 1697 NHS0 2 CH 3 3-pyridyl 2- (imidazol-1-ylacetyl) 1698 NHS0 2 CH 3 2-pyrimidyl 2- (N-pyrrolidinyl-methyl) phenyl 1699 NHS0 2 CH 3 2-pyrimidyl 2- (N-piperidinyl-methyl) phenyl 1700 NHS0 2 CH 3 2-pyrimidyl 2- (N-morpholino-methyl) phenyl 1701 NHS0 2 CH 3 2-pyrimidyl 2- (N,N' -methylmorpholinium- ethyl ) phenyl 1702 NHS0 2 CH 3 2-pyrimidyl 2- (N-pyridinium-methyl) phenyl 1703 NHS0 2 CH 3 2-pyrimidyl 2- (N-4- (N,N* -dimethylamino) - pyridinium-methyl) phenyl 1704 NHS0 2 CH 3 2-pyrimidyl 2- (N-azatanyl-methyl) phenyl 1705 NHS0 2 CH 3 2-pyrimidyl 2- (N-azetidinyl-methyl) phenyl 1706 NHS0 2 CH 3 2-pyrimidyl 2- (N-piperazinyl-methyl) henyl 1707 NHS0 2 CH 3 2-pyrimidyl 2- (N,N' -BOC-piperazinyl- methyl) phenyl 1708 NHS0 2 CH 3 2-pyrimidyl 2- (N-imidazolyl-methyl) phenyl 1709 NHS0 2 CH 3 2-pyrimidyl 2- (N-methoxy-N-methylamino- methyl) phenyl 1710 NHS0 2 CH 3 2-pyrimidyl 2- (N-pyridonyl-methyl ) phenyl 1711 NHS0 2 CH 3 2-pyrimidyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 1712 NHS0 2 CH 3 2-pyrimidyl 2- (amidinyl ) phenyl 1713 NHS0 2 CH 3 2-pyrimidyl 2- (N-guanidinyl ) phenyl 1714 NHS0 2 CH 3 2-pyrimidyl 2- ( imidazolyl ) phenyl 1715 NHS0 2 CH 3 2-pyrimidyl 2- (imidazolidinyl) phenyl 1716 NHS0 2 CH 3 2-pyrimidyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1717 NHS0CH 3 2-pyrimidyl 2- (2-pyrrolidinyl) phenyl 1718 NHS0 2 CH 3 2-pyrimidyl 2- ( 2-piperidinyl) phenyl 1719 NHS0 CH 3 2-pyrimidyl 2- (amidinyl-methyl ) phenyl 1720 NHS0 2 CH 3 2-pyrimidyl 2- (2-imidazolidinyl- methyl ) phenyl 1721 NHS0 CH 3 2-pyrimidyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 1722 NHS0 2 CH 3 2-pyrimidyl 2-dimethylaminoimidazol-l-yl 1723 NHS0 2 CH 3 2-pyrimidyl 2- (3 -aminophenyl ) 1724 NHS0 CH 3 2-pyrimidyl 2- (3 -pyrrolidinylcarbonyl) 1725 NHS0 2 CH 3 2-pyrimidyl 2-glycinoyl 1726 NHS0 2 CH 3 2-pyrimidyl 2- (imidazol-1-ylacetyl) 1727 NHS0 2 CH 3 2-Cl-phenyl 2- (N-pyrrolidinyl-methyl) phenyl 1728 NHS0 CH 3 2-Cl-phenyl 2- (N-piperidinyl-methyl) phenyl 1729 NHS0 2 CH 3 2-Cl-phenyl 2- (N-morpholino-methyl) phenyl 1730 NHS0 CH 3 2-Cl-phenyl 2- (N,N' -methylmorpholinium- methyl) phenyl 1731 NHS0CH 3 2-Cl-phenyl 2- (N-pyridinium-methyl) phenyl 1732 NHS0 2 CH 3 2-Cl-phenyl 2- (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1733 NHS0 2 CH 3 2-Cl-phenyl 2- (N-azatanyl-methyl) phenyl 1734 NHS0 2 CH 3 2-Cl-phenyl 2- (N-azetidinyl-methyl) phenyl 1735 NHS0 2 CH 3 2-Cl-phenyl 2- (N-piperazinyl-methyl) phenyl 1736 NHS0 2 CH 3 2-Cl-phenyl 2-(N,N' -BOC-piperazinyl- methyl) phenyl 1737 NHS0 2 CH 3 2-Cl-phenyl 2- (N-imidazolyl-methyl) phenyl 1738 NHSO 2 CH 3 2-Cl-phenyl 2- (N-methoxy-N-methylamino- methyl ) phenyl 1739 NHS0 2 CH 3 2-Cl-phenyl 2- (N-pyridonyl-methyl ) phenyl 1740 NHS0 2 CH 3 2-Cl-phenyl 2- (N- (N' ,N' -dimethylhydrazinyl- methyl ) phenyl 1741 NHS0 2 CH 3 2-Cl-phenyl 2- (amidinyl ) phenyl 1742 NHS0 2 CH 3 2-Cl-phenyl 2- (N-guanidinyl ) henyl 1743 NHS0 2 CH 3 2-Cl-phenyl 2- ( imidazolyl ) phen 1 1744 NHS0CH 3 2-Cl-phenyl 2- (imidazolidinyl) phenyl 1745 NHS0 2 CH 3 2-Cl-phenyl 2- (2-imidazolidinyl- sulfonyl ) phenyl 1746 NHS0 2 CH 3 2-Cl-phenyl 2- (2-pyrrolidinyl) phenyl 1747 NHS0 2 CH 3 2-Cl-phenyl 2- ( 2-piperidinyl) phenyl 1748 NHS0 2 CH 3 2-Cl-phenyl 2- (amidinyl-methyl ) phenyl 1749 NHS0 2 CH 3 2-Cl-phenyl 2- (2-imidazolidinyl- methyl ) phenyl 1750 NHS0 2 CH 3 2-Cl-phenyl 2- (N- (2-aminoimidazolyl) - methyl) phenyl 1751 NHS0 2 CH 3 2-Cl-phenyl 2-dimethylaminoimidazol-l-yl 1752 NHS0 2 CH 3 2-Cl-phenyl 2- ( 3-aminophenyl ) 1753 NHS0 2 CH 2-Cl-phenyl 2- (3 -pyrrolidinylcarbonyl) 1754 NHS0 2 CH 3 2-Cl-phenyl 2-glycinoyl 1755 NHS0 2 CH 3 2-Cl-phenyl 2- imidazol-1-ylacetyl) 1756 NHS0 2 CH 3 2-F-phenyl 2- N-pyrrolidinyl-methyl ) phenyl 1757 NHS0 2 CH 3 2-F-phenyl 2- N-piperidinyl-methyl ) phenyl 1758 NHS0 2 CH 3 2-F-phenyl 2- N-morpholino-methyl ) phenyl 1759 NHS0 CH 3 2-F-phenyl 2- N,N' -methylmorpholinium- methyl) phenyl 1760 NHS0 2 CH 3 2-F-phenyl 2- N-pyridinium-methyl) phenyl 1761 NHS0 2 CH 3 2-F-phenyl 2- N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1762 NHS0 2 CH 3 2-F-phenyl 2- N-azatanyl-methyl ) phenyl 1763 NHS0 2 CH 3 2-F-phenyl 2- N-azetidinyl-methyl) phenyl 1764 NHS0 2 CH 3 2-F-phenyl 2- N-piperazinyl-methyl) phenyl 1765 NHS0 CH 3 2-F-phenyl 2- N,N' -BOC-piperazinyl- methyl) phenyl 1766 NHS0 2 CH 3 2-F-phenyl 2- N-imidazolyl-methyl) phenyl 1767 NHS0 2 CH 3 2-F-phenyl 2- N-methoxy-N-methylamino- methyl) phenyl 1768 NHS0 2 CH 3 2-F-phenyl 2- N-pyridonyl-methyl ) phenyl 1769 NHS0 2 CH 3 2-F-phenyl 2- N- (N ' , N ' -dimethylhydrazinyl- methyl) phenyl 1770 NHS0 2 CH 3 2-F-phenyl 2- amidinyl ) phenyl 1771 NHS0 2 CH 3 2-F-phenyl 2- N-guanidinyl ) phenyl 1772 NHS0 2 CH 3 2-F-phenyl 2- imidazolyl) phenyl 1773 NHS0 2 CH 3 2-F-phenyl 2- imidazolidinyl) phenyl 1774 NHS0 2 CH 3 2-F-phenyl 2- 2-imidazolidinyl- sulfonyl ) phenyl 1775 NHS0 2 CH 3 2-F-phenyl 2- 2-pyrrolidinyl) phenyl 1776 NHS0 2 CH 3 2-F-phenyl 2- 2-piperidinyl) phenyl 1777 NHS0 2 CH 3 2-F-phenyl 2- amidinyl-methyl ) phenyl 1778 NHS0 2 CH 3 2-F-phenyl 2- 2-imidazolidinyl- methyl) phenyl 1779 NHS0 2 CH 3 2-F-phenyl 2- (N- (2-aminoimidazolyl) - methyl ) phenyl 1780 NHS0CH 3 2-F-phenyl 2-dimethylaminoimidazol-l-yl 1781 NHS0 2 CH 3 2-F-phenyl (3 -aminophenyl ) 1782 NHS0 CH 3 2-F-phenyl - (3-pyrrolidinylcarbonyl) 1783 NHS0 2 CH 3 2-F-phenyl -glycinoyl 1784 HHSO 2 CH 3 2-F-phenyl - (imidazol-i-ylacetyl) 1785 NHSO 2 CH 3 2 , 5-diF-phenyl - (N-pyrrolidinyl-methyl ) phenyl 1786 NHS0 2 CH 2 , 5-diF-phenyl (N-piperidinyl-methyl) phenyl 1787 NHS0 2 CH 3 2 , 5-diF-phenyl (N-morpholino-methyl ) phenyl 1788 NHS0 2 CH 3 2, 5-diF-phenyl (N, N ' -methylmorpholinium- methyl ) phenyl 1789 NHS0 2 CH 3 5-diF-phenyl (N-pyridinium-methyl ) phenyl 1790 NHS0 2 CH 3 5-diF-phenyl (N-4- (N,N' -dimethylamino) - pyridinium-methyl) phenyl 1791 NHS0 2 CH 3 5-diF-phenyl (N-azatanyl-methyl) phenyl 1792 NHS0CH 3 5-diF-phenyl (N-azetidinyl-methyl)phenyl 1793 NHS0 2 CH 3 5-diF-phenyl (N-piperazinyl-methyl) phenyl 1794 NHS0 2 CH 3 5-diF-phenyl (N,N' -BOC-piperazinyl- methyl ) phenyl 1795 NHS0 2 CH 3 5-diF-phenyl (N-imidazolyl-methyl) phenyl 1796 NHS0 2 CH 3 5-diF-phenyl (N-methoxy-N-methylamino- methyl) phenyl 1797 NHS0 CH 3 5-diF-phenyl (N-pyridonyl-methyl ) phenyl 1798 NHS0 2 CH 3 5-diF-phenyl (N- (N ' , N ' -dimethylhydrazinyl- methyl ) phenyl 1799 NHS0 2 CH 3 5-diF-phenyl (amidinyl) phenyl 1800 NHS0 2 CH 3 5-diF-phenyl (N-guanidinyl ) phenyl 1801 NHS0 2 CH 3 5-diF-phenyl ( imidazolyl ) henyl 1802 NHS0 2 CH 3 5-diF-phenyl ( imidazolidinyl) phenyl 1803 NHS0 2 CH 3 5-diF-phenyl (2-imidazolidinyl- sulfonyl ) phenyl 1804 NHS0 2 CH 3 5-diF-phenyl (2-pyrrolidinyl) phenyl 1805 NHS0 2 CH 3 5-diF-phenyl (2-piperidinyl ) phenyl 1806 NHS0 2 CH 3 5-diF-phenyl (amidinyl-methyl ) phenyl 1807 NHS0 2 CH 3 5-diF-phenyl (2-imidazolidinyl- methyl) phenyl 1808 NHS0 2 CH 3 2 5-diF-phenyl 2 (N- (2-aminoimidazolyl) - methyl) phenyl 1809 NHS0 CH 3 5-diF-phenyl 2-dimethylaminoimidazol-l-yl 1810 NHS0 2 CH 3 5-diF-phenyl 2- (3-aminophenyl) 1811 NHS0 2 CH 3 5-diF-phenyl 2- (3-pyrrolidinylcarbonyl) 1812 NHS0 2 CH 3 5-diF-phenyl 2-glycinoyl 1813 NHS0 2 CH 3 5-diF-phenyl 2- (imidazol-i-ylacetyl) Table 3 ai R=F, D=NH 2 bi R=F, D=NH 2 Ci R=F, D=NH a 2 R=H, D=NH 2 b 2 R=H, D=NH 2 c 2 R=H, D=NH 2 a 3 R=F, D=CH 2 NH 2 b 3 R=F, D=CH 2 NH 2 c 3 R=F, D=CH 2 NH 2 a 4 R=H, D=CH 2 NH 2 b 4 R=H, D=CH 2 NH 2 c 4 R=H, D=CH 2 NH 2 a 5 R=F, D=C(=NH)NH 2 b 5 R=F, D=C(=NH)NH 2 c 5 R=F, D=C(=NH)NH 2 a 6 R=H, D=C(=NH)NH 2 b 6 R=H, D=C(=NH)NH 2 c 6 R=H, D=C(=NH)NH 2 a 7 R=F, D=C(0)NH 2 b 7 R=F, D=C(0)NH 2 c 7 R=F, D=C(0)NH 2 a 8 R=H, D=C(0)NH 2 b 8 R=H, D=C(0)NH 2 c 8 R=H, D=C(0)NH 2 di R=F, D=NH 2 ei R=F, D=NH 2 fi R=F, D=NH 2 d 2 R=H, D=NH 2 e 2 R=H, D=NH 2 f 2 R=H, D=NH 2 d 3 R=F, D=CH 2 NH 2 e 3 R=F, D=CH 2 NH 2 f 3 R=F, D=CH 2 NH 2 d 4 R=H, D=CH 2 NH 2 e 4 R=H, D=CH 2 NH 2 f 4 R=H, D=CH 2 NH 2 d 5 R=F, D=C(=NH)NH 2 e 5 R=F, D=C(=NH)NH 2 f 5 R=F, D=C(=NH)NH 2 d 6 R=H, D=C(=NH)NH 2 e 6 R=H, D=C(=NH)NH 2 f 6 R=H, D=C(=NH)NH 2 d 7 R=F, D=C(0)NH 2 e 7 R=F, D=C(0)NH 2 f 7 R=F, D=C(0)NH 2 d 8 R=H, D=C(0)NH 2 e 8 R-H, D=C(0)NH 2 f 8 R=H, D=C(0)NH 2 gi R=F, D=NH 2 hi R= =F, D=NH 2 i R=F, D=NH 2 g 2 R=H, D=NH 2 h 2 R= =H, D=NH 2 2 R=H, D=NH 2 g 3 R=F, D=CH 2 NH 2 h 3 R= =F, D=CH 2 NH 2 3 R=F, D=CH 2 NH 2 g 4 R=H, D=CH 2 NH 2 h 4 R= =H, D=CH 2 NH 2 4 R=H, D=CH 2 NH 2 g 5 R=F, D=C(=NH)NH 2 hs R= =F, D=C(=NH)NH 2 5 R=F, D=C(=NH)NH g 6 R=H, D=C(=NH)NH 2 h 6 R= =H, D=C(=NH)NH 2 6 R=H, D=C(=NH)NH 2 g 7 R=F, D=C(0)NH 2 hy R= =F, D=C(0)NH 2 7 R=F, D=C(0)NH 2 g 8 R=H, D=C(0)NH 2 h 8 R=H, D=C(0)NH 2 8 R=H, D=C(0)NH 2 J1 R=F, D=NH 2 ki R=F, D=NH 2 R=F, D=NH 2 J2 R=H, D=NH 2 k 2 R=H, D=NH 2 1 2 R=H, D=NH 2 J3 R=F, D=CH 2 NH 2 k 3 R=F, D=CH NH 2 1 3 R=F, D=CH 2 NH 2 j R=H, D=CH 2 NH 2 IC4 R=H, D=CH 2 NH 2 1 4 R=H, D=CH 2 NH 2 j 5 R=F, D=C(=NH)NH 2 k 5 R=F, D=C(=NH)NH 2 1 5 R=F, D=C(=NH)NH 2 j 6 R=H, D=C(=NH)NH 2 ke R=H, D=C(=NH)NH 2 1 6 R=H, D=C(=NH)NH 2 j 7 R=F, D=C(0)NH 2 k 7 R=F, D=C(0)NH 2 1 7 R=F, D=C(0)NH 2 J8 R=H, D=C(0)NH 2 k 8 R=H, D=C(Q)NH 2 1 8 R=H, D=C(0)NH 2 mi R=F, D=NH 2 n-i R=F, D=NH 2 Oi R=F, D=NH 2 m 2 R=H, D=NH 2 n 2 R=H, D=NH 2 0 2 R=H, D=NH 2 m 3 R=F, D=CH 2 NH 2 n 3 R=F, D=CH 2 NH 2 0 3 R=F, D=CH 2 NH 2 m 4 R=H, D=CH 2 NH 2 n 4 R=H, D=CH 2 NH 2 0 4 R=H, D=CH 2 NH 2 m 5 R=F, D=C(=NH)NH 2 n 5 R=F, D=C(=NH)NH 2 0 5 R=F, D=C(=NH)NH 2 m 6 R=H, D=C(=NH)NH 2 n 6 R=H, D=C(=NH)NH 2 0 6 R=H, D=C(=NH)NH 2 m 7 R=F, D=C(0)NH 2 n 7 R=F, D=C(0)NH 2 0 7 R=F, D=C(0)NH 2 m 8 R=H, D=C(0)NH 2 n 8 R=H, D=C(0)NH 2 0 8 R=H, D=C(0)NH 2 Pi R=F, D= NH 2 qi R=F, D=NH 2 1 R=F, D=NH 2 p 2 R=CI, D= NH 2 q 2 R=CI, D=NH 2 2 R=CI, D=NH 2 p 3 R=OMe, D=NH 2 q 3 R=OMe, D=NH 2 3 R=OMe, D=NH 2 p 4 R=F, D= CH 2 NH 2 q 4 R=F, D=CH 2 NH 2 4 R=F, D=CH 2 NH 2 p 5 R=CI, D CH 2 NH 2 q 5 R=CI, D=CH 2 NH 2 5 R=CI, D=CH 2 NH 2 p 6 R=OMe, D=CH 2 NH 2 q 6 R=0Me, D=CH 2 NH 2 6 R=OMe, D=CH 2 NH 2 p 7 R=F, D= C(=NH)NH 2 q 7 R=F, D=C(=NH)NH 2 7 R=F, D=C(=NH)NH 2 p 8 R=CI, D =C(=NH)NH 2 q 8 R=CI, D=C(=NH)NH 2 8 R=CI, D=C(=NH)NH 2 p 9 R=OMe, D=C(=NH)NH 2 q 9 R=0Me, D=C(=NH)NH 2 g R=OMe, D=C(=NH)NH 2 P10 R=F, D =C(0)NH 2 qio R=F, D=C(0)NH 2 10 R=F, D=C(0)NH 2 Pii R=CI, D: =C(0)NH 2 qn R=CI, D=C(0)NH 2 11 R=CI, D=C(0)NH 2 Pi 2 R=OMe , D=C(0)NH 2 q 1 R=0Me, D=C(0)NH 2 ι 2 R=OMe, D=C(0)NH 2 Si R=F, D=NH 2 ti R=F, D=NH 2 uι R=F, D=NH 2 s 2 R=CI, D=NH 2 t 2 R=CI, D=NH 2 u 2 R=CI, D=NH 2 s 3 R=OMe, D=NH 2 t 3 R=OMe, D=NH 2 u 3 R=OMe, D=NH 2 s 4 R=F, D=CH 2 NH 2 t 4 R=F, D=CH 2 NH 2 u 4 R=F, D=CH 2 NH 2 s 5 R=CI, D=CH 2 NH 2 t 5 R=CI, D=CH 2 NH 2 u 5 R=CI, D=CH 2 NH 2 s 6 R=OMe, D=CH 2 NH 2 t 6 R=OMe, D=CH 2 NH 2 u 6 R=OMe, D=CH 2 NH2 s 7 R=F, D=C(=NH)NH 2 t 7 R=F, D=C(=NH)NH 2 u 7 R=F, D=C(=NH)NH 2 s 8 R=CI, D=C(=NH)NH 2 t 8 R=CI, D=C(=NH)NH 2 u 8 R=CI, D=C(=NH)NH 2 s 9 R=OMe, D=C(=NH)NH 2 t 9 R=OMe, D=C(=NH)NH 2 u 9 R=OMe, D=C(=NH)NH 2 Sιo R=F, D=C(0)NH 2 tιo R=F, D=C(0)NH 2 uιo R=F, D=C(0)NH 2 SH R=CI, D=C(0)NH 2 tn R=CI, D=C(0)NH 2 uιι R=CI, D=C(0)NH 2 s 12 R=OMe, D=C(0)NH 2 t i2 R=OMe, D=C(0)NH 2 Ui2 R=OMe, D=C(0)NH 2 Vi R=F, D=NH 2 wι R=F, D=NH 2 Xi R=F, D=NH 2 v 2 R=CI, D=NH 2 w 2 R=CI, D=NH 2 2 R= Cl, D=NH 2 v 3 R=OMe, D=NH 2 w 3 R=OMe, D=NH 2 X3 R= OMe, D=NH 2 v 4 R=F, D=CH 2 NH 2 w 4 R=F, D=CH 2 NH 2 X 4 R= F, D=CH 2 NH 2 v 5 R=CI, D=CH 2 NH 2 w 5 R=CI, D=CH 2 NH 2 5 R= Cl, D=CH 2 NH 2 v 6 R=OMe, D=CH 2 NH 2 w 6 R=OMe, D=CH 2 NH 2 β R= O< Me, D=CH 2 NH 2 v 7 R=F, D=C(=NH)NH 2 w 7 R=F, D=C(=NH)NH 2 7 R= F, D=C(=NH)NH 2 v 8 R=CI, D=C(=NH)NH 2 w 8 R=CI, D=C(=NH)NH 2 X8 R R==CI, D=C(=NH)NH 2 v 9 R=OMe, D=C(=NH)NH 2 w 9 R=OMe, D=C(=NH)NH 2 xg D=C(=NH)NH 2 V10 R=F, D=C(0)NH 2 Wιo R=F, D=C(0)NH 2 χ 10 C(0)NH 2 ι ι R=CI, D=C(0)NH 2 wι ι R=CI, D=C(0)NH 2 Xi i R=CI, D=C(0)NH 2 12 R=OMe, D=C(0)NH 2 W12 R=OMe, D=C(0)NH 2 x i 2 R=OMe, D=C(0)NH 2 yi R=F, D=NH 2 zι R=F, D=NH 2 aai R=F, D=NH 2 y 2 R=CI, D=NH 2 z 2 R=CI, D=NH 2 aa 2 R=CI, D=NH 2 y 3 R= O' Me, D=NH 2 z 3 R=OMe, D=NH 2 aa 3 R=OMe, D=NH 2 V4 R= F, D=CH 2 NH 2 z 4 R=F, D=CH 2 NH 2 aa 4 R=F, D=CH 2 NH 2 Y5 R= C ( l, D=CH 2 NH 2 z 5 R=CI, D=CH 2 NH 2 aa 5 R=CI, D=CH 2 NH 2 y 6 R= Oι Me, D=CH 2 NH 2 z 6 R=OMe, D=CH 2 NH 2 aa 6 R=OMe, D=CH 2 NH 2 y 7 R= F, D=C(=NH)NH 2 z 7 R=F, D=C(=NH)NH 2 aa 7 R=F, D=C(=NH)NH 2 y 8 R= Cι l, D=C(=NH)NH 2 z 8 R=CI, D=C(=NH)NH 2 aa 8 R s -CI, D=C(=NH)NH 2 y 9 R= OMe, D=C(=NH)NH 2 z 9 R=OMe, D=C(=NH)NH 2 aag R=OMe, D=C(=NH)NH 2 Yιo R =F, D=C(0)NH 2 Zιo R=F, D=C(0)NH 2 aaio R=F, D=C(0)NH 2 yn R Cl, D=C(0)NH 2 zι ι R=CI, D=C(0)NH 2 aai i R=CI, D=C(0)NH 2 y i 2 R OMe, D=C(0)NH 2 R=OMe, D=C(0)NH 2 aa i 2 R=0Me, D=C(Q)NH 2 bbi R=F, D= NH 2 ccι R=F, D=NH 2 ddi R=F, D= NH 2 bb 2 R=CI, D =NH 2 cc 2 R=CI, D=NH 2 dd 2 R=CI, D: NH 2 bb 3 R=OMe D=NH 2 cc 3 R=OMe, D=NH 2 dd 3 R=OMe, D=NH 2 bb 4 R=F, D=< CH 2 NH 2 cc 4 R=F, D=CH 2 NH 2 dd 4 R=F, D= CH 2 NH 2 bb 5 R=CI, D= CH 2 NH 2 cc 5 R=CI, D=CH 2 NH 2 dd 5 R=CI, D= =CH 2 NH 2 bb 6 R=OMe, D=CH 2 NH 2 cc 6 R=OMe, D=CH 2 NH 2 dd 6 R=OMe, D=CH 2 NH 2 bb 7 R=F, D= C(=NH)NH 2 cc 7 R=F, D=C(=NH)NH 2 dd 7 R=F, D= C(=NH)NH 2 bb 8 R=CI, D =C(=NH)NH 2 ccs R=CI, D=C(=NH)NH 2 dd 8 R=CI, D: C(=NH)NH 2 bbg R=OMe, D=C(=NH)NH 2 cc 9 R=0Me, D=C(=NH)NH 2 ddg R=OMe, D=C(=NH)NH 2 bbio R=F, Di =C(0)NH 2 CC10 R=F, D=C(0)NH 2 ddio R=F, D: =C(0)NH 2 bbn R=CI, D: =C(0)NH 2 ecu R=CI, D=C(0)NH 2 ddn R=CI, D =C(0)NH 2 bbi2 R=OMe , D=C(0)NH 2 CC12 R=OMe, D=C(0)NH 2 ddι 2 R=OMe D=C(0)NH 2 eei R=F, D=CH 2 NH 2 ffi R=F, D=CH 2 NH 2 ggi R=F, D=CH 2 NH 2 ee 2 R=CI, D=CH 2 NH 2 ff 2 R=CI, D=CH 2 NH 2 gg 2 R=CI, D=CH 2 NH 2 ee 3 R=OMe, D=CH 2 NH 2 ff 3 R=OMe, D=CH 2 NH2 gg 3 R=OMe, D=CH 2 NH 2 ee 4 R=CH 2 NH 2 , ff 4 R=CH 2 NH 2 , gg 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 hh, R=F, D=CH NH 2 h R=F, D=CH 2 NH 2 jji R=F, D=CH 2 NH 2 hh 2 R=CI, D=CH 2 NH 2 i 2 R=CI, D=CH 2 NH 2 jj 2 R=CI, D=CH 2 NH 2 hh 3 R=OMe, D=CH 2 NH 2 i 3 R=OMe, D=CH 2 NH 2 jj 3 R=OMe, D=CH 2 NH 2 hh 4 R=CH 2 NH 2 , i 4 R=CH 2 NH 2 , jj 4 R=CH 2 NH 2 , D=CH NH 2 D=CH 2 NH 2 D=CH 2 NH 2 kki R=F, D=CH 2 NH 2 11 1 R=F, D=CH 2 NH 2 mrriι R=F, D=CH 2 Nh 2 kk 2 R=CI, D=CH 2 NH 2 11 2 R=CI, D=CH 2 NH 2 mm 2 R=CI, D=CH 2 NH 2 kk 3 R=OMe, D=CH 2 NH 11 3 R=OMe, D=CH 2 NH 2 mm 3 R=OMe, D=CH 2 NH 2 kk 4 R=CH 2 NH 2 , 11 4 R=CH 2 NH 2> mm 4 R=CH NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 nnι R=F, D=CH 2 NH 2 001 R=F, D=CH 2 NH 2 PPT R=F, D=CH 2 NH 2 nn 2 R=CI, D=CH 2 NH 2 00 2 R=CI, D=CH 2 NH 2 PP2 R=CI, D=CH 2 NH 2 nn 3 R=OMe, D=CH 2 NH 2 003 R=OMe, D=CH 2 NH 2 pp 3 R=OMe, D=CH 2 NH 2 nn 4 R=CH 2 NH 2 , 00 4 R=CH 2 NH 2 , pp 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 qq ή R=F, D=CH 2 NH 2 rri R=F, D=CH 2 NH2 SS! R=F, D=CH 2 NH 2 qq 2 R=CI, D=CH 2 NH 2 rr 2 R=CI, D=CH 2 NH 2 ss 2 R=CI, D=CH 2 NH 2 qq 3 R=OMe, D=CH 2 NH 2 rr 3 R=OMe, D=CH 2 NH2 ss 3 R=OMe, D=CH 2 NH 2 qq 4 R=CH 2 NH 2 , rr 4 R=CH 2 NH 2 , ss 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 Ex# R" 3 B 1 H phenyl 2 - ( (Me ) 2 N-methyl ) phenyl 2 H phenyl 2 - ( (Me ) NH-methyl ) phenyl 3 H phenyl 2 - ( H 2 N-me thyl ) phenyl 4 H phenyl 2 -HOCH 2 -phenyl 5 H 2-F-phenyl 2 - ( (Me ) 2 N-methyl ) phenyl 6 H 2-F-phenyl 2 - ( (Me ) NH-methyl ) phenyl 7 H 2-F-phenyl 2- (H 2 N-methyl ) phenyl 8 H 2-F-phenyl 2 -HOCH 2 -phenyl 9 H phenyl 2-methylimidazol-l-yl 10 H phenyl 2-ethylimidazol-l-yl 11 H phenyl 2- ( (Me) 2 N-methyl ) imidazol-1-yl 12 H phenyl 2-CH 3 Sθ 2 -imidazol-l-yl H phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2-F-phenyl 2-methylimidazol-l-yl H 2-F-phenyl 2-ethylimidazol-l-yl H 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl H 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl H 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2-Cl-phenyl 2-methylimidazol-l-yl H 2-Cl-phenyl 2-ethylimidazol-l-yl H 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl H 2-Cl-phenyl 2-CH 3 S0 -imidazol-l-yl H 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2-(Me) 2 N-phenyl 2-methylimidazol-l-yl H 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl H 2- (Me) 2 N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl H 2- (Me) 2 N-phenyl 2 -CH 3 S0 2 -imidazol-l-yl H 2- (Me) 2 N-phenyl 2 -CH 3 OCH 2 -imidazol-l-yl H phenyl N-methylimidazol-2 -yl H phenyl 4 -methyl imidazol- 5 -yl H phenyl 5-CF 3 -pyrazol-l-yl H 2-F-phenyl N-methylimidazol-2-yl H 2-F-phenyl 4-methylimidazol-5-yl H 2-F-phenyl 5-CF 3 -pyrazol-l-yl H phenyl guanidino H phenyl 2-thiazolin-2-ylamine H phenyl N-methyl-2-imidazolin-2-yl H phenyl N-methyl-1,4,5, 6- tetrahydropyrimid-2-yl H phenyl N-methylimidazol-2-ylthiol H phenyl t-butoxycarbonylamine H phenyl (N-pyrrolidino) formylimino H phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino H 2-F-phenyl guanidino H 2-F-phenyl 2-thiazolin-2-ylamine H 2-F-phenyl N-methyl-2-imidazolin-2-yl H 2-F-phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2-yl H 2-F-phenyl N-methylimidazol-2-ylthio H 2-F-phenyl t-butoxycarbonylamine H 2-F-phenyl (N-pyrrolidino) formylimino H 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino H 2-CH 3 0-phenyl (N-pyrrolidino) formylimino H 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN phenyl 2- ( (Me) 2 N-methyl ) phenyl -CN phenyl 2- ( (Me) NH-methyl) phenyl -CN phenyl 2- (H 2 N-methyl) phenyl -CN phenyl 2-HOCH 2 -phenyl -CN 2-F-phenyl 2- ( (Me) 2 N-methyl ) phenyl -CN 2-F-phenyl 2- ( (Me) NH-methyl) phenyl -CN 2-F-phenyl 2- (H 2 N-methyl ) phenyl -CN 2-F-phenyl 2-HOCH 2 -phenyl -CN phenyl 2-methylimidazol-l-yl -CN phenyl 2-ethylimidazol-l-yl -CN phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl -CN phenyl 2-CH 3 S0 2 -imidazol-l-yl -CN phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN 2-F-phenyl 2-methylimidazol-l-yl -CN 2-F-phenyl 2-ethylimidazol-l-yl -CN 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl -CN 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl -CN 2-F-phenyl -Ch 3 OCH 2 -imidazol-1-yl -CN 2-Cl-phenyl 2-methylimidazol-l-yl -CN 2-Cl-phenyl 2-ethylimidazol-l-yl -CN 2-Cl-phenyl 2-( (Me) 2N-methyl) imidazol-1-yl -CN 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl -CN 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl -CN 2- (Me) N-phenyl 2-ethylimidazol-l-yl -CN 2- (Me) N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl -CN 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl -CN 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN phenyl N-methylimidazol-2-yl -CN phenyl 4-methylimidazol-5-yl -CN phenyl 5-CF -pyrazol-l-yl -CN 2-F-phenyl N-methylimidazol-2-yl -CN 2-F-phenyl 4-methylimidazol-5-yl -CN . 2-F-phenyl 5-CF 3 -pyrazol-l-yl -CN phenyl guanidino -CN phenyl 2-thiazolin-2-ylamine -CN phenyl N-methyl-2-imidazolin-2-yl -CN phenyl N-methyl-1,4,5, 6- tetrahydropyrimid-2-yl -CN phenyl N-methylimidazol-2-ylthiol -CN phenyl t-butoxycarbonylamine -CN phenyl (N-pyrrolidino) formylimino -CN phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN 2-F-phenyl guanidino -CN 2-F-phenyl 2-thiazolin-2-ylamine -CN 2-F-phenyl N-methyl-2-imidazolin-2-yl -CN 2-F-phenyl N-methyl-1,4, 5,6- tetrahydropyrimid-2-yl -CN 2-F-phenyl N-methylimidazol-2-ylthio -CN 2-F-phenyl t-butoxycarbonylamine -CN 2-F-phenyl (N-pyrrolidino) formylimino -CN 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN 2-CH 3 0-phenyl (N-pyrrolidino) formylimino -CN 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino CF 3 phenyl 2- ( (Me) N-methyl) phenyl CF 3 phenyl 2- ( (Me) H-methyl ) phenyl CF 3 phenyl 2- (H 2 N-methyl) phenyl CF 3 phenyl 2-HOCH 2 -phenyl CF 3 2-F-phenyl 2- ( (Me) 2 N-methyl ) phenyl CF 3 2-F-phenyl 2- ( (Me) NH-methyl) phenyl CF 3 2-F-phenyl 2- (H 2 N-methyl ) phenyl 112 CF 3 2-F-phenyl 2 -HOCH 2 -phenyl 113 CF 3 phenyl 2-methylimidazol-l-yl 114 CF 3 phenyl 2-ethylimidazol-l-yl 115 CF 3 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 116 CF 3 phenyl 2-CH 3 S0 2 -imidazol-1-yl 117 CF 3 phenyl 2-CH 3 OCH 2 -imidazol-1-yl 113 CF 3 2-F-phenyl 2 -methylimidazol-1-yl 119 CF 3 2-F-phenyl 2-ethylimidazol-l-yl 120 CF 3 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 121 CF 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 122 CF 3 2-F-phenyl 2 -CH 3 OCH 2 -imidazol-1-yl 123 CF 3 2-Cl-phenyl 2-methylimidazol-l-yl 124 CF 3 2-Cl-phenyl 2-ethylimidazol-l-yl 125 CF 3 2-Cl-phenyl 2- ( (Me) N-methyl) imidazol-1-yl 126 CF 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl 127 CF 3 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 128 CF 3 2 - (Me ) 2N-phenyl 2-methylimidazol-l-yl 129 CF 3 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl 130 CF 3 2- (Me) 2 N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 131 CF 3 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 132 CF 3 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 133 CF 3 phenyl N-methylimidazol-2-yl 134 CF 3 phenyl 4-methylimidazol-5-yl 135 CF 3 phenyl 5-CF 3 -pyrazol-1-yl 136 CF 3 2-F-phenyl N-methylimidazol-2-yl 137 CF 3 2-F-phenyl 4-methylimidazol-5-yl 138 CF 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 139 CF 3 phenyl guanidino 140 CF 3 phenyl 2-thiazolin-2-ylamine 141 CF 3 phenyl N-methyl-2-imidazolin-2-yl 142 CF 3 phenyl N-methyl-1,4,5, 6- tetrahydropyrimid-2 -yl 143 CF 3 phenyl N-methylimidazol-2-ylthiol 144 CF 3 phenyl t-butoxycarbonylamine 145 CF 3 phenyl (N-pyrrolidino) formylimino 146 CF 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 147 CF 3 2-F-phenyl guanidino 148 CF 3 2-F-phenyl 2-thiazolin-2-ylamine 149 CF 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 150 CF 3 2-F-phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2-yl 151 CF 3 2-F-phenyl N-methylimidazol-2-ylthio 152 CF 3 2-F-phenyl t-butoxycarbonylamine 153 CF 3 2-F-phenyl (N-pyrrolidino) formylimino 154 CF 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 155 CF 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 156 CF 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 157 CONH 2 phenyl 2- ( (Me) N-methyl ) phenyl 158 CONH 2 phenyl 2 - ( (Me) NH-methyl ) phenyl 159 C0NH 2 phenyl 2- (H 2 N-methyl ) phenyl 160 C0NH 2 phenyl 2-HOCH 2 -phenyl 161 C0NH 2 2-F-phenyl 2- ( (Me) 2 N-methyl) phenyl 162 C0NH 2 2-F-phenyl 2- ( (Me) NH-methyl ) phenyl 163 C0NH 2 2-F-phenyl 2- (H 2 N-methyl) phenyl 164 C0NH 2 2-F-phenyl 2-HOCH 2 -phenyl 165 C0NH 2 phenyl 2-methylimidazol-l-yl 166 C0NH 2 phenyl 2-ethylimidazol-l-yl 167 C0NH 2 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 168 C0NH 2 phenyl 2-CH 3 S0 2 -imidazol-l-yl 169 C0NH 2 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 170 C0NH 2 2-F-phenyl 2-methylimidazol-l-yl 171 C0NH 2 2-F-phenyl 2-ethylimidazol-l-yl 172 C0NH 2 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 173 C0NH 2 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 174 C0NH 2 2-F-phenyl 2-CH 3 OCH 2 -imidazol-1-yl 175 C0NH 2 2-Cl-phenyl 2-methylimidazol-l-yl 176 C0NH 2 2-Cl-phenyl 2-ethylimidazol-l-yl 177 C0NH 2 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 178 C0NH 2 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-1-yl 179 C0NH 2 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 180 C0NH 2 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl 181 CONH 2 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl 182 CONH 2 2- (Me) 2 N-phenyl 2-( (Me) 2 N-methyl)imidazol-l-yl 183 CONH 2 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 184 CONH 2 2-(Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 185 CONH 2 phenyl N-methylimidazol-2-yl 186 CONH 2 phenyl 4-methylimidazol-5-yl 187 CONH 2 phenyl 5-CF 3 -pyrazol-1-yl 188 CONH 2 2-F-phenyl N-methylimidazol-2-yl 189 CONH 2 2-F-phenyl 4-methylimidazol-5-yl 190 CONH 2 2-F-phenyl 5-CF 3 -pyrazol-1-yl 191 CONH 2 phenyl guanidino 192 CONH 2 phenyl 2-thiazolin-2-ylamine 193 CONH 2 phenyl N-methyl-2-imidazolin-2-yl 194 CONH 2 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 195 CONH 2 phenyl N-methylimidazol-2-ylthiol 196 CONH 2 phenyl t-butoxycarbonylamine 197 CONH 2 phenyl (N-pyrrolidino) formylimino 198 CONH 2 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 199 CONH 2 2-F-phenyl guanidino 200 CONH 2 2-F-phenyl 2-thiazolin-2-ylamine 201 CONH 2 2-F-phenyl N-methyl-2-imidazolin-2-yl 202 CONH 2 2-F-phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2-yl 203 CONH 2 2-F-phenyl N-methylimidazol-2-ylthio 204 CONH 2 2-F-phenyl t-butoxycarbonylamine 205 CONH 2 2-F-phenyl (N-pyrrolidino) formylimino 206 CONH 2 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 207 CONH 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 208 CONH 2 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 209 SCH 3 phenyl 2- ( (Me) 2 N-methyl) phenyl 210 SCH 3 phenyl 2- ( (Me) H-methyl) phenyl 211 SCH 3 phenyl 2- (H 2 N-methyl ) phenyl 212 SCH 3 phenyl 2-HOCH 2 -phenyl 213 SCH 2-F-phenyl 2- ( (Me) 2 N-methyl ) phenyl 214 SCH 3 2-F-phenyl 2- ( (Me) NH-methyl) henyl 215 SCH 3 2-F-phenyl 2- (H 2 N-methyl ) phenyl 216 SCH 3 2-F-phenyl 2-HOCH 2 -phenyl 217 SCH 3 phenyl 2-methylimidazol-l-yl 218 SCH 3 phenyl 2-ethylimidazol-l-yl 219 SCH 3 phenyl 2-( (Me) N-methyl) imidazol-1-yl 220 SCH 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 221 SCH 3 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 222 SCH 3 2-F-phenyl 2-methylimidazol-l-yl 223 SCH 3 2-F-phenyl 2-ethylimidazol-l-yl 224 SCH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 225 SCH 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 226 SCH 3 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 227 SCH 3 2-Cl-phenyl 2-methylimidazol-l-yl 228 SCH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 229 SCH 3 2-Cl-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 230 SCH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-1-yl 231 SCH 3 2-Cl-phenyl 2-CH 3 OCH -imidazol-l-yl 232 SCH 3 2-(Me) 2 N-phenyl 2-methylimidazol-1-yl 233 SCH 3 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl 234 SCH 3 2-(Me) 2 N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 235 SCH 3 2-(Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 236 SCH 3 2-(Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 237 SCH 3 phenyl N-methylimidazol-2-yl 238 SCH 3 phenyl 4-methylimidazol-5-yl 239 SCH 3 phenyl 5-CF 3 -pyrazol-1-yl 240 SCH 3 2-F-phenyl N-methylimidazol-2-yl 241 SCH 3 2-F-phenyl 4-methylimidazol-5-yl 242 SCH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 243 SCH 3 phenyl guanidino 244 SCH 3 phenyl 2-thiazolin-2-ylamine 245 SCH 3 phenyl N-methyl-2-imidazolin-2-yl 246 SCH 3 phenyl N-methyl-1,4,5,6- tetrahydropyrimid-2-y1 247 SCH 3 phenyl N-methylimidazol-2-ylthiol 248 SCH 3 phenyl t-butoxycarbonylamine 249 SCH 3 phenyl (N-pyrrolidino) formylimino 250 SCH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 251 SCH 3 2-F-phenyl guanidino 252 SCH 3 2-F-phenyl 2-thiazolin-2-ylamine 253 SCH 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 254 SCH 3 2-F-phenyl N-methyl-1,4,5,6- tetrahydropyrimid-2-yl 255 SCH 3 2-F-phenyl N-methylimidazol-2-ylthio 256 SCH 3 2-F-phenyl t-butoxycarbonylamine 257 SCH 3 2-F-phenyl (N-pyrrolidino) formylimino 258 SCH 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 259 SCH 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 260 SCH 3 2-CH 3 0-phenyl (N-pyrrolidino) -For yl-N- (methanesulfamoyl) imino 261 S0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl ) phenyl 262 S0 2 CH 3 phenyl 2- ( (Me) NH-methyl ) phenyl 263 S0 2 CH 3 phenyl 2- (H 2 N-methyl ) phenyl 264 S0 2 CH 3 phenyl 2-HOCH 2 -phenyl 265 S0 2 CH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) phenyl 266 S0 2 CH 3 2-F-phenyl 2-( (Me) NH-methyl) phenyl 267 S0 2 CH 3 2-F-phenyl 2- (H 2 N-methyl ) phenyl 268 S0 2 CH 3 2-F-phenyl 2-HOCH 2 -phenyl 269 S0 2 CH 3 phenyl 2-methylimidazol-1-yl 270 S0CH 3 phenyl 2-ethylimidazol-l-yl 271 S0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 272 S0 2 CH 3 phenyl 2-CH 3 S0 2 -imidazol-1-yl 273 S0CH 3 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 274 S0 2 CH 3 2-F-phenyl 2-methylimidazol-l-yl 275 S0 2 CH 3 2-F-phenyl 2-ethylimidazol-l-yl 276 S0CH 3 2-F-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 277 S0 2 CH 3 2-F-phenyl 2-CH 3 SO 2 -imidazol-1-yl 278 S0 2 CH 3 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 279 S0 2 CH 3 2-Cl-phenyl 2-methylimidazol-l-yl 280 S0 2 CH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 281 S0 2 CH 3 2-Cl-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 282 S0 2 CH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl 283 S0 2 CH 3 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-1-yl 284 S0 2 CH 3 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl 285 S0 2 CH 3 2- (Me) 2 N-phenyl 2-ethylimidazol-1-yl 286 S0 2 CH 3 2- (Me) 2 N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 287 S0 2 CH 3 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-1-yl 288 S0 2 CH 3 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 289 S0 2 CH 3 phenyl N-methylimidazol-2-yl 290 S0 2 CH 3 phenyl 4-methylimidazol-5-yl 291 S0CH 3 phenyl 5-CF 3 -pyrazol-1-y1 292 S0 2 CH 3 2-F-phenyl N-methylimidazol-2-yl 293 S0 2 CH 3 2-F-phenyl 4-me hylimidazol-5-yl 294 S0 2 CH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 295 S0 2 CH 3 phenyl guanidino 296 S0 2 CH 3 phenyl 2-thiazolin-2-ylamine 297 S0 2 CH 3 phenyl N-methyl-2-imidazolin-2-yl 298 S0 2 CH 3 phenyl N-methyl-1,4,5,6- tetrahydropyrimid-2-y1 299 S0 2 CH 3 phenyl N-methylimidazol-2-ylthiol 300 S0 2 CH 3 phenyl t-butoxycarbonylamine 301 S0 2 CH 3 phenyl (N-pyrrolidino) formylimino 302 S0 2 CH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 303 S0CH 3 2-F-phenyl guanidino 304 S0 2 CH 3 2-F-phenyl 2-thiazolin-2-ylamine 305 S0 2 CH 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 306 S0 2 CH 3 2-F-phenyl N-methyl-1,4,5,6- tetrahydropyrimid-2-yl 307 S0 2 CH 3 2-F-phenyl N-methylimidazol-2-ylthio 308 S0CH 3 2-F-phenyl t-butoxycarbonylamine 309 Sθ 2 CH 3 2-F-phenyl (N-pyrrolidino) formylimino 310 S0 2 CH 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 311 Sθ 2 CH 3 2-CH 3 0-phenyi (N-pyrrolidino) formylimino 312 Sθ 2 CH 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 313 NHS0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl ) phenyl 314 NHS0 2 CH 3 phenyl 2- ( (Me) NH-methyl ) phenyl 315 NHS0 2 CH 3 phenyl 2- (H 2 N-methyl ) phenyl 316 NHS0 2 CH 3 phenyl 2-H0CH 2 -phenyl 317 NHS0 2 CH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) phenyl 318 NHS0 2 CH 3 2-F-phenyl 2-( (Me) NH-methyl) phenyl 319 NHS0 2 CH 3 2-F-phenyl 2- (H 2 N-methy1 ) phenyl 320 NHS0 2 CH 3 2-F-phenyl 2-H0CH 2 -phenyl 321 NHS0 2 CH 3 phenyl 2-methylimidazol-l-yl 322 NHS0 2 CH 3 phenyl 2-ethylimidazol-l-yl 323 NHS0 2 CH 3 phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 324 NHS0 2 CH 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 325 NHS0 2 CH 3 phenyl 2-CH 3 0CH 2 -imidazol-l-yl 326 NHS0 2 CH 3 2-F-phenyl 2-methylimidazol-l-yl 327 NHS0 2 CH 3 2-F-phenyl 2-ethylimidazol-l-yl 328 NHS0 2 CH 3 2-F-phenyl 2- ( (Me) N-methyl) imidazol-1-yl 329 NHS0 2 CH 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 330 NHSθ 2 CH 3 2-F-phenyl 2-CH 3 0CH 2 -imidazol-l-yl 331 NHS0 2 CH 3 2-Cl-phenyl 2-methylimidazol-l-yl 332 NHS0 2 CH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 333 NHS0 2 CH 3 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 334 NHS0 2 CH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl 335 NHS0 2 CH 3 2-Cl-phenyl 2-CH 3 0CH 2 -imidazol-l-yl 336 NHS0 2 CH 3 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl 337 NHS0 2 CH 3 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl 338 NHS0 2 CH 3 2- (Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 339 NHS0CH 3 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 340 NHS0 2 CH 3 2-(Me) 2 N-phenyl 2-CH 3 0CH 2 -imidazol-l-yl 341 NHS0 2 CH 3 phenyl N-methylimidazol-2-yl 342 NHSθ 2 CH 3 phenyl 4-methylimidazol-5-yl 343 NHS0 2 CH 3 phenyl 5-CF 3 -pyrazol-l-yl 344 NHS0 2 CH 3 2-F-phenyl N-methylimidazol-2-yl 345 NHS0 2 CH 3 2-F-phenyl 4-methylimidazol-5-yl 346 NHS0 2 CH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 347 NHS0 2 CH 3 phenyl guanidino 348 NHS0 2 CH 3 phenyl 2-thiazolin-2-ylamine 349 NHS0 2 CH 3 phenyl N-methyl-2-imidazolin-2-yl 350 NHS0 2 CH 3 phenyl N-methyl-1,4,5, 6- tetrahydropyrimid-2-yl 351 NHS0 2 CH 3 phenyl N-methylimidazol-2-ylthiol 352 NHS0 2 CH 3 phenyl t-butoxycarbonylamine 353 NHS0 2 CH 3 phenyl (N-pyrrolidino) formylimino 354 NHS0 2 CH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 355 NHS0 2 CH 3 2-F-phenyl guanidino 356 NHS0 2 CH 2-F-phenyl 2-thiazolin-2 -ylamine 357 NHS0 2 CH 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 358 NHS0 2 CH 3 2-F-phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2 -yl 359 NHS0 2 CH 3 2-F-phenyl N-methylimidazol-2-ylthio 360 NHS0 2 CH 3 2-F-phenyl t-butoxycarbonylamine 361 NHS0 2 CH 3 2-F-phenyl (N-pyrrolidino) formylimino 362 NHS0 2 CH 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 363 NHS0 2 CH 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 364 NHS0 2 CH 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino Table 4 ai R=F, D=NH 2 bi R=F, D=NH 2 Ci R=F, D=NH 2 a 2 R=H, D=NH 2 b 2 R=H, D=NH 2 c 2 R=H, D=NH 2 a 3 R=F, D=CH 2 NH 2 b 3 R=F, D=CH 2 NH 2 c 3 R=F, D=CH 2 NH 2 a 4 R=H, D=CH 2 NH 2 b 4 R=H, D=CH 2 NH 2 c 4 R=H, D=CH 2 NH 2 a 5 R=F, D=C(=NH)NH 2 b 5 R=F, D=C(=NH)NH 2 c 5 R=F, D=C(=NH)NH 2 a 6 R=H, D=C(=NH)NH 2 b 6 R=H, D=C(=NH)NH 2 c 6 R=H, D=C(=NH)NH 2 a 7 R=F, D=C(0)NH 2 b 7 R=F, D=C(0)NH 2 c 7 R=F, D=C(0)NH 2 a 8 R=H, D=C(0)NH 2 b 8 R=H, D=C(0)NH 2 c 8 R=H, D=C(0)NH 2 di R=F, D=NH 2 ei R=F, D=NH 2 fi R=F, D=NH 2 d 2 R=H, D=NH 2 e 2 R=H, D=NH 2 f 2 R=H, D=NH 2 d 3 R=F, D=CH 2 NH 2 e 3 R=F, D=CH 2 NH 2 f 3 R=F, D=CH 2 NH 2 d 4 R=H, D=CH 2 NH 2 e 4 R=H, D=CH 2 NH 2 f 4 R=H, D=CH 2 NH 2 d 5 R=F, D=C(=NH)NH 2 e 5 R=F, D=C(=NH)NH 2 f 5 R=F, D=C(=NH)NH 2 d 6 R=H, D=C(=NH)NH 2 e 6 R=H, D=C(=NH)NH 2 f 6 R=H, D=C(=NH)NH 2 d 7 R=F, D=C(0)NH 2 e 7 R=F, D=C(0)NH 2 f 7 R=F, D=C(0)NH 2 d 8 R=H, D=C(0)NH 2 e 8 R=H, D=C(0)NH 2 f 8 R=H, D=C(0)NH 2 g R=F, D=NH 2 hi R=F, D=NH 2 R=F, D=NH 2 g 2 R=H, D=NH 2 h 2 R=H, D=NH 2 R=H, D=NH 2 g 3 R=F, D=CH 2 NH 2 h 3 R=F, D=CH 2 NH 2 R=F, D=CH 2 NH 2 g 4 R=H, D=CH 2 NH 2 h 4 R=H, D=CH 2 NH 2 R=H, D=CH 2 NH 2 g 5 R=F, D=C(=NH)NH 2 h 5 R=F, D=C(=NH)NH 2 R=F, D=C(=NH)NH 2 g 6 R=H, D=C(=NH)NH 2 h 6 R=H, D=C(=NH)NH 2 R=H, D=C(=NH)NH 2 g 7 R=F, D=C(0)NH 2 h 7 R=F, D=C(0)NH 2 R=F, D=C(0)NH 2 g 8 R=H, D=C(0)NH 2 h 8 R=H, D=C(0)NH 2 8 R=H, D=C(0)NH 2 ji R=F, D=NH 2 ki R=F, D=NH 2 h R=F, D=NH J2 R=H, D=NH 2 k 2 R=H, D=NH 2 1 2 R=H, D=NH 2 J3 R=F, D=CH 2 NH 2 k3 R=F, D=CH 2 NH 2 1 3 R=F, D=CH 2 NH 2 j 4 R=H, D=CH 2 NH 2 lc* R=H, D=CH 2 NH 2 1 4 R=H, D=CH 2 NH 2 J5 R=F, D=C(=NH)NH 2 k 5 R=F, D=C(=NH)NH 2 1 5 R=F, D=C(=NH)NH 2 j 6 R=H, D=C(=NH)NH 2 k 6 R=H, D=C(=NH)NH 2 1 6 R=H, D=C(=NH)NH 2 J7 R=F, D=C(0)NH 2 k 7 R=F, D=C(0)NH 2 1 7 R=F, D=C(0)NH 2 J8 R=H, D=C(0)NH 2 k 8 R=H, D=C(0)NH 2 1 8 R=H, D=C(Q)NH 2 mi R=F, D=NH 2 iii R=F, D=NH 2 01 R=F, D=NH 2 m 2 R=H, D=NH 2 n 2 R=H, D=NH 2 0 2 R=H, D=NH 2 m 3 R=F, D=CH NH 2 n 3 R=F, D=CH 2 NH 2 03 R=F, D=CH 2 NH 2 m 4 R=H, D=CH 2 NH 2 n 4 R=H, D=CH 2 NH 2 0 4 R=H, D=CH 2 NH 2 m 5 R=F, D=C(=NH)NH 2 n 5 R=F, D=C(=NH)NH 2 0 5 R=F, D=C(=NH)NH 2 m 6 R=H, D=C(=NH)NH 2 n 6 R=H, D=C(=NH)NH 2 0 6 R=H, D=C(=NH)NH 2 m 7 R=F, D=C(0)NH 2 n 7 R=F, D=C(0)NH 2 0 7 R=F, D=C(0)NH 2 m 8 R=H, D=C(0)NH 2 n 8 R=H, D=C(0)NH 2 0 8 R=H, D=C(0)NH 2 Pi R=F, D=NH 2 qi R=F, D=NH 2 ri R=F, D=NH 2 P2 R=CI, D=NH 2 q 2 R=CI, D=NH 2 r 2 R=CI, D=NH 2 p 3 R=OMe, D=NH 2 q 3 R=OMe, D=NH 2 r 3 R=OMe, D=NH 2 p 4 R=F, D=CH 2 NH 2 q 4 R=F, D=CH 2 NH 2 r 4 R=F, D=CH 2 NH 2 p 5 R=CI, D=CH 2 NH 2 q 5 R=CI, D=CH 2 NH 2 r 5 R=CI, D=CH 2 NH 2 p 6 R=OMe, D=CH 2 NH 2 q 6 R=OMe, D=CH 2 NH 2 r 6 R=OMe, D=CH 2 NH 2 p 7 R=F, D=C(=NH)NH 2 q 7 R=F, D=C(=NH)NH 2 r 7 R=F, D=C(=NH)NH 2 p 8 R=CI, D=C(=NH)NH 2 q 8 R=CI, D=C(=NH)NH 2 r 8 R=CI, D=C(=NH)NH 2 p 9 R=OMe, D=C(=NH)NH 2 q 9 R=OMe, D=C(=NH)NH 2 r 9 R=OMe, D=C(=NH)NH 2 P10 R=F, D=C(0)NH 2 qio R=F, D=C(0)NH 2 r 10 R=F, D=C(0)NH 2 P11 R=CI, D=C(0)NH 2 qn R=CI, D=C(0)NH 2 rn R=CI, D=C(0)NH 2 P12 R=OMe, D=C(0)NH 2 q i2 R=OMe, D=C(0)NH 2 ri2 R=OMe, D=C(0)NH 2 Si s 2 s 3 s 4 s 5 s 6 s 7 s 8 s 9 Sιo SH Sι 2 i R=F, D=NH 2 Wι R= F, D=NH 2 Xi R=F, D=NH 2 v 2 R=CI, D=NH 2 W2 R=< Cl, D=NH 2 x 2 R= Cl, D=NH 2 v 3 R=OMe, D=NH 2 w 3 R=< OMe, D=NH 2 x 3 R= OMe, D=NH 2 v 4 R=F, D=CH 2 NH 2 W4 R= F, D=CH 2 NH 2 x 4 R= F, D=CH 2 NH 2 v 5 R=CI, D=CH NH 2 W 5 R= Cl, D=CH 2 NH 2 x 5 R=CI, D=CH 2 NH 2 v 6 R=OMe, D=CH 2 NH 2 w 6 R=< OMe, D=CH 2 NH 2 x 6 R=OMe, D=CH 2 NH 2 v 7 R=F, D=C(=NH)NH 2 w R= F, D=C(=NH)NH2 x 7 R=F, D=C(=NH)NH 2 v 8 R=CI, D=C(=NH)NH 2 w 8 R= Cl, D=C(=NH)NH 2 x 8 R=CI, D=C(=NH)NH 2 v 9 R=OMe, D=C(=NH)NH 2 Wg R=< OMe, D=C(=NH)NH 2 x 9 R=OMe, D=C(=NH)NH 2 Vιo R=F, D=C(0)NH 2 Wιc 1 R= =F, D=C(0)NH 2 X10 R=F, D=C(0)NH 2 vιι R=CI, D=C(0)NH 2 W11 R= =CI, D=C(0)NH 2 X11 R=CI, D=C(0)NH 2 V12 R=0Me, D=C(0)NH 2 W12 >R= =OMe, D=C(0)NH 2 X12 R=OMe, D=C(0)NH 2 yi R=F, D=NH 2 Zι R=F, D=NH 2 aai R=F, D=NH 2 y 2 R=CI, D=NH 2 z 2 R=CI, D=NH 2 aa 2 R=CI, D=NH 2 y 3 R=OMe, D=NH 2 z 3 R=OMe, D=NH 2 aa 3 R=OMe, D=NH 2 y 4 R=F, D=CH 2 NH 2 z 4 R=F, D=CH 2 NH 2 aa 4 R=F, D=CH 2 NH 2 y 5 R=CI, D=CH 2 NH 2 z 5 R=CI, D=CH 2 NH 2 aa 5 R=CI, D=CH 2 NH 2 y 6 R=OMe, D=CH 2 NH 2 z 6 R=OMe, D=CH 2 NH 2 aa 6 R=OMe, D=CH 2 NH 2 y 7 R=F, D=C(=NH)NH 2 z 7 R=F, D=C(=NH)NH 2 aa 7 R=F, D=C(=NH)NH 2 y 8 R=CI, D=C(=NH)NH 2 z 8 R=CI, D=C(=NH)NH 2 aa 8 R=CI, D=C(=NH)NH 2 y 9 R=OMe, D=C(=NH)NH 2 z 9 R=OMe, D=C(=NH)NH 2 aa 9 R=OMe, D=C(=NH)NH 2 yio R=F, D=C(0)NH 2 Z10 R=F, D=C(0)NH 2 aa 10 R=F, D=C(0)NH 2 yii R=CI, D=C(0)NH 2 Z11 R=CI, D=C(0)NH 2 aan R=CI, D=C(0)NH 2 yi2 R=OMe, D=C(0)NH 2 Z12 R=OMe, D=C(0)NH 2 aai2 R=0Me, D=C(0)NH 2 bbi R=F, D=NH 2 cci R=F, D=NH 2 ddi R=F, D=NH 2 bb 2 R=CI, D=NH 2 cc 2 R=CI, D=NH 2 dd 2 R=CI, D=NH 2 bb 3 R=OMe, D=NH 2 cc 3 R=OMe, D=NH 2 dd 3 R=OMe, D=NH 2 bb 4 R=F, D=CH 2 NH 2 cc 4 R=F, D=CH 2 NH 2 dd 4 R=F, D=CH 2 NH 2 bb 5 R=CI, D=CH 2 NH 2 cc 5 R=CI, D=CH 2 NH 2 dd 5 R=CI, D=CH 2 NH 2 bb 6 R=OMe, D=CH 2 NH 2 cc 6 R=OMe, D=CH 2 NH 2 dd 6 R=OMe, D=CH 2 NH 2 bb 7 R=F, D=C(=NH)NH 2 cc 7 R=F, D=C(=NH)NH 2 dd 7 R=F, D=C(=NH)NH 2 bb 8 R=CI, D=C(=NH)NH 2 cc 8 R=CI, D=C(=NH)NH 2 dd 8 R=CI, D=C(=NH)NH 2 bbg R=OMe, D=C(=NH)NH 2 cc 9 R=OMe, D=C(=NH)NH 2 ddg R=OMe, D=C(=NH)NH 2 bb i0 R=F, D=C(0)NH 2 cc 10 R=F, D=C(0)NH 2 ddio R=F, D=C(0)NH 2 bbn R=CI, D=C(0)NH 2 ecu R=CI, D=C(0)NH 2 ddn R=CI, D=C(0)NH 2 bbi2 R=OMe, D=C(0)NH 2 cc i2 R=OMe, D=C(0)NH 2 ddi2 R=OMe, D=C(0)NH 2 eei R=F, D=CH 2 NH 2 ffi R=F, D=CH 2 NH 2 ggi R=F, D=CH 2 NH 2 ee 2 R=CI, D=CH 2 NH 2 ff 2 R=CI, D=CH 2 NH 2 gg 2 R=CI, D=CH 2 NH 2 ee 3 R=OMe, D=CH 2 NH 2 ff 3 R=OMe, D=CH 2 NH2 gg 3 R=OMe, D=CH 2 NH 2 ee 4 R=CH 2 NH 2 , ff 4 R=CH NH 2 , gg 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 hhi R=F, D=CH 2 NH 2 ii-t R=F, D=CH 2 NH 2 jj-i R=F, D=CH 2 NH 2 hh 2 R=CI, D=CH 2 NH 2 ii 2 R=CI, D=CH 2 NH 2 jj 2 R=CI, D=CH 2 NH 2 hh 3 R=OMe, D=CH 2 NH 2 ii 3 R=OMe, D=CH 2 NH 2 jj 3 R=OMe, D=CH 2 NH 2 hh 4 R=CH NH 2 , ii 4 R=CH 2 NH 2 , jj 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 kki R=F, D=CH 2 NH 2 lh R=F, D=CH 2 NH 2 mm-i R=F, D=CH 2 NH 2 kk 2 R=CI, D=CH 2 NH 2 11 2 R=CI, D=CH 2 NH 2 mm 2 R=CI, D=CH 2 NH 2 kk 3 R=OMe, D=CH 2 NH 2 11 3 R=OMe, D=CH 2 NH 2 mm 3 R=OMe, D=CH 2 NH 2 kk 4 R=CH 2 NH 2 , 11 4 R=CH 2 NH 2 , mm 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 nni R=F, D=CH 2 NH 2 001 R=F, D=CH 2 NH 2 PP 1 R=F, D=CH 2 NH 2 nn 2 R=CI, D=CH 2 NH 2 00 2 R=CI, D=CH 2 NH 2 pp 2 R=CI, D=CH 2 NH 2 nn 3 R=OMe, D=CH 2 NH 2 00 3 R=OMe, D=CH 2 NH 2 pp 3 R=OMe, D=CH 2 NH 2 nn 4 R=CH 2 NH 2 , 00 4 R=CH 2 NH 2 , pp R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 qqi R=F, D=CH 2 NH 2 rri R=F, D=CH 2 NH 2 ssi R=F, D=CH 2 NH 2 qq 2 R=CI, D=CH 2 NH 2 rr 2 R=CI, D=CH 2 NH 2 ss 2 R=CI, D=CH 2 NH 2 qq 3 R=OMe, D=CH 2 NH 2 rr 3 R=OMe, D=CH 2 NH2 ss 3 R=OMe, D=CH 2 NH 2 qq 4 R=CH 2 NH 2 , rr 4 R=CH 2 NH 2 , ss 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 Ex# R lb 1 H phenyl 2 - ( aminosul f onyl ) phenyl 2 H phenyl 2- (methylaminosulfonyl ) phenyl 3 H phenyl 1-pyrrolidinocarbonyl 4 H phenyl 2- (methylsulf onyl ) phenyl 5 H phenyl 4-morpholino 6 H phenyl 2 - ( 1 ' -CF3 -tetrazol-2 -yl ) phenyl 7 H phenyl 4-morpholinocarbonyl 8 H 2-pyridyl 2- (aminosulfonyl ) phenyl 9 H 2-pyridyl 2- (methylaminosulfonyl ) phenyl 10 H 2-pyridyl 1-pyrrolidinocarbonyl 11 H 2-pyridyl 2- (methylsulf onyl ) henyl 12 H 2 -pyridyl 4 -mo rpho 1 ino H 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl H 2-pyridyl 4-morpholinocarbonyl H 3-pyridyl 2- (aminosulfonyl) phenyl H 3-pyridyl 2- (methylaminosulfonyl) phenyl H 3-pyridyl 1-pyrrolidinocarbonyl H 3-pyridyl 2- (methylsulfonyl) phenyl H 3 -pyridyl 4-morpholino H -pyridyl 2 - (l' " -CF3-tetrazol-2-yDphenyl H 3-pyridyl 4-morpholinocarbonyl H 2-pyrimidyl 2- (aminosulfonyl) phenyl H 2-pyrimidyl 2- (methylaminosulfonyl) phenyl H 2-pyrimidyl 1-pyrrolidinocarbonyl H 2-pyrimidyl 2- (methylsulfonyl) phenyl H 2-pyrimidyl 4-morpho1ino H 2-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl H 2-pyrimidyl 4-morpholinocarbonyl H 5-pyrimidyl 2- (aminosulfonyl) phenyl H 5-pyrimidyl 2- (methylaminosulfonyl) phenyl H 5-pyrimidyl 1-pyrrolidinocarbonyl H 5-pyrimidyl 2- (methylsulfonyl) phenyl H 5-pyrimidyl 4-morpholino H 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl H 5-pyrimidyl 4-morpholinocarbonyl H 2-Cl-phenyl 2- (aminosulfonyl ) phenyl H 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl H 2-Cl-phenyl 1-pyrro1idinocarbony1 H 2-Cl-phenyl 2- (methylsulfonyl) phenyl H 2-Cl-phenyl 4-morpholino H 2-Cl-phenyl 2- (1 ' -CF3-tetrazol-2-yl)phenyl H 2-Cl-phenyl 4-morpholinocarbonyl H 2-F-phenyl 2- (aminosulfonyl) phenyl H 2-F-phenyl 2- (methylaminosulfonyl ) phenyl H 2-F-phenyl 1-pyrro1idinocarbonyl H 2-F-phenyl 2- (methylsulfonyl) phenyl H 2-F-phenyl 4-morpholino H 2-F-phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl H 2-F-phenyl 4-morpholinocarbonyl H 2,5-diF-phenyl 2- (aminosulfonyl) phenyl H 2 , 5-diF-phenyl 2- (methylaminosulfonyl) phenyl H 2, 5-diF-phenyl 1-pyrrolidinocarbonyl H 2 , 5-diF-phenyl 2- (methylsulfonyl) phenyl H 2,5-diF-phenyl 4-morpholino H 2,5-diF-phenyl 2- (1' -CF3-tetrazol-2-yDphenyl H 2,5-diF-phenyl 4-morpholinocarbonyl -CN phenyl 2- (aminosulfonyl) phenyl -CN phenyl 2- (methylaminosulfonyl) phenyl -CN phenyl 1-pyrro1idinocarbonyl -CN phenyl 2- (methylsulfonyl) phenyl -CN phenyl 4-morpholino -CN phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl -CN phenyl 4-morpholinocarbonyl -CN 2-pyridyl 2- (aminosulfonyl) phenyl -CN 2-pyridyl 2- (methylaminosulfonyl) phenyl -CN 2-pyridyl 1-pyrrolidinocarbonyl -CN 2-pyridyl 2- (methylsulfonyl) phenyl -CN 2-pyridyl 4-morpholino -CN 2-pyridyl 2- (1' -CF3-tetrazol-2-yl) phenyl -CN 2-pyridyl 4-morpholinocarbonyl -CN 3-pyridyl 2- (aminosulfonyl ) phenyl -CN 3-pyridyl 2- (methylaminosulfonyl) phenyl -CN 3-pyridyl 1-pyrrolidinocarbonyl -CN 3-pyridyl 2- (methylsulfonyl) phenyl -CN 3-pyridyl 4-morpholino -CN 3-pyridyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl -CN 3-pyridyl 4-morpholinocarbony1 -CN 2-pyrimidyl 2- (aminosulfonyl ) phenyl -CN 2-pyrimidyl 2- (methylaminosulfonyl) phenyl -CN 2-pyrimidyl 1-pyrrolidinocarbonyl -CN 2-pyrimidyl 2- (methylsulfonyl) phenyl -CN 2-pyrimidyl 4-morpholino -CN 2-pyrimidyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl -CN 2-pyrimidyl 4-morpholinocarbonyl -CN 5-pyrimidyl 2- (aminosulfonyl) phenyl -CN 5-pyrimidyl 2- (methylaminosulfonyl) phenyl -CN 5-pyrimidyl 1-pyrrolidinocarbonyl -CN 5-pyrimidyl 2- (methylsulfonyl) phenyl -CN 5-pyrimidyl 4-morpholino -CN 5-pyrimidyl 2- (1' -CF3 -tetrazol-2-yDphenyl -CN 5-pyrimidyl 4-morpholinocarbonyl -CN 2-Cl-phenyl 2- (aminosulfonyl) phenyl -CN 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl -CN 2-Cl-phenyl 1-pyrrolidinocarbonyl -CN 2-Cl-phenyl 2- (methylsulfonyl) p enyl -CN 2-Cl-phenyl 4-morpholino -CN 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl -CN 2-Cl-phenyl 4-morpholinocarbonyl -CN 2-F-phenyl 2- (aminosulfonyl ) phenyl -CN 2-F-phenyl 2- (methylaminosulfonyl)phenyl -CN 2-F-phenyl 1-pyrrolidinocarbonyl -CN 2-F-phenyl 2- (methylsulfonyl) phenyl -CN 2-F-phenyl 4-morpho1ino -CN 2-F-phenyl 2- (1' -CF3-tetrazol-2-yl)phenyl -CN 2-F-phenyl 4-morpholinocarbonyl -CN 2,5-diF-phenyl 2- (aminosulfonyl) phenyl -CN 2, 5-diF-phenyl 2- (methylaminosulfonyl) phenyl -CN 2, 5-diF-phenyl 1-pyrrolidinocarbonyl -CN 2,5-diF-phenyl 2- (methylsulfonyl) phenyl -CN 2,5-diF-phenyl 4-morpholino -CN 2,5-diF-phenyl 2- (1 ' -CF3 -tetrazol-2-yl ) phenyl -CN 2,5-diF-phenyl 4-morpholinocarbony1 CF 3 phenyl 2- (aminosulfonyl ) phenyl CF 3 phenyl 2- (methylaminosulfonyl) phenyl CF 3 phenyl 1-pyrrolidinocarbony1 CF 3 phenyl 2- (methylsulfonyl) phenyl CF 3 phenyl 4-morpholino CF 3 phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl CF 3 phenyl 4-morpholinocarbonyl CF 3 2-pyridyl 2- (aminosulfony1) phenyl CF 3 2-pyridyl 2- (methylaminosulfonyl) phenyl CF 3 2-pyridyl 1-pyrrolidinocarbonyl CF 3 2-pyridyl 2- (methylsulfonyl) phenyl 124 CF 3 2-pyridyl 4-morpholino 125 CF 3 2-pyridyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 126 CF 3 2-pyridyl 4-morpholinocarbonyl 127 CF 3 3 -pyridyl 2- (aminosulfonyl) henyl 128 CF 3 3 -pyridyl 2- (methylaminosulfonyl) phenyl 129 CF 3 3-pyridyl 1-pyrrolidinocarbonyl 130 CF 3 3 -pyridyl 2- (methylsulfonyl) phenyl 131 CF 3 3 -pyridyl 4-morpholino 132 CF 3 3-pyridyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 133 CF 3 3-pyridyl 4-morpho1inocarbony1 134 CF 3 2-pyrimidyl 2- (aminosulfonyl ) henyl 135 CF 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 136 CF 3 2-pyrimidyl 1-pyrro1idinocarbonyl 137 CF 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 138 CF 3 2-pyrimidyl 4-morpholino 139 CF 3 2-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 140 CF 3 2-pyrimidyl 4-morpholinocarbonyl 141 CF 3 5-pyrimidyl 2- (aminosulfonyl) phenyl 142 CF 3 5-pyrimidyl 2- (methylaminosulfonyl ) phenyl 143 CF 3 5-pyrimidyl 1-pyrrolidinocarbonyl 144 CF 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 145 CF 3 5-pyrimidyl 4-morpholino 146 CF 3 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 147 CF 3 5-pyrimidyl 4-morpholinocarbonyl 148 CF 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 149 CF 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 150 CF 3 2-Cl-phenyl 1-pyrro1idinocarbonyl 151 CF 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 152 CF 3 2-Cl-phenyl 4-morpholino 153 CF 3 2-Cl-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 154 CF 3 2-Cl-phenyl 4-morpholinocarbonyl 155 CF 3 2-F-phenyl 2- (aminosulfonyl) phenyl 156 CF 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 157 CF 3 2-F-phenyl 1-pyrrolidinocarbonyl 158 CF 3 2-F-phenyl 2- (methylsulfonyl) phenyl 159 CF 3 2-F-phenyl 4-morpholino 160 CF 3 2-F-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl ) phenyl 161 CF 3 2-F-phenyl 4-morpholinocarbonyl 162 CF 3 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 163 CF 3 2, 5-diF-phenyl 2- (methylaminosulfonyl) phenyl 164 CF 3 2, 5-diF-phenyl 1-pyrro1idinocarbonyl 165 CF 3 2, 5-diF-phenyl 2- (methylsulfonyl ) phenyl 166 CF 3 2, 5-diF-phenyl 4-morpholino 167 CF 3 2, 5-diF-phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 168 CF 3 2,5-diF-phenyl 4-morpho1inocarbony1 169 CONH 2 phenyl 2- (aminosulfony1 ) phenyl 170 CONH 2 phenyl 2- (methylaminosulfonyl ) phenyl 171 CONH 2 phenyl 1-pyrrolidinocarbonyl 172 CONH 2 phenyl 2- (methylsulfonyl) phenyl 173 CONH 2 phenyl 4-morpholino 174 CONH 2 phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 175 CONH 2 phenyl 4-morpholinocarbonyl 176 CONH 2 2-pyridyl 2- (aminosulfonyl ) phenyl 177 CONH 2 2-pyridyl 2- (methylaminosulfonyl) phenyl 178 CONH 2 2-pyridyl 1-pyrrolidinocarbonyl 179 CONH 2 2 -pyridyl 2- (methyls αlfonyl) phenyl 180 CONH 2 2-pyridyl 4-morpholino 181 CONH 2 2-pyridyl 2 - ( 1 ' -CF3 -tetrazol-2 -yl ) phenyl 182 CONH 2 2-pyridyl 4-morpholinocarbonyl 183 CONH 2 3 -pyridyl 2 - (aminosulfonyl ) phenyl 184 CONH 2 3 -pyridyl 2 - (methylaminosulfonyl ) phenyl 185 CONH 2 3 -pyridyl 1-pyrrolidinocarbonyl 186 CONH 2 3 -pyridyl 2- (methylsulfonyl) phenyl 187 CONH 2 3 -pyridyl 4-morpholino 188 CONH 2 3 -pyridyl 2- (l'-CF3-tetrazol-2 -yl) phenyl 189 CONH 2 3 -pyridyl 4-morpholinocarbonyl 190 CONH 2 2-pyrimidyl 2 - ( aminosulfonyl ) phenyl 191 CONH 2 2 -pyrimidyl 2- (methylaminosulfonyl) phenyl 192 CONH 2 2 -pyrimidyl 1-pyrrolidinocarbonyl 193 CONH 2 2 -pyrimidyl 2- (methylsulfonyl) phenyl 194 CONH 2 2-pyrimidyl 4-morpholino 195 CONH 2 2 -pyrimidyl 2-(l'-CF3-tetrazol-2-yl)phenyl 196 CONH 2 2-pyrimidyl 4-morpholinocarbony1 197 CONH 2 5-pyrimidyl 2- ( aminosulfonyl ) phenyl 198 CONH 2 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 199 CONH 2 5-pyrimidyl 1-pyrrolidinocarbonyl 200 CONH 2 5-pyrimidyl 2- (methylsulfonyl) phenyl 201 CONH 2 5-pyrimidyl 4-morpholino 202 CONH 2 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 203 CONH 2 5-pyrimidyl 4-morpholinocarbonyl 204 CONH 2 2-Cl-phenyl 2- (aminosulfonyl) phenyl 205 CONH 2 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 206 CONH 2 2-Cl-phenyl 1-pyrrolidinocarbonyl 207 CONH 2 2-Cl-phenyl 2- (methylsulfonyl) phenyl 208 CONH 2 2-Cl-phenyl 4-morpholino 209 CONH 2 2-Cl-phenyl 2 - ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 210 CONH 2 2-Cl-phenyl 4-morpholinocarbonyl 211 CONH 2 2-F-phenyl 2- (aminosulfonyl) phenyl 212 CONH 2 2-F-phenyl 2- (methylaminosulfonyl ) phenyl 213 CONH 2 2-F-phenyl 1-pyrro1idinocarbonyl 214 CONH 2 2-F-phenyl 2- (methylsulfonyl) phenyl 215 CONH 2 2-F-phenyl 4-morpholino 216 CONH 2 2-F-phenyl 2- ( l ' -CF 3 -tetrazol-2 -yD phenyl 217 CONH 2 2-F-phenyl 4-morpho1inocarbony1 218 CONH 2 2,5-diF-phenyl 2- (aminosulfonyl) phenyl 219 CONH 2 2,5-diF-phenyl 2 - (methylaminosulfonyl ) phenyl 220 CONH 2 2,5-diF-phenyl 1-pyrro1idinocarbonyl 221 CONH 2 2,5-diF-phenyl 2- (methylsulfonyl) phenyl 222 CONH 2 2,5-diF-phenyl 4-morpholino 223 CONH 2 2, 5-diF-phenyl 2- ( 1 ' -CF3 -tetrazol-2 -yl ) phenyl 224 CONH 2 2, 5-diF-phenyl 4-morpholinocarbonyl 225 SCH 3 phenyl 2- (aminosulfony1 ) phenyl 226 SCH 3 phenyl 2- (methylaminosulfonyl) phenyl 227 SCH 3 phenyl 1-pyrro1idinocarbonyl 228 SCH 3 phenyl 2- (methylsulfonyl) phenyl 229 SCH 3 phenyl 4-morpho1ino 230 SCH 3 phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 231 SCH 3 phenyl 4-morpholinocarbony1 232 SCH 3 2-pyridyl 2- (aminosulfonyl) phenyl 233 SCH 3 2-pyridyl 2- (methylaminosulfonyl ) phenyl 234 SCH 3 2-pyridyl 1-pyrro1idinocarbonyl 235 SCH 3 2-pyridyl 2- (methylsulfonyl) phenyl 236 SCH 3 2-pyridyl 4-morpholino 237 SCH 3 2-pyridyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl 238 SCH 3 2-pyridyl 4-morpholinocarbonyl 239 SCH 3 3-pyridyl 2- (aminosulfonyl) phenyl 240 SCH 3 3-pyridyl 2- (methylaminosulfonyl) phenyl 241 SCH 3 3-pyridyl 1-pyrrolidinocarbonyl 242 SCH 3 3-pyridyl 2- (methylsulfonyl) phenyl 243 SCH 3 3 -pyridyl 4-morpholino 244 SCH 3 3 -pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 245 SCH 3 3-pyridyl 4-morpho1inocarbony1 246 SCH 3 2-pyrimidyl 2- (aminosulfony1 ) henyl 247 SCH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 248 SCH 3 2-pyrimidyl 1-pyrrolidinocarbonyl 249 SCH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 250 SCH 3 2-pyrimidyl 4-morpho1ino 251 SCH 3 2-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 252 SCH 3 2-pyrimidyl 4-morpholinocarbonyl 253 SCH 3 5-pyrimidyl 2- (aminosulfonyl) phenyl 254 SCH 3 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 255 SCH 3 5-pyrimidyl 1-pyrrolidinocarbonyl 256 SCH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 257 SCH 3 5-pyrimidyl 4-morpholino 258 SCH 3 5-pyrimidyl 2-(l'-CF3-tetrazol-2-yl)phenyl 259 SCH 3 5-pyrimidyl 4-morpholinocarbonyl 260 SCH 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 261 SCH 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 262 SCH 3 2-Cl-phenyl 1-pyrrolidinocarbonyl 263 SCH 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 264 SCH 3 2-Cl-phenyl 4-morpholino 265 SCH 3 2-Cl-phenyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl 266 SCH 3 2-Cl-phenyl 4-morpholinocarbonyl 267 SCH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 268 SCH 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 269 SCH 3 2-F-phenyl 1-pyrro1idinocarbonyl 270 SCH 3 2-F-phenyl 2- (methylsulfonyl) phenyl 271 SCH 3 2-F-phenyl 4-morpho1ino 272 SCH 3 2-F-phenyl 2- ( 1 ' -CF3-tetrazol-2-yl) phenyl 273 SCH 3 2-F-phenyl 4-morpholinocarbonyl 274 SCH 3 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 275 SCH 3 2,5-diF-phenyl 2- (methylaminosulfonyl) phenyl 276 SCH 3 2, 5-diF-phenyl 1-pyrro1idinocarbony1 277 SCH 3 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 278 SCH 3 2,5-diF-phenyl 4-morpho1ino 279 SCH 3 2,5-diF-phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 280 SCH 3 2, 5-diF-phenyl 4-morpholinocarbonyl 281 S0 2 CH 3 phenyl 2- (aminosulfonyl) phenyl 282 S0 2 CH 3 phenyl 2- (methylaminosulfonyl) phenyl 283 S0 2 CH 3 phenyl 1-pyrrolidinocarbonyl 284 S0 2 CH 3 phenyl 2- (methylsulfonyl) phenyl 285 S0 2 CH 3 phenyl 4-morpholino 286 SϋCH 3 phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl) phenyl 287 S0 2 CH 3 phenyl 4-morpholinocarbonyl 288 S0 2 CH 3 2-pyridyl 2- (aminosulfony1 ) phenyl 289 S0 2 CH 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 290 S0 2 CH 3 2-pyridyl 1-pyrrolidinocarbonyl 291 S0 2 CH 3 2-pyridyl 2- (methylsulfonyl) phenyl 292 S0 2 CH 3 2-pyridyl 4-morpholino 293 S0 2 CH 3 2-pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 294 S0 2 CH 3 2-pyridyl 4-morpholinocarbonyl 295 S0 2 CH 3 3-pyridyl 2- (aminosulfonyl)phenyl 296 S0 2 CH 3 3-pyridyl 2- (methylaminosulfonyl) phenyl 297 S0 2 CH 3 3-pyridyl 1-pyrro1idinocarbonyl 298 S0CH 3 3-pyridyl 2- (methylsulfonyl) phenyl 299 S0 2 CH 3 3-pyridyl 4-morpholino 300 S0 2 CH 3 3-pyridyl 2 - ( 1 ' -CF3 -tetrazol-2 -yD phenyl 301 S0 2 CH 3 3-pyridyl 4-morpholinocarbonyl 302 S0 2 CH 3 2-pyrimidyl 2- (aminosulfonyl) phenyl 303 S0CH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 304 S0 2 CH 3 2-pyrimidyl 1-pyrro1idinocarbonyl 305 S0 2 CH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 306 S0 2 CH 3 2-pyrimidyl 4-morpholino 307 S0CH 3 2-pyrimidyl 2- (1' -CF3-tetrazol-2-yl) phenyl 308 S0 2 CH 3 2-pyrimidyl 4-morpholinocarbonyl 309 S0 2 CH 3 5-pyrimidyl 2- (aminosulfonyl)phenyl 310 S0 2 CH 3 5-pyrimidyl 2- (methylaminosulfonyl) henyl 311 S0 2 CH 3 5-pyrimidyl 1-pyrro1idinocarbonyl 312 S0 2 CH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 313 S0 2 CH 3 5-pyrimidyl 4-morpho1ino 314 S0 2 CH 3 5-pyrimidyl 2- ( 1 ' -CF3 - tetrazol-2 -yD phenyl 315 S0CH 3 5-pyrimidyl 4-morpholinocarbonyl 316 S0 2 CH 3 2-Cl-phenyl 2- (aminos lfonyl) phenyl 317 S0 2 CH 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 318 S0 2 CH 3 2-Cl-phenyl 1-pyrrolidinocarbonyl 319 S0 2 CH 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 320 S0 2 CH 3 2-Cl-phenyl 4-morpholino 321 S0 2 CH 3 2-Cl-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 322 Sθ 2 CH 3 2-Cl-phenyl 4-morpholinocarbonyl 323 S0 2 CH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 324 S0 2 CH 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 325 S0 2 CH 3 2-F-phenyl 1-pyrro1idinocarbonyl 326 S0 2 CH 3 2-F-phenyl 2- (methylsulfonyl) phenyl 327 S0CH 3 2-F-phenyl 4-morpho1ino 328 S0 2 CH 3 2-F-phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 329 S0 2 CH 3 2-F-phenyl 4-morpholinocarbonyl 330 S0 2 CH 3 2, 5-diF-phenyl 2- (aminosulfonyl) phenyl 331 S0 2 CH 3 2,5-diF-phenyl 2- (methylaminosulfonyl) phenyl 332 S0 2 CH 3 2, 5-diF-phenyl 1-pyrro1idinocarbonyl 333 S0 2 CH 3 2, 5-diF-phenyl 2- (methylsulfonyl) phenyl 334 S0 2 CH 3 2, 5-diF-phenyl 4-morpholino 335 S0CH 3 2, 5-diF-phenyl 2- (1 ' -CF3-tetrazol-2-yl) phenyl 336 S0 2 CH 3 2, 5-diF-phenyl 4-morpholinocarbonyl 337 NHS0 2 CH 3 phenyl 2- (aminosulfonyl ) phenyl 338 NHS0 2 CH 3 phenyl 2- (methylaminosulfonyl) phenyl 339 NHS0 2 CH 3 phenyl 1-pyrrolidinocarbonyl 340 NHS0 2 CH 3 phenyl 2- (methylsulfonyl) phenyl 341 NHS0CH 3 phenyl 4-morpholino 342 NHS0 2 CH 3 phenyl 2- (l'-CF3-tetrazol-2-yl) phenyl 343 NHS0 2 CH 3 phenyl 4-morpholinocarbonyl 344 NHS0 2 CH 3 2-pyridyl 2- (aminosulfonyl ) phenyl 345 NHS0 2 CH 3 2-pyridyl 2- (methylaminosulfonyl) phenyl 346 NHS0 2 CH 3 2-pyridyl 1-pyrro1idinocarbonyl 347 NHS0CH 3 2-pyridyl 2- (methylsulfonyl) phenyl 348 NHS0CH 3 2-pyridyl 4-morpholino 349 NHS0 2 CH 3 2-pyridyl 2- (1 ' -CF3 -tetrazol-2-yl ) phenyl 350 NHS0 2 CH 3 2-pyridyl 4-morpholinocarbonyl 351 NHS0 2 CH 3 3 -pyridyl 2- (aminosulfony1) phenyl 352 NHS0 2 CH 3 3 -pyridyl 2- (methylaminosulfonyl) phenyl 353 NHS0 2 CH 3 3 -pyridyl 1-pyrro1idinocarbonyl 354 NHS0 2 CH 3 3 -pyridyl 2- (methylsulfonyl) phenyl 355 NHS0 2 CH 3 3 -pyridyl 4-morpholino 356 NHS0 2 CH 3 3 -pyridyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 357 NHS0 2 CH 3 3-pyridyl 4-morpholinocarbonyl 358 NHS0 2 CH 3 2-pyrimidyl 2- (aminosulfony1) phenyl 359 NHS0CH 3 2-pyrimidyl 2- (methylaminosulfonyl) phenyl 360 NHS0 2 CH 3 2-pyrimidyl 1-pyrrolidinocarbonyl 361 NHS0 2 CH 3 2-pyrimidyl 2- (methylsulfonyl) phenyl 362 NHS0 2 CH 3 2-pyrimidyl 4-morpholino 363 NHS0 2 CH 3 2-pyrimidyl 2-(l'-CF3-tetrazol-2-yl)phenyl 364 NHS0 2 CH 3 2-pyrimidyl 4-morpholinocarbonyl 365 NHS0 2 CH 3 5-pyrimidyl 2- (aminosulfonyl) phenyl 366 NHS0 2 CH 3 5-pyrimidyl 2- (methylaminosulfonyl) phenyl 367 NHS0CH 3 5-pyrimidyl 1-pyrrolidinocarbonyl 368 NHS0 2 CH 3 5-pyrimidyl 2- (methylsulfonyl) phenyl 369 NHS0 2 CH 3 5-pyrimidyl 4-morpholino 370 NHS0 2 CH 3 5-pyrimidyl 2- ( 1 ' -CF3 -tetrazol-2 -yD phenyl 371 NHS0 2 CH 3 5-pyrimidyl 4-morpholinocarbonyl 372 NHS0 2 CH 3 2-Cl-phenyl 2- (aminosulfonyl) phenyl 373 NHS0 2 CH 3 2-Cl-phenyl 2- (methylaminosulfonyl) phenyl 374 NHS0 2 CH 3 2-Cl-phenyl 1-pyrro1idinocarbonyl 375 NHS0CH 3 2-Cl-phenyl 2- (methylsulfonyl) phenyl 376 NHS0 2 CH 3 2-Cl-phenyl 4-morpholino 377 NHS0CH 3 2-Cl-phenyl 2- (1' -CF3-tetrazol-2-yl) henyl 378 NHS0 2 CH 3 2-Cl-phenyl 4-morpholinocarbonyl 379 NHS0 2 CH 3 2-F-phenyl 2- (aminosulfonyl) phenyl 380 NHS0 2 CH 3 2-F-phenyl 2- (methylaminosulfonyl) phenyl 381 NHS0 2 CH 3 2-F-phenyl 1-pyrro1idinocarbony1 382 NHS0 2 CH 3 2-F-phenyl 2- (methylsulfonyl) phenyl 383 NHS0 2 CH 3 2-F-phenyl 4-morpholino 384 NHS0 2 CH 3 2--F--phenyl 2- (1' -CF3-tetrazol-2-yl) phenyl 385 NHS0 2 CH 3 2- -F- -phenyl 4-morpholinocarbonyl 386 NHS0 2 CH 3 2, ,5- -diF-phenyl 2- (aminosulfonyl) phenyl 387 NHS0 2 CH 3 2, ,5- -diF-phenyl 2- (methylaminosulfonyl) phenyl 388 NHS0 2 CH 3 2, ,5- -diF-phenyl 1-pyrro1idinocarbonyl 389 NHS0 2 CH 3 2, ,5- -diF-phenyl 2- (methylsulfonyl) phenyl 390 NHS0 2 CH 3 2, ,5- -diF-phenyl 4-morpholine 391 NHS0 2 CH 3 2, ,5- -diF-phenyl 2- ( 1 ' -CF3 -tetrazol-2-yl ) phenyl 392 NHS0 2 CH 3 2, ,5- -diF-phenyl 4-morpholinocarbonyl Table 5 a 1 R=F, D=NH 2 bi R=F, D=NH 2 Cι R=F, D=NH 2 a 2 R=H, D=NH 2 b 2 R=H, D=NH 2 c 2 R=H, D=NH 2 a 3 R=F, D=CH 2 NH 2 b 3 R=F, D=CH 2 NH 2 c 3 R=F, D=CH 2 NH 2 a 4 R=H, D=CH 2 NH 2 b 4 R=H, D=CH 2 NH 2 c 4 R=H, D=CH 2 NH 2 a 5 R=F, D=C(=NH)NH 2 b 5 R=F, D=C(=NH)NH 2 c 5 R=F, D=C(=NH)NH 2 a 6 R=H, D=C(=NH)NH 2 b 6 R=H, D=C(=NH)NH 2 c 6 R=H, D=C(=NH)NH 2 a 7 R=F, D=C(0)NH 2 b 7 R=F, D=C(0)NH 2 c 7 R=F, D=C(0)NH 2 a 8 R=H, D=C(0)NH 2 b 8 R=H, D=C(0)NH 2 c 8 R=H, D=C(0)NH 2 di R=F, D=NH 2 ei R=F, D=NH 2 fi R=F, D=NH 2 d 2 R=H, D=NH 2 e 2 R=H, D=NH 2 f 2 R=H, D=NH 2 d 3 R=F, D=CH 2 NH 2 e 3 R=F, D=CH 2 NH 2 f 3 R=F, D=CH 2 NH 2 d 4 R=H, D=CH 2 NH 2 e 4 R=H, D=CH 2 NH 2 f 4 R=H, D=CH 2 NH 2 d 5 R=F, D=C(=NH)NH 2 e 5 R=F, D=C(=NH)NH 2 f 5 R=F, D=C(=NH)NH 2 d 6 R=H, D=C(=NH)NH 2 e 6 R=H, D=C(=NH)NH 2 f 6 R=H, D=C(=NH)NH 2 d 7 R=F, D=C(0)NH 2 e 7 R=F, D=C(0)NH 2 f 7 R=F, D=C(0)NH 2 d 8 R=H, D=C(0)NH 2 e 8 R=H, D=C(0)NH 2 f 8 R=H, D=C(0)NH 2 g 1 R=F, D=NH 2 hi R=F, D=NH 2 1 R=F, D=NH 2 g 2 R=H, D=NH h 2 R=H, D=NH 2 2 R=H, D=NH 2 g 3 R=F, D=CH 2 NH 2 h 3 R=F, D=CH 2 NH 2 3 R=F, D=CH 2 NH 2 g 4 R=H, D=CH 2 NH 2 h 4 R=H, D=CH 2 NH 2 4 R=H, D=CH 2 NH 2 g 5 R=F, D=C(=NH)NH 2 h 5 R=F, D=C(=NH)NH 2 5 R=F, D=C(=NH)NH 2 g 6 R=H, D=C(=NH)NH 2 h 6 R=H, D=C(=NH)NH 2 e R=H, D=C(=NH)NH 2 g 7 R=F, D=C(0)NH 2 h R=F, D=C(0)NH 2 7 R=F, D=C(0)NH 2 g 8 R=H, D=C(0)NH 2 h 8 R=H, D=C(0)NH 8 R=H, D=C(0)NH 2 J1 R=F, D=NH 2 ki R=F, D=NH 2 h R=F, D=NH 2 j 2 R=H, D=NH 2 k 2 R=H, D=NH 2 1 2 R=H, D=NH 2 j 3 R=F, D=CH 2 NH 2 k 3 R=F, D=CH 2 Nh 2 1 3 R=F, D=CH 2 NH 2 j 4 R=H, D=CH 2 NH 2 l< R=H, D=CH 2 NH 2 1 4 R=H, D=CH 2 NH 2 j 5 R=F, D=C(=NH)NH 2 k 5 R=F, D=C(=NH)NH 2 1 5 R=F, D=C(=NH)NH 2 j 6 R=H, D=C(=NH)NH 2 k 6 R=H, D=C(=NH)NH 2 1 6 R=H, D=C(=NH)NH 2 j 7 R=F, D=C(0)NH 2 k 7 R=F, D=C(0)NH 2 1 7 R=F, D=C(0)NH 2 j 8 R=H, D=C(0)NH 2 k 8 R=H, D=C(0)NH 2 1 8 R=H, D=C(0)NH 2 mi R=F, D=NH 2 nι R=F, D=NH 2 oi R=F, D=NH 2 m 2 R=H, D=NH 2 n 2 R=H, D=NH 2 0 2 R=H, D=NH 2 m 3 R=F, D=CH 2 NH 2 n 3 R=F, D=CH 2 NH 2 0 3 R=F, D=CH 2 NH 2 m 4 R=H, D=CH 2 NH 2 n 4 R=H, D=CH 2 NH 2 0 4 R=H, D=CH 2 NH 2 m 5 R=F, D=C(=NH)NH 2 n 5 R=F, D=C(=NH)NH 2 0 5 R=F, D=C(=NH)NH 2 m 6 R=H, D=C(=NH)NH 2 n 6 R=H, D=C(=NH)NH 2 0 6 R=H, D=C(=NH)NH 2 m 7 R=F, D=C(0)NH 2 n 7 R=F, D=C(0)NH 2 0 7 R=F, D=C(0)NH m 8 R=H, D=C(0)NH 2 n 8 R=H, D=C(0)NH 2 0 8 R=H, D=C(0)NH 2 Pi R=F, D=NH 2 qi R=F, D=NH 2 R=F, D= NH 2 p 2 R=CI, D=NH 2 q 2 R=CI, D=NH 2 R=CI, D: :NH 2 p 3 R=OMe, D=NH 2 q 3 R=OMe, D=NH 2 R=OMe, D=NH 2 p 4 R=F, D=CH 2 NH 2 q 4 R=F, D=CH 2 NH 2 R=F, D= CH 2 NH 2 p 5 R=CI, D=CH 2 NH 2 q 5 R=CI, D=CH 2 NH 2 R=CI, D : CH 2 NH 2 p 6 R=OMe, D=CH 2 NH 2 q 6 R=OMe, D=CH 2 NH2 R=OMe, D=CH 2 NH 2 p 7 R=F, D=C(=NH)NH 2 q 7 R=F, D=C(=NH)NH 2 R=F, D= C(=NH)NH 2 p 8 R=CI, D=C(=NH)NH 2 q 8 R=CI, D=C(=NH)NH 2 R=CI, D =C(=NH)NH 2 p 9 R=OMe, D=C(=NH)NH 2 q 9 R=OMe, D=C(=NH)NH 2 R=OMe, D=C(=NH)NH 2 P10 R=F, D=C(0)NH 2 qio R=F, D=C(0)NH 2 10 R=F, D =C(0)NH 2 Pii R=CI, D=C(0)NH 2 qn R=CI, D=C(0)NH 2 n R=CI, D > =C(0)NH 2 P12 R=OMe, D=C(0)NH 2 qi2 R=OMe, D=C(0)NH 2 1 2 R=OMe , D=C(0)NH 2 Si R=F, D=NH 2 ti R=F, D=NH 2 uι R=F, D=NH 2 s 2 R=CI, D=NH 2 t 2 R=CI, D=NH 2 u 2 R=CI, D=NH 2 s 3 R=OMe, D=NH 2 t 3 R=OMe, D=NH 2 u 3 R=OMe, D=NH 2 s 4 R=F, D=CH 2 NH 2 t 4 R=F, D=CH 2 NH 2 u 4 R=F, D=CH 2 NH 2 s 5 R=CI, D=CH 2 NH 2 t 5 R=CI, D=CH 2 NH 2 u 5 R=CI, D=CH 2 NH 2 s 6 R=OMe, D=CH 2 NH 2 t 6 R=OMe, D=CH 2 NH 2 u 6 R=OMe, D^H^h^ s 7 R=F, D=C(=NH)NH 2 t 7 R=F, D=C(=NH)NH 2 u 7 R=F, D=C(=NH)NH 2 s 8 R=CI, D=C(=NH)NH 2 t 8 R=CI, D=C(=NH)NH 2 u 8 R=CI, D=C(=NH)NH 2 s 9 R=OMe, D=C(=NH)NH 2 t 9 R=OMe, D=C(=NH)NH 2 ug R=OMe, D=C(=NH)NH 2 Sιo R=F, D=C(0)NH 2 ti 0 R=F, D=C(0)NH 2 Uιo R=F, D=C(0)NH 2 SH R=CI, D=C(0)NH 2 tn R=CI, D=C(0)NH 2 Uιι R=CI, D=C(0)NH 2 sι 2 R=OMe, D=C(0)NH 2 tι 2 R=OMe, D=C(0)NH 2 uι 2 R=OMe, D=C(0)NH 2 vi R=F, D=NH 2 WT R=F, D=NH 2 xi R=F, D=NH 2 v 2 R=CI, D=NH 2 w 2 R=CI, D=NH 2 x 2 R=CI, D=NH 2 v 3 R=0Me, D=NH 2 w 3 R=OMe, D=NH 2 x 3 R=OMe, D=NH 2 v 4 R=F, D=CH 2 NH 2 w 4 R=F, D=CH 2 NH 2 x 4 R=F, D=CH 2 NH 2 v 5 R=CI, D=CH 2 NH 2 w 5 R=CI, D=CH 2 NH 2 x 5 R=CI, D=CH 2 NH 2 v 6 R=OMe, D=CH 2 NH 2 w 6 R=OMe, D=CH 2 NH 2 x 6 R=OMe, D=CH 2 NH 2 v 7 R=F, D=C(=NH)NH 2 w 7 R=F, D=C(=NH)NH 2 x 7 R=F, D=C(=NH)NH 2 v 8 R=CI, D=C(=NH)NH 2 w 8 R=CI, D=C(=NH)NH 2 x 8 R=CI, D=C(=NH)NH 2 v 9 R=OMe, D=C(=NH)NH 2 w 9 R=OMe, D=C(=NH)NH 2 x 9 R=OMe, D=C(=NH)NH 2 V10 R=F, D=C(0)NH 2 W10 R=F, D=C(0)NH 2 X10 R=F, D=C(0)NH 2 11 R=CI, D=C(0)NH 2 wn R=CI, D=C(0)NH 2 X 1 1 R=CI, D=C(0)NH 2 i2 R=OMe, D=C(0)NH 2 W12 R=OMe, D=C(0)NH 2 x 12 R=OMe, D=C(0)NH 2 yi R=F, D=NH 2 zι R=F, D=NH 2 aai R=F, D=NH 2 y 2 R=CI, D=NH 2 z 2 R=CI, D=NH 2 aa 2 R=CI, D=NH 2 y 3 R=OMe, D=NH 2 z 3 R=OMe, D=NH 2 aa 3 R=OMe, D=NH 2 y 4 R=F, D=CH 2 NH 2 z 4 R=F, D=CH 2 NH 2 aa 4 R=F, D=CH 2 NH 2 y 5 R=CI, D=CH 2 NH 2 z 5 R=CI, D=CH 2 NH 2 aa 5 R=CI, D=CH 2 NH 2 y 6 R=OMe, D=CH 2 NH 2 z 6 R=OMe, D=CH 2 NH 2 aa 6 R=OMe, D=CH 2 NH 2 y 7 R=F, D=C(=NH)NH 2 z 7 R=F, D=C(=NH)NH 2 aa 7 R=F, D=C(=NH)NH 2 y 8 R=CI, D=C(=NH)NH 2 z 8 R=CI, D=C(=NH)NH 2 aa 8 R=CI, D=C(=NH)NH 2 y 9 R=OMe, D=C(=NH)NH 2 z 9 R=OMe, D=C(=NH)NH 2 aa 9 R=OMe, D=C(=NH)NH 2 yio R=F, D=C(0)NH 2 Z 1 0 R=F, D=C(0)NH 2 aaio R=F, D=C(0)NH 2 yn R=CI, D=C(0)NH 2 Z11 R=CI, D=C(0)NH 2 aan R=CI, D=C(0)NH 2 yι 2 R=OMe, D=C(0)NH 2 zι 2 R=0Me, D=C(0)NH 2 aai2 R=OMe, D=C(0)NH 2 bbi R=F, D=NH 2 ccι R=F, D=NH 2 dd 1 R=F, D=NH 2 bb 2 R=CI, D=NH 2 cc 2 R=CI, D=NH 2 dd 2 R=CI, D=NH 2 bb 3 R=OMe, D=NH 2 cc 3 R=OMe, D=NH 2 dd 3 R=OMe, D=NH 2 bb 4 R=F, D=CH 2 NH 2 cc 4 R=F, D=CH 2 NH 2 dd 4 R=F, D=CH 2 NH 2 bb 5 R=CI, D=CH NH 2 cc 5 R=CI, D=CH 2 NH 2 dd 5 R=CI, D=CH 2 NH 2 bb 6 R=OMe, D=CH 2 NH 2 cc 6 R=OMe, D=CH 2 NH 2 dd 6 R=OMe, D=CH NH 2 bb 7 R=F, D=C(=NH)NH 2 cc 7 R=F, D=C(=NH)NH 2 dd 7 R=F, D=C(=NH)NH 2 bb 8 R=CI, D=C(=NH)NH 2 cc 8 R=CI, D=C(=NH)NH 2 dd 8 R=CI, D=C(=NH)NH 2 bbg R=OMe, D=C(=NH)NH 2 cc 9 R=OMe, D=C(=NH)NH 2 dd 9 R=OMe, D=C(=NH)NH 2 bbio R=F, D=C(0)NH 2 CC10 R=F, D=C(0)NH 2 ddio R=F, D=C(0)NH 2 bbn R=CI, D=C(0)NH 2 ecu R=CI, D=C(0)NH 2 ddn R=CI, D=C(0)NH 2 bb i2 R=OMe, D=C(0)NH 2 CC12 R=OMe, D=C(0)NH 2 ddι 2 R=OMe, D=C(0)NH 2 eβ! R=F, D=CH 2 NH 2 ffi R=F, D=CH 2 NH 2 ggi R=F, D=CH 2 NH 2 ee 2 R=CI, D=CH 2 NH 2 ff 2 R=CI, D=CH 2 NH 2 gg 2 R=CI, D-CH 2 NH 2 ee 3 R=OMe, D=CH 2 NH 2 ff 3 R=OMe, D=CH 2 NH2 gg 3 R=OMe, D=CH 2 NH 2 ee 4 R=CH 2 NH 2 , ff 4 R=CH 2 NH 2 , gg 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH NH 2 D=CH 2 NH 2 hhi R=F, D=CH 2 NH 2 ii R=F, D=CH 2 NH 2 jji R=F, D=CH 2 NH 2 hh 2 R=CI, D=CH 2 NH 2 i 2 R=CI, D=CH 2 NH 2 jj 2 R=CI, D=CH 2 NH 2 hh 3 R=OMe, D=CH 2 NH 2 i 3 R=OMe, D=CH 2 NH 2 jj 3 R=OMe, D=CH 2 NH 2 hh 4 R=CH 2 NH 2 , i 4 R=CH 2 NH 2 , jj 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 kki R=F, D=CH 2 NH 2 lh R=F, D=CH 2 NH 2 mmι R=F, D=CH 2 NH 2 kk 2 R=CI, D=CH 2 NH 2 11 2 R=CI, D=CH 2 NH 2 mm 2 R=CI, D=CH 2 NH 2 kk 3 R=OMe, D=CH 2 NH 2 11 3 R=OMe, D=CH 2 NH 2 mm 3 R=OMe, D=CH 2 NH 2 kk 4 R=CH 2 NH 2 , 11 4 R=CH 2 NH 2 , mm 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 nri ! R=F, D=CH 2 NH 2 001 R=F, D=CH 2 NH 2 PPT R=F, D=CH 2 NH 2 nn 2 R=CI, D=CH 2 NH 2 00 2 R=CI, D=CH 2 NH 2 pp 2 R=CI, D=CH 2 NH 2 nn 3 R=OMe, D=CH 2 NH 2 003 R=OMe, D=CH 2 NH 2 pp 3 R=OMe, D=CH 2 NH 2 nn 4 R=CH 2 NH 2 , 004 R=CH 2 NH 2 , pp 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 qqi R=F, D=CH 2 NH 2 rri R=F, D=CH 2 NH 2 ssι R=F, D=CH 2 NH 2 qq 2 R=CI, D=CH 2 NH 2 rr 2 R=CI, D=CH 2 NH 2 ss 2 R=CI, D=CH 2 NH 2 qq 3 R=OMe, D=CH 2 NH 2 rr 3 R=OMe, D=CH 2 NH 2 ss 3 R=OMe, D=CH 2 NH 2 qq 4 R=CH 2 NH 2 , rr 4 R=CH 2 NH 2 , ss 4 R=CH 2 NH 2 , D=CH 2 NH 2 D=CH 2 NH 2 D=CH 2 NH 2 Ex# R"* B 1 H phenyl 2- ( (Me) 2 N-methyl) phenyl 2 H phenyl 2 - ( (Me ) NH-methyl ) phenyl 3 H phenyl 2 - (H 2 N-methyl ) phenyl 4 H phenyl 2 -HOCH 2 -phenyl 5 H 2-F-phenyl 2- ( (Me) 2 N-me thyl ) phenyl 6 H 2-F-phenyl 2 - ( (Me ) NH-methyl ) phenyl 7 H 2-F-phenyl 2 - ( H 2 N-me thy 1 ) phenyl 8 H 2-F-phenyl 2 -HOCH 2 -phenyl 9 H phenyl 2-methylimidazol-l-yl 10 H phenyl 2-ethylimidazol-l-yl 11 H phenyl 2- ( (Me) 2 N-methyl ) imidazol-1-yl 12 H phenyl 2-CH 3 NHS0 2 -imidazol-l-yl H phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2-F-phenyl 2-methylimidazol-l-yl H 2-F-phenyl 2-ethylimidazol-l-yl H 2-F-phenyl 2- ( (Me) N-methyl) imidazol-1-yl H 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl H 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2-Cl-phenyl 2-methylimidazol-l-yl H 2-Cl-phenyl 2-ethylimidazol-l-yl H 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl H 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl H 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl H 2- (Me) 2 -phenyl 2-methylimidazol-l-yl H 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl H 2-(Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl H 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl H 2-(Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl H phenyl N-methylimidazol-2-yl H phenyl 4-methylimidazol-5-yl H phenyl 5-CF 3 -pyrazol-1-yl H 2-F-phenyl N-methylimidazol-2-yl H 2-F-phenyl 4-methylimidazol-5-yl H 2-F-phenyl 5-CF 3 -pyrazol-1-yl H phenyl guanidino H phenyl 2-thiazolin-2-ylamine H phenyl N-methyl-2-imidazolin-2-yl H phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2-yl H phenyl N-methylimidazol-2-ylthiol H phenyl t-butoxycarbonylamine H phenyl (N-pyrrolidino) formylimino H phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino H 2-F-phenyl guanidino H 2-F-phenyl 2-thiazolin-2-ylamine H 2-F-phenyl N-methyl-2-imidazolin-2-yl H 2-F-phenyl N-methyl-1,4,5, 6- tetrahydropyrimid-2-yl H 2-F-phenyl N-methylimidazol-2-ylthio H 2-F-phenyl t-butoxycarbonylamine H 2-F-phenyl (N-pyrrolidino) formylimino H 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino H 2-CH 3 0-phenyl (N-pyrrolidino) formylimino H 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN phenyl 2- ( (Me) 2 N-methyl) henyl -CN phenyl 2- ( (Me) NH-methyl) phenyl -CN phenyl 2- (H 2 N-methyl) phenyl -CN phenyl 2-HOCH 2 -phenyl -CN 2-F-phenyl 2- ( (Me) N-methyl) phenyl -CN 2-F-phenyl 2- ( (Me) NH-methyl) phenyl -CN 2-F-phenyl 2- (H 2 N-methyl) phenyl -CN 2-F-phenyl 2-HOCH 2 -phenyl -CN phenyl 2-methylimidazol-l-yl -CN phenyl 2-ethylimidazol-l-yl -CN pheryl 2 - ( (Me) N-methyl ) imidazol-1-yl -CN pheryl 2-CH 3 S0 2 -imidazol-l-yl -CN phenyl 2 -CH 3 OCH 2 - imidazol -1-yl -CN 2-F-phenyl 2-methylimidazol-l-yl -CN 2-F-phenyl 2-ethylimidazol-l-yl -CN 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl -CN 2-F-phenyl 2-CH 3 S0 2 -imidazol-1-yl -CN 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN 2-Cl-phenyl 2-methylimidazol-l-yl -CN 2-Cl-phenyl 2-ethylimidazol-l-yl -CN 2-Cl-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl -CN 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-1-yl -CN 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl -CN 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl -CN 2-(Me) 2 N-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl -CN 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl -CN 2-(Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl -CN phenyl N-methylimidazol-2-yl -CN phenyl 4-methylimidazol-5-yl -CN phenyl 5-CF 3 -pyrazol-1-yl -CN 2-F-phenyl N-methylimidazol-2-yl -CN 2-F-phenyl 4-methylimidazol-5-yl -CN 2-F-phenyl 5-CF 3 -pyrazol-1-yl -CN phenyl guanidino -CN phenyl 2-thiazolin-2-ylamine -CN phenyl N-methyl-2-imidazolin-2-yl -CN phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl -CN phenyl N-methylimidazol-2-ylthiol -CN phenyl t-butoxycarbonylamine -CN phenyl (N-pyrrolidino) formylimino -CN phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN 2-F-phenyl guanidino -CN 2-F-phenyl 2-thiazolin-2-ylamine -CN 2-F-phenyl N-methyl-2-imidazolin-2-yl -CN 2-F-phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl -CN 2-F-phenyl N-methylimidazol-2-ylthio -CN 2-F-phenyl t-butoxycarbonylamine -CN 2-F-phenyl (N-pyrrolidino) formylimino -CN 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino -CN 2-CH 3 0-phenyl (N-pyrrolidino) formylimino -CN 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino CF 3 phenyl 2- ( (Me) 2 N-methyl) phenyl CF 3 phenyl 2- ( (Me) NH-methyl ) phenyl CF 3 phenyl 2- (H 2 N-methyl ) phenyl CF 3 phenyl 2-HOCH 2 -phenyl CF 3 2-F-phenyl 2- ( (Me) 2 N-methyl ) phenyl CF 3 2-F-phenyl 2- ( (Me) NH-methyl) phenyl CF 3 2-F-phenyl 2- (H 2 N-methyl) phenyl 112 CF 3 2-F-phenyl 2-HOCH2-phenyl 113 CF 3 phenyl 2-methylimidazol-l-yl 114 CF 3 phenyl 2-ethylimidazol-l-yl 115 CF 3 phenyl 2-( (Me) 2N-methyl) imidazol-1-yl 116 CF 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 117 CF 3 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 118 CF 3 2-F-phenyl 2-methylimidazol-l-yl 119 CF 3 2-F-phenyl 2-ethylimidazol-l-yl 120 CF 3 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 121 CF 3 2-F-phenyl 2 -CH 3 S0 2 -imidazol-1-yl 122 CF 3 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 123 CF 3 2-Cl-phenyl 2-methylimidazol-l-yl 124 CF 3 2-Cl-phenyl 2-ethylimidazol-l-yl 125 CF 3 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 126 CF 3 2-Cl-phenyl 2-CH 3 S0 -imidazol-l-yl 127 CF 3 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 128 CF 3 2-(Me) 2 N-phenyl 2-methylimidazol-l-yl 129 CF 3 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl 130 CF 3 2- (Me) 2N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 131 CF 3 2- (Me) 2N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 132 CF 3 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 133 CF 3 phenyl N-methylimidazol-2 -yl 134 CF 3 phenyl 4-methylimidazol-5-yl 135 CF 3 phenyl 5-CF 3 -pyrazol-1-yl 136 CF 3 2-F-phenyl N-methylimidazol-2-yl 137 CF 3 2-F-phenyl 4-methylimidazol-5-yl 138 CF 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 139 CF 3 phenyl guanidino 140 CF 3 phenyl 2-thiazolin-2-ylamine 141 CF 3 phenyl N-methyl-2-imidazolin-2-yl 142 CF 3 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2 -yl 143 CF 3 phenyl N-methylimidazol-2-ylthiol 144 CF 3 phenyl t-butoxycarbonylamine 145 CF 3 phenyl (N-pyrrolidino) formylimino 146 CF 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 147 CF 3 2-F-phenyl guanidino 148 CF 3 2-F-phenyl 2-thiazolin-2 -ylamine 149 CF 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 150 CF 3 2-F-phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 151 CF 3 2-F-phenyl N-methylimidazol-2-ylthio 152 CF 3 2-F-phenyl t-butoxycarbonylamine 153 CF 3 2-F-phenyl (N-pyrrolidino) formylimino 154 CF 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 155 CF 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 156 CF 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 157 CONH2 phenyl 2- ( (Me) 2N-methyl) phenyl 158 CONH2 phenyl 2- ( (Me) NH-methyl) phenyl 159 CONH 2 phenyl 2- (H 2 N-methyl) phenyl 160 CONH 2 phenyl 2-HOCH 2 -phenyl 161 CONH 2-F-phenyl 2- ( (Me) 2 N-methyl)phenyl 162 CONH 2 2-F-phenyl 2- ( (Me) NH-methyl) phenyl 163 CONH 2 2-F-phenyl 2- (H 2 N-methyl) phenyl 164 CONH 2 2-F-phenyl 2-HOCH 2 -phenyl 165 CONH 2 phenyl 2-methylimidazol-l-yl 166 CONH 2 phenyl 2-ethylimidazol-l-yl 167 CONH 2 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 168 CONH 2 phenyl 2-CH 3 S0 2 -imidazol-l-yl 169 CONH 2 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 170 CONH 2 2-F-phenyl 2-methylimidazol-l-yl 171 CONH 2 2-F-phenyl 2-ethylimidazol-l-yl 172 CONH 2 2-F-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 173 CONH 2 2-F-phenyl 2-CH 3 S0 2 -imidazol-1-yl 174 CONH 2 2-F-phenyl 2-CH 3 OCH 2 -imidazol-1-yl 175 CONH 2 2-Cl-phenyl 2-methylimidazol-l-yl 176 CONH 2 2-Cl-phenyl 2-ethylimidazol-l-yl 177 CONH 2 2-Cl-phenyl 2- ( (Me) N-methyl) imidazol-1-yl 178 CONH 2 2-Cl-phenyl 2-CH 3 S0 -imidazol-l-yl 179 CONH 2 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 180 CONH 2-(Me) 2 N-phenyl 2-methylimidazol-l-yl 181 CONH 2 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl 182 CONH 2 2- (Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 183 CONH 2 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazoi-l-yl 184 CONH 2 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 185 CONH 2 phenyl N-methylimidazol-2-yl 186 CONH 2 phenyl 4-methylimidazol-5-yl 187 CONH 2 phenyl 5-CF 3 -pyrazol-1-yl 188 CONH 2 2-F-phenyl N-methylimidazol-2-yl 189 CONH 2 2-F-phenyl 4-methylimidazol-5-yl 190 CONH 2 2-F-phenyl 5-CF 3 -pyrazol-1-yl 191 CONH 2 phenyl guanidino 192 CONH 2 phenyl 2-thiazolin-2-ylamine 193 CONH 2 phenyl N-methyl-2-imidazolin-2-yl 194 CONH 2 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 195 CONH2 phenyl N-methylimidazol-2-ylthiol 196 CONH 2 phenyl t-butoxycarbonylamine 197 CONH 2 phenyl (N-pyrrolidino) formylimino 198 CONH 2 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 199 CONH 2 2-F-phenyl guanidino 200 CONH 2 2-F-phenyl 2-thiazolin-2-ylamine 201 CONH 2 2-F-phenyl N-methyl-2-imidazolin-2-yl 202 CONH 2 2-F-phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 203 CONH 2 2-F-phenyl N-methylimidazol-2-ylthio 204 CONH 2 2-F-phenyl t-butoxycarbonylamine 205 CONH 2 2-F-phenyl (N-pyrrolidino) formylimino 206 CONH 2 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 207 CONH 2 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 208 CONH 2 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 209 SCH 3 phenyl 2- ( (Me) 2 N-methyl ) phenyl 210 SCH 3 phenyl 2- ( (Me) NH-methyl) phenyl 211 SCH 3 phenyl 2- (H 2 N-methyl) phenyl 212 SCH 3 phenyl 2-HOCH 2 -phenyl 213 SCH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) phenyl 214 SCH 3 2-F-phenyl 2- ( (Me) NH-methyl ) phenyl 215 SCH 3 2-F-phenyl 2- (H 2 N-methyl ) phenyl 216 SCH 3 2-F-phenyl 2-HOCH 2 -phenyl 217 SCH 3 phenyl 2-methylimidazol-l-yl 218 SCH 3 phenyl 2-ethylimidazol-l-yl 219 SCH 3 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 220 SCH 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 221 SCH 3 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 222 SCH 3 2-F-phenyl 2-methylimidazol-l-yl 223 SCH 3 2-F-phenyl 2-ethylimidazol-l-yl 224 SCH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 225 SCH 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 226 SCH 3 2-F-phenyl 2-CH 3 OCH 2 -imidazol-1-yl 227 SCH 3 2-Cl-phenyl 2-methylimidazol-l-yl 228 SCH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 229 SCH 3 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 230 SCH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl 231 SCH 3 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 232 SCH 3 2- (Me) 2 N-phenyl 2-methylimidazol-l-yl 233 SCH 3 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl 234 SCH 3 2- (Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 235 SCH 3 2-(Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 236 SCH 3 2- (Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 237 SCH 3 phenyl N-methylimidazol-2-yl 238 SCH 3 phenyl 4-methylimidazol-5-yl 239 SCH 3 phenyl 5-CF 3 -pyrazol-1-yl 240 SCH 3 2-F-phenyl N-methylimidazol-2-yl 241 SCH 3 2-F-phenyl 4-methylimidazol-5-yl 242 SCH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 243 SCH 3 phenyl guanidino 244 SCH 3 phenyl 2-thiazolin-2-ylamine 245 SCH 3 phenyl N-methyl-2-imidazolin-2-yl 246 SCH 3 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-y1 247 SCH 3 phenyl N-methylimidazol-2-ylthiol 248 SCH 3 phenyl t-butoxycarbonylamine 249 SCH 3 phenyl (N-pyrrolidino) formylimino 250 SCH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 251 SCH 3 2-F-phenyl guanidino 252 SCH 3 2-F-phenyl 2-thiazolin-2 -ylamine 253 SCH 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 254 SCH 3 2-F-phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 255 SCH 3 2-F-phenyl N-methylimidazol-2-ylthio 256 SCH 3 2-F-phenyl t-butoxycarbonylamine 257 SCH 3 2-F-phenyl (N-pyrrolidino) formylimino 258 SCH 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 259 SCH 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 260 SCH 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 261 S0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl) phenyl 262 S0 2 CH 3 phenyl 2- ( (Me) NH-methyl) phenyl 263 S0 2 CH 3 phenyl 2- (H 2 N-methyl) phenyl 264 S0 2 CH 3 phenyl 2-HOCH -phenyl 265 S0 2 CH 3 2-F-phenyl 2- ( (Me) 2 N-methy1 ) phenyl 266 S0 2 CH 3 2-F-phenyl 2- ( (Me) NH-methyl ) phenyl 267 S0 2 CH 3 2-F-phenyl 2- (H 2 N-methyl) phenyl 268 S0 2 CH 3 2-F-phenyl 2-HOCH 2 -phenyl 269 S0 2 CH 3 phenyl 2-methylimidazol-1-yl 270 S0 2 CH 3 phenyl 2-ethylimidazol-l-yl 271 S0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 272 S0 2 CH 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 273 S0 2 CH 3 phenyl 2-CH 3 OCH 2 -imidazol-l-yl 274 S0 2 CH 3 2-F-phenyl 2-methylimidazol-l-yl 275 S0 2 CH 3 2-F-phenyl 2-ethylimidazol-l-yl 276 S0 2 CH 3 2-F-phenyl 2-( (Me) 2 N-methyl) imidazol-1-yl 277 S0 2 CH 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 278 S0 2 CH 3 2-F-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 279 S0CH 3 2-Cl-phenyl 2-methylimidazol-l-yl 280 S0 2 CH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 281 S0 2 CH 3 2-Cl-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 282 S0 2 CH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-1-yl 283 S0 2 CH 3 2-Cl-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 284 S0 2 CH 3 2- (Me) 2N-phenyl 2-methylimidazol-1-yl 285 S0CH 3 2- (Me) 2 N-phenyl 2-ethylimidazol-l-yl 286 S0 2 CH 3 2-(Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 287 S0 2 CH 3 2-(Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-l-yl 288 S0 2 CH 3 2-(Me) 2 N-phenyl 2-CH 3 OCH 2 -imidazol-l-yl 289 S0 2 CH 3 phenyl N-methylimidazol-2-yl 290 S0 2 CH 3 phenyl 4-methylimidazol-5-yl 291 S0 2 CH 3 phenyl 5-CF 3 -pyrazol-1-yl 292 S0 2 CH 3 2-F-phenyl N-methylimidazol-2-yl 293 S0 2 CH 3 2-F-phenyl 4-methylimidazol-5-yl 294 S0 2 CH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 295 S0 2 CH 3 phenyl guanidino 296 S0 2 CH 3 phenyl 2-thiazolin-2-ylamine 297 S0 2 CH 3 phenyl N-methyl-2-imidazolin-2-yl 298 S0 2 CH 3 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-y1 299 S0 2 CH 3 phenyl N-methylimidazol-2-ylthiol 300 S0 2 CH 3 phenyl t-butoxycarbonylamine 301 S0 2 CH 3 phenyl (N-pyrrolidino) formylimino 302 S0 2 CH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 303 S0CH 3 2-F-phenyl guanidino 304 S0 2 CH 3 2-F-phenyl 2-thiazolin-2-ylamine 305 S0 2 CH 3 2-F-phenyl N-methyl-2-imidazolin-2-yl 306 S0 2 CH 3 2-F-phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-yl 307 S0 2 CH 3 2-F-phenyl N-methylimidazol-2-ylthio 308 S0 2 CH 3 2-F-phenyl t-butoxycarbonylamine 309 S0 2 CH 3 2-F-phenyl (N-pyrrolidino) formylimino 310 S0 2 CH 3 2-F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 311 S0 2 CH 3 2-CH 3 0-phenyl (N-pyrrolidino) formylimino 312 S0 2 CH 3 2-CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 313 NHSθ 2 CH 3 phenyl 2- ( (Me) 2 N-methyl) phenyl 314 NHS0 2 CH 3 phenyl 2- ( (Me)NH-methyl) henyl 315 NHS0 2 CH 3 phenyl 2- (H 2 N-methyl ) phenyl 316 NHS0CH 3 phenyl 2-H0CH 2 -phenyl 317 NHS0CH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) phenyl 318 NHS0 2 CH 3 2-F-phenyl 2- ( (Me) NH-methyl) henyl 319 NHS0CH 3 2-F-phenyl 2- (H 2 N-methyl ) phenyl 320 NHS0CH 3 2-F-phenyl 2-H0CH 2 -phenyl 321 NHS0 2 CH 3 phenyl 2-methylimidazol-l-yl 322 NHS0 2 CH 3 phenyl 2-ethylimidazol-l-yl 323 NHS0 2 CH 3 phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 324 NHS0CH 3 phenyl 2-CH 3 S0 2 -imidazol-l-yl 325 NHS0CH 3 phenyl 2-CH 3 0CH 2 -imidazol-1-yl 326 NHS0 2 CH 3 2-F-phenyl 2-methylimidazol-l-yl 327 NHS0 2 CH 3 2-F-phenyl 2-ethylimidazol-l-yl 328 NHS0 2 CH 3 2-F-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 329 NHS0 2 CH 3 2-F-phenyl 2-CH 3 S0 2 -imidazol-l-yl 330 NHS0 2 CH 3 2-F-phenyl 2-CH 3 0CH 2 -imidazol-1-yl 331 NHS0 2 CH 3 2-Cl-phenyl 2-methylimidazol-1-yl 332 NHS0 2 CH 3 2-Cl-phenyl 2-ethylimidazol-l-yl 333 NHS0 2 CH 3 2-Cl-phenyl 2-( (Me) N-methyl) imidazol-1-yl 334 NHS0 2 CH 3 2-Cl-phenyl 2-CH 3 S0 2 -imidazol-l-yl 335 NHS0CH 3 2-Cl-phenyl 2-CH 3 0CH 2 -imidazol-l-yl 336 NHSθ 2 CH 3 2-(Me) 2 N-phenyl 2-methylimidazol-l-yl 337 NHS0 2 CH 3 2-(Me) 2 N-phenyl 2-ethylimidazol-l-yl 338 NHSθ 2 CH 3 2-(Me) 2 N-phenyl 2- ( (Me) 2 N-methyl) imidazol-1-yl 339 NHS0 2 CH 3 2- (Me) 2 N-phenyl 2-CH 3 S0 2 -imidazol-1-yl 340 NHS0CH 3 2-(Me) 2 N-phenyl 2-CH 3 0CH 2 -imidazol-1-yl 341 NHS0 2 CH 3 phenyl N-methylimidazol-2-yl 342 NHS0 2 CH 3 phenyl 4-methylimidazol-5-yl 343 NHS0 2 CH 3 phenyl 5-CF 3 -pyrazol-1-yl 344 NHS0 2 CH 3 2-F-phenyl N-methylimidazol-2-yl 345 NHS0 2 CH 3 2-F-phenyl 4-methylimidazol-5-yl 346 NHS0 2 CH 3 2-F-phenyl 5-CF 3 -pyrazol-1-yl 347 NHS0 2 CH 3 phenyl guanidino 348 NHS0 2 CH 3 phenyl 2-thiazolin-2-ylamine 349 NHS0 2 CH 3 phenyl N-methyl-2-imidazolin-2-yl 350 NHS0 2 CH 3 phenyl N-methyl-1,4, 5, 6- tetrahydropyrimid-2-y1 351 NHS0 2 CH 3 phenyl N-methylimidazol-2-ylthiol 352 NHS0 2 CH 3 phenyl t-butoxycarbonylamine 353 NHS0 2 CH 3 phenyl (N-pyrrolidino) formylimino 354 NHS0CH 3 phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 355 NHS0 2 CH 3 2- -F-phenyl guanidino 356 NHS0 2 CH 3 2- -F-phenyl 2-thiazolin-2-ylamine 357 NHS0 2 CH 3 2- -F-phenyl N-methyl-2-imιdazolin-2-yl 358 NHS0 2 CH 3 2- -F-phenyl N-methyl-1, 4,5,6- tetrahydropyrimid-2-yl 359 NHS0 2 CH 3 2- -F-phenyl N-methylimidazol-2-ylthio 360 NHS0CH 3 2- -F-phenyl t-butoxycarbonylamine 361 NHS0 2 CH 3 2- -F-phenyl (N-pyrrolidino) formylimino 362 NHS0 2 CH 3 2- -F-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino 363 NHS0CH 3 2- -CH 3 0-phenyl (N-pyrrolidino) formylimino 364 NHS0 2 CH 3 2- -CH 3 0-phenyl (N-pyrrolidino) formyl-N- (methanesulfamoyl) imino Utility The compounds of this invention are useful as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals. The term "thromboembolic disorders" as used herein includes arterial or venous cardiovascular or cerebrovascular thromboembolic disorders, including, for example, unstable angina, first or recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary and cerebral arterial thrombosis, cerebral embolism, kidney embolisms, and pulmonary embolisms. The anticoagulant effect of compounds of the present invention is believed to be due to inhibition of factor Xa or thrombin. The effectiveness of compounds of the present invention as inhibitors of factor Xa was determined using purified human factor Xa and synthetic substrate. The rate of factor Xa hydrolysis of chromogenic substrate S2222 (Kabi Pharmacia, Franklin, OH) was measured both in the absence and presence of compounds of the present invention. Hydrolysis of the substrate resulted in the release of pNA, which was monitored spectrophotometrically by measuring the increase in absorbance at 405 nM. A decrease in the rate of absorbance change at 405 nm in the presence of inhibitor is indicative of enzyme inhibition. The results of this assay are expressed as inhibitory constant, Ki . Factor Xa determinations were made in 0.10 M sodium phosphate buffer, pH 7.5, containing 0.20 M NaCl, and 0.5 % PEG 8000. The Michaelis constant, K m , for substrate hydrolysis was determined at 25°C using the method of ineweaver and Burk. Values of Ki were determined by allowing 0.2-0.5 nM human factor Xa (Enzyme Research Laboratories, South Bend, IN) to react with the substrate (0.20 ιrιM-1 mM) in the presence of inhibitor. Reactions were allowed to go for 30 minutes and the velocities (rate of absorbance change vs time) were measured in the time frame of 25-30 minutes. The following relationship was used to calculate Ki values: (v 0 -v s )/v s = I/(Ki (1 + S/Kπ ) where : v 0 is the velocity of the control in the absence of inhibitor; v s is the velocity in the presence of inhibitor; I is the concentration of inhibitor; Ki is the dissociation constant of the enzyme : inhibitor complex; S is the concentration of substrate; K m is the Michaelis constant. Using the methodology described above, a number of compounds of the present invention were found to exhibit a Ki of <.15 μM, thereby confirming the utility of the compounds of the present invention as effective Xa inhibitors. The antithrombotic effect of compounds of the present invention can be demonstrated in a rabbit arterio-venous (AV) shunt thrombosis model. In this model, rabbits weighing 2-3 kg anesthetized with a mixture of xylazine (10 mg/kg i.m.) and ketamine (50 mg/kg i.m.) are used A saline-filled AV shunt device is connected between the femoral arterial and the femoral venous cannulae. The AV shunt device consists of a piece of 6-cm tygon tubing which contains a piece of silk thread. Blood will flow from the femoral artery via the AV- shunt into the femoral vein. The exposure of flowing blood to a silk thread will induce the formation of a significant thrombus. After forty minutes, the shunt is disconnected and the silk thread covered with thrombus is weighed. Test agents or vehicle will be given (i.v., i.p., s.c, or orally) prior to the opening of the AV shunt. The percentage inhibition of thrombus formation is determined for each treatment group. The ID50 values (dose which produces 50% inhibition of thrombus formation) are estimated by linear regression. The compounds of formula (I) may also be useful as inhibitors of serine proteases, notably human thrombin, plasma kallikrein and plasmin. Because of their inhibitory action, these compounds are indicated for use in the prevention or treatment of physiological reactions, blood coagulation and inflammation, catalyzed by the aforesaid class of enzymes. Specifically, the compounds have utility as drugs for the treatment of diseases arising from elevated thrombin activity such as myocardial infarction, and as reagents used as anticoagulants in the processing of blood to plasma for diagnostic and other commercial purposes. Some compounds of the present invention were shown to be direct acting inhibitors of the serine protease thrombin py their ability to inhibit the cleavage of small molecule substrates by thrombin in a purified system. In vi tro inhibition constants were determined by the method described by Kettner et al . in J. Biol . Chem . 265, 18289-18297 (1990), herein incorporated by reference. In these assays, thrombin- mediated hydrolysis of the chromogenic substrate S2238 (Helena Laboratories, Beaumont, TX) was monitored spectrophotometrically. Addition of an inhibitor to the assay mixture results in decreased absorbance and is indicative of thrombin inhibition. Human thrombin (Enzyme Research Laboratories, Inc., South Bend, IN) at a concentration of 0.2 nM in 0.10 M sodium phosphate buffer, pH 7.5 , 0.20 M NaCl, and 0.5% PEG 6000, was incubated with various substrate concentrations ranging from 0.20 to 0.02 mM. After 25 to 30 minutes of incubation, thrombin activity was assayed by monitoring the rate of increase in absorbance at 405 nm which arises owing to substrate hydrolysis. Inhibition constants were derived from reciprocal plots of the reaction velocity as a function of substrate concentration using the standard method of Lineweaver and Burk. Using the methodology described above, some compounds of this invention were evaluated and found to exhibit a Ki of less than 15 μm, thereby confirming the utility of the compounds of the present invention as effective Xa inhibitors. The compounds of the present invention can be administered alone or in combination with one or more additional therapeutic agents. These include other anticoagulant or coagulation inhibitory agents, anti-platelet or platelet inhibitory agents, thrombin inhibitors, or thrombolytic or fibrinolytic agents . The compounds are administered to a mammal in a therapeutically effective amount. By "therapeutically effective amount" it is meant an amount of a compound of Formula I that, when administered alone or in combination with an additional therapeutic agent to a mammal, is effective to prevent or ameliorate the thromboembolic disease condition or the progression of the, disease. By "administered in combination" or "combination therapy" it is meant that the compound of Formula I and one or more additional therapeutic agents are administered concurrently to the mammal being treated. When administered in combination each component may be administered at the same time or sequentially in any order at different points in time. Thus, each component may be administered separately but sufficiently closely in time so as to provide the desired therapeutic effect. Other anticoagulant agents (or coagulation inhibitory agents) that may be used in combination with the compounds of this invention include warfarin and heparin, as well as other factor Xa inhibitors such as those described in the publications identified above under Background of the Invention. The term anti-platelet agents (or platelet inhibitory agents) , as used herein, denotes agents that inhibit platelet function such as by inhibiting the aggregation, adhesion or granular secretion of platelets. Such agents include, but are not limited to, the various known non-steroidal anti- inflammatory drugs (NSAIDS) such as aspirin, ibuprofen, naproxen, sulindac, indomethacin, mefenamate, droxicam, diclofenac, sulfinpyrazone, and piroxicam, including pharmaceutically acceptable salts or prodrugs thereof. Of the NSAIDS, aspirin (acetylsalicyclic acid or ASA) , and piroxicam are preferred. Other suitable anti-platelet agents include ticlopidine, including pharmaceutically acceptable salts or prodrugs thereof . Ticlopidine is also a preferred compound since it is known to be gentle on the gastro-intestinal tract in use. Still other suitable platelet inhibitory agents include lib/Ilia antagonists, thromboxane-A2-receptor antagonists and thromboxane-A2-synthetase inhibitors, as well as pharmaceutically acceptable salts or prodrugs thereof. The term thrombin inhibitors (or anti-thrombin agents) , as used herein, denotes inhibitors of the serine protease thrombin. By inhibiting thrombin, various thrombin-mediated processes, such as thrombin-mediated platelet activation (that is, for example, the aggregation of platelets, and/or the granular secretion of plasminogen activator inhibitor-1 and/or serotonin) and/or fibrin formation are disrupted. A number of thrombin inhibitors are known to one of skill in the art and these inhibitors are contemplated to be used in combination with the present compounds. Such inhibitors include, but are not limited to, boroarginine derivatives, boropeptides , heparins, hirudin and argatroban, including pharmaceutically acceptable salts and prodrugs thereof . Boroarginine derivatives and boropeptides include N-acetyl and peptide derivatives of boronic acid, such as C-terminal a-aminoboronic acid derivatives of lysine, ornithine, arginine, homoarginine and corresponding isothiouronium analogs thereof . The term hirudin, as used herein, includes suitable derivatives or analogs of hirudin, referred to herein as hirulogs, such as disulfatohirudin. Boropeptide thrombin inhibitors include compounds described in Kettner et al . , U.S. Patent No. 5,187,157 and European Patent Application Publication Number 293 881 A2, the disclosures of which are hereby incorporated herein by reference. Other suitable boroarginine derivatives and boropeptide thrombin inhibitors include those disclosed in PCT Application Publication Number 92/07869 and European Patent Application Publication Number 471,651 A2 , the disclosures of which are hereby incorporated herein by reference. The term thrombolytics (or fibrinolytic) agents (or thrombolytics or fibrinolytics) , as used herein, denotes agents that lyse blood clots (thrombi) . Such agents include tissue plasminogen activator, anistreplase, urokinase or streptokinase, including pharmaceutically acceptable salts or prodrugs thereof. The term anistreplase, as used herein, refers to anisoylated plasminogen streptokinase activator complex, as described, for example, in European Patent Application No. 028,489, the disclosure of which is hereby incorporated herein by reference herein. The term urokinase, as used herein, is intended to denote both dual and single chain urokinase, the latter also being referred to herein as prourokinase . Administration of the compounds of Formula I of the invention in combination with such additional therapeutic agent, may afford an efficacy advantage over the compounds and agents alone, and may do so while permitting the use of lower doses of each. A lower dosage minimizes the potential of side effects, thereby providing an increased margin of safety. The compounds of the present invention are also useful as standard or reference compounds, for example as a quality standard or control, in tests or assays involving the inhibition of factor Xa. Such compounds may be provided in a commercial kit, for example, for use in pharmaceutical research involving factor Xa. For example, a compound of the present invention could be used as a reference in an assay to compare its known activity to a compound with an unknown activity. This would ensure the experimenter that the assay was being performed properly and provide a basis for comparison, especially if the test compound was a derivative of the reference compound. When developing new assays or protocols, compounds according to the present invention could be used to test their effectiveness . The compounds of the present invention may also be used in diagnostic assays involving factor Xa. For example, the presence of factor Xa in an unknown sample could be determined by addition of chromogenic substrate S2222 to a series of solutions containing test sample and optionally one of the compounds of the present invention. If production of pNA is observed in the solutions containing test sample, but no compound of the present invention, then one would conclude factor Xa was present . Dosaσe and Formulation The compounds of this invention can be administered in such oral dosage forms as tablets, capsules (each of which includes sustained release or timed release formulations) , pills, powders, granules, elixirs, tinctures, suspensions, syrups, and emulsions. They may also be administered in intravenous (bolus or infusion) , intraperitoneal, subcutaneous, or intramuscular form, all using dosage forms well known to those of ordinary skill in the pharmaceutical arts. They can be administered alone, but generally will be administered with a pharmaceutical carrier selected on the basis of the chosen route of administration and standard pharmaceutical practice. The dosage regimen for the compounds of the present invention will, of course, vary depending upon known factors, such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration; the species, age, sex, health, medical condition, and weight of the recipient; the nature and extent of the symptoms; the kind of concurrent treatment; the frequency of treatment; the route of administration, the renal and hepatic function of the patient, and the effect desired. A physician or veterinarian can determine and prescribe the effective amount of the drug required to prevent, counter, or arrest the progress of the thromboembolic disorder. By way of general guidance, the daily oral dosage of each active ingredient, when used for the indicated effects, will range between about 0.001 to 1000 mg/kg of body weight, preferably between about 0.01 to 100 mg/kg of body weight per day, and most preferably between about 1.0 to 20 mg/kg/day. Intravenously, the most preferred doses will range from about 1 to about 10 mg/kg/minute during a constant rate infusion. Compounds of this invention may be administered in a single daily dose, or the total daily dosage may be administered in divided doses of two, three, or four times daily. Compounds of this invention can be administered in intranasal form via topical use of suitable intranasal vehicles, or via transdermal routes, using transdermal skin patches. When administered in the form of a transdermal delivery system, the dosage administration will, of course, be continuous rather than intermittent throughout the dosage regimen. The compounds are typically administered in admixture with suitable pharmaceutical diluents, excipients, or carriers (collectively referred to herein as pharmaceutical carriers) suitably selected with respect to the intended form of administration, that is, oral tablets, capsules, elixirs, syrups and the like, and consistent with conventional pharmaceutical practices . For instance, for oral administration in the form of a tablet or capsule, the active drug component can be combined with an oral, non-toxic, pharmaceutically acceptable, inert carrier such as lactose, starch, sucrose, glucose, methyl callulose, magnesium stearate, dicalcium phosphate, calcium sulfate, mannitol, sorbitol and the like; for oral administration in liquid form, the oral drug components can be combined with any oral, non-toxic, pharmaceutically acceptable inert carrier such as ethanol, glycerol, water, and the like. Moreover, when desired or necessary, suitable binders, lubricants, disintegrating agents, and coloring agents can also be incorporated into the mixture. Suitable binders include starch, gelatin, natural sugars such as glucose or beta-lactose, corn sweeteners, natural and synthetic gums such as acacia, tragacanth, or sodium alginate, carboxymethylcellulose, polyethylene glycol, waxes, and the like. Lubricants used in these dosage forms include sodium oleate, sodium stearate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride, and the like. Disintegrators include, without limitation, starch, methyl cellulose, agar, bentonite, xanthan gum, and the like. The compounds of the present invention can also be administered in the form of liposome delivery systems, such as small unilamellar vesicles, large unilamellar vesicles, and multilamellar vesicles . Liposomes can be formed from a variety of phospholipids, such as cholesterol, stearylamine, or phosphatidylcholines. Compounds of the present invention may also be coupled with soluble polymers as targetable drug carriers. Such polymers can include polyvinylpyrrolidone, pyran copolymer, polyhydroxypropylmethacrylamide-phenol, polyhydroxyethylaspartamidephenol, or polyethyleneoxide- polylysine substituted with palmitoyl residues. Furthermore, the compounds of the present invention may be coupled to a class of biodegradable polymers useful in achieving controlled release of a drug, for example, polylactic acid, polyglycolic acid, copolymers of polylactic and polyglycolic acid, polyepsilon caprolactone, polyhydroxy butyric acid, polyorthoesters, polyacetals, polydihydropyrans , polycyanoacylates , and crosslinked or amphipathic block copolymers of hydrogels. Dosage forms (pharmaceutical compositions) suitable for administration may contain from about 1 milligram to about 100 milligrams of active ingredient per dosage unit. In these pharmaceutical compositions the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition. Gelatin capsules may contain the active ingredient and powdered carriers, such as lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours . Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract. Liquid dosage forms for oral administration can contain coloring and flavoring to increase patient acceptance . In general, water, a suitable oil, saline, aqueous dextrose (glucose) , and related sugar solutions and glycols such as propylene glycol or polyethylene glycols are suitable carriers for parenteral solutions . Solutions for parenteral administration preferably contain a water soluble salt of the active ingredient, suitable stabilizing agents, and if necessary, buffer substances. Antioxidizing agents such as sodium bisulfite, sodium sulfite, or ascorbic acid, either alone or combined, are suitable stabilizing agents. Also used are citric acid and its salts and sodium EDTA. In addition, parenteral solutions can contain preservatives, such as benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol . Suitable pharmaceutical carriers are described in Remington's Pharmaceutical Sciences, Mack Publishing Company, a standard reference text in this field. Representative useful pharmaceutical dosage-forms for administration of the compounds of this invention can be illustrated as follows: Capsules A large number of unit capsules can be prepared by filling standard two-piece hard gelatin capsules each with 100 milligrams of powdered active ingredient, 150 milligrams of lactose, 50 milligrams of cellulose, and 6 milligrams magnesium stearate. Soft Gelatin Capsules A mixture of active ingredient in a digestable oil such as soybean oil, cottonseed oil or olive oil may be prepared and injected by means of a positive displacement pump into gelatin to form soft gelatin capsules containing 100 milligrams of the active ingredient. The capsules should be washed and dried. Tablets Tablets may be prepared by conventional procedures so that the dosage unit is 100 milligrams of active ingredient, 0.2 milligrams of colloidal silicon dioxide, 5 milligrams of magnesium stearate, 275 milligrams of microcrystalline cellulose, 11 milligrams of starch and 98.8 milligrams of lactose. Appropriate coatings may be applied to increase palatability or delay absorption. Inπectable A parenteral composition suitable for administration by injection may be prepared by stirring 1.5% by weight of active ingredient in 10% by volume propylene glycol and water. The solution should be made isotonic with sodium chloride and sterilized. Suspension An aqueous suspension can be prepared for oral administration so that each 5 mL contain 100 mg of finely divided active ingredient, 200 mg of sodium carboxymethyl cellulose, 5 mg of sodium benzoate, 1.0 g of sorbitol solution, U.S. P., and 0.025 L of vanillin. Where the compounds of this invention are combined with other anticoagulant agents, for example, a daily dosage may be about 0.1 to 100 milligrams of the compound of Formula I and about 1 to 7.5 milligrams of the second anticoagulant, per kilogram of patient body weight. For a tablet dosage form, the compounds of this invention generally may be present in an amount of about 5 to 10 milligrams per dosage unit, and the second anti-coagulant in an amount of about 1 to 5 milligrams per dosage unit . Where the compounds of Formula I are administered in combination with an anti-platelet agent, by way of general guidance, typically a daily dosage may be about 0.01 to 25 milligrams of the compound of Formula I and about 50 to 150 milligrams of the anti-platelet agent, preferably about 0.1 to 1 milligrams of the compound of Formula I and about 1 to 3 milligrams of antiplatelet agents, per kilogram of patient body weight . Where the compounds of Formula I are adminstered in combination with thrombolytic agent, typically a daily dosage may be about 0.1 to 1 milligrams of the compound of Formula I, per kilogram of patient body weight and, in the case of the thrombolytic agents, the usual dosage of the thrombolyic agent when administered alone may be reduced by about 70-80% when administered with a compound of Formula I. Where two or more of the foregoing second therapeutic agents are administered with the compound of Formula I, generally the amount of each component in a typical daily dosage and typical dosage form may be reduced relative to the usual dosage of the agent when administered alone, in view of the additive or synergistic effect of the therapeutic agents when administered in combination. Particularly when provided as a single dosage unit, the potential exists for a chemical interaction between the combined active ingredients. For this reason, when the compound of Formula I and a second therapeutic agent are combined in a single dosage unit they are formulated such that although the active ingredients are combined in a single dosage unit, the physical contact between the active ingredients is minimized (that is, reduced). For example, one active ingredient may be enteric coated. By enteric coating one of the active ingredients, it is possible not only to minimize the contact between the combined active ingredients, but also, it is possible to control the release of one of these components in the gastrointestinal tract such that one of these components is not released in the stomach but rather is released in the intestines. One of the active ingredients may also be coated with a material which effects a sustained- release throughout the gastrointestinal tract and also serves to minimize physical contact between the combined active ingredients. Furthermore, the sustained-released component can be additionally enteric coated such that the release of this component occurs only in the intestine. Still another approach would involve the formulation of a combination product in which the one component is coated with a sustained and/or enteric release polymer, and the other component is also coated with a polymer such as a lowviscosity grade of hydroxypropyl methylcellulose (HPMC) or other appropriate materials as known in the art, in order to further separate the active components . The polymer coating serves to form an additional barrier to interaction with the other component. These as well as other ways of minimizing contact between the components of combination products of the present invention, whether administered in a single dosage form or administered in separate forms but at the same time by the same manner, will be readily apparent to those skilled in the art, once armed with the present disclosure. Obviously, numerous modifications and variations of the present invention are possible in light of the above teachings. It is therefore to be understood that within the scope of the appended claims, the invention may be practiced otherwise that as specifically described herein.

Claims: WHAT IS CLAIMED AS NEW AND DESIRED TO BE SECURED BY LETTER PATENT OF UNITED STATES IS: 1. A compound of formula I : I or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein; ring M contains from 0-4 N atoms; D is selected from CN, C (=NR 7 ) NR 8 R 9 , NHC (=NR 7 )NR 8 R 9 , NR 8 CH(=NR 7 ), C(0)NR 8 R 9 , and (CR 8 R 9 ) t NR 8 R 9 ; E is selected from phenyl, 2-pyridyl, 4-pyridyl, pyrimidyl, and piperidinyl substituted with 1 R; R is selected from H, F, Cl, Br, I, OR 3 , SR 3 , CO 2 R 3 , NO 2 , and CH 2 OR 3 , and (CR 8 R 9 ) t NR 8 R 9 ; alternatively, E and R combine to form methylenedioxy or ethylenedioxy; Z is selected from a bond, C 1 - 4 alkylene, (CH 2 ) r O (CH 2 ) , (CH 2 ) r NR 3 (CH 2 ) r , (CH ) r C (0) (CH 2 ) r , (CH 2 ) r C (O) 0 (CH 2 ) r , (CH 2 ) r OC(0) (CH 2 ) r , (CH 2 ) r C (O)NR 3 (CH 2 ) r , (CH 2 ) r R 3 C(0) (CH 2 ) r , (CH 2 ) r OC (0) 0 (CH 2 ) r , (CH 2 ) r OC (0)NR 3 (CH 2 ) r , (CH 2 ) r NR 3 C (0) 0 (CH 2 ) r . (CH 2 )rNR 3 C(0)NR 3 (CH 2 )r, (CH 2 ) r S (0) p (CH 2 ) r , (CH 2 )rS0 2 NR 3 (CH2)r, (CH 2 ) r R 3 S0 2 (CH 2 ) r and (CH2) r N 3 Sθ2NR 3 (CH2)r provided that Z does not form a N- N, N-O, N-S, NCH 2 N, NCH0, or NCH 2 S bond with ring M or group A; R la and R lb are independently absent or selected from -(CH 2 ) r -R 1 ', -CH^CH-R 1 ', NCH 2 R 1 ", OCH2R 1 ", SCH 2 R 1 ". NH(CH 2 ) 2 (CH 2 ) t R 1 ', 0(CH 2 ) 2 (CH 2 ) t R 1' , and S (CH 2 ) 2 (CH 2 ) tR 1 ' ; alternatively, R la and R lb , when attached to adjacent carbon atoms, together with the atoms to which they are attached form a 5-8 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R 4 and which contains from 0-2 heteroatoms selected from the group consisting of N, 0, and S; alternatively, when Z is C(0)NH and R la is attached to a ring carbon adjacent to Z, then R la is a C(0) which replaces the amide hydrogen of Z to form a cyclic imide; R 1 ' is selected from H, Cι_ 3 alkyl, F, Cl , Br, I, -CN, -CHO, (CF 2 ) r CF 3 , (CH 2 ) r OR 2 , NR 2 R 2a , C(0)R 2c , 0C(0)R 2 , (CF 2 ) r C0 2 R 2c , S(0) p R 2b , NR 2 (CH 2 ) r OR 2 , CH (=NR 2c ) NR 2 R 2a , NR 2 C(0)R 2b , NR 2 C(0)NHR 2b , NR 2 C(0) R 2a , OC (0)NR 2a R 2b , C(0)NR 2 R 2a , C(0)NR 2 (CH 2 ) r OR 2 , S0 2 NR 2 R 2a , NR 2 S0 2 R 2b , C 3 _ 6 carbocyclic residue substituted with 0-2 R 4 , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R 4 ; R 1 " is selected from H, CH(CH 2 OR 2 ) 2 , C(0)R 2c , C(0)NR 2 R 2a , S(0)R 2b , S(0) 2 R 2b , and S0NR 2 R 2a ; R 2 , at each occurrence, is selected from H, CF 3 , Cι_ 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R b ; R 2a , at each occurrence, is selected from H, CF , Cχ_ 6 alkyl, benzyl, phenethyl, C 3 - 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2b , at each occurrence, is selected from CF 3 , Cι_ 4 alkoxy, Cι- 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2c , at each occurrence, is selected from CF 3 , OH, C 1 -. 4 alkoxy, Cι- 6 alkyl, benzyl, C 3 _ 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; alternatively, R 2 and R a , together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R b and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; R 3 , at each occurrence, is selected from H, C 1 -. 4 alkyl, and phenyl ,- R 3a , at each occurrence, is selected from H, Cι_ 4 alkyl, and phenyl ; R 3b , at each occurrence, is selected from H, C 1 - 4 alkyl, and phenyl ; R c , at each occurrence, is selected from Cι_ 4 alkyl, and phenyl ; A is selected from: C3- 10 carbocyclic residue substituted with 0-2 R 4 , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4 ; B is selected from: H, Y, and X-Y; X is selected from Cι_ alkylene, -CR 2 (CR 2 R 2b ) (CH 2 ) t -, -C(0)-, -C(=NR ! ")-, -CR 2 (NR 1 "R 2 )-, -CR 2 (OR 2 )-, -CR 2 (SR 2 )-, -C(0)CR 2 R 2a -, -CR 2 R 2a C(0), -S(0) p -, -S (0) p CR 2 R 2a - , -CR 2 R 2a S(0) p -, -S(0) 2 NR 2 -, -NR 2 S(0) 2 -, -NR 2 S (O) 2 CR 2 R 2a - , -CR 2 R 2 S(0) 2 NR 2 -, -NR 2 S(0) 2 NR 2 -, -C(0)NR 2 -, -NR 2 C(0)-, -C(0)NR 2 CR 2 R 2a -, -NR 2 C(0)CR 2 R 2a -, -CR 2 R 2a C (0) NR 2 - , -CR 2 R 2a NR 2 C(0)-, -NR 2 C(0)0-, -0C(0)NR 2 -, -NR 2 C (0) NR 2 - , -NR 2 -, -NR 2 CR 2 R 2a -, -CR 2 R 2a NR 2 -, 0, -CR 2 R 2a 0-, and -0CR 2 R 2a -; Y is selected from: (CH 2 ) r NR 2 R 2a , provided that X-Y do not form a N-N, 0-N, or S-N bond, C 3 _io carbocyclic residue substituted with 0-2 R a , and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4a ; R 4 , at each occurrence, is selected from H, =0, (CH 2 ) r OR 2 , F, Cl, Br, I, Cι_ 4 alkyl, -CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(0)R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , NR 2 C (O) NR 2 R 2a , CH(=NR 2 )NR 2 R 2a , CH(=NS(0) 2 R 5 )NR 2 R 2a , NHC (=NR 2 ) NR 2 R 2a , C(0)NHC(=NR 2 )NR 2 R 2a , S0 2 NR 2 R 2a , NR 2 S0NR 2 R 2 , NR 2 S0 2 -Cι_ alkyl, NR 2 S0 2 R 5 , S(0) P R 5 , (CF 2 ) r CF 3 , NCH 2 R 1 ", OCH 2 R 1 ", SCH 2 R ! \ N(CH 2 ) 2 (CH 2 ) t R 1' , 0 (CH 2 ) 2 (CH 2 ) t 1 ' , and S ( CH 2 ) 2 ( CH 2 ) tR 1' ; alternatively, one R 4 is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R 4a , at each occurrence, is selected from H, =0, (CH 2 ) r 0R 2 , (CH 2 ) r -F, (CH 2 ) r -Br, (CH 2 ) r -Cl, I, C 1 -4 alkyl, -CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r NR 2 R 2b , (CH 2 ) r C (0) R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , C(0)NH(CH 2 ) 2 NR 2 R 2a , NR 2 C (0) NR 2 R 2a , CH(=NR 2 )NR 2 R 2a , NHC (=NR 2 ) NR 2 R 2a . S0NR 2 R 2a , NR 2 S0 2 NR 2 R 2a , NR 2 S0 2 -Cι_ 4 alkyl, C (0)NHS0 2 -Cι_ 4 alkyl, NR 2 S0 2 R 5 , S(0) p R 5 , and (CF 2 ) r CF 3 ; alternatively, one R a is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S and substituted with 0-1 R 5 ; R 4b , at each occurrence, is selected from H, =0, (CH 2 ) r 0R 3 , F, Cl, Br, I, Cι_ 4 alkyl, -CN, N0 2 , (CH 2 ) r NR 3 R 3a , (CH 2 ) r C(0)R 3 , (CH 2 ) r C(0)0R 3c , NR 3 C(0)R 3a , C(0)NR 3 R 3a , NR 3 C(0)NR 3 R 3a , CH(=NR 3 )NR 3 R 3a , NH 3 C (=NR 3 ) NR 3 R 3a , S0 2 NR 3 R 3a , NR 3 S0NR 3 R 3 , NR 3 S0 2 -Cι_ 4 alkyl, NR 3 S0 2 CF 3 , NR 3 S0 2 -phenyl , S(0) P CF 3 , S(0) p -Ci- 4 alkyl, S (0) p -phenyl , and (CF 2 ) r CF 3 ; R 5 , at each occurrence, is selected from CF 3 , Cι_ 6 alkyl, phenyl substituted with 0-2 R 6 , and benzyl substituted with 0-2 R 6 ; R 6 , at each occurrence, is selected from H, OH, (CH 2 ) r 0R 2 , F, Cl, Br, I, C 1 - 4 alkyl, CN, N0 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(0)R 2b , NR 2 C(0)R 2b , NR 2 C (0)NR 2 R 2a , CH(=NH)NH 2 , NHC(=NH)NH 2 , S0 2 NR 2 R 2a , NR 2 S0 2 NR 2 R 2a , and NR 2 S0 2 Cι_ 4 alkyl; R 7 , at each occurrence, is selected from H, OH, Cι_ 6 alkyl, Cι_ 6 alkylcarbonyl , C -β alkoxy, Cι_ 4 alkoxycarbonyl, (CH 2 ) n -phenyl, C 6 -ιo aryloxy, C 6 -ιo aryloxycarbonyl , C 6 -ιo arylmethylcarbonyl , Cι_ 4 alkylcarbonyloxy C 1 -. 4 alkoxycarbonyl, C 6 - 10 arylcarbonyloxy Cι_ 4 alkoxycarbonyl, Cι- alkylaminocarbonyl , phenylaminocarbonyl , and phenyl-Cι_ 4 alkoxycarbonyl; R 8 , at each occurrence, is selected from H, Cι_ 6 alkyl and (CH 2 ) n -phenyl; alternatively, R 7 and R 8 combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, 0, and S; R 9 , at each occurrence, is selected from H, Cι_ 6 alkyl and (CH ) n -phenyl; n is selected from 0, 1, 2, and 3; m is selected from 0, 1, and 2 ; p is selected from 0, 1, and 2 ; r is selected from 0, 1, 2, and 3; s is selected from 0, 1, and 2; and, t is selected from 0 and 1 2. A compound according to Claim 1, wherein the compound is of formulae Ia-Io: wherein : Z is selected from a bond, CH 2 0, OCH 2 , CH 2 NH, NHCH 2 , CH 2 C(0), C(0)CH 2 , C(0)NH, C(0)NH, CH 2 S(0) 2 , S(0) 2 (CH 2 ), S0 2 NH, and S0 2 NH; B is selected from: Y, X-Y, and NR 2 R 2a ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3-oxadiazole, 1,2,4- oxadiazole, 1, 2 , 5-oxadiazole, 1, 3 , 4-oxadiazole, 1,2,3- thiadiazole, 1, 2 , 4-thiadiazole, 1, 2 , 5-thiadiazole, 1,3,4- thiadiazole, 1, 2 , 3-triazole, 1, 2 , 4-triazole, 1,2,5- triazole, 1, 3 , 4-triazole, benzofuran, benzothiofuran, indole, benzimidazole, benzoxazole, benzthiazole, indazole, benzisoxazole, benzisothiazole, and isoindazole; Y may also be selected from the following bicyclic heteroaryl ring systems K is selected from 0, S, NH, and N. 3. A compound according to Claim 2 , wherein the compound is of formulae: wherein : D is selected from C(=NR 7 )NR 8 R 9 and (CR 8 R 9 ) t NR 8 R 9 ; R is selected from H, F, Cl, OR 3 , CH 2 0R 3 , CH 2 NH 2 ; A is selected from: piperidinyl , piperazinyl, C 5 _ 6 carbocyclic residue substituted with 0-2 R 4 , and 5-6 membered heteroaryl containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R 4 ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R 4a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3-oxadiazole, 1,2, 4-oxadiazole, 1, 2, 5-oxadiazole, 1, 3 , 4-oxadiazole, 1,2, 3-thiadiazole, 1, 2 , 4-thiadiazole, 1, 2 , 5-thiadiazole, 1,3, 4-thiadiazole, 1, 2 , 3-triazole, 1, 2, 4-triazole, 1,2,5- triazole, and 1, 3 , 4-triazole. 4. A compound according to Claim 3, wherein: E is phenyl ; D is selected from C(=NH)NH and CH 2 NH ; R is selected from H, F, Cl, and Br; A is selected from: C 5 _ 6 carbocyclic residue substituted with 0-2 R 4 , and 5-6 membered heteroaryl containing from 1-3 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4 ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R a ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1, 2 , 3-oxadiazole, 1, 2 , 4-oxadiazole, 1, 2 , 5-oxadiazole, 1, 3 , 4-oxadiazole, 1, 2, 3-thiadiazole, 1, 2 , 4-thiadiazole, 1, 2 , 5-thiadiazole, 1,3 , 4-thiadiazole, 1, 2 , 3-triazole, 1, 2 , 4-triazole, 1,2,5- triazole, and 1, 3 , 4-triazole; R 2 , at each occurrence, is selected from H, CF 3 , Cι_ 6 alkyl, benzyl, C 5 - 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2a , at each occurrence, is selected from H, CF 3 , Cι_ alkyl, benzyl, phenethyl, Cs_ 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2b , at each occurrence, is selected from CF 3 , C 1 - 4 alkoxy, Cι_ 6 alkyl, benzyl, Cs_ 6 carbocyclic residue substituted with 0-2 R 4b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R 4b ; R 2c , at each occurrence, is selected from CF 3 , OH, C 1 - 4 alkoxy, Cι_ 6 alkyl, benzyl, C 5 - 6 carbocyclic residue substituted with 0-2 R b , and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, 0, and S substituted with 0-2 R b ; alternatively, R 2 and R 2a , together with the atom to which they are attached, combine to form a ring selected from imidazolyl, morpholino, piperazinyl, pyridyl, and pyrrolidinyl, substituted with 0-2 R b ; R , at each occurrence, is selected from H, =0, OR 2 , CH 2 OR 2 , F, Cl, Cι_ 4 alkyl, NR 2 R 2a , CH 2 NR 2 R 2 , C(0)R 2c , CH 2 C(0)R 2c , C(0)NR 2 R 2a , CH(=NR 2 )NR 2 R 2a , CH (=NS (0) 2 R 5 ) NR 2 R 2a , S0 2 NR 2 R a , NR 2 S0 2 -Ci- alkyl, S(0) 2 R 5 , and CF 3 provided that if B is H, then R 4 is other than tetrazole, C(0)-alkoxy, and C (0)NR 2 R 2 ; R a , at each occurrence, is selected from H, =0, (CH 2 ) r 0R 2 , F, Cl, Cι_ 4 alkyl, NR 2 R 2a , CHNR 2 R 2a , NR 2 R 2b , CH 2 NR 2 R 2b , (CH 2 ) r C(0)R 2c , NR 2 C(0)R 2b , C(0)NR 2 R 2a , C (0) NH (CH 2 ) 2 NR 2 R 2a , NR 2 C(0)NR 2 R 2a , S0NR 2 R 2a , S(0) 2 R 5 , and CF 3 ; and, R b , at each occurrence, is selected from H, =0, (CH 2 ) r 0R 3 , F, Cl, Cι_ 4 alkyl, NR 3 R 3 , CH 2 NR 3 R 3a , C(0)R 3 , CH 2 C(0)R 3 , C(0)0R 3c , C(0)NR 3 R 3a , CH(=NR 3 )NR 3 R 3a , S0 2 NR 3 R 3a , NR 3 S0 2 -Cι_ 4 alkyl, NR S0 2 CF 3 NR 3 S0 2 -phenyl, S(0) 2 CF 3 , S(0) 2 -Cι_ 4 alkyl, S (0) 2 -phenyl, and CF 3 . 5. A compound according to Claim 1, wherein the compound is selected from: N- (2 '-Aminosulfonyl- [1,1' ]biphen-4-yl) -2- (3'- amidinophenyl) nicotinamide; N- [5- (2-aminosulfonyl )phenylpyrid-2-yl] -2- (3 ' - amidinophenyl) nicotinamide; N- [5- (2-t-butylaminosulfonyl)phenylpyrid-2-yl] -2- (3 ' - amidinophenyl ) nicotinamide; and, N- [5- (2-aminosulfonyl) phenylpyrid-2-yl] -2- (3 ' - carboxamidophenyl) nicotinamide; or a pharmaceutically acceptable salt thereof . 6. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to Claim 1 or a pharmaceutically acceptable salt thereof . 7. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to Claim 2 or a pharmaceutically acceptable salt thereof . 8. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to Claim 3 or a pharmaceutically acceptable salt thereof . 9. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to Claim 4 or a pharmaceutically acceptable salt thereof . 10. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to Claim 5 or a pharmaceutically acceptable salt thereof. 11. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of <_ι compound according to Claim 1 or a pharmaceutically acceptable salt thereof . 12. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to Claim 2 or a pharmaceutically acceptable salt thereof . 13. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to Claim 3 or a pharmaceutically acceptable salt thereof. 14. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to Claim 4 or a pharmaceutically acceptable salt thereof . 15. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to Claim 5 or a pharmaceutically acceptable salt thereof .

Inventors: PINTO DONALD JOSEPH PHILLIP, PRUITT JAMES RUSSELL, QUAN MIMI LIFEN, WEXLER RUTH RICHMOND, PINTO, DONALD, JOSEPH, PHILLIP, PRUITT, JAMES, RUSSELL, QUAN, MIMI, LIFEN, WEXLER, RUTH, RICHMOND
Applicants: DU PONT MERCK PHARMA, THE DU PONT MERCK PHARMACEUTICAL COMPANY
Application year: 1998
Main classification: C07D213
IPC codes: C07D213