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

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 conditions 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):

or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, D, E, M, R 1a , R 1b , 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:

 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(O)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 ) r , (CH 2 ) r NR 3 (CH 2 ) r , (CH 2 ) r C(O)(CH 2 ) r , (CH 2 ) r C(O)O(CH 2 ) r , (CH 2 ) r OC(O)(CH 2 ) r , (CH 2 ) r C(O)NR 3 (CH 2 ) r , (CH 2 ) r NR 3 C(O)(CH 2 ) r , (CH 2 ) r OC(O)O(CH 2 ) r , (CH 2 ) r OC(O)NR 3 (CH 2 ) r , (CH 2 ) r NR 3 C(O)O(CH 2 ) r , (CH 2 ) r NR 3 C(O)NR 3 (CH 2 ) r , (CH 2 ) r S(O) p (CH 2 ) r , (CH 2 ) r SO 2 NR 3 (CH 2 ) r , (CH 2 ) r NR 3 SO 2 (CH 2 ) r , and (CH 2 ) r NR 3 SO 2 NR 3 (CH 2 ) r , provided that Z does not form a N—-N, N—O, N—S, NCH 2 N, NCH 2 O, or NCH 2 S bond with ring M or group A;

R 1a and R 1b are independently absent or selected from —(CH 2 ) r —R 1′ , —CH═CH—R 1′ , NCH 2 R 1″ , OCH 2 R 1″ , SCH 2 R 1″ , NH(CH 2 ) 2 (CH 2 ) t R 1′ , O(CH 2 ) 2 (CH 2 ) t R 1′ , and S(CH 2 ) 2 (CH 2 ) t R 1′ ;

alternatively, R 1a and R 1b , 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, O, and S;

alternatively, when Z is C(O)NH and R 1a is attached to a ring carbon adjacent to Z, then R 1a is a C(O) 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 ) r CF 3 , (CH 2 ) r OR 2 , NR 2 R 2a , C(O)R 2c , OC(O)R 2 , (CF 2 ) r CO 2 R 2c , S(O) p R 2b , NR 2 (CH 2 ) r OR 2 , CH(═NR 2c )NR 2 R 2a , NR 2 C(O)R 2b , NR 2 C(O)NHR 2b , NR 2 C(O) 2 R 2a , OC(O)NR 2a R 2b , C(O)NR 2 R 2a , C(O)NR 2 (CH 2 ) r OR 2 , SO 2 NR 2 R 2a , NR 2 SO 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(O)R 2c , C(O)NR 2 R 2a , S(O)R 2b , S(O) 2 R 2b , and SO 2 NR 2 R 2a ;

R 2 , at each occurrence, is selected from H, CF 3 , C 1-6 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 2a , at each occurrence, is selected from H, CF 3 , C 1-6 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, O, and S substituted with 0-2 R 4b ;

R 2b , at each occurrence, is selected from CF 3 , C 1-4 alkoxy, C 1-6 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 2c , at each occurrence, is selected from CF 3 , OH, C 1-4 alkoxy, C 1-6 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 ;

alternatively, R 2 and R 2a , 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 4b 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, C 1-4 alkyl, and phenyl;

R 3b , at each occurrence, is selected from H, C 1-4 alkyl, and phenyl;

R 3c , at each occurrence, is selected from C 1-4 alkyl, and phenyl;

A is selected from:

C 3-10 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, O, and S substituted with 0-2 R 4 ;

B is selected from: H, Y, and X—Y;

X is selected from C 1-4 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(O)CR 2 R 2a —, —CR 2 R 2a C(O), —S(O) p —, —S(O) p CR 2 R 2a —, —CR 2 R 2a S(O) p —, —S(O) 2 NR 2 —, —NR 2 S(O) 2 —, —NR 2 S(O) 2 CR 2 R 2a —, —CR 2 R 2a S(O) 2 NR 2 —, —NR 2 S(O) 2 NR 2 —, —C(O)NR 2 —, —NR 2 C(O)—, —C(O)NR 2 CR 2 R 2a —, —NR 2 C(O)CR 2 R 2a —, —CR 2 R 2a C(O)NR 2 —, —CR 2 R 2a NR 2 C(O)—, —NR 2 C(O)O—, —OC(O)NR 2 —, —NR 2 C(O)NR 2 —, —NR 2 —, —NR 2 CR 2 R 2a —, —CR 2 R 2a NR 2 —, O, —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 3-10 carbocyclic residue substituted with 0-2 R 4a , 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 4a ;

R 4 , at each occurrence, is selected from H, ═O, (CH 2 ) r OR 2 , F, Cl, Br, I, C 1-4 alkyl, —CN, NO 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(O)R 2c , NR 2 C(O)R 2b , C(O)NR 2 R 2a , NR 2 C(O)NR 2 R 2a , CH(═NR 2 )NR 2 R 2a , CH(═NS(O) 2 R 5 )NR 2 R 2a , NHC(═NR 2 )NR 2 R 2a , C(O)NHC(═NR 2 )NR 2 R 2a , SO 2 NR 2 R 2a , NR 2 SO 2 NR 2 R 2a , NR 2 SO 2 —C 1-4 alkyl, NR 2 SO 2 R 5 , S(O) p R 5 , (CF 2 ) r CF 3 , NCH 2 R 1″ , OCH 2 R 1″ , SCH 2 R 1″ , N(CH 2 ) 2 (CH 2 ) t R 1′ , O(CH 2 ) 2 (CH 2 ) t R 1′ , and S(CH 2 ) 2 (CH 2 ) t R 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, ═O, (CH 2 ) r OR 2 , (CH 2 ) r —F, (CH 2 ) r —Br, (CH 2 ) r —Cl, I, C 1-4 alkyl, —CN, NO 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r NR 2 R 2b , (CH 2 ) r C(O)R 2c , NR 2 C(O)R 2b , C(O)NR 2 R 2a , C(O)NH(CH 2 ) 2 NR 2 R 2a , NR 2 C(O)NR 2 R 2a , CH(═NR 2 )NR 2 R 2a , NHC(═NR 2 )NR 2 R 2a , SO 2 NR 2 R 2a , NR 2 SO 2 NR 2 R 2a , NR 2 SO 2 —C 1-4 alkyl, C(O)NHSO 2 —C 1-4 alkyl, NR 2 SO 2 R 5 , S(O) p R 5 , and (CF 2 ) r CF 3 ;

alternatively, one R 4a is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-1 R 5 ;

R 4b , at each occurrence, is selected from H, ═O, (CH 2 ) r OR 3 , F, Cl, Br, I, C 1-4 alkyl, —CN, NO 2 , (CH 2 ) r NR 3 R 3a , (CH 2 ) r C(O)R 3 , (CH 2 ) r C(O)OR 3c , NR 3 C(O)R 3a , C(O)NR 3 R 3a , NR 3 C(O)NR 3 R 3a , CH(═NR 3 )NR 3 R 3a , NH 3 C(═NR 3 )NR 3 R 3a , SO 2 NR 3 R 3a , NR 3 SO 2 NR 3 R 3a , NR 3 SO 2 —C 1-4 alkyl, NR 3 SO 2 CF 3 , NR 3 SO 2 -phenyl, S(O) p CF 3 , S(O) p —C 1-4 alkyl, S(O) p -phenyl, and (CF 2 ) r CF 3 ;

R 5 , at each occurrence, is selected from CF 3 , C 1-6 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, C 1-4 alkyl, CN, NO 2 , (CH 2 ) r NR 2 R 2a , (CH 2 ) r C(O)R 2b , NR 2 C(O)R 2b , NR 2 C(O)NR 2 R 2a , CH(═NH)NH 2 , NHC(═NH)NH 2 , SO 2 NR 2 R 2a , NR 2 SO 2 NR 2 R 2a , and NR 2 SO 2 C 1-4 alkyl;

R 7 , at each occurrence, is selected from H, OH, C 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkoxy, C 1-4 alkoxycarbonyl, (CH 2 ) n -phenyl, C 6-10 aryloxy, C 6-10 aryloxycarbonyl, C 6-10 arylmethylcarbonyl, C 1-4 alkylcarbonyloxy C 1-4 alkoxycarbonyl, C 6-10 arylcarbonyloxy C 1-4 alkoxycarbonyl, C 1-6 alkylaminocarbonyl, phenylaminocarbonyl, and phenyl-C 1-4 alkoxycarbonyl;

R 8 , at each occurrence, is selected from H, C 1-6 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, O, 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 O, OCH 2 , CH 2 NH, NHCH 2 , CH 2 C(O), C(O)CH 2 , C(O)NH, C(O)NH, CH 2 S(O) 2 , S(O) 2 (CH 2 ), SO 2 NH, and SO 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 O, 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 R 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] 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, 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;

R 2 , at each occurrence, is selected from H, CF 3 , C 1-6 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, O, and S substituted with 0-2 R 4b ;

R 2a , at each occurrence, is selected from H, CF 3 , C 1-6 alkyl, benzyl, phenethyl, 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, O, and S substituted with 0-2 R 4b ;

R 2b , at each occurrence, is selected from CF 3 , C 1-4 alkoxy, C 1-6 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, O, and S substituted with 0-2 R 4b ;

R 2c , at each occurrence, is selected from CF 3 , OH, C 1-4 alkoxy, C 1-6 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, O, and S substituted with 0-2 R 4b ;

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, ═O, OR 2 , CH 2 OR 2 , F, Cl, C 1-4 alkyl, NR 2 R 2a , CH 2 NR 2 R 2a , C(O)R 2c , CH 2 C(O)R 2c , C(O)NR 2 R 2a , CH(═NR 2 )NR 2 R 2a , CH(═NS(O) 2 R 5 )NR 2 R 2a , SO 2 NR 2 R 2a , NR 2 SO 2 —C 1-4 alkyl, S(O) 2 R 5 , and CF 3

provided that if B is H, then R 4 is other than tetrazole, C(O)-alkoxy, and C(O)NR 2 R 2a ;

R 4a , at each occurrence, is selected from H, ═O, (CH 2 ) r OR 2 , F, Cl, C 1-4 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(O)R 2c , NR 2 C(O)R 2b , C(O)NR 2 R 2a , C(O)NH(CH 2 ) 2 NR 2 R 2a , NR 2 C(O)NR 2 R 2a , SO 2 NR 2 R 2a , S(O) 2 R 5 , and CF 3 ; and,

R 4b , at each occurrence, is selected from H, ═O, (CH 2 ) r OR 3 , F, Cl, C 1-4 alkyl, NR 3 R 3a , CH 2 NR 3 R 3a , C(O)R 3 , CH 2 C(O)R 3 , C(O)OR 3c , C(O)NR 3 R 3a , CH(═NR 3 )NR 3 R 3a , SO 2 NR 3 R 3a , NR 3 SO 2 —C 1-4 alkyl, NR 3 SO 2 CF 3 , NR 3 SO 2 -phenyl, S(O) 2 CF 3 , S(O) 2 —C 1-4 alkyl, S(O) 2 -phenyl, and CF 3 .

[5] In a further preferred embodiment, the present invention provides novel compounds 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.

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., ═O), 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 6 ) 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+1)). 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, [3.3.0]bicyclooctane, [4.3.0]bicyclononane, [4.4.0]bicyclodecane, [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, O 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 O 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 O 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, O and S. It is preferred that the total number of S and O 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, 1H-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, phenanthrolinyl, 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, 1H-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 2 , and R 7 is selected from OH, C 1-4 alkoxy, C 6-10 aryloxy, C 1-4 alkoxycarbonyl, C 6-10 aryloxycarbonyl, C 6-10 arylmethylcarbonyl, C 1-4 alkylcarbonyloxy C 1-4 alkoxycarbonyl, and C 6-10 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., ═O) 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 4 . W is defined as a suitable protected nitrogen, such as NO 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 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.

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.
	then the reactive	to give the following
If A contains:	substituent of Y is:	product A-X-Y:
A-NHR 2 as a	ClC(O)—Y	A-NR 2 —C(O)—Y
substituent
a secondary NH	ClC(O)—Y	A-C(O)—Y
as part of a
ring or chain
A-OH as a	ClC(O)—Y	A-O—C(O)—Y
substituent
A-NHR 2 as a	ClC(O)—CR 2 R 2a —Y	A-NR 2 —C(O)—CR 2 R 2a —Y
substituent
a secondary NH	ClC(O)—CR 2 R 2a —Y	A-C(O)—CR 2 R 2a —Y
as part of a
ring or chain
A-OH as a	ClC(O)—CR 2 R 2a —Y	A-O—C(O)—CR 2 R 2a —Y
substituent
A-NHR 2 as a	ClC(O)—CNR 2 —Y	A-NR 2 —C(O)—CNR 2 —Y
substituent
a secondary NH	ClC(O)—CNR 2 —Y	A-C(O)—CNR 2 —Y
as part of a
ring or chain
A-OH as a	ClC(O)—CNR 2 —Y	A-O—C(O)—CNR 2 —Y
substituent
A-NHR 2 as a	ClSO 2 —Y	A-NR 2 —SO 2 —Y
substituent
a secondary NH	ClSO 2 —Y	A-SO 2 —Y
as part of a
ring or chain
A-NHR 2 as a	ClSO 2 —CR 2 R 2a —Y	A-NR 2 —SO 2 —CR 2 R 2a —Y
substituent
a secondary NH	ClSO 2 —CR 2 R 2a —Y	A-SO 2 —CR 2 R 2a —Y
as part of a
ring or chain
A-NHR 2 as a	ClSO 2 —NR 2 —Y	A-NR 2 —SO 2 —NR 2 —Y
substituent
a secondary NH	ClSO 2 —NR 2 —Y	A-SO 2 —NR 2 —Y
as part of a
ring or chain
A-C(O)Cl	HO—Y as a	A-C(O)—O—Y
A-C(O)Cl	NHR 2 —Y as a	A-C(O)—NR 2 —Y
	substituent
A-C(O)Cl	a secondary NH as	A-C(O)—Y
	part of a ring or
	chain
A-CR 2 R 2a C(O)Cl	HO—Y as a substituent	A-CR 2 R 2a C(O)—O—Y
A-CR 2 R 2a C(O)Cl	NHR 2 —Y as a	A-CR 2 R 2a C(O)—NR 2 —Y
	substituent
A-CR 2 R 2a C(O)Cl	a secondary NH as	A-CR 2 R 2a C(O)—Y
	part of a ring or
	chain
A-SO 2 Cl	NHR 2 —Y as a	A-SO 2 —NR 2 —Y
	substituent
A-SO 2 Cl	a secondary NH as	A-SO 2—Y
	part of a ring or
	chain
A-CR 2 R 2a SO 2 Cl	NHR 2 —Y as a	A-CR 2 R 2a SO 2 2—NR 2 —Y
	substituent
A-CR 2 R 2a SO 2 Cl	a secondary NH as	A-CR 2 R 2a SO 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.
	then the reactive	to give the following
If A contains:	substituent of Y is:	product A-X-Y:
A-C(O)Cl	BrMg—Y	A-C(O)—Y
A-CR 2 R 2a C(O)Cl	BrMg—Y	A-CR 2 R 2a C(O)—Y
A-C(O)Cl	BrMgCR 2 R 2a —Y	A-CR 2 R 2a C(O)—Y
A-CR 2 R 2a C(O)Cl	BrMgCR 2 R 2a —Y	A-CR 2 R 2a C(O)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 Laboue, Tetr. Lett. 1992, 33(31), 4437).

TABLE C
Preparation of Ether and Thioether linkages between
A and B.
		then the reactive	to give the following
	If A contains:	substituent of Y is:	product A-X-Y:
	A-OH	Br—Y	A-O—Y
	A-CR 2 R 2a —OH	Br—Y	A-CR 2 R 2a O—Y
	A-OH	Br—CR 2 R 2a —Y	2 A-OCR 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 —SO 2 — linkages from
thioether of Table C.
	then it is oxidized	then it is oxidized
	with wet	with m—
If the starting	Alumina/Oxone to	chloroperbenzoic acid
material is:	give:	to give:
A-S—Y	A-S(O)—Y	A-SO 2 —Y
A-CR 2 R 2a S—Y	A-CR 2 R 2a S(O)—Y	A-CR 2 R 2a SO 2 —Y
A-SCR 2 R 2a —Y	A-S(O)CR 2 R 2a —Y	A-SO 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.

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. Chim. 1948, 67, 380) to give the desired 2-bromopyridine. Suzuki coupling with the appropriate boronic acid provides the desired substituted pyridine.

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 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 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.

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.

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.

By analogy to Scheme 9, in Scheme 10 a aldehyde can be reacted with an activated ketone, brominated, dehydro-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.

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.

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.

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. Pat. No. 2,403,710) yields the intermediate for the palladium-catalyzed coupling step which occurs as shown above.

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 1b . 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.

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.

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 ( J. 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.

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 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.

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-yl)-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 CHCl 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 <100 mL. 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 <100 mL 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%). 1 H NMR (DMSO-d 6 ): δ13.76 (bs, 1H), 8.46 (m, 1H), 8.09 (dd, 1H, J=7.7, J′=2.2), 7.51 (m, 1H).

Part B. Preparation of methyl 2-bromonicotinate

2-Bromonicotinic acid (7.33 g, 36 mmol) was suspended in dry Et 2 O (40 mL), and MeOH (2.3 mL) and diethyl azodicarboxylate (5.8 mL, 37 mmol) were added. Triphenylphosphine (9.61 g in 40 mL Et 2 O, 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/hexanes) to yield a clear oil (8.63 g, 100%). 1 H NMR (CDCl 1 3 ): δ8.49 (dd, 1H, J=4.8, J′=2.2), 8.09 (dd, 1H, J=7.7, J′=1.8), 7.36 (m, 1H), 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 O/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 ): δ8.37 (s, 2H), 8.10 (s, 1H), 8.03 (dt, 1H, J=7.3, J′=1.1), 7.83 (dt, 1H, J=7.6, J′=1.4), 7.53 (t, 1H, 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 SO 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%). 1 H NMR (CDCl 3 ): δ8.81 (dd, 1H, J=4.8, J′=1.8), 8.23 (dd, 1H, J=8.0, J′=1.9), 7.85 (s, 1H), 7.73 (m, 2H), 7.55 (t, 1H, J=7.7), 7.43 (m, 1H), 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, 1N 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 1N 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 MgSO 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.; 1 H NMR (CDCl 3 ): δ8.00 (d, 1H); 7.82 (d, 1H); 7.53 (m, 2H); 6.29 (br s, 2H); 5.13 (s, 1H); 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(0) (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 MgSO 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. 1 H NMR (CDCl 3 ): δ8.14 (d, 1H); 7.53 (t, 1H); 7.43 (t, 1H); 7.33 (d, 2H); 7.27 (d, 1H); 6.76 (d, 2H); 3.7 (br s, 1H); 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 Cl 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 SO 4 , filtered, and evaporated. A small amount of additional material was obtained from the aqueous extract by adjusting the pH to 8 with sat. NaHCO 3 and extracting with EtOAc. This material was dried over Na 2 SO 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%). 1 H NMR (CDCl 3 ): δ8.86 (dd, 1H, J=4.7, J′=1.9), 8.14 (m, 3H), 8.00 (d, 1H, J=7.7), 7.73 (d, 1H, J=8.1), 7.50 (m, 9H), 7.29 (dd, 1H, J=7.4, J′=1.1), 3.60 (s, 1H), 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 SO 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 SO 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%). 1 H NMR (DMSO-d 6 ): δ10.65 (s, 1H), 9.38 (s, 2H), 8.92 (s, 2H), 8.81 (dd, 1H, J=4.4, J′=1.4), 8.10 (m, 2H), 7.97 (m, 2H), 7.76 (m, 1H), 7.67 (t, 1H, J=8.0), 7.57 (m, 5H), 7.29 (m, 5H). HRMS calc. for C 25 H 22 N 5 O 3 S: m/z 472.1443; found, 472.1457.

Examples 2, 3 and 4

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)

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 H 2 O, 5.6 mmol) was added. After 20 hours, the resulting solution was diluted with water and extracted with CHCl 3 . The aqueous was acidified to pH 4 with 1 M HCl and extracted several times with CHCl 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 SO 4 , filtered, and evaporated to yield a white solid (1.06 g, 93%). 1 H NMR (CDCl 3 ): δ8.85 (dd, 1H, J=5.1, J′=1.5), 8.35 (dd, 1H, J=7.6, J′=1.4), 7.84 (s, 1H), 7.75 (m, 2H), 7.55 (t, 1H, J=7.7), 7.47 (m, 1H).

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(0) (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 MgSO 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 (CDCl 3 ): δ8.18 (d, 1H); 8.07 (m, 1H); 7.70 (dd, 1H); 7.58 (dt, 1H); 7.48 (dt, 1H); 7.28 (d, 1H); 6.56 (d, 1H); 4.62 (br s, 2H); 3.88 (br s, 1H); 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 Cl 1 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 Cl 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 Cl 2 , extracted with saturated NaHCO 3 , dried over Na 2 SO 4 , filtered, and evaporated. The resulting material was chromatographed on silica gel (50-75% EtOAc/hexanes) to yield the desired product (423 mg, 62%). 1 H NMR (CDCl 3 ): δ8.83 (dd, 1H, J=4.8, J′=1.5), 8.40 (bs, 1H), 8.29 (bd, 1H, J=8.4), 8.17 (dd, 1H), J=8.0, J′=1.1), 8.09 (m, 3H), 7.97 (d, 1H, J=7.7), 7.79 (d, 1H, J=8.4), 7.69 (d, 1H, J=7.7), 7.54 (m, 4H), 7.25 (m, 1H), 4.19 (bs, 1H), 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 (5 mL) and dry CHCl 3 (15 mL) and cooled to 0° C. HCl(g) was generated by the addition of concentrated H 2 SO 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% MeCNH/H2O/0.05% TFA) to yield N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3′-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 2), (250 mg, 45%). 1 H NMR (DMSO-d 6 ): δ11.27 (s, 1H), 9.43 (s, 2H), 8.98 (s, 2H), 8.83 (dd, 1H, J=4.8, J′=1.9), 8.32 (s, 1H), 8.13 (m, 2H), 8.05 (m, 2H), 7.96 (d, 1H, J=7.3), 7.81 (d, 2H, J=8.4), 7.65 (m, 4H), 7.47 (s, 2H), 7.37 (m, 1H). HRMS calc. for C 24 H 21 N 6 O 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%). 1 H NMR (DMSO-d 6 ): δ9.7 (s, 1H), 9.41 (s, 2H), 8.95 (s, 2H), 8.82 (m, 1H), 8.28 (s, 1H), 8.09 (m, 4H), 7.95 (d, 1H, J=7.7), 7.79 (m, 2H), 7.63 (m, 4H), 7.34 (d, 1H, J=7.7), 7.18 (s, 1H), 1.04 (s, 9H). HRMS calc. for C 28 H 29 N 6 O 3 S: 529.2022; found, 529.2050. A third product, N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3′-carboxamidophenyl)nicotinamide, trifluoroacetic acid salt (Example 4) was isolated and chromatographed on silica gel (10-20% MeOH/CHCl 3 ) to yield a white solid (77 mg, 20%). 1 H NMR (DMSO-d 6 ): δ11.13 (s, 1H), 8.75 (dd, 1H, J=4.8, J′=1.9), 8.26 (m, 2H), 8.02 (m, 4H), 7.84 (d, 1H, J=7.7), 7.74 (m, 2H), 7.59 (m, 2H), 7.47 (m, 2H), 7.36 (m, 4H).

TABLE 1
				MS
Ex	D	R 2	A′	(M + H) +
1	C(═NH)NH 2	SO 2 NH 2	CH	472.1
2	C(═NH)NH 2	SO 2 NH 2	N	473.1
3	C(═NH)NH 2	SO 2 NHtBu	N	529.2
4	C(O)NH 2	SO 2 NH 2	N	474.1

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 a 1 -ss 4 .

TABLE 2
a 1 R = F, D = NH 2	b 1 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(O)NH 2	b 7 R = F, D = C(O)NH 2	c 7 R = F, D = C(O)NH 2
a 8 R = H, D = C(O)NH 2	b 8 R = H, D = C(O)NH 2	c 8 R = H, D = C(O)NH 2
d 1 R = F, D = NH 2	e 1 R = F, D = NH 2	f 1 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(O)NH 2	e 7 R = F, D = C(O)NH 2	f 7 R = F, D = C(O)NH 2
d 8 R = H, D = C(O)NH 2	e 8 R = H, D = C(O)NH 2	f 8 R = H, D = C(O)NH 2
g 1 R = F, D = NH 2	h 1 R = F, D = NH 2	i 1 R = F, D = NH 2
g 2 R = H, D = NH 2	h 2 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(O)NH 2	h 7 R = F, D = C(O)NH 2	i 7 R = F, D = C(O)NH 2
g 8 R = H, D = C(O)NH 2	h 8 R = H, D = C(O)NH 2	i 8 R = H, D = C(O)NH 2
j 1 R = F, D = NH 2	k 1 R = F, D = NH 2	l 1 R = F, D = NH 2
j 2 R = H, D = NH 2	k 2 R = H, D = NH 2	l 2 R = H, D = NH 2
j 3 R = F, D = CH 2 NH 2	k 3 R = F, D = CH 2 NH 2	l 3 R = F, D = CH 2 NH 2
j 4 R = H, D = CH 2 NH 2	k 4 R = H, D = CH 2 NH 2	l 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	l 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	l 6 R = H, D = C(═NH)NH 2
j 7 R = F, D = C(O)NH 2	k 7 R = F, D = C(O)NH 2	l 7 R = F, D = C(O)NH 2
j 8 R = H, D = C(O)NH 2	k 8 R = H, D = C(O)NH 2	l 8 R = H, D = C(O)NH 2
m 1 R = F, D = NH 2	n 1 R = F, D = NH 2	o 1 R = F, D = NH 2
m 2 R = H, D = NH 2	n 2 R = H, D = NH 2	o 2 R = H, D = NH 2
m 3 R = F, D = CH 2 NH 2	n 3 R = F, D = CH 2 NH 2	o 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	o 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	o 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	o 6 R = H, D = C(═NH)NH 2
m 7 R = F, D = C(O)NH 2	n 7 R = F, D = C(O)NH 2	o 7 R = F, D = C(O)NH 2
m 8 R = H, D = C(O)NH 2	n 8 R = H, D = C(O)NH 2	o 8 R = H, D = C(O)NH 2
p 1 R = F, D = NH 2	q 1 R = F, D = NH 2	r 1 R = F, D = NH 2
p 2 R = Cl, D = NH 2	q 2 R = Cl, D = NH 2	r 2 R = Cl, 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 = Cl, D = CH 2 NH 2	q 5 R = Cl, D = CH 2 NH 2	r 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	q 8 R = Cl, D = C(═NH)NH 2	r 8 R = Cl, 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
p 10 R = F, D = C(O)NH 2	q 10 R = F, D = C(O)NH 2	r 10 R = F, D = C(O)NH 2
p 11 R = Cl, D = C(O)NH 2	q 11 R = Cl, D = C(O)NH 2	r 11 R = Cl, D = C(O)NH 2
p 12 R = OMe, D = C(O)NH 2	q 12 R = OMe, D = C(O)NH 2	r 12 R = OMe, D = C(O)NH 2
s 1 R = F, D = NH 2	t 1 R = F, D = NH 2	u 1 R = F, D = NH 2
s 2 R = Cl, D = NH 2	t 2 R = Cl, D = NH 2	u 2 R = Cl, 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 = Cl, D = CH 2 NH 2	t 5 R = Cl, D = CH 2 NH 2	u 5 R = Cl, 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 NH 2
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 = Cl, D = C(═NH)NH 2	t 8 R = Cl, D = C(═NH)NH 2	u 8 R = Cl, 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
s 10 R = F, D = C(O)NH 2	t 10 R = F, D = C(O)NH 2	u 10 R = F, D = C(O)NH 2
s 11 R = Cl, D = C(O)NH 2	t 11 R = Cl, D = C(O)NH 2	u 11 R = Cl, D = C(O)NH 2
s 12 R = OMe, D = C(O)NH 2	t 12 R = OMe, D = C(O)NH 2	u 12 R = OMe, D = C(O)NH 2
v 1 R = F, D = NH 2	w 1 R = F, D = NH 2	x 1 R = F, D = NH 2
v 2 R = Cl, D = NH 2	w 2 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	w 4 R = F, D = CH 2 NH 2	x 4 R = F, D = CH 2 NH 2
v 5 R = Cl, D = CH 2 NH 2	w 5 R = Cl, D = CH 2 NH 2	x 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	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 = Cl, D = C(═NH)NH 2	w 8 R = Cl, D = C(═NH)NH 2	x 6 R = Cl, 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
v 10 R = F, D = C(O)NH 2	w 10 R = F, D = C(O)NH 2	x 10 R = F, D = C(O)NH 2
v 11 R = Cl, D = C(O)NH 2	w 11 R = Cl, D = C(O)NH 2	x 11 R = Cl, D = C(O)NH 2
v 12 R = OMe, D = C(O)NH 2	w 12 R = OMe, D = C(O)NH 2	x 12 R = OMe, D = C(O)NH 2
y 1 R = F, D = NH 2	z 1 R = F, D = NH 2	aa 1 R = F, D = NH 2
y 2 R = Cl, D = NH 2	z 2 R = Cl, D = NH 2	aa 2 R = Cl, 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 = Cl, D = CH 2 NH 2	z 5 R = Cl, D = CH 2 NH 2	aa 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	z 8 R = Cl, D = C(═NH)NH 2	aa 8 R = Cl, 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(O)NH 2	z 10 R = F, D = C(O)NH 2	aa 10 R = F, D = C(O)NH 2
y 11 R = Cl, D = C(O)NH 2	z 11 R = Cl, D = C(O)NH 2	aa 11 R = Cl, D = C(O)NH 2
y 12 R = OMe, D = C(O)NH 2	z 12 R = OMe, D = C(O)NH 2	aa 12 R = OMe, D = C(O)NH 2
bb 1 R = F, D = NH 2	cc 1 R = F, D = NH 2	dd 1 R = F, D = NH 2
bb 2 R = Cl, D = NH 2	cc 2 R = Cl, D = NH 2	dd 2 R = Cl, 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 = Cl, D = CH 2 NH 2	cc 5 R = Cl, D = CH 2 NH 2	dd 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	cc 8 R = Cl, D = C(═NH)NH 2	dd 8 R = Cl, D = C(═NH)NH 2
bb 9 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
bb 10 R = F, D = C(O)NH 2	cc 10 R = F, D = C(O)NH 2	dd 10 R = F, D = C(O)NH 2
bb 11 R = Cl, D = C(O)NH 2	cc 11 R = Cl, D = C(O)NH 2	dd 11 R = Cl, D = C(O)NH 2
bb 12 R = OMe, D = C(O)NH 2	cc 12 R = OMe, D = C(O)NH 2	dd 12 R = OMe, D = C(O)NH 2
ee 1 R = F, D = CH 2 NH 2	ff 1 R = F, D = CH 2 NH 2	gg 1 R = F, D = CH 2 NH 2
ee 2 R = Cl, D = CH 2 NH 2	ff 2 R = Cl, D = CH 2 NH 2	gg 2 R = Cl, 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 , D = CH 2 NH 2	ff 4 R = CH 2 NH 2 , D = CH 2 NH 2	gg 4 R = CH 2 NH 2 , D = CH 2 NH 2
hh 1 R = F, D = CH 2 NH 2	ii 1 R = F, D = CH 2 NH 2	jj 1 R = F, D = CH 2 NH 2
hh 2 R = Cl, D = CH 2 NH 2	ii 2 R = Cl, D = CH 2 NH 2	jj 2 R = Cl, 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 2 NH 2 , D = CH 2 NH 2	ii 4 R = CH 2 NH 2 , D = CH 2 NH 2	jj 4 R = CH 2 NH 2 , D = CH 2 NH 2
kk 1 R = F, D = CH 2 NH 2	ll 1 R = F, D = CH 2 NH 2	mm 1 R = F, D = CH 2 NH 2
kk 2 R = Cl, D = CH 2 NH 2	ll 2 R = Cl, D = CH 2 NH 2	mm 2 R = Cl, D = CH 2 NH 2
kk 3 R = OMe, D = CH 2 NH 2	ll 3 R = OMe, D = CH 2 NH 2	mm 3 R = OMe, D = CH 2 NH 2
kk 4 R = CH 2 NH 2 , D = CH 2 NH 2	ll 4 R = CH 2 NH 2 , D = CH 2 NH 2	mm 4 R = CH 2 NH 2 , D = CH 2 NH 2
nn 1 R = F, D = CH 2 NH 2	oo 1 R = F, D = CH 2 NH 2	pp 1 R = F, D = CH 2 NH 2
nn 2 R = Cl, D = CH 2 NH 2	oo 2 R = Cl, D = CH 2 NH 2	pp 2 R = Cl, D = CH 2 NH 2
nn 3 R = OMe, D = CH 2 NH 2	oo 3 R = OMe, D = CH 2 NH 2	pp 3 R = OMe, D = CH 2 NH 2
nn 4 R = CH 2 NH 2 , D = CH 2 NH 2	oo 4 R = CH 2 NH 2 , D = CH 2 NH 2	pp 4 R = CH 2 NH 2 , D = CH 2 NH 2
qq 1 R = F, D = CH 2 NH 2	rr 1 R = F, D = CH 2 NH 2	ss 1 R = F, D = CH 2 NH 2
qq 2 R = Cl, D = CH 2 NH 2	rr 2 R = Cl, D = CH 2 NH 2	ss 2 R = Cl, 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 , D = CH 2 NH 2	rr 4 R = CH 2 NH 2 , D = CH 2 NH 2	ss 4 R = CH 2 NH 2 , D = CH 2 NH 2
Ex #	R 1b	A	B
1	H	phenyl	2-(aminosulfonyl)phenyl
2	H	phenyl	2-(methylaminosulfonyl)phenyl
3	H	phenyl	1-pyrrolidinocarbonyl
4	H	phenyl	2-(methylsulfonyl)phenyl
5	H	phenyl	4-morpholino
6	H	phenyl	2-(1′-CF 3 -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-(methylsulfonyl)phenyl
12	H	2-pyridyl	4-morpholino
13	H	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
14	H	2-pyridyl	4-morpholinocarbonyl
15	H	3-pyridyl	2-(aminosulfonyl)phenyl
16	H	3-pyridyl	2-(methylaminosulfonyl)phenyl
17	H	3-pyridyl	1-pyrrolidinocarbonyl
18	H	3-pyridyl	2-(methylsulfonyl)phenyl
19	H	3-pyridyl	4-morpholino
20	H	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
21	H	3-pyridyl	4-morpholinocarbonyl
22	H	2-pyrimidyl	2-(aminosulfonyl)phenyl
23	H	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
24	H	2-pyrimidyl	1-pyrrolidinocarbonyl
25	H	2-pyrimidyl	2-(methylsulfonyl)phenyl
26	H	2-pyrimidyl	4-morpholino
27	H	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
28	H	2-pyrimidyl	4-morpholinocarbonyl
29	H	5-pyrimidyl	2-(aminosulfonyl)phenyl
30	H	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
31	H	5-pyrimidyl	1-pyrrolidinocarbonyl
32	H	5-pyrimidyl	2-(methylsulfonyl)phenyl
33	H	5-pyrimidyl	4-morpholino
34	H	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
35	H	5-pyrimidyl	4-morpholinocarbonyl
36	H	2-Cl-phenyl	2-(aminosulfonyl)phenyl
37	H	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
38	H	2-Cl-phenyl	1-pyrrolidinocarbonyl
39	H	2-Cl-phenyl	2-(methylsulfonyl)phenyl
40	H	2-Cl-phenyl	4-morpholino
41	H	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
42	H	2-Cl-phenyl	4-morpholinocarbonyl
43	H	2-F-phenyl	2-(aminosulfonyl)phenyl
44	H	2-F-phenyl	2-(methylaminosulfonyl)phenyl
45	H	2-F-phenyl	1-pyrrolidinocarbonyl
46	H	2-F-phenyl	2-(methylsulfonyl)phenyl
47	H	2-F-phenyl	4-morpholino
48	H	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
49	H	2-F-phenyl	4-morpholinocarbonyl
50	H	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
51	H	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
52	H	2,5-diF-phenyl	1-pyrrolidinocarbonyl
53	H	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
54	H	2,5-diF-phenyl	4-morpholino
55	H	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
56	H	2,5-diF-phenyl	4-morpholinocarbonyl
57	H	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
58	H	phenyl	2-(N-piperidinyl-methyl)phenyl
59	H	phenyl	2-(N-morpholino-methyl)phenyl
60	H	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
61	H	phenyl	2-(N-pyridinium-methyl)phenyl
62	H	phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
63	H	phenyl	2-(N-azatanyl-methyl)phenyl
64	H	phenyl	2-(N-azetidinyl-methyl)phenyl
65	H	phenyl	2-(N-piperazinyl-methyl)phenyl
66	H	phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
67	H	phenyl	2-(N-imidazolyl-methyl)phenyl
68	H	phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
69	H	phenyl	2-(N-pyridonyl-methyl)phenyl
70	H	phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
71	H	phenyl	2-(amidinyl)phenyl
72	H	phenyl	2-(N-guanidinyl)phenyl
73	H	phenyl	2-(imidazolyl)phenyl
74	H	phenyl	2-(imidazolidinyl)phenyl
75	H	phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
76	H	phenyl	2-(2-pyrrolidinyl)phenyl
77	H	phenyl	2-(2-piperidinyl)phenyl
78	H	phenyl	2-(amidinyl-methyl)phenyl
79	H	phenyl	2-(2-imidazolidinyl-methyl)phenyl
80	H	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
81	H	phenyl	2-dimethylaminoimidazol-1-yl
82	H	phenyl	2-(3-aminophenyl)
83	H	phenyl	2-(3-pyrrolidinylcarbonyl)
84	H	phenyl	2-glycinoyl
85	H	phenyl	2-(imidazol-1-ylacetyl)
86	H	2-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
87	H	2-pyridyl	2-(N-piperidinyl-methyl)phenyl
88	H	2-pyridyl	2-(N-morpholino-methyl)phenyl
89	H	2-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
90	H	2-pyridyl	2-(N-pyridinium-methyl)phenyl
91	H	2-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
92	H	2-pyridyl	2-(N-azatanyl-methyl)phenyl
93	H	2-pyridyl	2-(N-azetidinyl-methyl)phenyl
94	H	2-pyridyl	2-(N-piperazinyl-methyl)phenyl
95	H	2-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
96	H	2-pyridyl	2-(N-imidazolyl-methyl)phenyl
97	H	2-pyridyl	2-(N-methoxy-N-methylamino-methyl)phenyl
98	H	2-pyridyl	2-(N-pyridonyl-methyl)phenyl
99	H	2-pyridyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
100	H	2-pyridyl	2-(amidinyl)phenyl
101	H	2-pyridyl	2-(N-guanidinyl)phenyl
102	H	2-pyridyl	2-(imidazolyl)phenyl
103	H	2-pyridyl	2-(imidazolidinyl)phenyl
104	H	2-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
105	H	2-pyridyl	2-(2-pyrrolidinyl)phenyl
106	H	2-pyridyl	2-(2-piperidinyl)phenyl
107	H	2-pyridyl	2-(amidinyl-methyl)phenyl
108	H	2-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
109	H	2-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
110	H	2-pyridyl	2-dimethylaminoimidazol-1-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	2-(imidazol-1-ylacetyl)
115	H	3-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
116	H	3-pyridyl	2-(N-piperidinyl-methyl)phenyl
117	H	3-pyridyl	2-(N-morpholino-methyl)phenyl
118	H	3-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
119	H	3-pyridyl	2-(N-pyridinium-methyl)phenyl
120	H	3-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
121	H	3-pyridyl	2-(N-azatanyl-methyl)phenyl
122	H	3-pyridyl	2-(N-azetidinyl-methyl)phenyl
123	H	3-pyridyl	2-(N-piperazinyl-methyl)phenyl
124	H	3-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
125	H	3-pyridyl	2-(N-imidazolyl-methyl)phenyl
126	H	3-pyridyl	2-(N-methoxy-N-methylamino-methyl)phenyl
127	H	3-pyridyl	2-(N-pyridonyl-methyl)phenyl
128	H	3-pyridyl	2-(N-(N′,N-dimethylhydrazinyl-methyl)phenyl
129	H	3-pyridyl	2-(amidinyl)phenyl
130	H	3-pyridyl	2-(N-guanidinyl)phenyl
131	H	3-pyridyl	2-(imidazolyl)phenyl
132	H	3-pyridyl	2-(imidazolidinyl)phenyl
133	H	3-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
134	H	3-pyridyl	2-(2-pyrrolidinyl)phenyl
135	H	3-pyridyl	2-(2-piperidinyl)phenyl
136	H	3-pyridyl	2-(amidinyl-methyl)phenyl
137	H	3-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
138	H	3-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
139	H	3-pyridyl	2-dimethylaminoimidazol-1-yl
140	H	3-pyridyl	2-(3-aminophenyl)
141	H	3-pyridyl	2-(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-morpho1ino-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-Cl-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-Cl-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′-methylmorpholinium-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)phenyl
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-pyrrolidinyl)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-imidazolidinyl-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,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-1-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-pyrrolidinocarbonyl
263	—CN	phenyl	2-(methylsulfonyl)phenyl
264	—CN	phenyl	4-morpholino
265	—CN	phenyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
270	—CN	2-pyridyl	2-(methylsulfonyl)phenyl
271	—CN	2-pyridyl	4-morpholino
272	—CN	2-pyridyl	2-(1′-CF 3 -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-(1′-CF 3 -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-(1′-CF 3 -tetrazol-2-yl)phenyl
287	—CN	2-pyrimidyl	4-morpholinocarbonyl
288	—CN	5-pyrimidyl	2-(aminosulfonyl)phenyl
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-morpholino
293	—CN	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
294	—CN	5-pyrimidyl	4-morpholinocarbonyl
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′-CF 3 -tetrazol-2-yl)phenyl
301	—CN	2-Cl-phenyl	4-morpholinocarbonyl
302	—CN	2-F-phenyl	2-(aminosulfonyl)phenyl
303	—CN	2-F-phenyl	2-(methylaminosulfonyl)phenyl
304	—CN	2-F-phenyl	1-pyrrolidinocarbonyl
305	—CN	2-F-phenyl	2-(methylsulfonyl)phenyl
306	—CN	2-F-phenyl	4-morpholino
307	—CN	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
308	—CN	2-F-phenyl	4-morpholinocarbonyl
309	—CN	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
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′-CF 3 -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′,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)phehyl
347	—CN	2-pyridyl	2-(N-morpholino-methyl)phenyl
348	—CN	2-pyridyl	2-(N,N′-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′,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)phenyl
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-1-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′,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-1-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)phenyl
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-pyrrolidinyl)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)phehyl
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′,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-imidazolidinyl-methyl)phenyl
455	—CN	2-Cl-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
456	—CN	2-Cl-phenyl	2-dimethylaminoimidazol-1-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)phenyl
474	—CN	2-F-phenyl	2-(N-(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-pyrrolidinyl)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-imidazolidinyl-methyl)phenyl
484	—CN	2-F-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
485	—CN	2-F-phenyl	2-dimethylaminoimidazol-1-yl
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	2,5-diF-phenyl	2-(N-piperidinyl-methyl)phenyl
492	—CN	2,5-diF-phenyl	2-(N-morpholino-methyl)phenyl
493	—CN	2,5-diF-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
494	—CN	2,5-diF-phenyl	2-(N-pyridinium-methyl)phenyl
495	—CN	2,5-diF-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
496	—CN	2,5-diF-phenyl	2-(N-azatanyl-methyl)phenyl
497	—CN	2,5-diF-phenyl	2-(N-azetidinyl-methyl)phenyl
498	—CN	2,5-diF-phenyl	2-(N-piperazinyl-methyl)phenyl
499	—CN	2,5-diF-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
500	—CN	2,5-diF-phenyl	2-(N-imidazolyl-methyl)phenyl
501	—CN	2,5-diF-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
502	—CN	2,5-diF-phenyl	2-(N-pyridonyl-methyl)phenyl
503	—CN	2,5-diF-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
504	—CN	2,5-diF-phenyl	2-(amidinyl)phenyl
505	—CN	2,5-diF-phenyl	2-(N-guanidinyl)phenyl
506	—CN	2,5-diF-phenyl	2-(imidazolyl)phenyl
507	—CN	2,5-diF-phenyl	2-(imidazolidinyl)phenyl
508	—CN	2,5-diF-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
509	—CN	2,5-diF-phenyl	2-(2-pyrrolidinyl)phenyl
510	—CN	2,5-diF-phenyl	2-(2-piperidinyl)phenyl
511	—CN	2,5-diF-phenyl	2-(amidinyl-methyl)phenyl
512	—CN	2,5-diF-phenyl	2-(2-imidazolidinyl-methyl)phenyl
513	—CN	2,5-diF-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
514	—CN	2,5-diF-phenyl	2-dimethylaminoimidazol-1-yl
515	—CN	2,5-diF-phenyl	2-(3-aminophenyl)
516	—CN	2,5-diF-phenyl	2-(3-pyrrolidinylcarbonyl)
517	—CN	2,5-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-(1′-CF 3 -tetrazol-2-yl)phenyl
525	CF 3	phenyl	4-morpholinocarbonyl
526	CF 3	2-pyridyl	2-(aminosulfonyl)phenyl
527	CF 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
528	CF 3	2-pyridyl	1-pyrrolidinocarbonyl
529	CF 3	2-pyridyl	2-(methylsulfonyl)phenyl
530	CF 3	2-pyridyl	4-morpholino
531	CF 3	2-pyridyl	2-(1′-CF 3 -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′-CF 3 -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-(1′-CF 3 -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-pyrrolidinocarbonyl
550	CF 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
551	CF 3	5-pyrimidyl	4-morpholino
552	CF 3	5-pyrimidyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
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′-CF 3 -tetrazol-2-yl)phenyl
560	CF 3	2-Cl-phenyl	4-morpholinocarbonyl
561	CF 3	2-F-phenyl	2-(aminosulfonyl)phenyl
562	CF 3	2-F-phenyl	2-(methylaminosulfonyl)phenyl
563	CF 3	2-F-phenyl	1-pyrrolidinocarbonyl
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′-CF 3 -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′-CF 3 -tetrazol-2-yl)phenyl
574	CF 3	2,5-diF-phenyl	4-morpholinocarbonyl
575	CF 3	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
576	CF 3	phenyl	2-(N-piperidinyl-methyl)phenyl
577	CF 3	phenyl	2-(N-morpholino-methyl)phenyl
578	CF 3	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
579	CF 3	phenyl	2-(N-pyridinium-methyl)phenyl
580	CF 3	phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
581	CF 3	phenyl	2-(N-azatanyl-methyl)phenyl
582	CF 3	phenyl	2-(N-azetidinyl-methyl)phenyl
583	CF 3	phenyl	2-(N-piperazinyl-methyl)phenyl
584	CF 3	phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
585	CF 3	phenyl	2-(N-imidazolyl-methyl)phenyl
586	CF 3	phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
587	CF 3	phenyl	2-(N-pyridonyl-methyl)phenyl
588	CF 3	phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
589	CF 3	phenyl	2-(amidinyl)phenyl
590	CF 3	phenyl	2-(N-guanidinyl)phenyl
591	CF 3	phenyl	2-(imidazolyl)phenyl
592	CF 3	phenyl	2-(imidazolidinyl)phenyl
593	CF 3	phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
594	CF 3	phenyl	2-(2-pyrrolidinyl)phenyl
595	CF 3	phenyl	2-(2-piperidinyl)phenyl
596	CF 3	phenyl	2-(amidinyl-methyl)phenyl
597	CF 3	phenyl	2-(2-imidazolidinyl-methyl)phenyl
598	CF 3	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
599	CF 3	phenyl	2-dimethylaminoimidazol-1-yl
600	CF 3	phenyl	2-(3-aminophenyl)
601	CF 3	phenyl	2-(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-(N-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	2-(N-(2-aminoimidazolyl)-methyl)phenyl
628	CF 3	2-pyridyl	2-dimethylaminoimidazol-1-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-imidazolidinyl-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	2-(3-aminophenyl)
659	CF 3	3-pyridyl	2-(3-pyrrolidinylcarbonyl)
660	CF 3	3-pyridyl	2-glycinoyl
661	CF 3	3-pyridyl	2-(imidazol-1-ylacetyl)
662	CF 3	2-pyrimidyl	2-(N-pyrrolidinyl-methyl)phenyl
663	CF 3	2-pyrimidyl	2-(N-piperidinyl-methyl)phenyl
664	CF 3	2-pyrimidyl	2-(N-morpholino-methyl)phenyl
665	CF 3	2-pyrimidyl	2-(N,N′-methylmorpholinium-methyl)phenyl
666	CF 3	2-pyrimidyl	2-(N-pyridinium-methyl)phenyl
667	CF 3	2-pyrimidyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
668	CF 3	2-pyrimidyl	2-(N-azatanyl-methyl)phenyl
669	CF 3	2-pyrimidyl	2-(N-azetidinyl-methyl)phenyl
670	CF 3	2-pyrimidyl	2-(N-piperazinyl-methyl)phenyl
671	CF 3	2-pyrimidyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
672	CF 3	2-pyrimidyl	2-(N-imidazolyl-methyl)phenyl
673	CF 3	2-pyrimidyl	2-(N-methoxy-N-methylamino-methyl)phenyl
674	CF 3	2-pyrimidyl	2-(N-pyridonyl-methyl)phenyl
675	CF 3	2-pyrimidyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
676	CF 3	2-pyrimidyl	2-(amidinyl)phenyl
677	CF 3	2-pyrimidyl	2-(N-guanidinyl)phenyl
678	CF 3	2-pyrimidyl	2-(imidazolyl)phenyl
679	CF 3	2-pyrimidyl	2-(imidazolidinyl)phenyl
680	CF 3	2-pyrimidyl	2-(2-imidazolidinyl-sulfonyl)phenyl
681	CF 3	2-pyrimidyl	2-(2-pyrrolidinyl)phenyl
682	CF 3	2-pyrimidyl	2-(2-piperidinyl)phenyl
683	CF 3	2-pyrimidyl	2-(amidinyl-methyl)phenyl
684	CF 3	2-pyrimidyl	2-(2-imidazolidinyl-methyl)phenyl
685	CF 3	2-pyrimidyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
686	CF 3	2-pyrimidyl	2-dimethylaminoimidazol-1-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	2-(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′-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)phenyl
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-1-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)phenyl
743	CF 3	2-F-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
744	CF 3	2-F-phenyl	2-dimethylaminoimidazol-1-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)phenyl
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-pyrrolidinocarbonyl
781	CONH 2	phenyl	2-(methylsulfonyl)phenyl
782	CONH 2	phenyl	4-morpholino
783	CONH 2	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
784	CONH 2	phenyl	4-morpholinocarbonyl
785	CONH 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	CONH 2	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
791	CONH 2	2-pyridyl	4-morpholinocarbonyl
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′-CF 3 -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-pyrrolidinocarbonyl
802	CONH 2	2-pyrimidyl	2-(methylsulfonyl)phenyl
803	CONH 2	2-pyrimidyl	4-morpholino
804	CONH 2	2-pyrimidyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
809	CONH 2	5-pyrimidyl	2-(methylsulfonyl)phenyl
810	CONH 2	5-pyrimidyl	4-morpholino
811	CONH 2	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
812	CONH 2	5-pyrimidyl	4-morpholinocarbonyl
813	CONH 2	2-Cl-phenyl	2-(aminosulfonyl)phenyl
814	CONH 2	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
815	CONH 2	2-Cl-phenyl	1-pyrrolidinocarbonyl
816	CONH 2	2-Cl-phenyl	2-(methylsulfonyl)phenyl
817	CONH 2	2-Cl-phenyl	4-morpholino
818	CONH 2	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
819	CONH 2	2-Cl-phenyl	4-morpholinocarbonyl
820	CONH 2	2-F-phenyl	2-(aminosulfonyl)phenyl
821	CONH 2	2-F-phenyl	2-(methylaminosulfonyl)phenyl
822	CONH 2	2-F-phenyl	1-pyrrolidinocarbonyl
823	CONH 2	2-F-phenyl	2-(methylsulfonyl)phenyl
824	CONH 2	2-F-phenyl	4-morpholino
825	CONH 2	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
826	CONH 2	2-F-phenyl	4-morpholinocarbonyl
827	CONH 2	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
828	CONH 2	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
829	CONH 2	2,5-diF-phenyl	1-pyrrolidinocarbonyl
830	CONH 2	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
831	CONH 2	2,5-diF-phenyl	4-morpholino
832	CONH 2	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
833	CONH 2	2,5-diF-phenyl	4-morpholinocarbonyl
834	CONH 2	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
835	CONH 2	phenyl	2-(N-piperidinyl-methyl)phenyl
836	CONH 2	phenyl	2-(N-morpholino-methyl)phenyl
837	CONH 2	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
838	CONH 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)phenyl
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
857	CONH 2	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
858	CONH 2	phenyl	2-dimethylaminoimidazol-1-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-imidazolidinyl-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 2	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-imidazolidinyl-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 2	3-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
916	CONH 2	3-pyridyl	2-dimethylaminoimidazol-1-yl
917	CONH 2	3-pyridyl	2-(3-aminophenyl)
918	CONH 2	3-pyridyl	2-(3-pyrrolidinylcarbonyl)
919	CONH 2	3-pyridyl	2-glycinoyl
920	CONH 2	3-pyridyl	2-(imidazol-1-ylacetyl)
921	CONH 2	2-pyrimidyl	2-(N-pyrrolidinyl-methyl)phenyl
922	CONH 2	2-pyrimidyl	2-(N-piperidinyl-methyl)phenyl
923	CONH 2	2-pyrimidyl	2-(N-morpholino-methyl)phenyl
924	CONH 2	2-pyrimidyl	2-(N,N′-methylmorpholinium-methyl)phenyl
925	CONH 2	2-pyrimidyl	2-(N-pyridinium-methyl)phenyl
926	CONH 2	2-pyrimidyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
927	CONH 2	2-pyrimidyl	2-(N-azatanyl-methyl)phenyl
928	CONH 2	2-pyrimidyl	2-(N-azetidinyl-methyl)phenyl
929	CONH 2	2-pyrimidyl	2-(N-piperazinyl-methyl)phenyl
930	CONH 2	2-pyrimidyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
931	CONH 2	2-pyrimidyl	2-(N-imidazolyl-methyl)phenyl
932	CONH 2	2-pyrimidyl	2-(N-methoxy-N-methylamino-methyl)phenyl
933	CONH 2	2-pyrimidyl	2-(N-pyridonyl-methyl)phenyl
934	CONH 2	2-pyrimidyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
935	CONH 2	2-pyrimidyl	2-(amidinyl)phenyl
936	CONH 2	2-pyrimidyl	2-(N-guanidinyl)phenyl
937	CONH 2	2-pyrimidyl	2-(imidazolyl)phenyl
938	CONH 2	2-pyrimidyl	2-(imidazolidinyl)phenyl
939	CONH 2	2-pyrimidyl	2-(2-imidazolidinyl-sulfonyl)phenyl
940	CONH 2	2-pyrimidyl	2-(2-pyrrolidinyl)phenyl
941	CONH 2	2-pyrimidyl	2-(2-piperidinyl)phenyl
942	CONH 2	2-pyrimidyl	2-(amidinyl-methyl)phenyl
943	CONH 2	2-pyrimidyl	2-(2-imidazolidinyl-methyl)phenyl
944	CONH 2	2-pyrimidyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
945	CONH 2	2-pyrimidyl	2-dimethylaminoimidazol-1-yl
946	CONH 2	2-pyrimidyl	2-(3-aminophenyl)
947	CONH 2	2-pyrimidyl	2-(3-pyrrolidinylcarbonyl)
948	CONH 2	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	CONH 2	2-Cl-phenyl	2-(N-piperidinyl-methyl)phenyl
952	CONH 2	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)phenyl
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	CONH 2	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	CONH 2	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	2-(N-(2-aminoimidazolyl)-methyl)phenyl
974	CONH 2	2-Cl-phenyl	2-dimethylaminoimidazol-1-yl
975	CONH 2	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-morpholino-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)phenyl
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	CONH 2	2-F-phenyl	2-(N-imidazolyl-methyl)phenyl
990	CONH 2	2-F-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
991	CONH 2	2-F-phenyl	2-(N-pyridonyl-methyl)phenyl
992	CONH 2	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	2-(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	2-(imidazol-1-ylacetyl)
1008	CONH 2	2,5-diF-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1009	CONH 2	2,5-diF-phenyl	2-(N-piperidinyl-methyl)phenyl
1010	CONH 2	2,5-diF-phenyl	2-(N-morpholino-methyl)phenyl
1011	CONH 2	2,5-diF-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1012	CONH 2	2,5-diF-phenyl	2-(N-pyridinium-methyl)phenyl
1013	CONH 2	2,5-diF-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1014	CONH 2	2,5-diF-phenyl	2-(N-azatanyl-methyl)phenyl
1015	CONH 2	2,5-diF-phenyl	2-(N-azetidinyl-methyl)phenyl
1016	CONH 2	2,5-diF-phenyl	2-(N-piperazinyl-methyl)phenyl
1017	CONH 2	2,5-diF-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1018	CONH 2	2,5-diF-phenyl	2-(N-imidazolyl-methyl)phenyl
1019	CONH 2	2,5-diF-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1020	CONH 2	2,5-diF-phenyl	2-(N-pyridonyl-methyl)phenyl
1021	CONH 2	2,5-diF-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1022	CONH 2	2,5-diF-phenyl	2-(amidinyl)phenyl
1023	CONH 2	2,5-diF-phenyl	2-(N-guanidinyl)phenyl
1024	CONH 2	2,5-diF-phenyl	2-(imidazolyl)phenyl
1025	CONH 2	2,5-diF-phenyl	2-(imidazolidinyl)phenyl
1026	CONH 2	2,5-diF-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1027	CONH 2	2,5-diF-phenyl	2-(2-pyrrolidinyl)phenyl
1028	CONH 2	2,5-diF-phenyl	2-(2-piperidinyl)phenyl
1029	CONH 2	2,5-diF-phenyl	2-(amidinyl-methyl)phenyl
1030	CONH 2	2,5-diF-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1031	CONH 2	2,5-diF-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1032	CONH 2	2,5-diF-phenyl	2-dimethylaminoimidazol-1-yl
1033	CONH 2	2,5-diF-phenyl	2-(3-aminophenyl)
1034	CONH 2	2,5-diF-phenyl	2-(3-pyrrolidinylcarbonyl)
1035	CONH 2	2,5-diF-phenyl	2-glycinoyl
1036	CONH 2	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-(1′-CF 3 -tetrazol-2-yl)phenyl
1043	SCH 3	phenyl	4-morpholinocarbonyl
1044	SCH 3	2-pyridyl	2-(aminosulfonyl)phenyl
1045	SCH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
1046	SCH 3	2-pyridyl	1-pyrrolidinocarbonyl
1047	SCH 3	2-pyridyl	2-(methylsulfonyl)phenyl
1048	SCH 3	2-pyridyl	4-morpholino
1049	SCH 3	2-pyridyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
1054	SCH 3	3-pyridyl	2-(methylsulfonyl)phenyl
1055	SCH 3	3-pyridyl	4-morpholino
1056	SCH 3	3-pyridyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
1061	SCH 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
1062	SCH 3	2-pyrimidyl	4-morpholino
1063	SCH 3	2-pyrimidyl	2 (1′-CF 3 -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-pyrrolidinocarbonyl
1068	SCH 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
1069	SCH 3	5-pyrimidyl	4-morpholino
1070	SCH 3	5-pyrimidyl	2-(1′-CF 3 -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′-CF 3 -tetrazol-2-yl)phenyl
1078	SCH 3	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′-CF 3 -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)phenyl
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′-CF 3 -tetrazol-2-yl)phenyl
1092	SCH 3	2,5-diF-phenyl	4-morpholinocarbonyl
1093	SCH 3	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1094	SCH 3	phenyl	2-(N-piperidinyl-methyl)phenyl
1095	SCH 3	phenyl	2-(N-morpholino-methyl)phenyl
1096	SCH 3	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1097	SCH 3	phenyl	2-(N-pyridinium-methyl)phenyl
1098	SCH 3	phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1099	SCH 3	phenyl	2-(N-azatanyl-methyl)phenyl
1100	SCH 3	phenyl	2-(N-azetidinyl-methyl)phenyl
1101	SCH 3	phenyl	2-(N-piperazinyl-methyl)phenyl
1102	SCH 3	phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1103	SCH 3	phenyl	2-(N-imidazolyl-methyl)phenyl
1104	SCH 3	phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1105	SCH 3	phenyl	2-(N-pyridonyl-methyl)phenyl
1106	SCH 3	phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1107	SCH 3	phenyl	2-(amidinyl)phenyl
1108	SCH 3	phenyl	2-(N-guanidinyl)phenyl
1109	SCH 3	phenyl	2-(imidazolyl)phenyl
1110	SCH 3	phenyl	2-(imidazolidinyl)phenyl
1111	SCH 3	phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1112	SCH 3	phenyl	2-(2-pyrrolidinyl)phenyl
1113	SCH 3	phenyl	2-(2-piperidinyl)phenyl
1114	SCH 3	phenyl	2-(amidinyl-methyl)phenyl
1115	SCH 3	phenyl	2-(2-imidazolidinyl-methyl)phenyl
1116	SCH 3	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1117	SCH 3	phenyl	2-dimethylaminoimidazol-1-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-(imidazolidinyl)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-pyridel	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-piperidinyl)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-1-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-pyrrolidinyl-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-piperazinyl-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-methyl)phenyl
1192	SCH 3	2-pyrimidyl	2-(N-pyridonyl-methyl)phenyl
1193	SCH 3	2-pyrimidyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1194	SCH 3	2-pyrimidyl	2-(amidinyl)phenyl
1195	SCH 3	2-pyrimidyl	2-(N-guanidinyl)phenyl
1196	SCH 3	2-pyrimidyl	2-(imidazolyl)phenyl
1197	SCH 3	2-pyrimidyl	2-(imidazolidinyl)phenyl
1198	SCH 3	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
1203	SCH 3	2-pyrimidyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1204	SCH 3	2-pyrimidyl	2-dimethylaminoimidazol-1-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-methyl)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	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1233	SCH 3	2-Cl-phenyl	2-dimethylaminoimidazol-1-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	SCH 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 3	2-F-phenyl	2-(imidazolidinyl)phenyl
1256	SCH 3	2-F-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1257	SCH 3	2-F-phenyl	2-(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-methyl)phenyl
1261	SCH 3	2-F-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1262	SCH 3	2-F-phenyl	2-dimethylaminoimidazol-1-yl
1263	SCH 3	2-F-phenyl	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′,N′-dimethylhydrazinyl-methyl)phenyl
1281	SCH 3	2,5-diF-phenyl	2-(amidinyl)phenyl
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-aminolinidazolyl)-methyl)phenyl
1291	SCH 3	2,5-diF-phenyl	2-dimethylaminoimidazol-1-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	SO 2 CH 3	phenyl	2-(aminosulfonyl)phenyl
1297	SO 2 CH 3	phenyl	2-(methylaminosulfonyl)phenyl
1298	SO 2 CH 3	phenyl	1-pyrrolidinocarbonyl
1299	SO 2 CH 3	phenyl	2-(methylsulfonyl)phenyl
1300	SO 2 CH 3	phenyl	4-morpholino
1301	SO 2 CH 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1302	SO 2 CH 3	phenyl	4-morpholinocarbonyl
1303	SO 2 CH 3	2-pyridyl	2-(aminosulfonyl)phenyl
1304	SO 2 CH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
1305	SO 2 CH 3	2-pyridyl	1-pyrrolidinocarbonyl
1306	SO 2 CH 3	2-pyridyl	2-(methylsulfonyl)phenyl
1307	SO 2 CH 3	2-pyridyl	4-morpholino
1308	SO 2 CH 3	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1309	SO 2 CH 3	2-pyridyl	4-morpholinocarbonyl
1310	SO 2 CH 3	3-pyridyl	2-(aminosulfonyl)phenyl
1311	SO 2 CH 3	3-pyridyl	2-(methylaminosulfonyl)phenyl
1312	SO 2 CH 3	3-pyridyl	1-pyrrolidinocarbonyl
1313	SO 2 CH 3	3-pyridyl	2-(methylsulfonyl)phenyl
1314	SO 2 CH 3	3-pyridyl	4-morpholino
1315	SO 2 CH 3	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1316	SO 2 CH 3	3-pyridyl	4-morpholinocarbonyl
1317	SO 2 CH 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
1318	SO 2 CH 3	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
1319	SO 2 CH 3	2-pyrimidyl	1-pyrrolidinocarbonyl
1320	SO 2 CH 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
1321	SO 2 CH 3	2-pyrimidyl	4-morpholino
1322	SO 2 CH 3	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1323	SO 2 CH 3	2-pyrimidyl	4-morpholinocarbonyl
1324	SO 2 CH 3	5-pyrimidyl	2-(aminosulfonyl)phenyl
1325	SO 2 CH 3	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
1326	SO 2 CH 3	5-pyrimidyl	1-pyrrolidinocarbonyl
1327	SO 2 CH 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
1328	SO 2 CH 3	5-pyrimidyl	4-morpholino
1329	SO 2 CH 3	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1330	SO 2 CH 3	5-pyrimidyl	4-morpholinocarbonyl
1331	SO 2 CH 3	2-Cl-phenyl	2-(aminosulfonyl)phenyl
1332	SO 2 CH 3	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
1333	SO 2 CH 3	2-Cl-phenyl	1-pyrrolidinocarbonyl
1334	SO 2 CH 3	2-Cl-phenyl	2-(methylsulfonyl)phenyl
1335	SO 2 CH 3	2-Cl-phenyl	4-morpholino
1336	SO 2 CH 3	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1337	SO 2 CH 3	2-Cl-phenyl	4-morpholinocarbonyl
1338	SO 2 CH 3	2-F-phenyl	2-(aminosulfonyl)phenyl
1339	SO 2 CH 3	2-F-phenyl	2-(methylaminosulfonyl)phenyl
1340	SO 2 CH 3	2-F-phenyl	1-pyrrolidinocarbonyl
1341	SO 2 CH 3	2-F-phenyl	2-(methylsulfonyl)phenyl
1342	SO 2 CH 3	2-F-phenyl	4-morpholino
1343	SO 2 CH 3	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1344	SO 2 CH 3	2-F-phenyl	4-morpholinocarbonyl
1345	SO 2 CH 3	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
1346	SO 2 CH 3	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
1347	SO 2 CH 3	2,5-diF-phenyl	1-pyrrolidinocarbonyl
1348	SO 2 CH 3	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
1349	SO 2 CH 3	2,5-diF-phenyl	4-morpholino
1350	SO 2 CH 3	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1351	SO 2 CH 3	2,5-diF-phenyl	4-morpholinocarbonyl
1352	SO 2 CH 3	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1353	SO 2 CH 3	phenyl	2-(N-piperidinyl-methyl)phenyl
1354	SO 2 CH 3	phenyl	2-(N-morpholino-methyl)phenyl
1355	SO 2 CH 3	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1356	SO 2 CH 3	phenyl	2-(N-pyridinium-methyl)phenyl
1357	SO 2 CH 3	phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1358	SO 2 CH 3	phenyl	2-(N-azatanyl-methyl)phenyl
1359	SO 2 CH 3	phenyl	2-(N-azetidinyl-methyl)phenyl
1360	SO 2 CH 3	phenyl	2-(N-piperazinyl-methyl)phenyl
1361	SO 2 CH 3	phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1362	SO 2 CH 3	phenyl	2-(N-imidazolyl-methyl)phenyl
1363	SO 2 CH 3	phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1364	SO 2 CH 3	phenyl	2-(N-pyridonyl-methyl)phenyl
1365	SO 2 CH 3	phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1366	SO 2 CH 3	phenyl	2-(amidinyl)phenyl
1367	SO 2 CH 3	phenyl	2-(N-guanidinyl)phenyl
1368	SO 2 CH 3	phenyl	2-(imidazolyl)phenyl
1369	SO 2 CH 3	phenyl	2-(imidazolidinyl)phenyl
1370	SO 2 CH 3	phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1371	SO 2 CH 3	phenyl	2-(2-pyrrolidinyl)phenyl
1372	SO 2 CH 3	phenyl	2-(2-piperidinyl)phenyl
1373	SO 2 CH 3	phenyl	2-(amidinyl-methyl)phenyl
1374	SO 2 CH 3	phenyl	2-(2-imidazolidinyl-methyl)phenyl
1375	SO 2 CH 3	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1376	SO 2 CH 3	phenyl	2-dimethylaminoimidazol-1-yl
1377	SO 2 CH 3	phenyl	2-(3-aminophenyl)
1378	SO 2 CH 3	phenyl	2-(3-pyrrolidinylcarbonyl)
1379	SO 2 CH 3	phenyl	2-glycinoyl
1380	SO 2 CH 3	phenyl	2-(imidazol-1-ylacetyl)
1381	SO 2 CH 3	2-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
1382	SO 2 CH 3	2-pyridyl	2-(N-piperidinyl-methyl)phenyl
1383	SO 2 CH 3	2-pyridyl	2-(N-morpholino-methyl)phenyl
1384	SO 2 CH 3	2-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1385	SO 2 CH 3	2-pyridyl	2-(N-pyridinium-methyl)phenyl
1386	SO 2 CH 3	2-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1387	SO 2 CH 3	2-pyridyl	2-(N-azatanyl-methyl)phenyl
1388	SO 2 CH 3	2-pyridyl	2-(N-azetidinyl-methyl)phenyl
1389	SO 2 CH 3	2-pyridyl	2-(N-piperazinyl-methyl)phenyl
1390	SO 2 CH 3	2-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1391	SO 2 CH 3	2-pyridyl	2-(N-imidazolyl-methyl)phenyl
1392	SO 2 CH 3	2-pyridyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1393	SO 2 CH 3	2-pyridyl	2-(N-pyridonyl-methyl)phenyl
1394	SO 2 CH 3	2-pyridyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1395	SO 2 CH 3	2-pyridyl	2-(amidinyl)phenyl
1396	SO 2 CH 3	2-pyridyl	2-(N-guanidinyl)phenyl
1397	SO 2 CH 3	2-pyridyl	2-(imidazolyl)phenyl
1398	SO 2 CH 3	2-pyridyl	2-(imidazolidinyl)phenyl
1399	SO 2 CH 3	2-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1400	SO 2 CH 3	2-pyridyl	2-(2-pyrrolidinyl)phenyl
1401	SO 2 CH 3	2-pyridyl	2-(2-piperidinyl)phenyl
1402	SO 2 CH 3	2-pyridyl	2-(amidinyl-methyl)phenyl
1403	SO 2 CH 3	2-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
1404	SO 2 CH 3	2-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1405	SO 2 CH 3	2-pyridyl	2-dimethylaminoimidazol-1-yl
1406	SO 2 CH 3	2-pyridyl	2-(3-aminophenyl)
1407	SO 2 CH 3	2-pyridyl	2-(3-pyrrolidinylcarbonyl)
1408	SO 2 CH 3	2-pyridyl	2-glycinoyl
1409	SO 2 CH 3	2-pyridyl	2-(imidazol-1-ylacetyl)
1410	SO 2 CH 3	3-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
1411	SO 2 CH 3	3-pyridyl	2-(N-piperidinyl-methyl)phenyl
1412	SO 2 CH 3	3-pyridyl	2-(N-morpholino-methyl)phenyl
1413	SO 2 CH 3	3-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1414	SO 2 CH 3	3-pyridyl	2-(N-pyridinium-methyl)phenyl
1415	SO 2 CH 3	3-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1416	SO 2 CH 3	3-pyridyl	2-(N-azatanyl-methyl)phenyl
1417	SO 2 CH 3	3-pyridyl	2-(N-azetidinyl-methyl)phenyl
1418	SO 2 CH 3	3-pyridyl	2-(N-piperazinyl-methyl)phenyl
1419	SO 2 CH 3	3-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1420	SO 2 CH 3	3-pyridyl	2-(N-imidazolyl-methyl)phenyl
1421	SO 2 CH 3	3-pyridyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1422	SO 2 CH 3	3-pyridyl	2-(N-pyridonyl-methyl)phenyl
1423	SO 2 CH 3	3-pyridyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1424	SO 2 CH 3	3-pyridyl	2-(amidinyl)phenyl
1425	SO 2 CH 3	3-pyridyl	2-(N-guanidinyl)phenyl
1426	SO 2 CH 3	3-pyridyl	2-(imidazolyl)phenyl
1427	SO 2 CH 3	3-pyridyl	2-(imidazolidinyl)phenyl
1428	SO 2 CH 3	3-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1429	SO 2 CH 3	3-pyridyl	2-(2-pyrrolidinyl)phenyl
1430	SO 2 CH 3	3-pyridyl	2-(2-piperidinyl)phenyl
1431	SO 2 CH 3	3-pyridyl	2-(amidinyl-methyl)phenyl
1432	SO 2 CH 3	3-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
1433	SO 2 CH 3	3-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1434	SO 2 CH 3	3-pyridyl	2-dimethylaminoimidazol-1-yl
1435	SO 2 CH 3	3-pyridyl	2-(3-aminophenyl)
1436	SO 2 CH 3	3-pyridyl	2-(3-pyrrolidinylcarbonyl)
1437	SO 2 CH 3	3-pyridyl	2-glycinoyl
1438	SO 2 CH 3	3-pyridyl	2-(imidazol-1-ylacetyl)
1439	SO 2 CH 3	2-pyrimidyl	2-(N-pyrrolidinyl-methyl)phenyl
1440	SO 2 CH 3	2-pyrimidyl	2-(N-piperidinyl-methyl)phenyl
1441	SO 2 CH 3	2-pyrimidyl	2-(N-morpholino-methyl)phenyl
1442	SO 2 CH 3	2-pyrimidyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1443	SO 2 CH 3	2-pyrimidyl	2-(N-pyridinium-methyl)phenyl
1444	SO 2 CH 3	2-pyrimidyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1445	SO 2 CH 3	2-pyrimidyl	2-(N-azatanyl-methyl)phenyl
1446	SO 2 CH 3	2-pyrimidyl	2-(N-azetidinyl-methyl)phenyl
1447	SO 2 CH 3	2-pyrimidyl	2-(N-piperazinyl-methyl)phenyl
1448	SO 2 CH 3	2-pyrimidyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1449	SO 2 CH 3	2-pyrimidyl	2-(N-imidazolyl-methyl)phenyl
1450	SO 2 CH 3	2-pyrimidyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1451	SO 2 CH 3	2-pyrimidyl	2-(N-pyridonyl-methyl)phenyl
1452	SO 2 CH 3	2-pyrimidyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1453	SO 2 CH 3	2-pyrimidyl	2-(amidinyl)phenyl
1454	SO 2 CH 3	2-pyrimidyl	2-(N-guanidinyl)phenyl
1455	SO 2 CH 3	2-pyrimidyl	2-(imidazolyl)phenyl
1456	SO 2 CH 3	2-pyrimidyl	2-(imidazolidinyl)phenyl
1457	SO 2 CH 3	2-pyrimidyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1458	SO 2 CH 3	2-pyrimidyl	2-(2-pyrrolidinyl)phenyl
1459	SO 2 CH 3	2-pyrimidyl	2-(2-piperidinyl)phenyl
1460	SO 2 CH 3	2-pyrimidyl	2-(amidinyl-methyl)phenyl
1461	SO 2 CH 3	2-pyrimidyl	2-(2-imidazolidinyl-methyl)phenyl
1462	SO 2 CH 3	2-pyrimidyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1463	SO 2 CH 3	2-pyrimidyl	2-dimethylaminoimidazol-1-yl
1464	SO 2 CH 3	2-pyrimidyl	2-(3-aminophenyl)
1465	SO 2 CH 3	2-pyrimidyl	2-(3-pyrrolidinylcarbonyl)
1466	SO 2 CH 3	2-pyrimidyl	2-glycinoyl
1467	SO 2 CH 3	2-pyrimidyl	2-(imidazol-1-ylacetyl)
1468	SO 2 CH 3	2-Cl-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1469	SO 2 CH 3	2-Cl-phenyl	2-(N-piperidinyl-methyl)phenyl
1470	SO 2 CH 3	2-Cl-phenyl	2-(N-morpholino-methyl)phenyl
1471	SO 2 CH 3	2-Cl-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1472	SO 2 CH 3	2-Cl-phenyl	2-(N-pyridinium-methyl)phenyl
1473	SO 2 CH 3	2-Cl-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1474	SO 2 CH 3	2-Cl-phenyl	2-(N-azatanyl-methyl)phenyl
1475	SO 2 CH 3	2-Cl-phenyl	2-(N-azetidinyl-methyl)phenyl
1476	SO 2 CH 3	2-Cl-phenyl	2-(N-piperazinyl-methyl)phenyl
1477	SO 2 CH 3	2-Cl-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1478	SO 2 CH 3	2-Cl-phenyl	2-(N-imidazolyl-methyl)phenyl
1479	SO 2 CH 3	2-Cl-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1480	SO 2 CH 3	2-Cl-phenyl	2-(N-pyridonyl-methyl)phenyl
1481	SO 2 CH 3	2-Cl-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1482	SO 2 CH 3	2-Cl-phenyl	2-(amidinyl)phenyl
1483	SO 2 CH 3	2-Cl-phenyl	2-(N-guanidinyl)phenyl
1484	SO 2 CH 3	2-Cl-phenyl	2-(imidazolyl)phenyl
1485	SO 2 CH 3	2-Cl-phenyl	2-(imidazolidinyl)phenyl
1486	SO 2 CH 3	2-Cl-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1487	SO 2 CH 3	2-Cl-phenyl	2-(2-pyrrolidinyl)phenyl
1488	SO 2 CH 3	2-Cl-phenyl	2-(2-piperidinyl)phenyl
1489	SO 2 CH 3	2-Cl-phenyl	2-(amidinyl-methyl)phenyl
1490	SO 2 CH 3	2-Cl-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1491	SO 2 CH 3	2-Cl-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1492	SO 2 CH 3	2-Cl-phenyl	2-dimethylaminoimidazol-1-yl
1493	SO 2 CH 3	2-Cl-phenyl	2-(3-aminophenyl)
1494	SO 2 CH 3	2-Cl-phenyl	2-(3-pyrrolidinylcarbonyl)
1495	SO 2 CH 3	2-Cl-phenyl	2-glycinoyl
1496	SO 2 CH 3	2-Cl-phenyl	2-(imidazol-1-ylacetyl)
1497	SO 2 CH 3	2-F-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1498	SO 2 CH 3	2-F-phenyl	2-(N-piperidinyl-methyl)phenyl
1499	SO 2 CH 3	2-F-phenyl	2-(N-morpholino-methyl)phenyl
1500	SO 2 CH 3	2-F-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1501	SO 2 CH 3	2-F-phenyl	2-(N-Pyridinium-methyl)phenyl
1502	SO 2 CH 3	2-F-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1503	SO 2 CH 3	2-F-phenyl	2-(N-azatanyl-methyl)phenyl
1504	SO 2 CH 3	2-F-phenyl	2-(N-azetidinyl-methyl)phenyl
1505	SO 2 CH 3	2-F-phenyl	2-(N-piperazinyl-methyl)phenyl
1506	SO 2 CH 3	2-F-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1507	SO 2 CH 3	2-F-phenyl	2-(N-imidazolyl-methyl)phenyl
1508	SO 2 CH 3	2-F-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1509	SO 2 CH 3	2-F-phenyl	2-(N-pyridonyl-methyl)phenyl
1510	SO 2 CH 3	2-F-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1511	SO 2 CH 3	2-F-phenyl	2-(amidinyl)phenyl
1512	SO 2 CH 3	2-F-phenyl	2-(N-guanidinyl)phenyl
1513	SO 2 CH 3	2-F-phenyl	2-(imidazolyl)phenyl
1514	SO 2 CH 3	2-F-phenyl	2-(imidazolidinyl)phenyl
1515	SO 2 CH 3	2-F-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1516	SO 2 CH 3	2-F-phenyl	2-(2-pyrrolidinyl)phenyl
1517	SO 2 CH 3	2-F-phenyl	2-(2-piperidinyl)phenyl
1518	SO 2 CH 3	2-F-phenyl	2-(amidinyl-methyl)phenyl
1519	SO 2 CH 3	2-F-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1520	SO 2 CH 3	2-F-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1521	SO 2 CH 3	2-F-phenyl	2-dimethylaminoimidazol-1-yl
1522	SO 2 CH 3	2-F-phenyl	2-(3-aminophenyl)
1523	SO 2 CH 3	2-F-phenyl	2-(3-pyrrolidinylcarbonyl)
1524	SO 2 CH 3	2-F-phenyl	2-glycinoyl
1525	SO 2 CH 3	2-F-phenyl	2-(imidazol-1-ylacetyl)
1526	SO 2 CH 3	2,5-diF-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1527	SO 2 CH 3	2,5-diF-phenyl	2-(N-piperidinyl-methyl)phenyl
1528	SO 2 CH 3	2,5-diF-phenyl	2-(N-morpholino-methyl)phenyl
1529	SO 2 CH 3	2,5-diF-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1530	SO 2 CH 3	2,5-diF-phenyl	2-(N-pyridinium-methyl)phenyl
1531	SO 2 CH 3	2,5-diF-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1532	SO 2 CH 3	2,5-diF-phenyl	2-(N-azatanyl-methyl)phenyl
1533	SO 2 CH 3	2,5-diF-phenyl	2-(N-azetidinyl-methyl)phenyl
1534	SO 2 CH 3	2,5-diF-phenyl	2-(N-piperazinyl-methyl)phenyl
1535	SO 2 CH 3	2,5-diF-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1536	SO 2 CH 3	2,5-diF-phenyl	2-(N-imidazolyl-methyl)phenyl
1537	SO 2 CH 3	2,5-diF-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1538	SO 2 CH 3	2,5-diF-phenyl	2-(N-pyridonyl-methyl)phenyl
1539	SO 2 CH 3	2,5-diF-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1540	SO 2 CH 3	2,5-diF-phenyl	2-(amidinyl)phenyl
1541	SO 2 CH 3	2,5-diF-phenyl	2-(N-guanidinyl)phenyl
1542	SO 2 CH 3	2,5-diF-phenyl	2-(imidazolyl)phenyl
1543	SO 2 CH 3	2,5-diF-phenyl	2-(imidazolidinyl)phenyl
1544	SO 2 CH 3	2,5-diF-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1545	SO 2 CH 3	2,5-diF-phenyl	2-(2-pyrrolidinyl)phenyl
1546	SO 2 CH 3	2,5-diF-phenyl	2-(2-piperidinyl)phenyl
1547	SO 2 CH 3	2,5-diF-phenyl	2-(amidinyl-methyl)phenyl
1548	SO 2 CH 3	2,5-diF-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1549	SO 2 CH 3	2,5-diF-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1550	SO 2 CH 3	2,5-diF-phenyl	2-dimethylaminoimidazol-1-yl
1551	SO 2 CH 3	2,5-diF-phenyl	2-(3-aminophenyl)
1552	SO 2 CH 3	2,5-diF-phenyl	2-(3-pyrrolidinylcarbonyl)
1553	SO 2 CH 3	2,5-diF-phenyl	2-glycinoyl
1554	SO 2 CH 3	2,5-diF-phenyl	2-(imidazol-1-ylacetyl)
1555	NHSO 2 CH 3	phenyl	2-(aminosulfonyl)phenyl
1556	NHSO 2 CH 3	phenyl	2-(methylaminosulfonyl)phenyl
1557	NHSO 2 CH 3	phenyl	1-pyrrolidinocarbonyl
1558	NHSO 2 CH 3	phenyl	2-(methylsulfonyl)phenyl
1559	NHSO 2 CH 3	phenyl	4-morpholino
1560	NHSO 2 CH 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1561	NHSO 2 CH 3	phenyl	4-morpholinocarbonyl
1562	NHSO 2 CH 3	2-pyridyl	2-(aminosulfonyl)phenyl
1563	NHSO 2 CH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
1564	NHSO 2 CH 3	2-pyridyl	1-pyrrolidinocarbonyl
1565	NHSO 2 CH 3	2-pyridyl	2-(methylsulfonyl)phenyl
1566	NHSO 2 CH 3	2-pyridyl	4-morpholino
1567	NHSO 2 CH 3	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1568	NHSO 2 CH 3	2-pyridyl	4-morpholinocarbonyl
1569	NHSO 2 CH 3	3-pyridyl	2-(aminosulfonyl)phenyl
1570	NHSO 2 CH 3	3-pyridyl	2-(methylaminosulfonyl)phenyl
1571	NHSO 2 CH 3	3-pyridyl	1-pyrrolidinocarbonyl
1572	NHSO 2 CH 3	3-pyridyl	2-(methylsulfonyl)phenyl
1573	NHSO 2 CH 3	3-pyridyl	4-morpholino
1574	NHSO 2 CH 3	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1575	NHSO 2 CH 3	3-pyridyl	4-morpholinocarbonyl
1576	NHSO 2 CH 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
1577	NHSO 2 CH 3	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
1578	NHSO 2 CH 3	2-pyrimidyl	1-pyrrolidinocarbonyl
1579	NHSO 2 CH 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
1580	NHSO 2 CH 3	2-pyrimidyl	4-morpholino
1581	NHSO 2 CH 3	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1582	NHSO 2 CH 3	2-pyrimidyl	4-morpholinocarbonyl
1583	NHSO 2 CH 3	5-pyrimidyl	2-(aminosulfonyl)phenyl
1584	NHSO 2 CH 3	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
1585	NHSO 2 CH 3	5-pyrimidyl	1-pyrrolidinocarbonyl
1586	NHSO 2 CH 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
1587	NHSO 2 CH 3	5-pyrimidyl	4-morpholino
1588	NHSO 2 CH 3	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1589	NHSO 2 CH 3	5-pyrimidyl	4-morpholinocarbonyl
1590	NHSO 2 CH 3	2-Cl-phenyl	2-(aminosulfonyl)phenyl
1591	NHSO 2 CH 3	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
1592	NHSO 2 CH 3	2-Cl-phenyl	1-pyrrolidinocarbonyl
1593	NHSO 2 CH 3	2-Cl-phenyl	2-(methylsulfonyl)phenyl
1594	NHSO 2 CH 3	2-Cl-phenyl	4-morpholino
1595	NHSO 2 CH 3	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1596	NHSO 2 CH 3	2-Cl-phenyl	4-morpholinocarbonyl
1597	NHSO 2 CH 3	2-F-phenyl	2-(aminosulfonyl)phenyl
1598	NHSO 2 CH 3	2-F-phenyl	2-(methylaminosulfonyl)phenyl
1599	NHSO 2 CH 3	2-F-phenyl	1-pyrrolidinocarbonyl
1600	NHSO 2 CH 3	2-F-phenyl	2-(methylsulfonyl)phenyl
1601	NHSO 2 CH 3	2-F-phenyl	4-morpholino
1602	NHSO 2 CH 3	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1603	NHSO 2 CH 3	2-F-phenyl	4-morpholinocarbonyl
1604	NHSO 2 CH 3	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
1605	NHSO 2 CH 3	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
1606	NHSO 2 CH 3	2,5-diF-phenyl	1-pyrrolidinocarbonyl
1607	NHSO 2 CH 3	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
1608	NHSO 2 CH 3	2,5-diF-phenyl	4-morpholino
1609	NHSO 2 CH 3	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
1610	NHSO 2 CH 3	2,5-diF-phenyl	4-morpholinocarbonyl
1611	NHSO 2 CH 3	phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1612	NHSO 2 CH 3	phenyl	2-(N-piperidinyl-methyl)phenyl
1613	NHSO 2 CH 3	phenyl	2-(N-morpholino-methyl)phenyl
1614	NHSO 2 CH 3	phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1615	NHSO 2 CH 3	phenyl	2-(N-pyridinium-methyl)phenyl
1616	NHSO 2 CH 3	phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1617	NHSO 2 CH 3	phenyl	2-(N-azatanyl-methyl)phenyl
1618	NHSO 2 CH 3	phenyl	2-(N-azetidinyl-methyl)phenyl
1619	NHSO 2 CH 3	phenyl	2-(N-piperazinyl-methyl)phenyl
1620	NHSO 2 CH 3	phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1621	NHSO 2 CH 3	phenyl	2-(N-imidazolyl-methyl)phenyl
1622	NHSO 2 CH 3	phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1623	NHSO 2 CH 3	phenyl	2-(N-pyridonyl-methyl)phenyl
1624	NHSO 2 CH 3	phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1625	NHSO 2 CH 3	phenyl	2-(amidinyl)phenyl
1626	NHSO 2 CH 3	phenyl	2-(N-guanidinyl)phenyl
1627	NHSO 2 CH 3	phenyl	2-(imidazolyl)phenyl
1628	NHSO 2 CH 3	phenyl	2-(imidazolidinyl)phenyl
1629	NHSO 2 CH 3	phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1630	NHSO 2 CH 3	phenyl	2-(2-pyrrolidinyl)phenyl
1631	NHSO 2 CH 3	phenyl	2-(2-piperidinyl)phenyl
1632	NHSO 2 CH 3	phenyl	2-(amidinyl-methyl)phenyl
1633	NHSO 2 CH 3	phenyl	2-(2-imidazolidinyl-methyl)phenyl
1634	NHSO 2 CH 3	phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1635	NHSO 2 CH 3	phenyl	2-dimethylaminoimidazol-1-yl
1636	NHSO 2 CH 3	phenyl	2-(3-aminophenyl)
1637	NHSO 2 CH 3	phenyl	2-(3-pyrrolidinylcarbonyl)
1638	NHSO 2 CH 3	phenyl	2-glycinoyl
1639	NHSO 2 CH 3	phenyl	2-(imidazol-1-ylacetyl)
1640	NHSO 2 CH 3	2-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
1641	NHSO 2 CH 3	2-pyridyl	2-(N-piperidinyl-methyl)phenyl
1642	NHSO 2 CH 3	2-pyridyl	2-(N-morpholino-methyl)phenyl
1643	NHSO 2 CH 3	2-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1644	NHSO 2 CH 3	2-pyridyl	2-(N-pyridinium-methyl)phenyl
1645	NHSO 2 CH 3	2-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1646	NHSO 2 CH 3	2-pyridyl	2-(N-azatanyl-methyl)phenyl
1647	NHSO 2 CH 3	2-pyridyl	2-(N-azetidinyl-methyl)phenyl
1648	NHSO 2 CH 3	2-pyridyl	2-(N-piperazinyl-methyl)phenyl
1649	NHSO 2 CH 3	2-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1650	NHSO 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	NHSO 2 CH 3	2-pyridyl	2-(N-pyridonyl-methyl)phenyl
1653	NHSO 2 CH 3	2-pyridyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1654	NHSO 2 CH 3	2-pyridyl	2-(amidinyl)phenyl
1655	NHSO 2 CH 3	2-pyridyl	2-(N-guanidinyl)phenyl
1656	NHSO 2 CH 3	2-pyridyl	2-(imidazolyl)phenyl
1657	NHSO 2 CH 3	2-pyridyl	2-(imidazolidinyl)phenyl
1658	NHSO 2 CH 3	2-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1659	NHSO 2 CH 3	2-pyridyl	2-(2-pyrrolidinyl)phenyl
1660	NHSO 2 CH 3	2-pyridyl	2-(2-piperidinyl)phenyl
1661	NHSO 2 CH 3	2-pyridyl	2-(amidinyl-methyl)phenyl
1662	NHSO 2 CH 3	2-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
1663	NHSO 2 CH 3	2-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1664	NHSO 2 CH 3	2-pyridyl	2-dimethylaminoimidazol-1-yl
1665	NHSO 2 CH 3	2-pyridyl	2-(3-aminophenyl)
1666	NHSO 2 CH 3	2-pyridyl	2-(3-pyrrolidinylcarbonyl)
1667	NHSO 2 CH 3	2-pyridyl	2-glycinoyl
1668	NHSO 2 CH 3	2-pyridyl	2-(imidazol-1-ylacetyl)
1669	NHSO 2 CH 3	3-pyridyl	2-(N-pyrrolidinyl-methyl)phenyl
1670	NHSO 2 CH 3	3-pyridyl	2-(N-piperidinyl-methyl)phenyl
1671	NHSO 2 CH 3	3-pyridyl	2-(N-morpholino-methyl)phenyl
1672	NHSO 2 CH 3	3-pyridyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1673	NHSO 2 CH 3	3-pyridyl	2-(N-pyridinium-methyl)phenyl
1674	NHSO 2 CH 3	3-pyridyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1675	NHSO 2 CH 3	3-pyridyl	2-(N-azatanyl-methyl)phenyl
1676	NHSO 2 CH 3	3-pyridyl	2-(N-azetidinyl-methyl)phenyl
1677	NHSO 2 CH 3	3-pyridyl	2-(N-piperazinyl-methyl)phenyl
1678	NHSO 2 CH 3	3-pyridyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1679	NHSO 2 CH 3	3-pyridyl	2-(N-imidazolyl-methyl)phenyl
1680	NHSO 2 CH 3	3-pyridyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1681	NHSO 2 CH 3	3-pyridyl	2-(N-pyridonyl-methyl)phenyl
1682	NHSO 2 CH 3	3-pyridyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1683	NHSO 2 CH 3	3-pyridyl	2-(amidinyl)phenyl
1684	NHSO 2 CH 3	3-pyridyl	2-(N-guanidinyl)phenyl
1685	NHSO 2 CH 3	3-pyridyl	2-(imidazolyl)phenyl
1686	NHSO 2 CH 3	3-pyridyl	2-(imidazolidinyl)phenyl
1687	NHSO 2 CH 3	3-pyridyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1688	NHSO 2 CH 3	3-pyridyl	2-(2-pyrrolidinyl)phenyl
1689	NHSO 2 CH 3	3-pyridyl	2-(2-piperidinyl)phenyl
1690	NHSO 2 CH 3	3-pyridyl	2-(amidinyl-methyl)phenyl
1691	NHSO 2 CH 3	3-pyridyl	2-(2-imidazolidinyl-methyl)phenyl
1692	NHSO 2 CH 3	3-pyridyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1693	NHSO 2 CH 3	3-pyridyl	2-dimethylaminoimidazol-1-yl
1694	NHSO 2 CH 3	3-pyridyl	2-(3-aminophenyl)
1695	NHSO 2 CH 3	3-pyridyl	2-(3-pyrrolidinylcarbonyl)
1696	NHSO 2 CH 3	3-pyridyl	2-glycinoyl
1697	NHSO 2 CH 3	3-pyridyl	2-(imidazol-1-ylacetyl)
1698	NHSO 2 CH 3	2-pyrimidyl	2-(N-pyrrolidinyl-methyl)phenyl
1699	NHSO 2 CH 3	2-pyrimidyl	2-(N-piperidinyl-methyl)phenyl
1700	NHSO 2 CH 3	2-pyrimidyl	2-(N-morpholino-methyl)phenyl
1701	NHSO 2 CH 3	2-pyrimidyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1702	NHSO 2 CH 3	2-pyrimidyl	2-(N-pyridinium-methyl)phenyl
1703	NHSO 2 CH 3	2-pyrimidyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1704	NHSO 2 CH 3	2-pyrimidyl	2-(N-azatanyl-methyl)phenyl
1705	NHSO 2 CH 3	2-pyrimidyl	2-(N-azetidinyl-methyl)phenyl
1706	NHSO 2 CH 3	2-pyrimidyl	2-(N-piperazinyl-methyl)phenyl
1707	NHSO 2 CH 3	2-pyrimidyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1708	NHSO 2 CH 3	2-pyrimidyl	2-(N-imidazolyl-methyl)phenyl
1709	NHSO 2 CH 3	2-pyrimidyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1710	NHSO 2 CH 3	2-pyrimidyl	2-(N-pyridonyl-methyl)phenyl
1711	NHSO 2 CH 3	2-pyrimidyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1712	NHSO 2 CH 3	2-pyrimidyl	2-(amidinyl)phenyl
1713	NHSO 2 CH 3	2-pyrimidyl	2-(N-guanidinyl)phenyl
1714	NHSO 2 CH 3	2-pyrimidyl	2-(imidazolyl)phenyl
1715	NHSO 2 CH 3	2-pyrimidyl	2-(imidazolidinyl)phenyl
1716	NHSO 2 CH 3	2-pyrimidyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1717	NHSO 2 CH 3	2-pyrimidyl	2-(2-pyrrolidinyl)phenyl
1718	NHSO 2 CH 3	2-pyrimidyl	2-(2-piperidinyl)phenyl
1719	NHSO 2 CH 3	2-pyrimidyl	2-(amidinyl-methyl)phenyl
1720	NHSO 2 CH 3	2-pyrimidyl	2-(2-imidazolidinyl-methyl)phenyl
1721	NHSO 2 CH 3	2-pyrimidyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1722	NHSO 2 CH 3	2-pyrimidyl	2-dimethylaminoimidazol-1-yl
1723	NHSO 2 CH 3	2-pyrimidyl	2-(3-aminophenyl)
1724	NHSO 2 CH 3	2-pyrimidyl	2-(3-pyrrolidinylcarbonyl)
1725	NHSO 2 CH 3	2-pyrimidyl	2-glycinoyl
1726	NHSO 2 CH 3	2-pyrimidyl	2-(imidazol-1-ylacetyl)
1727	NHSO 2 CH 3	2-Cl-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1728	NHSO 2 CH 3	2-Cl-phenyl	2-(N-piperidinyl-methyl)phenyl
1729	NHSO 2 CH 3	2-Cl-phenyl	2-(N-morpholino-methyl)phenyl
1730	NHSO 2 CH 3	2-Cl-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1731	NHSO 2 CH 3	2-Cl-phenyl	2-(N-pyridinium-methyl)phenyl
1732	NHSO 2 CH 3	2-Cl-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1733	NHSO 2 CH 3	2-Cl-phenyl	2-(N-azatanyl-methyl)phenyl
1734	NHSO 2 CH 3	2-Cl-phenyl	2-(N-azetidinyl-methyl)phenyl
1735	NHSO 2 CH 3	2-Cl-phenyl	2-(N-piperazinyl-methyl)phenyl
1736	NHSO 2 CH 3	2-Cl-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1737	NHSO 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	NHSO 2 CH 3	2-Cl-phenyl	2-(N-pyridonyl-methyl)phenyl
1740	NHSO 2 CH 3	2-Cl-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1741	NHSO 2 CH 3	2-Cl-phenyl	2-(amidinyl)phenyl
1742	NHSO 2 CH 3	2-Cl-phenyl	2-(N-guanidinyl)phenyl
1743	NHSO 2 CH 3	2-Cl-phenyl	2-(imidazolyl)phenyl
1744	NHSO 2 CH 3	2-Cl-phenyl	2-(imidazolidinyl)phenyl
1745	NHSO 2 CH 3	2-Cl-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1746	NHSO 2 CH 3	2-Cl-phenyl	2-(2-pyrrolidinyl)phenyl
1747	NHSO 2 CH 3	2-Cl-phenyl	2-(2-piperidinyl)phenyl
1748	NHSO 2 CH 3	2-Cl-phenyl	2-(amidinyl-methyl)phenyl
1749	NHSO 2 CH 3	2-Cl-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1750	NHSO 2 CH 3	2-Cl-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1751	NHSO 2 CH 3	2-Cl-phenyl	2-dimethylaminoimidazol-1-yl
1752	NHSO 2 CH 3	2-Cl-phenyl	2-(3-aminophenyl)
1753	NHSO 2 CH 3	2-Cl-phenyl	2-(3-pyrrolidinylcarbonyl)
1754	NHSO 2 CH 3	2-Cl-phenyl	2-glycinoyl
1755	NHSO 2 CH 3	2-Cl-phenyl	2-(imidazol-1-ylacetyl)
1756	NHSO 2 CH 3	2-F-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1757	NHSO 2 CH 3	2-F-phenyl	2-(N-piperidinyl-methyl)phenyl
1758	NHSO 2 CH 3	2-F-phenyl	2-(N-morpholino-methyl)phenyl
1759	NHSO 2 CH 3	2-F-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1760	NHSO 2 CH 3	2-F-phenyl	2-(N-pyridinium-methyl)phenyl
1761	NHSO 2 CH 3	2-F-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1762	NHSO 2 CH 3	2-F-phenyl	2-(N-azatanyl-methyl)phenyl
1763	NHSO 2 CH 3	2-F-phenyl	2-(N-azetidinyl-methyl)phenyl
1764	NHSO 2 CH 3	2-F-phenyl	2-(N-piperazinyl-methyl)phenyl
1765	NHSO 2 CH 3	2-F-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1766	NHSO 2 CH 3	2-F-phenyl	2-(N-imidazolyl-methyl)phenyl
1767	NHSO 2 CH 3	2-F-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1768	NHSO 2 CH 3	2-F-phenyl	2-(N-pyridonyl-methyl)phenyl
1769	NHSO 2 CH 3	2-F-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1770	NHSO 2 CH 3	2-F-phenyl	2-(amidinyl)phenyl
1771	NHSO 2 CH 3	2-F-phenyl	2-(N-guanidinyl)phenyl
1772	NHSO 2 CH 3	2-F-phenyl	2-(imidazolyl)phenyl
1773	NHSO 2 CH 3	2-F-phenyl	2-(imidazolidinyl)phenyl
1774	NHSO 2 CH 3	2-F-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1775	NHSO 2 CH 3	2-F-phenyl	2-(2-pyrrolidinyl)phenyl
1776	NHSO 2 CH 3	2-F-phenyl	2-(2-piperidinyl)phenyl
1777	NHSO 2 CH 3	2-F-phenyl	2-(amidinyl-methyl)phenyl
1778	NHSO 2 CH 3	2-F-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1779	NHSO 2 CH 3	2-F-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1780	NHSO 2 CH 3	2-F-phenyl	2-dimethylaminoimidazol-1-yl
1781	NHSO 2 CH 3	2-F-phenyl	2-(3-aminophenyl)
1782	NHSO 2 CH 3	2-F-phenyl	2-(3-pyrrolidinylcarbonyl)
1783	NHSO 2 CH 3	2-F-phenyl	2-glycinoyl
1784	NHSO 2 CH 3	2-F-phenyl	2-(imidazol-1-ylacetyl)
1785	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-pyrrolidinyl-methyl)phenyl
1786	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-piperidinyl-methyl)phenyl
1787	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-morpholino-methyl)phenyl
1788	NHSO 2 CH 3	2,5-diF-phenyl	2-(N,N′-methylmorpholinium-methyl)phenyl
1789	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-pyridinium-methyl)phenyl
1790	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-4-(N,N′-dimethylamino)-pyridinium-methyl)phenyl
1791	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-azatanyl-methyl)phenyl
1792	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-azetidinyl-methyl)phenyl
1793	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-piperazinyl-methyl)phenyl
1794	NHSO 2 CH 3	2,5-diF-phenyl	2-(N,N′-BOC-piperazinyl-methyl)phenyl
1795	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-imidazolyl-methyl)phenyl
1796	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-methoxy-N-methylamino-methyl)phenyl
1797	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-pyridonyl-methyl)phenyl
1798	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-(N′,N′-dimethylhydrazinyl-methyl)phenyl
1799	NHSO 2 CH 3	2,5-diF-phenyl	2-(amidinyl)phenyl
1800	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-guanidinyl)phenyl
1801	NHSO 2 CH 3	2,5-diF-phenyl	2-(imidazolyl)phenyl
1802	NHSO 2 CH 3	2,5-diF-phenyl	2-(imidazolidinyl)phenyl
1803	NHSO 2 CH 3	2,5-diF-phenyl	2-(2-imidazolidinyl-sulfonyl)phenyl
1804	NHSO 2 CH 3	2,5-diF-phenyl	2-(2-pyrrolidinyl)phenyl
1805	NHSO 2 CH 3	2,5-diF-phenyl	2-(2-piperidinyl)phenyl
1806	NHSO 2 CH 3	2,5-diF-phenyl	2-(amidinyl-methyl)phenyl
1807	NHSO 2 CH 3	2,5-diF-phenyl	2-(2-imidazolidinyl-methyl)phenyl
1808	NHSO 2 CH 3	2,5-diF-phenyl	2-(N-(2-aminoimidazolyl)-methyl)phenyl
1809	NHSO 2 CH 3	2,5-diF-phenyl	2-dimethylaminoimidazol-1-yl
1810	NHSO 2 CH 3	2,5-diF-phenyl	2-(3-aminophenyl)
1811	NHSO 2 CH 3	2,5-diF-phenyl	2-(3-pyrrolidinylcarbonyl)
1812	NHSO 2 CH 3	2,5-diF-phenyl	2-glycinoyl
1813	NHSO 2 CH 3	2,5-diF-phenyl	2-(imidazol-1-ylacetyl)

TABLE 3
a 1 R = F, D = NH 2	b 1 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(O)NH 2	b 7 R = F, D = C(O)NH 2	c 7 R = F, D = C(O)NH 2
a 8 R = H, D = C(O)NH 2	b 8 R = H, D = C(O)NH 2	c 8 R = H, D = C(O)NH 2
d 1 R = F, D = NH 2	e 1 R = F, D = NH 2	f 1 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(O)NH 2	e 7 R = F, D = C(O)NH 2	f 7 R = F, D = C(O)NH 2
d 8 R = H, D = C(O)NH 2	e 8 R = H, D = C(O)NH 2	f 8 R = H, D = C(O)NH 2
g 1 R = F, D = NH 2	h 1 R = F, D = NH 2	i 1 R = F, D = NH 2
g 2 R = H, D = NH 2	h 2 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(O)NH 2	h 7 R = F, D = C(O)NH 2	i 7 R = F, D = C(O)NH 2
g 8 R = H, D = C(O)NH 2	h 8 R = H, D = C(O)NH 2	i 8 R = H, D = C(O)NH 2
j 1 R = F, D = NH 2	k 1 R = F, D = NH 2	l 1 R = F, D = NH 2
j 2 R = H, D = NH 2	k 2 R = H, D = NH 2	l 2 R = H, D = NH 2
j 3 R = F, D = CH 2 NH 2	k 3 R = F, D = CH 2 NH 2	l 3 R = F, D = CH 2 NH 2
j 4 R = H, D = CH 2 NH 2	k 4 R = H, D = CH 2 NH 2	l 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	l 6 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	l 6 R = H, D = C(═NH)NH 2
j 7 R = F, D = C(O)NH 2	k 7 R = F, D = C(O)NH 2	l 7 R = F, D = C(O)NH 2
j 8 R = H, D = C(O)NH 2	k 8 R = H, D = C(O)NH 2	l 8 R = H, D = C(O)NH 2
m 1 R = F, D = NH 2	n 1 R = F, D = NH 2	o 1 R = F, D = NH 2
m 2 R = H, D = NH 2	n 2 R = H, D = NH 2	o 2 R = H, D = NH 2
m 3 R = F, D = CH 2 NH 2	n 3 R = F, D = CH 2 NH 2	o 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	o 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	o 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	o 6 R = H, D = C(═NH)NH 2
m 7 R = F, D = C(O)NH 2	n 7 R = F, D = C(O)NH 2	o 7 R = F, D = C(O)NH 2
m 8 R = H, D = C(O)NH 2	n 8 R = H, D = C(O)NH 2	o 8 R = H, D = C(O)NH 2
p 1 R = F, D = NH 2	q 1 R = F, D = NH 2	r 1 R = F, D = NH 2
p 2 R = Cl, D = NH 2	q 2 R = Cl, D = NH 2	r 2 R = Cl, 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 = Cl, D = CH 2 NH 2	q 5 R = Cl, D = CH 2 NH 2	r 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	q 8 R = Cl, D = C(═NH)NH 2	r 8 R = Cl, 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
p 10 R = F, D = C(O)NH 2	q 10 R = F, D = C(O)NH 2	r 10 R = F, D = C(O)NH 2
p 11 R = Cl, D = C(O)NH 2	q 11 R = Cl, D = C(O)NH 2	r 11 R = Cl, D = C(O)NH 2
p 12 R = OMe, D = C(O)NH 2	q 12 R = OMe, D = C(O)NH 2	r 12 R = OMe, D = C(O)NH 2
s 1 R = F, D = NH 2	t 1 R = F, D = NH 2	u 1 R = F, D = NH 2
s 2 R = Cl, D = NH 2	t 2 R = Cl, D = NH 2	u 2 R = Cl, 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 = Cl, D = CH 2 NH 2	t 5 R = Cl, D = CH 2 NH 2	u 5 R = Cl, 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 NH 2
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 = Cl, D = C(═NH)NH 2	t 8 R = Cl, D = C(═NH)NH 2	u 8 R = Cl, 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
s 10 R = F, D = C(O)NH 2	t 10 R = F, D = C(O)NH 2	u 10 R = F, D = C(O)NH 2
s 11 R = Cl, D = C(O)NH 2	t 11 R = Cl, D = C(O)NH 2	u 11 R = Cl, D = C(O)NH 2
s 12 R = OMe, D = C(O)NH 2	t 12 R = OMe, D = C(O)NH 2	u 12 R = OMe, D = C(O)NH 2
v 1 R = F, D = NH 2	w 1 R = F, D = NH 2	x 1 R = F, D = NH 2
v 2 R = Cl, D = NH 2	w 2 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	w 4 R = F, D = CH 2 NH 2	x 4 R = F, D = CH 2 NH 2
v 5 R = Cl, D = CH 2 NH 2	w 5 R = Cl, D = CH 2 NH 2	x 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	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 = Cl, D = C(═NH)NH 2	w 8 R = Cl, D = C(═NH)NH 2	x 8 R = Cl, 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
v 10 R = F, D = C(O)NH 2	w 10 R = F, D = C(O)NH 2	x 10 R = F, D = C(O)NH 2
v 11 R = Cl, D = C(O)NH 2	w 11 R = Cl, D = C(O)NH 2	x 11 R = Cl, D = C(O)NH 2
v 12 R = OMe, D = C(O)NH 2	w 12 R = OMe, D = C(O)NH 2	x 12 R = OMe, D = C(O)NH 2
y 1 R = F, D = NH 2	z 1 R = F, D = NH 2	aa 1 R = F, D = NH 2
y 2 R = Cl, D = NH 2	z 2 R = Cl, D = NH 2	aa 2 R = Cl, 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 = Cl, D = CH 2 NH 2	z 5 R = Cl, D = CH 2 NH 2	aa 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	z 8 R = Cl, D = C(═NH)NH 2	aa 8 R = Cl, 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(O)NH 2	z 10 R = F, D = C(O)NH 2	aa 10 R = F, D = C(O)NH 2
y 11 R = Cl, D = C(O)NH 2	z 11 R = Cl, D = C(O)NH 2	aa 11 R = Cl, D = C(O)NH 2
y 12 R = OMe, D = C(O)NH 2	z 12 R = OMe, D = C(O)NH 2	aa 12 R = OMe, D = C(O)NH 2
bb 1 R = F, D = NH 2	cc 1 R = F, D = NH 2	dd 1 R = F, D = NH 2
bb 2 R = Cl, D = NH 2	cc 2 R = Cl, D = NH 2	dd 2 R = Cl, 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 = Cl, D = CH 2 NH 2	cc 5 R = Cl, D = CH 2 NH 2	dd 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	cc 8 R = Cl, D = C(═NH)NH 2	dd 8 R = Cl, D = C(═NH)NH 2
bb 9 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
bb 10 R = F, D = C(O)NH 2	cc 10 R = F, D = C(O)NH 2	dd 10 R = F, D = C(O)NH 2
bb 11 R = Cl, D = C(O)NH 2	cc 11 R = Cl, D = C(O)NH 2	dd 11 R = Cl, D = C(O)NH 2
bb 12 R = OMe, D = C(O)NH 2	cc 12 R = OMe, D = C(O)NH 2	dd 12 R = OMe, D = C(O)NH 2
ee 1 R = F, D = CH 2 NH 2	ff 1 R = F, D = CH 2 NH 2	gg 1 R = F, D = CH 2 NH 2
ee 2 R = Cl, D = CH 2 NH 2	ff 2 R = Cl, D = CH 2 NH 2	gg 2 R = Cl, 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 , D = CH 2 NH 2	ff 4 R = CH 2 NH 2 , D = CH 2 NH 2	gg 4 R = CH 2 NH 2 , D = CH 2 NH 2
hh 1 R = F, D = CH 2 NH 2	ii 1 R = F, D = CH 2 NH 2	jj 1 R = F, D = CH 2 NH 2
hh 2 R = Cl, D = CH 2 NH 2	ii 2 R = Cl, D = CH 2 NH 2	jj 2 R = Cl, 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 2 NH 2 , D = CH 2 NH 2	ii 4 R = CH 2 NH 2 , D = CH 2 NH 2	jj 4 R = CH 2 NH 2 , D = CH 2 NH 2
kk 1 R = F, D = CH 2 NH 2	ll 1 R = F, D = CH 2 NH 2	mm 1 R = F, D = CH 2 NH 2
kk 2 R = Cl, D = CH 2 NH 2	ll 2 R = Cl, D = CH 2 NH 2	mm 2 R = Cl, D = CH 2 NH 2
kk 3 R = OMe, D = CH 2 NH 2	ll 3 R = OMe, D = CH 2 NH 2	mm 3 R = OMe, D = CH 2 NH 2
kk 4 R = CH 2 NH 2 , D = CH 2 NH 2	ll 4 R = CH 2 NH 2 , D = CH 2 NH 2	mm 4 R = CH 2 NH 2 , D = CH 2 NH 2
nn 1 R = F, D = CH 2 NH 2	oo 1 R = F, D = CH 2 NH 2	pp 1 R = F, D = CH 2 NH 2
nn 2 R = Cl, D = CH 2 NH 2	oo 2 R = Cl, D = CH 2 NH 2	pp 2 R = Cl, D = CH 2 NH 2
nn 3 R = OMe, D = CH 2 NH 2	oo 3 R = OMe, D = CH 2 NH 2	pp 3 R = OMe, D = CH 2 NH 2
nn 4 R = CH 2 NH 2 , D = CH 2 NH 2	oo 4 R = CH 2 NH 2 , D = CH 2 NH 2	pp 4 R = CH 2 NH 2 , D = CH 2 NH 2
qq 1 R = F, D = CH 2 NH 2	rr 1 R = F, D = CH 2 NH 2	ss 1 R = F, D = CH 2 NH 2
qq 2 R = Cl, D = CH 2 NH 2	rr 2 R = Cl, D = CH 2 NH 2	ss 2 R = Cl, 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 , D = CH 2 NH 2	rr 4 R = CH 2 NH 2 , D = CH 2 NH 2	ss 4 R = CH 2 NH 2 , D = CH 2 NH 2
Ex #	R 1b	A	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-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-1-yl
10	H	phenyl	2-ethylimidazol-1-yl
11	H	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
12	H	phenyl	2-CH 3 SO 2 -imidazol-1-yl
13	H	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
14	H	2-F-phenyl	2-methylimidazol-1-yl
15	H	2-F-phenyl	2-ethylimidazol-1-yl
16	H	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
17	H	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
18	H	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
19	H	2-Cl-phenyl	2-methylimidazol-1-yl
20	H	2-Cl-phenyl	2-ethylimidazol-1-yl
21	H	2-Cl-phenyl	2- ((Me) 2 N-methyl)imidazol-1-yl
22	H	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
23	H	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
24	H	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
25	H	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
26	H	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
27	H	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
28	H	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
29	H	phenyl	N-methylimidazol-2-yl
30	H	phenyl	4-methylimidazol-5-yl
31	H	phenyl	5-CF 3 -pyrazol-1-yl
32	H	2-F-phenyl	N-methylimidazol-2-yl
33	H	2-F-phenyl	4-methylimidazol-5-yl
34	H	2-F-phenyl	5-CF 3 -pyrazol-1-yl
35	H	phenyl	guanidino
36	H	phenyl	2-thiazolin-2-ylamine
37	H	phenyl	N-methyl-2-imidazolin-2-yl
38	H	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
39	H	phenyl	N-methylimidazol-2-ylthiol
40	H	phenyl	t-butoxycarbonylamine
41	H	phenyl	(N-pyrrolidino)formylimino
42	H	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
43	H	2-F-phenyl	guanidino
44	H	2-F-phenyl	2-thiazolin-2-ylamine
45	H	2-F-phenyl	N-methyl-2-imidazolin-2-yl
46	H	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
47	H	2-F-phenyl	N-methylimidazol-2-ylthio
48	H	2-F-phenyl	t-butoxycarbonylamine
49	H	2-F-phenyl	(N-pyrrolidino)formylimino
50	H	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
51	H	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
52	H	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
53	—CN	phenyl	2-((Me) 2 N-methyl)phenyl
54	—CN	phenyl	2-((Me)NH-methyl)phenyl
55	—CN	phenyl	2-(H 2 N-methyl)phenyl
56	—CN	phenyl	2-HOCH 2 -phenyl
57	—CN	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
58	—CN	2-F-phenyl	2-((Me)NH-methyl)phenyl
59	—CN	2-F-phenyl	2-(H 2 N-methyl)phenyl
60	—CN	2-F-phenyl	2-HOCH 2 -phenyl
61	—CN	phenyl	2-methylimidazol-1-yl
62	—CN	phenyl	2-ethylimidazol-1-yl
63	—CN	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
64	—CN	phenyl	2-CH 3 SO 2 -imidazol-1-yl
65	—CN	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
66	—CN	2-F-phenyl	2-methylimidazol-1-yl
67	—CN	2-F-phenyl	2-ethylimidazol-1-yl
68	—CN	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
69	—CN	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
70	—CN	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
71	—CN	2-Cl-phenyl	2-methylimidazol-1-yl
72	—CN	2-Cl-phenyl	2-ethylimidazol-1-yl
73	—CN	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
74	—CN	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
75	—CN	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
76	—CN	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
77	—CN	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
78	—CN	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
79	—CN	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
80	—CN	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
81	—CN	phenyl	N-methylimidazol-2-yl
82	—CN	phenyl	4-methylimidazol-5-yl
83	—CN	phenyl	5-CF 3 -pyrazol-1-yl
84	—CN	2-F-phenyl	N-methylimidazol-2-yl
85	—CN	2-F-phenyl	4-methylimidazol-5-yl
86	—CN	2-F-phenyl	5-CF 3 -pyrazol-1-yl
87	—CN	phenyl	guanidino
88	—CN	phenyl	2-thiazolin-2-ylamine
89	—CN	phenyl	N-methyl-2-imidazolin-2-yl
90	—CN	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
91	—CN	phenyl	N-methylimidazol-2-ylthiol
92	—CN	phenyl	t-butoxycarbonylamine
93	—CN	phenyl	(N-pyrrolidino)formylimino
94	—CN	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
95	—CN	2-F-phenyl	guanidind
96	—CN	2-F-phenyl	2-thiazolin-2-ylamine
97	—CN	2-F-phenyl	N-methyl-2-imidazolin-2-yl
98	—CN	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
99	—CN	2-F-phenyl	N-methylimidazol-2-ylthio
100	—CN	2-F-phenyl	t-butoxycarbonylamine
101	—CN	2-F-phenyl	(N-pyrrolidino)formylimino
102	—CN	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
103	—CN	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
104	—CN	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
105	CF 3	phenyl	2-((Me) 2 N-methyl)phenyl
106	CF 3	phenyl	2-((Me)NH-methyl)phenyl
107	CF 3	phenyl	2-(H 2 N-methyl)phenyl
108	CF 3	phenyl	2-HOCH 2 -phenyl
109	CF 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
110	CF 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
111	CF 3	2-F-phehyl	2-(H 2 N-methyl )phenyl
112	CF 3	2-F-phenyl	2-HOCH 2 -phenyl
113	CF 3	phenyl	2-methylimidazol-1-yl
114	CF 3	phenyl	2-ethylimidazol-1-yl
115	CF 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
116	CF 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
117	CF 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
118	CF 3	2-F-phenyl	2-methylimidazol-1-y1
119	CF 3	2-F-phenyl	2-ethylimidazol-1-yl
120	CF 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
121	CF 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
122	CF 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
123	CF 3	2-Cl-phenyl	2-methylimidazol-1-yl
124	CF 3	2-Cl-phenyl	2-ethylimidazol-1-yl
125	CF 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
126	CF 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
127	CF 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
128	CF 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
129	CF 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
132	CF 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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 O-phenyl	(N-pyrrolidino)formylimino
156	CF 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
157	CONH 2	phenyl	2-((Me) 2 N-methyl)phenyl
158	CONH 2	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	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-1-yl
166	CONH 2	phenyl	2-ethylimidazol-1-yl
167	CONH 2	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
168	CONH 2	phenyl	2-CH 3 SO 2 -imidazol-1-yl
169	CONH 2	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
170	CONH 2	2-F-phenyl	2-methylimidazol-1-yl
171	CONH 2	2-F-phenyl	2-ethylimidazol-1-yl
172	CONH 2	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
173	CONH 2	2-F-phenyl	2-CH 3 SO 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-1-yl
176	CONH 2	2-Cl-phenyl	2-ethylimidazol-1-yl
177	CONH 2	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
178	CONH 2	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
179	CONH 2	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
180	CONH 2	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
181	CONH 2	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
184	CONH 2	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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-butoxycarbdnylamine
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 O-phenyl	(N-pyrrolidino)formylimino
208	CONH 2	2-CH 3 O-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-1-yl
218	SCH 3	phenyl	2-ethylimidazol-1-yl
219	SCH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
220	SCH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
221	SCH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
222	SCH 3	2-F-phenyl	2-methylimidazol-1-yl
223	SCH 3	2-F-phenyl	2-ethylimidazol-1-yl
224	SCH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
225	SCH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
226	SCH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
227	SCH 3	2-Cl-phenyl	2-methylimidazol-1-yl
228	SCH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
229	SCH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
230	SCH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
231	SCH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
232	SCH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
233	SCH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
236	SCH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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-yl
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 O-phenyl	(N-pyrrolidino)formylimino
260	SCH 3	2-CH 3 O-phenyl	(N-pyrrclidino)formyl-N-(methanesulfamoyl)imino
261	SO 2 CH 3	phenyl	2-((Me) 2 N-methyl)phenyl
262	SO 2 CH 3	phenyl	2-((Me)NH-methyl)phenyl
263	SO 2 CH 3	phenyl	2-(H 2 N-methyl)phenyl
264	SO 2 CH 3	phenyl	2-HOCH 2 -phenyl
265	SO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
266	SO 2 CH 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
267	SO 2 CH 3	2-F-phenyl	2-(H 2 N-methyl)phenyl
268	SO 2 CH 3	2-F-phenyl	2-HOCH 2 -phenyl
269	SO 2 CH 3	phenyl	2-methylimidazol-1-yl
270	SO 2 CH 3	phenyl	2-ethylimidazol-1-yl
271	SO 2 CH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
272	SO 2 CH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
273	SO 2 CH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
274	SO 2 CH 3	2-F-phenyl	2-methylimidazol-1-yl
275	SO 2 CH 3	2-F-phenyl	2-ethylimidazol-1-yl
276	SO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
277	SO 2 CH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
278	SO 2 CH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
279	SO 2 CH 3	2-Cl-phenyl	2-methylimidazol-1-yl
280	SO 2 CH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
281	SO 2 CH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
282	SO 2 CH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
283	SO 2 CH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
284	SO 2 CH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
285	SO 2 CH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
286	SO 2 CH 3	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
287	SO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
288	SO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
289	SO 2 CH 3	phenyl	N-methylimidazol-2-yl
290	SO 2 CH 3	phenyl	4-methylimidazol-5-yl
291	SO 2 CH 3	phenyl	5-CF 3 -pyrazol-1-yl
292	SO 2 CH 3	2-F-phenyl	N-methylimidazol-2-yl
293	SO 2 CH 3	2-F-phenyl	4-methylimidazol-5-yl
294	SO 2 CH 3	2-F-phenyl	5-CF 3 -pyrazol-1-yl
295	SO 2 CH 3	phenyl	guanidino
296	SO 2 CH 3	phenyl	2-thiazolin-2-ylamine
297	SO 2 CH 3	phenyl	N-methyl-2-imidazolin-2-yl
298	SO 2 CH 3	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
299	SO 2 CH 3	phenyl	N-methylimidazol-2-ylthiol
300	SO 2 CH 3	phenyl	t-butoxycarbonylamine
301	SO 2 CH 3	phenyl	(N-pyrrolidino)formylimino
302	SO 2 CH 3	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
303	SO 2 CH 3	2-F-phenyl	guanidino
304	SO 2 CH 3	2-F-phenyl	2-thiazolin-2-ylamine
305	SO 2 CH 3	2-F-phenyl	N-methyl-2-imidazolin-2-yl
306	SO 2 CH 3	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
307	SO 2 CH 3	2-F-phenyl	N-methylimidazol-2-ylthio
308	SO 2 CH 3	2-F-phenyl	t-butoxycarbonylamine
309	SO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formylimino
310	SO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
311	SO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
312	SO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
313	NHSO 2 CH 3	phenyl	2-((Me) 2 N-methyl)phenyl
314	NHSO 2 CH 3	phenyl	2-((Me)NH-methyl)phenyl
315	NHSO 2 CH 3	phenyl	2-(H 2 N-methyl)phenyl
316	NHSO 2 CH 3	phenyl	2-HOCH 2 -phenyl
317	NHSO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
318	NHSO 2 CH 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
319	NHSO 2 CH 3	2-F-phenyl	2-(H 2 N-methyl)phenyl
320	NHSO 2 CH 3	2-F-phenyl	2-HOCH 2 -phenyl
321	NHSO 2 CH 3	phenyl	2-methylimidazol-1-yl
322	NHSO 2 CH 3	phenyl	2-ethylimidazol-1-yl
323	NHSO 2 CH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
324	NHSO 2 CH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
325	NHSO 2 CH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
326	NHSO 2 CH 3	2-F-phenyl	2-methylimidazol-1-yl
327	NHSO 2 CH 3	2-F-phenyl	2-ethylimidazol-1-yl
328	NHSO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
329	NHSO 2 CH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
330	NHSO 2 CH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
331	NHSO 2 CH 3	2-Cl-phenyl	2-methylimidazol-1-yl
332	NHSO 2 CH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
333	NHSO 2 CH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
334	NHSO 2 CH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
335	NHSO 2 CH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
336	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
337	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
338	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
339	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
340	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
341	NHSO 2 CH 3	phenyl	N-methylimidazol-2-yl
342	NHSO 2 CH 3	phenyl	4-methylimidazol-5-yl
343	NHSO 2 CH 3	phenyl	5-CF 3 -pyrazol-1-yl
344	NHSO 2 CH 3	2-F-phenyl	N-methylimidazol-2-yl
345	NHSO 2 CH 3	2-F-phenyl	4-methylimidazol-5-yl
346	NHSO 2 CH 3	2-F-phenyl	5-CF 3 -pyrazol-1-yl
347	NHSO 2 CH 3	phenyl	guanidino
348	NHSO 2 CH 3	phenyl	2-thiazolin-2-ylamine
349	NHSO 2 CH 3	phenyl	N-methyl-2-imidazolin-2-yl
350	NHSO 2 CH 3	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
351	NHSO 2 CH 3	phenyl	N-methylimidazol-2-ylthiol
352	NHSO 2 CH 3	phenyl	t-butoxycarbonylamine
353	NHSO 2 CH 3	phenyl	(N-pyrrolidino)formylimino
354	NHSO 2 CH 3	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
355	NHSO 2 CH 3	2-F-phenyl	guanidino
356	NHSO 2 CH 3	2-F-phenyl	2-thiazolin-2-ylamine
357	NHSO 2 CH 3	2-F-phenyl	N-methyl-2-imidazolin-2-yl
358	NHSO 2 CH 3	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
359	NHSO 2 CH 3	2-F-phenyl	N-methylimidazol-2-ylthio
360	NHSO 2 CH 3	2-F-phenyl	t-butoxycarbonylamine
361	NHSO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formylimino
362	NHSO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
363	NHSO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
364	NHSO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino

TABLE 4
a 1 R = F, D = NH 2	b 1 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(O)NH 2	b 7 R = F, D = C(O)NH 2	c 7 R = F, D = C(O)NH 2
a 8 R = H, D = C(O)NH 2	b 6 R = H, D = C(O)NH 2	c 8 R = H, D = C(O)NH 2
d 1 R = F, D = NH 2	e 1 R = F, D = NH 2	f 1 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(O)NH 2	e 7 R = F, D = C(O)NH 2	f 7 R = F, D = C(O)NH 2
d 6 R = H, D = C(O)NH 2	e 8 R = H, D = C(O)NH 2	f 8 R = H, D = C(O)NH 2
g 1 R = F, D = NH 2	h 1 R = F, D = NH 2	i 1 R = F, D = NH 2
g 2 R = H, D = NH 2	h 2 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(O)NH 2	h 7 R = F, D = C(O)NH 2	i 7 R = F, D = C(O)NH 2
g 8 R = H, D = C(O)NH 2	h 8 R = H, D = C(O)NH 2	i 8 R = H, D = C(O)NH 2
j 1 R = F, D = NH 2	k 1 R = F, D = NH 2	l 1 R = F, D = NH 2
j 2 R = H, D = NH 2	k 2 R = H, D = NH 2	l 2 R = H, D = NH 2
j 3 R = F, D = CH 2 NH 2	k 3 R = F, D = CH 2 NH 2	l 3 R = F, D = CH 2 NH 2
j 4 R = H, D = CH 2 NH 2	k 4 R = H, D = CH 2 NH 2	l 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	l 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	l 6 R = H, D = C(═NH)NH 2
j 7 R = F, D = C(O)NH 2	k 7 R = F, D = C(O)NH 2	l 7 R = F, D = C(O)NH 2
j 8 R = H, D = C(O)NH 2	k 8 R = H, D = C(O)NH 2	l 8 R = H, D = C(O)NH 2
m 1 R = F, D = NH 2	n 1 R = F, D = NH 2	o 1 R = F, D = NH 2
m 2 R = H, D = NH 2	n 2 R = H, D = NH 2	o 2 R = H, D = NH 2
m 3 R = F, D = CH 2 NH 2	n 3 R = F, D = CH 2 NH 2	o 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	o 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	o 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	o 6 R = H, D = C(═NH)NH 2
m 7 R = F, D = C(O)NH 2	n 7 R = F, D = C(O)NH 2	o 7 R = F, D = C(O)NH 2
m 8 R = H, D = C(O)NH 2	n 8 R = H, D = C(O)NH 2	o 8 R = H, D = C(O)NH 2
p 1 R = F, D = NH 2	q 1 R = F, D = NH 2	r 1 R = F, D = NH 2
p 2 R = Cl, D = NH 2	q 2 R = Cl, D = NH 2	r 2 R = Cl, 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 = Cl, D = CH 2 NH 2	q 5 R = Cl, D = CH 2 NH 2	r 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	q 8 R = Cl, D = C(═NH)NH 2	r 8 R = Cl, 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
p 10 R = F, D = C(O)NH 2	q 10 R = F, D = C(O)NH 2	r 10 R = F, D = C(O)NH 2
p 11 R = Cl, D = C(O)NH 2	q 11 R = Cl, D = C(O)NH 2	r 11 R = Cl, D = C(O)NH 2
p 12 R = OMe, D = C(O)NH 2	q 12 R = OMe, D = C(9)NH 2	r 12 R = OMe, D = C(O)NH 2
s 1 R = F, D = NH 2	t 1 R = F, D = NH 2	u 1 R = F, D = NH 2
s 2 R = Cl, D = NH 2	t 2 R = Cl, D = NH 2	u 2 R = Cl, 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 = Cl, D = CH 2 NH 2	t 5 R = Cl, D = CH 2 NH 2	u 5 R = Cl, 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 NH 2
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 = Cl, D = C(═NH)NH 2	t 8 R = Cl, D = C(═NH)NH 2	u 8 R = Cl, 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
s 10 R = F, D = C(O)NH 2	t 10 R = F, D = C(O)NH 2	u 10 R = F, D = C(O)NH 2
s 11 R = Cl, D = C(O)NH 2	t 11 R = Cl, D = C(O)NH 2	u 11 R = Cl, D = C(O)NH 2
s 12 R = OMe, D = C(O)NH 2	t 12 R = OMe, D = C(O)NH 2	u 12 R = OMe, D = C(O)NH 2
v 1 R = F, D = NH 2	w 1 R = F, D = NH 2	x 1 R = F, D = NH 2
v 2 R = Cl, D = NH 2	w 2 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	w 4 R = F, D = CH 2 NH 2	x 4 R = F, D = CH 2 NH 2
v 5 R = Cl, D = CH 2 NH 2	w 5 R = Cl, D = CH 2 NH 2	x 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	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 = Cl, D = C(═NH)NH 2	w 8 R = Cl, D = C(═NH)NH 2	x 8 R = Cl, 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
v 10 R = F, D = C(O)NH 2	w 10 R = F, D = C(O)NH 2	x 10 R = F, D = C(O)NH 2
v 11 R = Cl, D = C(O)NH 2	w 11 R = Cl, D = C(O)NH 2	x 11 R = Cl, D = C(O)NH 2
v 12 R = OMe, D = C(O)NH 2	w 12 R = OMe, D = C(O)NH 2	x 12 R = OMe, D = C(O)NH 2
y 1 R = F, D = NH 2	z 1 R = F, D = NH 2	aa 1 R = F, D = NH 2
y 2 R = Cl, D = NH 2	z 2 R = Cl, D = NH 2	aa 2 R = Cl, 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 = Cl, D = CH 2 NH 2	z 5 R = Cl, D = CH 2 NH 2	aa 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	z 8 R = Cl, D = C(═NH)NH 2	aa 8 R = Cl, 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(O)NH 2	z 10 R = F, D = C(O)NH 2	aa 10 R = F, D = C(O)NH 2
y 11 R = Cl, D = C(O)NH 2	z 11 R = Cl, D = C(O)NH 2	aa 11 R = Cl, D = C(O)NH 2
y 12 R = OMe, D = C(O)NH 2	z 12 R = OMe, D = C(O)NH 2	aa 12 R = OMe, D = C(O)NH 2
bb 1 R = F, D = NH 2	cc 1 R = F, D = NH 2	dd 1 R = F, D = NH 2
bb 2 R = Cl, D = NH 2	cc 2 R = Cl, D = NH 2	dd 2 R = Cl, 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 = Cl, D = CH 2 NH 2	cc 5 R = Cl, D = CH 2 NH 2	dd 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	cc 8 R = Cl, D = C(═NH)NH 2	dd 8 R = Cl, D = C(═NH)NH 2
bb 9 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
bb 10 R = F, D = C(O)NH 2	cc 10 R = F, D = C(O)NH 2	dd 10 R = F, D = C(O)NH 2
bb 11 R = Cl, D = C(O)NH 2	cc 11 R = Cl, D = C(O)NH 2	dd 11 R = Cl, D = C(O)NH 2
bb 12 R = OMe, D = C(O)NH 2	cc 12 R = OMe, D = C(O)NH 2	dd 12 R = OMe, D = C(O)NH 2
ee 1 R = F, D = CH 2 NH 2	ff 1 R = F, D = CH 2 NH 2	gg 1 R = F, D = CH 2 NH 2
ee 2 R = Cl, D = CH 2 NH 2	ff 2 R = Cl, D = CH 2 NH 2	gg 2 R = Cl, 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 , D = CH 2 NH 2	ff 4 R = CH 2 NH 2 , D = CH 2 NH 2	gg 4 R = CH 2 NH 2 , D = CH 2 NH 2
hh 1 R = F, D = CH 2 NH 2	ii 1 R = F, D = CH 2 NH 2	jj 1 R = F, D = CH 2 NH 2
hh 2 R = Cl, D = CH 2 NH 2	ii 2 R = Cl, D = CH 2 NH 2	jj 2 R = Cl, 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 2 NH 2 , D = CH 2 NH 2	ii 4 R = CH 2 NH 2 , D = CH 2 NH 2	jj 4 R = CH 2 NH 2 , D = CH 2 NH 2
kk 1 R = F, D = CH 2 NH 2	ll 1 R = F, D = CH 2 NH 2	mm 1 R = F, D = CH 2 NH 2
kk 2 R = Cl, D = CH 2 NH 2	ll 2 R = Cl, D = CH 2 NH 2	mm 2 R = Cl, D = CH 2 NH 2
kk 3 R = OMe, D = CH 2 NH 2	ll 3 R = OMe, D = CH 2 NH 2	mm 3 R = OMe, D = CH 2 NH 2
kk 4 R = CH 2 NH 2 , D = CH 2 NH 2	ll 4 R = CH 2 NH 2 , D = CH 2 NH 2	mm 4 R = CH 2 NH 2 , D = CH 2 NH 2
nn 1 R = F, D = CH 2 NH 2	oo 1 R = F, D = CH 2 NH 2	pp 1 R = F, D = CH 2 NH 2
nn 2 R = Cl, D = CH 2 NH 2	oo 2 R = Cl, D = CH 2 NH 2	pp 2 R = Cl, D = CH 2 NH 2
nn 3 R = OMe, D = CH 2 NH 2	oo 3 R = OMe, D = CH 2 NH 2	pp 3 R = OMe, D = CH 2 NH 2
nn 4 R = CH 2 NH 2 , D = CH 2 NH 2	oo 4 R = CH 2 NH 2 , D = CH 2 NH 2	pp 4 R = CH 2 NH 2 , D = CH 2 NH 2
qq 1 R = F, D = CH 2 NH 2	rr 1 R = F, D = CH 2 NH 2	ss 1 R = F, D = CH 2 NH 2
qq 2 R = Cl, D = CH 2 NH 2	rr 2 R = Cl, D = CH 2 NH 2	ss 2 R = Cl, 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 , D = CH 2 NH 2	rr 4 R = CH 2 NH 2 , D = CH 2 NH 2	ss 4 R = CH 2 NH 2 , D = CH 2 NH 2
Ex. #	R 1b	A	B
1	H	phenyl	2-(aminosulfonyl)phenyl
2	H	phenyl	2-(methylaminosulfonyl)phenyl
3	H	phenyl	1-pyrrolidinocarbonyl
4	H	phenyl	2-(methylsulfonyl)phenyl
5	H	phenyl	4-morpholino
6	H	phenyl	2-(1′-CF 3 -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-(methylsulfonyl)phenyl
12	H	2-pyridyl	4-morpholino
13	H	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
14	H	2-pyridyl	4-morpholinocarbonyl
15	H	3-pyridyl	2-(aminosulfonyl)phenyl
16	H	3-pyridyl	2-(methylaminosulfonyl)phenyl
17	H	3-pyridyl	1-pyrrolidinocarbonyl
18	H	3-pyridyl	2-(methylsulfonyl)phenyl
19	H	3-pyridyl	4-morpholino
20	H	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
21	H	3-pyridyl	4-morpholinocarbonyl
22	H	2-pyrimidyl	2-(aminosulfonyl)phenyl
23	H	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
24	H	2-pyrimidyl	1-pyrrolidinocarbonyl
25	H	2-pyrimidyl	2-(methylsulfonyl)phenyl
26	H	2-pyrimidyl	4-morpholino
27	H	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
28	H	2-pyrimidyl	4-morpholinocarbonyl
29	H	5-pyrimidyl	2-(aminosulfonyl)phenyl
30	H	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
31	H	5-pyrimidyl	1-pyrrolidinocarbonyl
32	H	5-pyrimidyl	2-(methylsulfonyl)phenyl
33	H	5-pyrimidyl	4-morpholino
34	H	5-pyrimidyl	2-(1-CF 3 -tetrazol-2-yl)phenyl
35	H	5-pyrimidyl	4-morpholinocarbonyl
36	H	2-Cl-phenyl	2-(aminosulfonyl)phenyl
37	H	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
38	H	2-Cl-phenyl	1-pyrrolidinocarbonyl
39	H	2-Cl-phenyl	2-(methylsulfonyl)phenyl
40	H	2-Cl-phenyl	4-morpholino
41	H	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
42	H	2-Cl-phenyl	4-morpholinocarbonyl
43	H	2-F-phenyl	2-(aminosulfonyl)phenyl
44	H	2-F-phenyl	2-(methylaminosulfonyl)phenyl
45	H	2-F-phenyl	1-pyrrolidinocarbonyl
46	H	2-F-phenyl	2-(methylsulfonyl)phenyl
47	H	2-F-phenyl	4-morpholino
48	H	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
49	H	2-F-phenyl	4-morpholinocarbonyl
50	H	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
51	H	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
52	H	2,5-diF-phenyl	1-pyrrolidinocarbonyl
53	H	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
54	H	2,5-diF-phenyl	4-morpholino
55	H	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
56	H	2,5-diF-phenyl	4-morpholinocarbonyl
57	H	phenyl	2-(aminosulfonyl)phenyl
58	—CN	phenyl	2-(methylaminosulfonyl)phenyl
59	—CN	phenyl	1-pyrrolidinocarbonyl
60	—CN	phenyl	2-(methylsulfonyl)phenyl
61	—CN	phenyl	4-morpholino
62	—CN	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
63	—CN	phenyl	4-morpholinocarbonyl
64	—CN	2-pyridyl	2-(aminosulfonyl)phenyl
65	—CN	2-pyridyl	2-(methylaminosulfonyl)phenyl
66	—CN	2-pyridyl	1-pyrrolidinocarbonyl
67	—CN	2-pyridyl	2-(methylsulfonyl)phenyl
68	—CN	2-pyridyl	4-morpholino
69	—CN	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
70	—CN	2-pyridyl	4-morpholinocarbonyl
71	—CN	3-pyridyl	2-(aminosulfonyl)phenyl
72	—CN	3-pyridyl	2-(methylaminosulfonyl)phenyl
73	—CN	3-pyridyl	1-pyrrolidinocarbonyl
74	—CN	3-pyridyl	2-(methylsulfonyl)phenyl
75	—CN	3-pyridyl	4-morpholino
76	—CN	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
77	—CN	3-pyridyl	4-morpholinocarbonyl
78	—CN	2-pyrimidyl	2-(aminosulfonyl)phenyl
79	—CN	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
80	—CN	2-pyrimidyl	1-pyrrolidinocarbonyl
81	—CN	2-pyrimidyl	2-(methylsulfonyl)phenyl
82	—CN	2-pyrimidyl	4-morpholino
83	—CN	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
84	—CN	2-pyrimidyl	4-morpholinocarbonyl
85	—CN	5-pyrimidyl	2-(aminosulfonyl)phenyl
86	—CN	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
87	—CN	5-pyrimidyl	1-pyrrolidinocarbonyl
88	—CN	5-pyrimidyl	2-(methylsulfonyl)phenyl
89	—CN	5-pyrimidyl	4-morpholino
90	—CN	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
91	—CN	5-pyrimidyl	4-morpholinocarbonyl
92	—CN	2-Cl-phenyl	2-(aminosulfonyl)phenyl
93	—CN	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
94	—CN	2-Cl-phenyl	1-pyrrolidinocarbonyl
95	—CN	2-Cl-phenyl	2-(methylsulfonyl)phenyl
96	—CN	2-Cl-phenyl	4-morpholino
97	—CN	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
98	—CN	2-Cl-phenyl	4-morpholinocarbonyl
99	—CN	2-F-phenyl	2-(aminosulfonyl)phenyl
100	—CN	2-F-phenyl	2-(methylaminosulfonyl)phenyl
101	—CN	2-F-phenyl	1-pyrrolidinocarbonyl
102	—CN	2-F-phenyl	2-(methylsulfonyl)phenyl
103	—CN	2-F-phenyl	4-morpholino
104	—CN	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
105	—CN	2-F-phenyl	4-morpholinocarbonyl
106	—CN	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
107	—CN	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyll
108	—CN	2,5-diF-phenyl	1-pyrrolidinocarbonyl
109	—CN	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
110	—CN	2,5-diF-phenyl	4-morpholino
111	—CN	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
112	—CN	2,5-diF-phenyl	4-morpholinocarbonyl
113	CF 3	phenyl	2-(aminosulfonyl)phenyl
114	CF 3	phenyl	2-(methylaminosulfonyl)phenyl
115	CF 3	phenyl	1-pyrrolidinocarbonyl
116	CF 3	phenyl	2-(methylsulfonyl)phenyl
117	CF 3	phenyl	4-morpholino
118	CF 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
119	CF 3	phenyl	4-morpholinocarbonyl
120	CF 3	2-pyridyl	2-(aminosulfonyl)phenyl
121	CF 3	2-pyridyl	2-(methylaininosulfonyl)phenyl
122	CF 3	2-pyridyl	1-pyrrolidinocarbonyl
123	CF 3	2-pyridyl	2-(methylsulfonyl)phenyl
124	CF 3	2-pyridyl	4-morpholino
125	CF 3	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
126	CF 3	2-pyridyl	4-morpholinocarbonyl
127	CF 3	3-pyridyl	2-(aminosulfonyl)phenyl
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′-CF 3 -tetrazol-2-yl)phenyl
133	CF 3	3-pyridyl	4-morpholinocarbonyl
134	CF 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
135	CF 3	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
136	CF 3	2-pyrimidyl	1-pyrrolidinocarbonyl
137	CF 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
138	CF 3	2-pyrimidyl	4-morpholino
139	CF 3	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)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′-CF 3 -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-pyrrolidinocarbonyl
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′-CF 3 -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′-CF 3 -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-pyrrolidinocarbonyl
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-(1′-CF 3 -tetrazol-2-yl)phenyl
168	CF 3	2,5-diF-phenyl	4-morpholinocarbonyl
169	CONH 2	phenyl	2-(aminosulfonyl)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′-CF 3 -tetrazol-2-yl)phenyl
175	CONH 2	phenyl	4-morpholinocarbonyl
176	CONH 2	2-pyridyl	2-(aminosuifonyl)phenyl
177	CONH 2	2-pyridyl	2-(methylaminosulfonyl)phenyl
178	CONH 2	2-pyridyl	1-pyrrolidinocarbonyl
179	CONH 2	2-pyridyl	2-(methylsulfonyl)phenyl
180	CONH 2	2-pyridyl	4-morpholino
181	CONH 2	2-pyridyl	2-(1′-CF 3 -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-(1′-CF 3 -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-(1′-CF 3 -tetrazol-2-yl)phenyl
196	CONH 2	2-pyrimidyl	4-morpholinocarbonyl
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′-CF 3 -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′-CF 3 -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-pyrrolidinocarbonyl
214	CONH 2	2-F-phenyl	2-(methylsulfonyl)phenyl
215	CONH 2	2-F-phenyl	4-morpholino
216	CONH 2	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
217	CONH 2	2-F-phenyl	4-morpholinocarbonyl
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-pyrrolidinocarbonyl
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′-CF 3 -tetrazol-2-yl)phenyl
224	CONH 2	2,5-diF-phenyl	4-morpholinocarbonyl
225	SCH 3	phenyl	2-(aminosulfonyl)phenyl
226	SCH 3	phenyl	2-(methylaminosulfonyl)phenyl
227	SCH 3	phenyl	1-pyrrolidinocarbonyl
228	SCH 3	phenyl	2-(methylsulfonyl)phenyl
229	SCH 3	phenyl	4-morpholino
230	SCH 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
231	SCH 3	phenyl	4-morpholinocarbonyl
232	SCH 3	2-pyridyl	2-(aminosulfonyl)phenyl
233	SCH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
234	SCH 3	2-pyridyl	1-pyrrolidinocarbonyl
235	SCH 3	2-pyridyl	2-(methylsulfonyl)phenyl
236	SCH 3	2-pyridyl	4-morpholino
237	SCH 3	2-pyridyl	2-(1′-CF 3 -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′-CF 3 -tetrazol-2-yl)phenyl
245	SCH 3	3-pyridyl	4-morpholinocarbonyl
246	SCH 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
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-morpholino
251	SCH 3	2-pyrimidyl	2-(1′-CF 3 -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-(1′-CF 3 -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′-CF 3 -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-pyrrolidinocarbonyl
270	SCH 3	2-F-phenyl	2-(methylsulfonyl)phenyl
271	SCH 3	2-F-phenyl	4-morpholino
272	SCH 3	2-F-phenyl	2-(1′-CF 3 -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-pyrrolidinocarbonyl
277	SCH 3	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
278	SCH 3	2,5-diF-phenyl	4-morpholino
279	SCH 3	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
280	SCH 3	2,5-diF-phenyl	4-morpholinocarbonyl
281	SO 2 CH 3	phenyl	2-(aminosulfonyl)phenyl
282	SO 2 CH 3	phenyl	2-(methylaminosulfonyl)phenyl
283	SO 2 CH 3	phenyl	1-pyrrolidinocarbonyl
284	SO 2 CH 3	phenyl	2-(methylsulfonyl)phenyl
285	SO 2 CH 3	phenyl	4-morpholino
286	SO 2 CH 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
287	SO 2 CH 3	phenyl	4-morpholinocarbonyl
288	SO 2 CH 3	2-pyridyl	2-(aminosulfonyl)phenyl
289	SO 2 CH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
290	SO 2 CH 3	2-pyridyl	1-pyrrolidinocarbonyl
291	SO 2 CH 3	2-pyridyl	2-(methylsulfonyl)phenyl
292	SO 2 CH 3	2-pyridyl	4-morpholino
293	SO 2 CH 3	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
294	SO 2 CH 3	2-pyridyl	4-morpholinocarbonyl
295	SO 2 CH 3	3-pyridyl	2-(aminosulforiyl)phenyl
296	SO 2 CH 3	3-pyridyl	2-(methylaminosulfonyl)phenyl
297	SO 2 CH 3	3-pyridyl	1-pyrrolidinocarbonyL
298	SO 2 CH 3	3-pyridyl	2-(methylsulfonyl)phenyl
299	SO 2 CH 3	3-pyridyl	4-morpholino
300	SO 2 CH 3	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
301	SO 2 CH 3	3-pyridyl	4-morpholinocarbonyl
302	SO 2 CH 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
303	SO 2 CH 3	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
304	SO 2 CH 3	2-pyrimidyl	1-pyrrolidinocarbonyl
305	SO 2 CH 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
306	SO 2 CH 3	2-pyrimidyl	4-morpholino
307	SO 2 CH 3	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
308	SO 2 CH 3	2-pyrimidyl	4-morpholinocarbonyl
309	SO 2 CH 3	5-pyrimidyl	2-(aminosulfonyl)phenyl
310	SO 2 CH 3	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
311	SO 2 CH 3	5-pyrimidyl	1-pyrrolidinocarbonyl
312	SO 2 CH 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
313	SO 2 CH 3	5-pyrimidyl	4-morpholino
314	SO 2 CH 3	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
315	SO 2 CH 3	5-pyrimidyl	4-morpholinocarbonyl
316	SO 2 CH 3	2-Cl-phenyl	2-(aminosulfonyl)phenyl
317	SO 2 CH 3	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
318	SO 2 CH 3	2-Cl-phenyl	1-pyrrolidinocarbonyl
319	SO 2 CH 3	2-Cl-phenyl	2-(methylsulfonyl)phenyl
320	SO 2 CH 3	2-Cl-phenyl	4-morpholino
321	SO 2 CH 3	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
322	SO 2 CH 3	2-Cl-phenyl	4-morpholinocarbonyl
323	SO 2 CH 3	2-F-phenyl	2-(aminosulfonyl)phenyl
324	SO 2 CH 3	2-F-phenyl	2-(methylaminosulfonyl)phenyl
325	SO 2 CH 3	2-F-phenyl	1-pyrrolidinocarbonyl
326	SO 2 CH 3	2-F-phenyl	2-(methylsulfonyl)phenyl
327	SO 2 CH 3	2-F-phenyl	4-morpholino
328	SO 2 CH 3	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
329	SO 2 CH 3	2-F-phenyl	4-morpholinocarbonyl
330	SO 2 CH 3	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
331	SO 2 CH 3	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
332	SO 2 CH 3	2,5-diF-phenyl	1-pyrrolidinocarbonyl
333	SO 2 CH 3	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
334	SO 2 CH 3	2,5-diF-phenyl	4-morpholino
335	SO 2 CH 3	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
336	SO 2 CH 3	2,5-diF-phenyl	4-morpholinocarbonyl
337	NHSO 2 CH 3	phenyl	2-(aminosulfonyl)phenyl
338	NHSO 2 CH 3	phenyl	2-(methylaminosulfonyl)phenyl
339	NHSO 2 CH 3	phenyl	1-pyrrolidinocarbonyl
340	NHSO 2 CH 3	phenyl	2-(methylsulfonyl)phenyl
341	NHSO 2 CH 3	phenyl	4-morpholino
342	NHSO 2 CH 3	phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
343	NHSO 2 CH 3	phenyl	4-morpholinocarbonyl
344	NHSO 2 CH 3	2-pyridyl	2-(aminosulfonyl)phenyl
345	NHSO 2 CH 3	2-pyridyl	2-(methylaminosulfonyl)phenyl
346	NHSO 2 CH 3	2-pyridyl	1-pyrrolidinocarbonyl
347	NHSO 2 CH 3	2-pyridyl	2-(methylsulfonyl)phenyl
348	NHSO 2 CH 3	2-pyridyl	4-morpholino
349	NHSO 2 CH 3	2-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
350	NHSO 2 CH 3	2-pyridyl	4-morpholinocarbonyl
351	NHSO 2 CH 3	3-pyridyl	2-(aminosulfonyl)phenyl
352	NHSO 2 CH 3	3-pyridyl	2-(methylaminosulfonyl)phenyl
353	NHSO 2 CH 3	3-pyridyl	1-pyrrolidinocarbonyl
354	NHSO 2 CH 3	3-pyridyl	2-(methylsulfonyl)phenyl
355	NHSO 2 CH 3	3-pyridyl	4-morpholino
356	NHSO 2 CH 3	3-pyridyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
357	NHSO 2 CH 3	3-pyridyl	4-morpholinocarbonyl
358	NHSO 2 CH 3	2-pyrimidyl	2-(aminosulfonyl)phenyl
359	NHSO 2 CH 3	2-pyrimidyl	2-(methylaminosulfonyl)phenyl
360	NHSO 2 CH 3	2-pyrimidyl	1-pyrrolidinocarbonyl
361	NHSO 2 CH 3	2-pyrimidyl	2-(methylsulfonyl)phenyl
362	NHSO 2 CH 3	2-pyrimidyl	4-morpholino
363	NHSO 2 CH 3	2-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
364	NHSO 2 CH 3	2-pyrimidyl	4-morpholinocarbonyl
365	NHSO 2 CH 3	5-pyrimidyl	2-(aminosulfonyl)phenyl
366	NHSO 2 CH 3	5-pyrimidyl	2-(methylaminosulfonyl)phenyl
367	NHSO 2 CH 3	5-pyrimidyl	1-pyrrolidinocarbonyl
368	NHSO 2 CH 3	5-pyrimidyl	2-(methylsulfonyl)phenyl
369	NHSO 2 CH 3	5-pyrimidyl	4-morpholino
370	NHSO 2 CH 3	5-pyrimidyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
371	NHSO 2 CH 3	5-pyrimidyl	4-morpholinocarbonyl
372	NHSO 2 CH 3	2-Cl-phenyl	2-(aminosulfonyl)phenyl
373	NHSO 2 CH 3	2-Cl-phenyl	2-(methylaminosulfonyl)phenyl
374	NHSO 2 CH 3	2-Cl-phenyl	1-pyrrolidinocarbonyl
375	NHSO 2 CH 3	2-Cl-phenyl	2-(methylsulfonyl)phenyl
376	NHSO 2 CH 3	2-Cl-phenyl	4-morpholino
377	NHSO 2 CH 3	2-Cl-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
378	NHSO 2 CH 3	2-Cl-phenyl	4-morpholinocarbonyl
379	NHSO 2 CH 3	2-F-phenyl	2-(aminosulfonyl)phenyl
380	NHSO 2 CH 3	2-F-phenyl	2-(methylaminosulfonyl)phenyl
381	NHSO 2 CH 3	2-F-phenyl	1-pyrrolidinocarbonyl
382	NHSO 2 CH 3	2-F-phenyl	2-(methylsulfonyl)phenyl
383	NHSO 2 CH 3	2-F-phenyl	4-morpholino
384	NHSO 2 CH 3	2-F-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
385	NHSO 2 CH 3	2-F-phenyl	4-morpholinocarbonyl
386	NHSO 2 CH 3	2,5-diF-phenyl	2-(aminosulfonyl)phenyl
387	NHSO 2 CH 3	2,5-diF-phenyl	2-(methylaminosulfonyl)phenyl
388	NHSO 2 CH 3	2,5-diF-phenyl	1-pyrrolidinocarbonyl
389	NHSO 2 CH 3	2,5-diF-phenyl	2-(methylsulfonyl)phenyl
390	NHSO 2 CH 3	2,5-diF-phenyl	4-morpholino
391	NHSO 2 CH 3	2,5-diF-phenyl	2-(1′-CF 3 -tetrazol-2-yl)phenyl
392	NHSO 2 CH 3	2,5-diF-phenyl	4-morpholinocarbonyl

TABLE 5
a 1 R = F, D = NH 2	b 1 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(O)NH 2	b 7 R = F, D = C(O)NH 2	c 7 R = F, D = C(O)NH 2
a 8 R = H, D = C(O)NH 2	b 8 R = H, D = C(O)NH 2	c 8 R = H, D = C(O)NH 2
d 1 R = F, D = NH 2	e 1 R = F, D = NH 2	f 1 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(O)NH 2	e 7 R = F, D = C(O)NH 2	f 7 R = F, D = C(O)NH 2
d 8 R = H, D = C(O)NH 2	e 8 R = H, D = C(O)NH 2	f 8 R = H, D = C(O)NH 2
g 1 R = F, D = NH 2	h 1 R = F, D = NH 2	i 1 R = F, D = NH 2
g 2 R = H, D = NH 2	h 2 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(O)NH 2	h 7 R = F, D = C(O)NH 2	i 7 R = F, D = C(O)NH 2
g 8 R = H, D = C(O)NH 2	h 8 R = H, D = C(O)NH 2	i 8 R = H, D = C(O)NH 2
j 1 R = F, D = NH 2	k 1 R = F, D = NH 2	l 1 R = F, D = NH 2
j 2 R = H, D = NH 2	k 2 R = H, D = NH 2	l 2 R = H, D = NH 2
j 3 R = F, D = CH 2 NH 2	k 3 R = F, D = CH 2 NH 2	l 3 R = F, D = CH 2 NH 2
j 4 R = H, D = CH 2 NH 2	k 4 R = H, D = CH 2 NH 2	l 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	l 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	l 6 R = H, D = C(═NH)NH 2
j 7 R = F, D = C(O)NH 2	k 7 R = F, D = C(O)NH 2	l 7 R = F, D = C(O)NH 2
j 8 R = H, D = C(O)NH 2	k 8 R = H, D = C(O)NH 2	l 8 R = H, D = C(O)NH 2
m 1 R = F, D = NH 2	n 1 R = F, D = NH 2	o 1 R = F, D = NH 2
m 2 R = H, D = NH 2	n 2 R = H, D = NH 2	o 2 R = H, D = NH 2
m 3 R = F, D = CH 2 NH 2	n 3 R = F, D = CH 2 NH 2	o 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	o 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	o 5 R = F, D = C(═NH)NH 2
m 6 R = H, D = C(═NH)NH 2	n 5 R = H, D = C(═NH)NH 2	o 6 R = H, D = C(═NH)NH 2
m 7 R = F, D = C(O)NH 2	n 7 R = F, D = C(O)NH 2	o 7 R = F, D = C(O)NH 2
m 8 R = H, D = C(O)NH 2	n 8 R = H, D = C(O)NH 2	o 8 R = H, D = C(O)NH 2
p 1 R = F, D = NH 2	q 1 R = F, D = NH 2	r 1 R = F, D = NH 2
p 2 R = Cl, D = NH 2	q 2 R = Cl, D = NH 2	r 2 R = Cl, 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 = Cl, D = CH 2 NH 2	q 5 R = Cl, D = CH 2 NH 2	r 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	q 8 R = Cl, D = C(═NH)NH 2	r 8 R = Cl, 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
p 10 R = F, D = C(O)NH 2	q 10 R = F, D = C(O)NH 2	r 10 R = F, D = C(O)NH 2
p 11 R = Cl, D = C(O)NH 2	q 11 R = Cl, D = C(O)NH 2	r 11 R = Cl, D = C(O)NH 2
p 12 R = OMe, D = C(O)NH 2	q 12 R = OMe, D = C(O)NH 2	r 12 R = OMe, D = C(O)NH 2
s 1 R = F, D = NH 2	t 1 R = F, D = NH 2	u 1 R = F, D = NH 2
s 2 R = Cl, D = NH 2	t 2 R = Cl, D = NH 2	u 2 R = Cl, 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 = Cl, D = CH 2 NH 2	t 5 R = Cl, D = CH 2 NH 2	u 5 R = Cl, 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 NH 2
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 = Cl, D = C(═NH)NH 2	t 8 R = Cl, D = C(═NH)NH 2	u 8 R = Cl, 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
s 10 R = F, D = C(O)NH 2	t 10 R = F, D = C(O)NH 2	u 10 R = F, D = C(O)NH 2
s 11 R = Cl, D = C(O)NH 2	t 11 R = Cl, D = C(O)NH 2	u 11 R = Cl, D = C(O)NH 2
s 12 R = OMe, D = C(O)NH 2	t 12 R = OMe, D = C(O)NH 2	u 12 R = OMe, D = C(O)NH 2
v 1 R = F, D = NH 2	w 1 R = F, D = NH 2	x 1 R = F, D = NH 2
v 2 R = Cl, D = NH 2	w 2 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	w 4 R = F, D = CH 2 NH 2	x 4 R = F, D = CH 2 NH 2
v 5 R = Cl, D = CH 2 NH 2	w 5 R = Cl, D = CH 2 NH 2	x 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	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 = Cl, D = C(═NH)NH 2	w 8 R = Cl, D = C(═NH)NH 2	x 6 R = Cl, 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
v 10 R = F, D = C(O)NH 2	w 10 R = F, D = C(O)NH 2	x 10 R = F, D = C(O)NH 2
v 11 R = Cl, D = C(O)NH 2	w 11 R = Cl, D = C(O)NH 2	x 11 R = Cl, D = C(O)NH 2
v 12 R = OMe, D = C(O)NH 2	w 12 R = OMe, D = C(O)NH 2	x 12 R = OMe, D = C(O)NH 2
y 1 R = F, D = NH 2	z 1 R = F, D = NH 2	aa 1 R = F, D = NH 2
y 2 R = Cl, D = NH 2	z 2 R = Cl, D = NH 2	aa 2 R = Cl, 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 = Cl, D = CH 2 NH 2	z 5 R = Cl, D = CH 2 NH 2	aa 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	z 8 R = Cl, D = C(═NH)NH 2	aa 8 R = Cl, 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(O)NH 2	z 10 R = F, D = C(O)NH 2	aa 10 R = F, D = C(O)NH 2
y 11 R = Cl, D = C(O)NH 2	z 11 R = Cl, D = C(O)NH 2	aa 11 R = Cl, D = C(O)NH 2
y 12 R = OMe, D = C(O)NH 2	z 12 R = OMe, D = C(O)NH 2	aa 12 R = OMe, D = C(O)NH 2
bb 1 R = F, D = NH 2	cc 1 R = F, D = NH 2	dd 1 R = F, D = NH 2
bb 2 R = Cl, D = NH 2	cc 2 R = Cl, D = NH 2	dd 2 R = Cl, 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 = Cl, D = CH 2 NH 2	cc 5 R = Cl, D = CH 2 NH 2	dd 5 R = Cl, 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 = Cl, D = C(═NH)NH 2	cc 8 R = Cl, D = C(═NH)NH 2	dd 8 R = Cl, D = C(═NH)NH 2
bb 9 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
bb 10 R = F, D = C(O)NH 2	cc 10 R = F, D = C(O)NH 2	dd 10 R = F, D = C(O)NH 2
bb 11 R = Cl, D = C(O)NH 2	cc 11 R = Cl, D = C(O)NH 2	dd 11 R = Cl, D = C(O)NH 2
bb 12 R = OMe, D = C(O)NH 2	cc 12 R = OMe, D = C(O)NH 2	dd 12 R = OMe, D = C(O)NH 2
ee 1 R = F, D = CH 2 NH 2	ff 1 R = F, D = CH 2 NH 2	ff 1 R = F, D = CH 2 NH 2
ee 2 R = Cl, D = CH 2 NH 2	ff 2 R = Cl, D = CH 2 NH 2	gg 2 R = Cl, 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 , D = CH 2 NH 2	ff 4 R = CH 2 NH 2 , D = CH 2 NH 2	gg 4 R = CH 2 NH 2 , D = CH 2 NH 2
hh 1 R = F, D = CH 2 NH 2	ii 1 R = F, D = CH 2 NH 2	jj 1 R = F, D = CH 2 NH 2
hh 2 R = Cl, D = CH 2 NH 2	ii 2 R = Cl, D = CH 2 NH 2	jj 2 R = Cl, 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 2 NH 2 , D = CH 2 NH 2	ii 4 R = CH 2 NH 2 , D = CH 2 NH 2	jj 4 R = CH 2 NH 2 , D = CH 2 NH 2
kk 1 R = F, D = CH 2 NH 2	ll 1 R = F, D = CH 2 NH 2	mm 1 R = F, D = CH 2 NH 2
kk 2 R = Cl, D = CH 2 NH 2	ll 2 R = Cl, D = CH 2 NH 2	mm 2 R = Cl, D = CH 2 NH 2
kk 3 R = OMe, D = CH 2 NH 2	ll 3 R = OMe, D = CH 2 NH 2	mm 3 R = OMe, D = CH 2 NH 2
kk 4 R = CH 2 NH 2 , D = CH 2 NH 2	ll 4 R = CH 2 NH 2 , D = CH 2 NH 2	mm 4 R = CH 2 NH 2 , D = CH 2 NH 2
nn 1 R = F, D = CH 2 NH 2	oo 1 R = F, D = CH 2 NH 2	pp 1 R = F, D = CH 2 NH 2
nn 2 R = Cl, D = CH 2 NH 2	oo 2 R = Cl, D = CH 2 NH 2	pp 2 R = Cl, D = CH 2 NH 2
nn 3 R = OMe, D = CH 2 NH 2	oo 3 R = OMe, D = CH 2 NH 2	pp 3 R = OMe, D = CH 2 NH 2
nn 4 R = CH 2 NH 2 , D = CH 2 NH 2	oo 4 R = CH 2 NH 2 , D = CH 2 NH 2	pp 4 R = CH 2 NH 2 , D = CH 2 NH 2
qq 1 R = F, D = CH 2 NH 2	rr 1 R = F, D = CH 2 NH 2	ss 1 R = F, D = CH 2 NH 2
qq 2 R = Cl, D = CH 2 NH 2	rr 2 R = Cl, D = CH 2 NH 2	ss 2 R = Cl, 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 , D = CH 2 NH 2	rr 4 R = CH 2 NH 2 , D = CH 2 NH 2	ss 4 R = CH 2 NH 2 , D = CH 2 NH 2
Ex #	R 1b	A	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-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-1-yl
10	H	phenyl	2-ethylimidazol-1-yl
11	H	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
12	H	phenyl	2-CH 3 NHSO 2 -imidazol-1-yl
13	H	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
14	H	2-F-phenyl	2-methylimidazol-1-yl
15	H	2-F-phenyl	2-ethylimidazol-1-yl
16	H	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
17	H	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
18	H	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
19	H	2-Cl-phenyl	2-methylimidazol-1-yl
20	H	2-Cl-phenyl	2-ethylimidazol-1-yl
21	H	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
22	H	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
23	H	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
24	H	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
25	H	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
26	H	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
27	H	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
28	H	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
29	H	phenyl	N-methylimidazol-2-yl
30	H	phenyl	4-methylimidazol-5-yl
31	H	phenyl	5-CF 3 -pyrazol-1-yl
32	H	2-F-phenyl	N-methylimidazol-2-yl
33	H	2-F-phenyl	4-methylimidazol-5-yl
34	H	2-F-phenyl	5-CF 3 -pyrazol-1-yl
35	H	phenyl	guanidino
36	H	phenyl	2-thiazolin-2-ylamine
37	H	phenyl	N-methyl-2-imidazolin-2-yl
38	H	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
39	H	phenyl	N-methylimidazol-2-ylthiol
40	H	phenyl	t-butoxycarbonylamine
41	H	phenyl	(N-pyrrolidino)formylimino
42	H	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
43	H	2-F-phenyl	guanidino
44	H	2-F-phenyl	2-thiazolin-2-ylamine
45	H	2-F-phenyl	N-methyl-2-imidazolin-2-yl
46	H	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
47	H	2-F-phenyl	N-methylimidazol-2-ylthio
48	H	2-F-phenyl	t-butoxycarbonylamine
49	H	2-F-phenyl	(N-pyrrolidino)formylimino
50	H	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
51	H	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
52	H	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
53	—CN	phenyl	2-((Me) 2 N-methyl)phenyl
54	—CN	phenyl	2-((Me)NH-methyl)phenyl
55	—CN	phenyl	2-(H 2 N-methyl)phenyl
56	—CN	phenyl	2-HOCH 2 -phenyl
57	—CN	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
58	—CN	2-F-phenyl	2-((Me)NH-methyl)phenyl
59	—CN	2-F-phenyl	2-(H 2 N-methyl)phenyl
60	—CN	2-F-phenyl	2-HOCH 2 -phenyl
61	—CN	phenyl	2-methylimidazol-1-yl
62	—CN	phenyl	2-ethylimidazol-1-yl
63	—CN	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
64	—CN	phenyl	2-CH 3 SO 2 -imidazol-1-yl
65	—CN	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
66	—CN	2-F-phenyl	2-methylimidazol-1-yl
67	—CN	2-F-phenyl	2-ethylimidazol-1-yl
68	—CN	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
69	—CN	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
70	—CN	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
71	—CN	2-Cl-phenyl	2-methylimidazol-1-yl
72	—CN	2-Cl-phenyl	2-ethylimidazol-1-yl
73	—CN	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
74	—CN	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
75	—CN	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
76	—CN	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
77	—CN	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
78	—CN	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
79	—CN	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
80	—CN	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
81	—CN	phenyl	N-methylimidazol-2-yl
82	—CN	phenyl	4-methylimidazol-5-yl
83	—CN	phenyl	5-CF 3 -pyrazol-1-yl
84	—CN	2-F-phenyl	N-methylimidazol-2-yl
85	—CN	2-F-phenyl	4-methylimidazol-5-yl
86	—CN	2-F-phenyl	5-CF 3 -pyrazol-1-yl
87	—CN	phenyl	guanidino
88	—CN	phenyl	2-thiazolin-2-ylamine
89	—CN	phenyl	N-methyl-2-imidazolin-2-yl
90	—CN	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
91	—CN	phenyl	N-methylimidazol-2-ylthiol
92	—CN	phenyl	t-butoxycarbonylamine
93	—CN	phenyl	(N-pyrrolidino)formylimino
94	—CN	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
95	—CN	2-F-phenyl	guanidino
96	—CN	2-F-phenyl	2-thiazolin-2-ylamine
97	—CN	2-F-phenyl	N-methyl-2-imidazolin-2-yl
98	—CN	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
99	—CN	2-F-phenyl	N-methylimidazol-2-ylthio
100	—CN	2-F-phenyl	t-butoxycarbonylamine
101	—CN	2-F-phenyl	(N-pyrrolidino)formylimino
102	—CN	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
103	—CN	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
104	—CN	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
105	CF 3	phenyl	2-((Me) 2 N-methyl)phenyl
106	CF 3	phenyl	2-((Me)NH-methyl)phenyl
107	CF 3	phenyl	2-(H 2 N-methyl)phenyl
108	CF 3	phenyl	2-HOCH 2 -phenyl
109	CF 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
110	CF 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
111	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-1-yl
114	CF 3	phenyl	2-ethylimidazol-1-yl
115	CF 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
116	CF 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
117	CF 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
118	CF 3	2-F-phenyl	2-methylimidazol-1-yl
119	CF 3	2-F-phenyl	2-ethylimidazol-1-yl
120	CF 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
121	CF 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
122	CF 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
123	CF 3	2-Cl-phenyl	2-methylimidazol-1-yl
124	CF 3	2-Cl-phenyl	2-ethylimidazol-1-yl
125	CF 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
126	CF 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
127	CF 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
128	CF 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
129	CF 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
132	CF 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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 O-phenyl	(N-pyrrolidino)formylimino
156	CF 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
157	CONH 2	phenyl	2-((Me) 2 N-methyl)phenyl
158	CONH 2	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	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-1-yl
166	CONH 2	phenyl	2-ethylimidazol-1-yl
167	CONH 2	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
168	CONH 2	phenyl	2-CH 3 SO 2 -imidazol-1-yl
169	CONH 2	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
170	CONH 2	2-F-phenyl	2-methylimidazol-1-yl
171	CONH 2	2-F-phenyl	2-ethylimidazol-1-yl
172	CONH 2	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
173	CONH 2	2-F-phenyl	2-CH 3 SO 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-1-yl
176	CONH 2	2-Cl-phenyl	2-ethylimidazol-1-yl
177	CONH 2	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
178	CONH 2	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
179	CONH 2	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
180	CONH 2	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
181	CONH 2	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
184	CONH 2	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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-pyrrplidino)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 O-phenyl	(N-pyrrolidino)formylimino
208	CONH 2	2-CH 3 O-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-1-yl
218	SCH 3	phenyl	2-ethylimidazol-1-yl
219	SCH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
220	SCH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
221	SCH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
222	SCH 3	2-F-phenyl	2-methylimidazol-1-yl
223	SCH 3	2-F-phenyl	2-ethylimidazol-1-yl
224	SCH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
225	SCH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
226	SCH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
227	SCH 3	2-Cl-phenyl	2-methylimidazol-1-yl
228	SCH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
229	SCH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
230	SCH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
231	SCH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
232	SCH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
233	SCH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-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 SO 2 -imidazol-1-yl
236	SCH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-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-yl
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 O-phenyl	(N-pyrrolidino)formylimino
260	SCH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
261	SO 2 CH 3	phenyl	2-((Me) 2 N-methyl)phenyl
262	SO 2 CH 3	phenyl	2-((Me)NH-methyl)phenyl
263	SO 2 CH 3	phenyl	2-(H 2 N-methyl)phenyl
264	SO 2 CH 3	phenyl	2-HOCH 2 -phenyl
265	SO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
266	SO 2 CH 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
267	SO 2 CH 3	2-F-phenyl	2-(H 2 N-methyl)phenyl
268	SO 2 CH 3	2-F-phenyl	2-HOCH 2 -phenyl
269	SO 2 CH 3	phenyl	2-methylimidazol-1-yl
270	SO 2 CH 3	phenyl	2-ethylimidazol-1-yl
271	SO 2 CH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
272	SO 2 CH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
273	SO 2 CH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
274	SO 2 CH 3	2-F-phenyl	2-methylimidazol-1-yl
275	SO 2 CH 3	2-F-phenyl	2-ethylimidazol-1-yl
276	SO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-1yl
277	SO 2 CH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
278	SO 2 CH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
279	SO 2 CH 3	2-Cl-phenyl	2-methylimidazol-1-yl
280	SO 2 CH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
281	SO 2 CH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
282	SO 2 CH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
283	SO 2 CH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
284	SO 2 CH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
285	SO 2 CH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
286	SO 2 CH 3	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
287	SO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
288	SO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
289	SO 2 CH 3	phenyl	N-methylimidazol-2-yl
290	SO 2 CH 3	phenyl	4-methylimidazol-5-yl
291	SO 2 CH 3	phenyl	5-CF 3 -pyrazol-1-yl
292	SO 2 CH 3	2-F-phenyl	N-methylimidazol-2-yl
293	SO 2 CH 3	2-F-phenyl	4-methylimidazol-5-yl
294	SO 2 CH 3	2-F-phenyl	5-CF 3 -pyrazol-1-yl
295	SO 2 CH 3	phenyl	guanidino
296	SO 2 CH 3	phenyl	2-thiazolin-2-ylamine
297	SO 2 CH 3	phenyl	N-methyl-2-imidazolin-2-yl
298	SO 2 CH 3	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
299	SO 2 CH 3	phenyl	N-methylimidazol-2-ylthiol
300	SO 2 CH 3	phenyl	t-butoxycarbonylamine
301	SO 2 CH 3	phenyl	(N-pyrrolidino)formylimino
302	SO 2 CH 3	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
303	SO 2 CH 3	2-F-phenyl	guanidino
304	SO 2 CH 3	2-F-phenyl	2-thiazolin-2-ylamine
305	SO 2 CH 3	2-F-phenyl	N-methyl-2-imidazolin-2-yl
306	SO 2 CH 3	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
307	SO 2 CH 3	2-F-phenyl	N-methylimidazol-2-ylthio
308	SO 2 CH 3	2-F-phenyl	t-butoxycarbonylamine
309	SO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formylimino
310	SO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
311	SO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
312	SO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
313	NHSO 2 CH 3	phenyl	2-((Me) 2 N-methyl)phenyl
314	NHSO 2 CH 3	phenyl	2-((Me)NH-methyl)phenyl
315	NHSO 2 CH 3	phenyl	2-(H 2 N-methyl)phenyl
316	NHSO 2 CH 3	phenyl	2-HOCH 2 -phenyl
317	NHSO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)phenyl
318	NHSO 2 CH 3	2-F-phenyl	2-((Me)NH-methyl)phenyl
319	NHSO 2 CH 3	2-F-phenyl	2-(H 2 N-methyl)phenyl
320	NHSO 2 CH 3	2-F-phenyl	2-HOCH 2 -phenyl
321	NHSO 2 CH 3	phenyl	2-methylimidazol-1-yl
322	NHSO 2 CH 3	phenyl	2-ethylimidazol-1-yl
323	NHSO 2 CH 3	phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
324	NHSO 2 CH 3	phenyl	2-CH 3 SO 2 -imidazol-1-yl
325	NHSO 2 CH 3	phenyl	2-CH 3 OCH 2 -imidazol-1-yl
326	NHSO 2 CH 3	2-F-phenyl	2-methylimidazol-1-yl
327	NHSO 2 CH 3	2-F-phenyl	2-ethylimidazol-1-yl
328	NHSO 2 CH 3	2-F-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
329	NHSO 2 CH 3	2-F-phenyl	2-CH 3 SO 2 -imidazol-1-yl
330	NHSO 2 CH 3	2-F-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
331	NHSO 2 CH 3	2-Cl-phenyl	2-methylimidazol-1-yl
332	NHSO 2 CH 3	2-Cl-phenyl	2-ethylimidazol-1-yl
333	NHSO 2 CH 3	2-Cl-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
334	NHSO 2 CH 3	2-Cl-phenyl	2-CH 3 SO 2 -imidazol-1-yl
335	NHSO 2 CH 3	2-Cl-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
336	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-methylimidazol-1-yl
337	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-ethylimidazol-1-yl
338	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-((Me) 2 N-methyl)imidazol-1-yl
339	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 SO 2 -imidazol-1-yl
340	NHSO 2 CH 3	2-(Me) 2 N-phenyl	2-CH 3 OCH 2 -imidazol-1-yl
341	NHSO 2 CH 3	phenyl	N-methylimidazol-2-yl
342	NHSO 2 CH 3	phenyl	4-methylimidazol-5-yl
343	NHSO 2 CH 3	phenyl	5-CF 3 -pyrazol-1-yl
344	NHSO 2 CH 3	2-F-phenyl	N-methylimidazol-2-yl
345	NHSO 2 CH 3	2-F-phenyl	4-methylimidazol-5-yl
346	NHSO 2 CH 3	2-F-phenyl	5-CF 3 -pyrazol-1-yl
347	NHSO 2 CH 3	phenyl	guanidino
348	NHSO 2 CH 3	phenyl	2-thiazolin-2-ylamine
349	NHSO 2 CH 3	phenyl	N-methyl-2-imidazolin-2-yl
350	NHSO 2 CH 3	phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
351	NHSO 2 CH 3	phenyl	N-methylimidazol-2-ylthiol
352	NHSO 2 CH 3	phenyl	t-butoxycarbonylamine
353	NHSO 2 CH 3	phenyl	(N-pyrrolidino)formylimino
354	NHSO 2 CH 3	phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
355	NHSO 2 CH 3	2-F-phenyl	guanidino
356	NHSO 2 CH 3	2-F-phenyl	2-thiazolin-2-ylamine
357	NHSO 2 CH 3	2-F-phenyl	N-methyl-2-imidazolin-2-yl
358	NHSO 2 CH 3	2-F-phenyl	N-methyl-1,4,5,6-tetrahydropyrimid-2-yl
359	NHSO 2 CH 3	2-F-phenyl	N-methylimidazol-2-ylthio
360	NHSO 2 CH 3	2-F-phenyl	t-butoxycarbonylamine
361	NHSO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formylimino
362	NHSO 2 CH 3	2-F-phenyl	(N-pyrrolidino)formyl-N-(methanesulfamoyl)imino
363	NHSO 2 CH 3	2-CH 3 O-phenyl	(N-pyrrolidino)formylimino
364	NHSO 2 CH 3	2-CH 3 O-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, Ohio) 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, K i .

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 Lineweaver and Burk. Values of K i were determined by allowing 0.2-0.5 nM human factor Xa (Enzyme Research Laboratories, South Bend, Ind.) to react with the substrate (0.20 mM-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 K i values:

( v o −v s )/ v s =I/ ( K i (1+ S/K m ))

where:

v o 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;

K i 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 K i 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 by their ability to inhibit the cleavage of small molecule substrates by thrombin in a purified system. In vitro 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, Tex.) 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, Ind.) 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 K i 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 anti-coagulant 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 IIb/IIIa 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. Pat. 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.

Dosage 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 orali 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.

Injectable

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 mL 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 low viscosity 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

1. A compound of formula I: or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein;ring M is of formula h or i: D is selected from CN, C(═NR7)NR8R9, NHC(═NR7)NR8R9, NR8CH(═NR7), C(O)NR8R9, and (CR8R9)NR8R9; 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, OR3, SR3, CO2R3, NO2, and CH2OR3, and (CR8R9)tNR8R9; alternatively, E and R combine to form methylenedioxy or ethylenedioxy; Z is selected from a bond, C1-4 alkylene, (CH2)rO(CH2)r, (CH2)rNR3(CH2)r, (CH2)rC(O) (CH2)r, (CH2)rC(O)O(CH2)r, (CH2)rOC(O) (CH2)r, (CH2)rC(O)NR3(CH2)r, (CH2)rNR3C(O) (CH2)r, (CH2)rOC(O)O(CH2)r, (CH2)rOC (O)NR3 (CH2)r, (CH2)rNR3C(O)O (CH2)r, (CH2)rNR3C(O)NR3(CH2)r, (CH2)rS(O)p(CH2)r, (CH2)rSO2NR3(CH2)r, (CH2)rNR3SO2(CH2)r, and (CH2)rNR3SO2NR3 (CH2)r, provided that Z does not form a N—N, N—O, N—S, NCH2N, NCH2O, or NCH2S bond with ring M or group A; R1a and R1b are independently absent or selected from —(CH2)r—R1′, —CH═CH—R1′, NCH2R1″, OCH2R1″, SCH2R1″, NH(CH2)2(CH2)tR1′, O(CH2)2(CH2)tR1′, and S(CH2)2(CH2)tR1′; alternatively, R1a and R1b, 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 R4 and which contains from 0-2 heteroatoms selected from the group consisting of N, O, and S; alternatively, when Z is C(O)NH and R1a is attached to a ring carbon adjacent to Z, then R1a is a C(O) which replaces the amide hydrogen of Z to form a cyclic imide; R1′ is selected from H, C1-3 alkyl, F, Cl, Br, I, —CN, —CHO, (CF2)rCF3, (CH2)rOR2, NR2R2a, C(O)R2c, OC(O)R2, (CF2)rCO2R2c, S(O)pR2b, NR2(CH2)rOR2, CH(═NR2c)NR2R 2a, NR2C(O)R2b, NR2C(O)NHR2b, NR2C(O)2R2a, OC(O)NR2aR2b, C(O)NR2R2a, C(O)NR2(CH2)rOR2, SO2NR2R2a, NR2SO2R2b, C3-6 carbocyclic residue substituted with 0-2 R4, 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 R4; R1″ is selected from H, CH(CH2OR2)2, C(O)R2c, C(O)NR2R2a, S(O)R2b, S(O)2R2b, and SO2NR2R2a; R2, at each occurrence, is selected from H, CF3, C1-6 alkyl, benzyl, C3-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2a, at each occurrence, is selected from H, CF3, C1-6 alkyl, benzyl, phenethyl, C3-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2b, at each occurrence, is selected from CF3, C1-4 alkoxy, C1-6 alkyl, benzyl, C3-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2c, at each occurrence, is selected from CF3, OH, C1-4 alkoxy, C1-6 alkyl, benzyl, C3-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; alternatively, R2 and R2a, 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 R4b and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; R3, at each occurrence, is selected from H, C1-4 alkyl, and phenyl; R3a, at each occurrence, is selected from H, C1-4 alkyl, and phenyl; R3b, at each occurrence, is selected from H, C1-4 alkyl, and phenyl; R3c, at each occurrence, is selected from C1-4 alkyl, and phenyl; A is selected from: C3-10 carbocyclic residue substituted with 0-2 R4, 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 R4; B is selected from: Y and X-Y; X is selected from C1-4 alkylene, —CR2(CR2R2b) (CH2)t—, —C(O)—, —C(═NR1″)—, —CR2(NR1″R2)—, —CR2 (OR2)—, —CR2(SR2)—, —C(O) CR2R2a—, —CR2R2aC(O), —S(O)p—, —S(O)pCR2R2a—, —CR2R2aS(O)p—, —S(O)2NR2—, —NR2S(O)2—, —NR2S(O)2CR2R2a—, —CR2R2aS(O)2NR2—, —NR2S(O)2NR2—, —C(O)NR2—, —NR2C(O)—, —C(O)NR2CR2R2a—, —NR2C(O)CR2R2a—, —CR2R2aC(O)NR2—, —CR2R2aNR2C(O)—, —NR2C(O)O—, —OC(O)NR2—, —NR2C(O)NR2—, —NR2—, —NR2CR2R2a—, —CR2R2aNR2—, O, —CR2R2aO—, and —OCR2R2a—; Y is selected from: C3-10 carbocyclic residue substituted with 0-2 R4a 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 R4a; R4, at each occurrence, is selected from H, ═O, (CH2)rOR2, F, Cl, Br, I, C1-4 alkyl, —CN, NO2, (CH2)rNR2R2a, (CH2)rC(O)R2c, NR2C(O)R2b, C(O)NR2R2a, NR2C(O)NR2R2a, CH(═NR2)NR2R2a, CH(═NS(O)2R5)NR2R2a, NHC(═NR2)NR2R2a, C(O)NHC(═NR2)NR2R2a, SO2NR2R2a, NR2SO2NR2R2a, NR2SO2—C1-4 alkyl, NR2SO2R5, S(O)pR5, (CF2)rCF3, NCH2R1″, OCH2R1″, SCH2R1″, N(CH2)2(CH2)tR1′, O(CH2)2(CH2)tR1′, and S(CH2)2(CH2)tR1′; alternatively, one R4 is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R4a, at each occurrence, is selected from H, ═O, (CH2)rOR2, (CH2)r—F, (CH2)r—Br, (CH2)r—Cl, I, C1-4 alkyl, —CN, NO2, (CH2)rNR2R2a, (CH2)rNR2R2b, (CH2)rC(O)R2c, NR2C(O)R2b, C(O)NR2R2a, C(O)NH(CH2)2NR2R2a, NR2C(O)NR2R2a, CH(═NR2)NR2R2a, NHC (═NR2)NR2R2a, SO2NR2R2a, NR2SO2NR2R2a, NR2SO2—C1-4 alkyl, C(O)NHSO2—C1-4 alkyl, NR2SO2R5, S(O)pR5, and (CF2)rCF3; alternatively, one R4a is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-1 R5; R4b, at each occurrence, is selected from H, ═O, (CH2)rOR3, F, Cl, Br, I, C1-4 alkyl, —CN, NO2 , (CH2)rNR3R3a, (CH2)rC(O) R3, (CH2)rC(O)OR3c, NR3C(O)R3a, C(O)NR3R3a, NR3C(O)NR3R3a, CH(═NR3)NR3R3a, NH3C(═NR3)NR3R3a, SO2NR3R3a, NR3SO2NR3R3a, NR3SO2—C1-4 alkyl, NR3SO2CF3, NR3SO2-phenyl, S(O)pCF3, S(O)p—C1-4 alkyl, S(O)p-phenyl, and (CF2)rCF3; R5, at each occurrence, is selected from CF3, C1-6 alkyl, phenyl substituted with 0-2 R6, and benzyl substituted with 0-2 R6; R6, at each occurrence, is selected from H, OH, (CH2)rOR2, F, Cl, Br, I, C1-4 alkyl, CN, NO2, (CH2)rNR2R2a, (CH2)rC(O)R2b, NR2C(O)R2b, NR2C(O)NR2R2a, CH(═NH)NH2, NHC(═NH)NH2, SO2NR2R2a, NR2SO2NR2R2a, and NR2SO2C1-4 alkyl; R7, at each occurrence, is selected from H, OH, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-4 alkoxycarbonyl, (CH2)n-phenyl, C6-10 aryloxy, C6-10 aryloxycarbonyl, C6-10 arylmethylcarbonyl, C1-4 alkylcarbonyloxy C1-4 alkoxycarbonyl, C6-10 arylcarbonyloxy C1-4 alkoxycarbonyl, C1-6 alkylaminocarbonyl, phenylaminocarbonyl, and phenyl-C1-4 alkoxycarbonyl; R8, at each occurrence, is selected from H, C1-6 alkyl and (CH2)n-phenyl; alternatively, R7 and R8 combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; R9, at each occurrence, is selected from H, C1-6 alkyl and (CH2)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:Z is selected from a bond, CH2O, OCH2, CH2NH, NHCH2, CH2C(O), C(O)CH2, C(O)NH, C(O)NH, CH2S(O)2, S(O)2(CH2), SO2NH, and SO2NH; B is selected from: Y and X-Y; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R4a; 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 O, S, NH, and N.

3. A compound according to claim 2, wherein Ring M is of formula h: wherein:D is selected from C(═NR7)NR8R9 and (CR8R9)NR8R9; R is selected from H, F, Cl, OR3, CH2OR3, CH2NH2; A is selected from: piperidinyl, piperazinyl, C5-6 carbocyclic residue substituted with 0-2 R4, and 5-6 membered heteroaryl containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R4a; 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)NH2 and CH2NH2; R is selected from H, F, Cl, and Br; A is selected from: C5-6 carbocyclic residue substituted with 0-2 R4, and 5-6 membered heteroaryl containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R4a; 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; R2, at each occurrence, is selected from H, CF3, C1-6 alkyl, benzyl, C5-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2a, at each occurrence, is selected from H, CF3, C1-6 alkyl, benzyl, phenethyl, C5-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2b, at each occurrence, is selected from CF3, C1-4 alkoxy, C1-6 alkyl, benzyl, C5-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; R2c, at each occurrence, is selected from CF3, OH, C1-4 alkoxy, C1-6 alkyl, benzyl, C5-6 carbocyclic residue substituted with 0-2 R4b, 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 R4b; alternatively, R2 and R2a, 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 R4b; R4, at each occurrence, is selected from H, ═O, OR2, CH2OR2, F, Cl, C1-4 alkyl, NR2R2a, CH2NR2R2a, C(O)R2c, CH2C(O)R2c, C(O)NR2R2a, CH(═NR2)NR2R2a, CH(═NS(O)2R5)NR2R2a, SO2NR2R2a, NR2SO2—C1-4 alkyl, S(O)2R5, and CF3 provided that if B is H, then R4 is other than tetrazole, C(O)-alkoxy, and C(O)NR2R2a; R4a, at each occurrence, is selected from H, ═O, (CH2)rOR2, F, Cl, C1-4 alkyl, NR2R2a, CH2NR2R2a, NR2R2b, CH2NR2R2b, (CH2)rC(O)R2c, NR2C(O)R2b, C(O)NR2R2a, C(O)NH(CH2)2NR2R2a, NR2C(O)NR2R2a, SO2NR2R2a, S(O)2R5, and CF3; and, R4b, at each occurrence, is selected from H, ═O, (CH2)rOR3, F, Cl, C1-4 alkyl, NR3R3a, CH2NR3R3a, C(O)R3, CH2C(O)R3, C(O)OR3c, C(O)NR3R3a, CH(═NR3)NR3R3a, SO2NR3R3a, NR3SO2—C1-4 alkyl, NR3SO2CF3, NR3SO2-phenyl, S(O)2CF3, S(O)2—C1-4 alkyl, S(O)2-phenyl, and CF3.

5. 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.

6. 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.

7. 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.

8. 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.

9. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

10. A method for treating 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.

11. A method for treating 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.

12. A method for treating 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.