Benzamide inhibitors of factor Xa

1. A compound of formula Ia:

wherein:

Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of Cl, OMe, NHMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 , —SMe, —SO 2 Me,

L1 is a direct link, —CONH, —CH 2 NH, or —NHCO—;

L2 is —CONH, or —NHCO;

Ar3 is

Ar2 is independently selected from the group consisting of:

Ar2 may be optionally substituted with 0-3 R 1d group; each R 1d is independently selected from the group consisting of:

H, —Me, —F, —Cl, —Br, I, —CH 3 , —CF 3 , —CN, —CO 2 H, —CO 2 Me, —CO 2 Et, —CONH 2 , —CONHMe, —CONMe 2 , —CH 2 NMe 2 , —COMe, —CH 2 COOH,

—OCH 3 , —OCF 3 , —OCH 2 F, —OCHF 2 , —OCH 2 CF 3 , —OCF 2 CF 3 , —OCH 2 CO 2 H, —OCH 2 CO 2 Me, —OCH 2 CO 2 Et, —OCH 2 CONH 2 , —OCH 2 CONMe 2 , —OCH 2 CONHMe, —OCH 2 CH 2 OMe, —OCH 2 CH 2 NHMe, —OCH 2 CH 2 NMe 2 ,

—SCH 3 , —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 , —NMe 2 , —NHCH 2 NMe 2 , —N(CH 2 CH 2 OH) 2 , —N(CH 2 CH 2 OMe) 2 , —NHCH 2 CO 2 H, —NHCH 2 CO 2 Et, —NHCH 2 CO 2 Et, —NHCH 2 CONH 2 , —NHCH 2 CONMe 2 , —N(Me)CH 2 CH 2 NMe 2 , —N(Me)CH 2 CH 2 OMe, —NHCH 2 CH 2 OMe, —NHCH 2 CH 2 OMe;

A is independently selected from the group consisting of:

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrugs derivatives thereof.

2. The compound according to claim 1 wherein L1 or L2 is —CONH.

3. The compound according to claim 1 , wherein Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of Cl, OMe, NHMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 , —SMe, —SO 2 Me,

Ar3 is

Ar2 may be optionally substituted with 0-3 R 1d groups;

each R 1d is independently selected from the group consisting of:

H, —Me, —Cl, —Br, —OCH 3 , —OCF 3 , —OCH 2 F, —OCHF 2 , —OCH 2 CF 3 , —OCF 2 CF 3 , —OCH 2 CO 2 H, —OCH 2 CO 2 Me, —OCH 2 CO 2 Et, —OCH 2 CONH 2 , —OCH 2 CONMe 2 , —OCH 2 CONHMe, —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

—F, —I, —CH 2 —CF 3 —CN, —CO 2 H, —CO 2 Me, —CO 2 Et, —CONH 2 , —CONHMe, —CONMe 2 , —CH 2 NH 2 , —CH 2 NHMe, —CH 2 NMe 2 , —COMe, —CH 2 COOH, —CH 2 COOEt,

—SCH 3 , —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 ,

—NMe 2 , —NHCH 2 NMe 2 , —N(CH 2 CH 2 OH) 2 , —N(CH 2 CH 2 OMe) 2 , —NHCH 2 CO 2 H, —NHCH 2 CO 2 Et, —NHCH 2 CO 2 Et, —NHCH 2 CONH 2 , —NHCH 2 CONMe 2 , —N(Me)CH 2 CH 2 NMe 2 , —N(Me)CH 2 CH 2 OMe, —NHCH 2 CH 2 OMe, —NHCH 2 CH 2 OMe,

A is independently selected from the group consisting of:

and all pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives therof.

4. The compound according to claim 1 having the formula:

wherein:

Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of Me, OMe, NH 2 , NHMe, —NME 2 , —SMe, —SO 2 Me, —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

Ar3 is

each R 1d1 is independently selected from the group consisting of:

H, —Me, —Cl, —OCH 3 , —OCF 3 , —OCH 2 F, —OCHF 2 , —OCH 2 CF 3 , —OCF 2 CF 3 , —OCH 2 CO 2 H, —OCH 2 CO 2 Me, —OCH 2 CO 2 Et, —OCH 2 CONH 2 , —OCH 2 CONMe 2 , —OCH 2 CONHMe, —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

—NMe 2 , —NHCH 2 NMe 2 , —N(CH 2 CH 2 OMe) 2 , —NHCH 2 CO 2 H, —NHCH 2 CO 2 Et, —NHCH 2 CO 2 Et, —NHCH 2 CONH 2 , —NHCH 2 CONMe 2 , —N(Me)CH 2 CH 2 NMe 2 , —N(Me)CH 2 CH 2 OMe, —NHCH 2 CH 2 OMe,

each R 1d2 and R 1d3 is independently selected from the group consisting of:

H, —Me, —F, —Cl, —Br, —I, —CH 2 —CF 3 , —CN, —CO 2 H, —CO 2 Me, —CO 2 Et, —CONH 2 , —CONHMe, —CONMe 2 , —CH 2 NH 2 , —CH 2 NHMe, —CH 2 NMe 2 , —COMe, —CH 2 COOH, —CH 2 COOEt,

—OCH 3 , —OCF 3 , —OCH 2 F, —OCHF 2 , —OCH 2 CF 3 , —OCF 2 CF 3 , —OCH 2 CO 2 H, —OCH 2 CO 2 Me, —OCH 2 CO 2 Et, —OCH 2 CONH 2 , —OCH 2 CONMe 2 , —OCH 2 CONHMe, —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

—SCH 3 , —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 , —SCH 2 CH 2 OMe, —SO 2 CH 2 CH 2 OMe, —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 , —SO 2 CH 2 CH 2 NMe, —NMe 2 , —NHCH 2 CH 2 NMe 2 , —N(CH 2 CH 2 OH) 2 , —N(CH 2 CH 2 OMe) 2 , —NHCH 2 CO 2 H, —NHCH 2 CO 2 Et, —NHCH 2 CO 2 Et, —NHCH 2 CONH 2 , —NHCH 2 CONMe 2 , —N(Me)CH 2 CH 2 NMe 2 , —N(Me)CH 2 CH 2 OMe;

and A is independently selected from the group consisting of:

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

5. The compound according to claim 1 , having the formula:

wherein Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of Cl, OMe, NHMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

Ar3is

each R 1d1 is independently selected from the group consisting of H, —Me, —Cl, —OCH 3 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 , —NMe 2 , —N(Me)CH 2 CH 2 NMe 2 , —N(Me)CH 2 CH 2 OMe,

each R 1d1 and R 1d3 is independently selected from the group consisting of:

H, —C≡CH, —Me, —F, —Cl, —Br, —CF 3 , —CN, —CO 2 H, —CO 2 Me, —CO 2 Et, —CONH 2 , —CH 2 NMe 2 , —COMe, —NMe 2 , —SMe, —SCH 2 CH 2 OMe, —SO 2 CH 2 CH 2 OMe, —SCH 3 , —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 , and —SO 2 CH 2 CH 2 NMe 2 ;

and A is independently selected from the group consisting of:

and pharmaceutically acceptable isomers salts, hydrates, solvates and prodrug derivatives thereof.

6. The compound according to claim 1 having the formula:

wherein:

Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of Cl, OMe, NHMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

Ar3 is

7. The compound according to claim 1 having the formula:

wherein:

Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of —Cl, —OMe, —NHMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

and A is independently selected from the group consisting of:

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

8. The compound according to claim 1 having the formula:

wherein:

Ar1 is independently

each R is independently selected from the group consisting of —Cl, —OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

A is independently selected from the group consisting of:

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

9. The compound according to claim 1 having the formula

wherein

Ar1 is independently selected from the group consisting of:

each R is independently selected from the group consisting of —Cl, —OMe, —NHMe, —NMe 2 , —OCH 2 CH 2 OMe, and —OCH 2 CH 2 NMe 2 ;

A is independently selected from the group consisting of:

10. The compound according to claim 1 having the formula

wherein

each R is independently selected from the group consisting of —H, —F, —Cl, —OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

11. The compound according to claim 1 having the formula:

wherein

each R 1d2 is independently selected from the group consisting of:

H, —C≡CH, —C—≡—CH, —Me, —F, —Cl, —Br, —CF 3 , —CN, —CO 2 H, —CO 2 Me, —CO 2 Et, —CONH 2 , —CH 2 NMe 2 , —COMe, —NMe 2 , —SMe, —SCH 2 CH 2 OMe, —SO 2 CH 2 CH 2 OMe, —SCH 3 , —SO 2 NH 2 , —SO 2 CH 3 , —SO 2 NMe 2 , and —SO 2 CH 2 CH 2 NMe 2 .

12. The compound according to claim 1 having the formula:

wherein:

each R 1d1 is independently selected from the group consisting of H, OMe, and NMe 2 :

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and —C—≡—CH;

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

13. The compound according to claim 1 having the formula:

wherein:

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH;

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

14. The compound according to claim 1 having the formula:

wherein:

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH;

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

15. The compound according to claim 1 having the formula:

wherein:

each R is independently selected from the group consisting of —H, —F, —Cl, —OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH.

16. The compound according to claim 1 having the formula:

wherein:

each R is independently selected from the group consisting of —H, —F, —Cl, —OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

each R 1d2 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH;

and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.

17. The compound according to claim 1 having the formula:

wherein:

each R is independently selected from the group consisting of —H, —F, —Cl, —OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH.

18. The compound according to claim 1 having the formula:

wherein:

each R is independently selected from the group consisting of —H, —F, —Cl, —OMe, —SMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH.

19. The compound according to claim 1 having the formula:

wherein:

each R is independently selected from the group consisting of Cl, OMe, —NMe 2 , —OCH 2 CH 2 OMe, —OCH 2 CH 2 NMe 2 ,

each R 1d3 is independently selected from the group consisting of Cl, Br, —C≡CH, and C—≡—CH.

20. The compound according to claim 1 selected from the group consisting of:

{4-[(dimethylamino)iminomethyl]phenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-( 1-methyl(2-imidazolin-2-yl))phenyl]-carboxamide;

N-(2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chlorophenyl}[4-(iminopyrrolidinylmethyl)phenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chlorophenyl}[4-(piperidyliminomethyl)phenyl]carboxamide;

ethyl 1-{[4-(N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylate;

1-{[4-(N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxamide;

{4-[(N-ethylmethylamino)iminomethyl]phenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methylpropylamino)iminomethyl]phenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[Azetidinylazetidinylidenemethy]phenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

[4-({[2-(dimethylamino)ethyl]methylamino}iminomethyl)phenyl]-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[(N-methyl-2-propynylamino)iminomethyl]phenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methyl-2-cyanoethylamino)iminomethyl]phenyl}-N-(4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(dimethylamino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chlorophenyl}[4-(iminopyrrolidinylmethyl)-2-fluorophenyl]carboxamide;

ethyl 1-{[4-(N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-3-fluorophenyl]iminomethyl}piperidine-4-carboxylate;

1-{[4-(N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-3-fluorophenyl]iminomethyl}piperidine-4-carboxamide;

N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))-2-fluorophenyl]-carboxamide;

{4-[(N-methyl(phenylmethyl)amino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-(2-methoxyethyl)methylamino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methyl(furanylmethyl)amino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-(4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-(2-hydroxyethyl)(2-imidazolin-2-yl))-2-fluorophenyl]-carboxamide;

N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-propyl(2-imidazolin-2-yl))-2-fluorophenyl]-carboxamide;

{4-[(N-(2-[1,3]Dioxolan-2-yl-ethyl)methylamino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

1-{[4-(N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-3-fluorophenyl]iminomethyl}-4-phenylpiperazine;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-methoxyphenyl}[4-(iminopyrrolidinylmethyl)phenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-methoxyphenyl}[4-(iminopiperidylmethyl)phenyl]carboxamide;

ethyl 1-{[4-(N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylate;

(4-[(dimethylamino)iminomethyl]-2-fluorophenyl}-N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))-2-fluorophenyl]-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-methoxyphenyl}[4-(iminopyrrolidinylmethyl)-2-fluorophenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chlorophenyl}[4-(iminopiperidinylmethyl)-2-fluorophenyl]carboxamide;

ethyl 1-{[4-(N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-3-fluorophenyl]iminomethyl}piperidine-4-carboxylate;

{4-[(N-methylethylamino)iminomethyl]-2-fluorophenyl}-N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[(N-propylmethylamino)iminomethyl]-2-fluorophenyl}-N-4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[Azetidinyiminomethyl]-2-fluorophenyl}-N-{4-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-6-methoxyphenyl}[4-(iminopyrrolidinylmethyl)phenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-6-methoxyphenyl}[4-(iminopiperidylmethyl)phenyl]carboxamide;

ethyl 1-{[4-(N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylate;

{4-[(N-ethylmethylamino)iminomethyl]phenyl}-N-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methylpropylamino)iminomethyl]phenyl}-N-{6-methoxy-2-[n-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[Azetidinyliminomethyl]phenyl}-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[Azetidinylazetidinylidenemethy]phenyl}-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

[4-({[2-(dimethylamino)ethyl]methylamino}iminomethyl)phenyl]-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

{4-[(N-methyl-2-propynylamino)iminomethyl]phenyl}-N-{6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))phenyl]-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chloro-6-methoxyphenyl}[4-(iminopyrrolidinylmethyl)phenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]4-chloro-6-methoxyphenyl}[4-(iminopiperidylmethyl)phenyl]carboxamide;

ethyl 1-{[4-(N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylate;

1-{[4-(N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylic acid;

{4-[(N-ethylmethylamino)iminomethyl]phenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methylpropylamino)iminomethyl]phenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

4-[Azetidinylazetidinylidenemethy]phenyl)-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

1-{[4-(N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxamide;

{4-[(dimethylamino)iminomethyl]-2-fluorophenyl-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))-2-fluorophenyl]-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-4-chloro-6-methoxyphenyl}[4-(iminopyrrolidinylmethyl)-2-fluorophenyl]carboxamide;

N-{4-chloro-6-methoxy--2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2-imidazolin-2-yl))2-fluorophenyl]-carboxamide;

ethyl 1-{[4-(N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-2-fluorophenyl]iminomethyl}-piperidine-4-carboxylate;

1-{[4-(N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)-2-fluorophenyl]iminomethyl}-piperidine4-carboxylic acid;

{4-[azetidinyliminomethyl]-2-fluorophenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[Azetidinylazetidinylidenemethy]-2-fluorophenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-ethylmethylamino)iminomethyl]-2-fluorophenyl}-N-(4chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(N-methylpropylamino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

[4-({[2-(dimethylamino)ethyl]methylamino}iminomethyl)-2-fluorophenyl]-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carboxamide;

1-{[4-(N-{4-chloro-6methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]-2-fluorophenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxamide;

{4-[(N-methyl(furanylmethyl)amino)iminomethyl]-2-fluorophenyl}-N-{4-chloro-6-methoxy-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}-carboxamide;

{4-[(dimethylamino)iminomethyl]phenyl}-N-{2-[N-(5-ethynyl(2pyridyl))carbamoyl]phenyl}-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-methyl(2imidazolin-2-yl))phenyl]-carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]}[4-(iminopyrrolidinylmethyl)phenyl]carboxamide;

N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]}[4-(iminopiperidylmethyl)phenyl]carboxamide;

ethyl 1-{[4-(N-{2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}carbamoyl)phenyl]iminomethyl}-piperidine-4-carboxylate;

N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-propyl(2-imidazolin-2-yl))phenyl]-carboxamide; and

N-{4-chloro-2-[N-(5-ethynyl(2-pyridyl))carbamoyl]phenyl}[4-(1-(2-hydroxy)ethyl(2-imidazolin-2-yl))phenyl]-carboxamide.