Claims
- 1. A compound selected from the group consisting of Formula (I) and Formula (II):
- 2. The compound of claim 1 wherein R1 is selected from the group consisting of hydrogen, aryl(C1-8)alkyl and heteroaryl(C1-8)alkyl, wherein the aryl and heteroaryl portion of arylalkyl and heteroarylalkyl are optionally substituted with a substituent selected from R4.
- 3. The compound of claim 1 wherein R1 is selected from the group consisting of hydrogen, benzyl, phenethyl, phenylpropyl and benzofurylmethyl, wherein phenyl, the phenyl portion of benzyl and the benzofuryl portion of benzofurylmethyl are optionally substituted with a substituent selected from R4.
- 4. The compound of claim 1 wherein R1 is selected from the group consisting of hydrogen, benzyl, phenylpropyl and benzofurylmethyl, wherein phenyl, the phenyl portion of benzyl and the benzofuryl portion of benzofurylmethyl are optionally substituted with a substituent selected from R4.
- 5. The compound of claim 1 wherein R2 is hydrogen.
- 6. The compound of claim 1 wherein R3 is aryl(C2-8)alkenyl, wherein aryl is optionally substituted with one to three substituents independently selected from halogen.
- 7. The compound of claim 1 wherein R3 is a substituent independently selected from the group consisting of phenethenylene and phenylpropenylene, wherein phenyl is optionally substituted with one to three substituents independently selected from the group consisting of chlorine and fluorine.
- 8. The compound of claim 1 wherein R3 is phenethenylene, wherein phenyl is substituted with one to three substituents selected from chlorine.
- 9. The compound of claim 1 wherein R4 is selected from the group consisting of hydroxy, di(C1-4alkyl)amino, C1-8alkoxy, carboxy, carboxy(C1-8)alkoxy, aryl(C1-8)alkoxy, C1-8alkoxycarbonyl, C1-8alkoxycarbonyl(C1-8)alkoxy, aminocarbonyl, (C1-8alkyl)aminocarbonyl, (carboxy(C1-8)alkyl)aminocarbonyl and C1-8alkoxycarbonyl(C1-8)alkyl)aminocarbonyl.
- 10. The compound of claim 1 wherein R4 is selected from the group consisting of hydroxy, carboxy, carboxy(C1-8)alkoxy, C1-8alkoxycarbonyl, C1-8alkoxycarbonyl(C1-8)alkoxy, aminocarbonyl, (carboxy(C1-8)alkyl)aminocarbonyl and C1-8alkoxycarbonyl(C1-8)alkyl)aminocarbonyl.
- 11. The compound of claim 1 wherein R4 is selected from the group consisting of hydroxy, carboxy, carboxymethoxy, methoxycarbonyl, aminocarbonyl, (carboxymethylene)aminocarbonyl and methoxycarbonylmethylene)aminocarbonyl.
- 12. The compound of claim 1 wherein G is selected from the group consisting of hydrogen, halogen, hydroxy, C1-4alkyl, C1-8alkoxy, aryl, aryloxy, aryl(C1-8)alkyl, aryl(C1-8)alkoxy, amino and trihalo(C1-8)alkyl.
- 13. The compound of claim 1 wherein G is hydrogen.
- 14. The compound of claim 1 of the formula:
- 15. The compound of claim 1 of the formula:
- 16. The compound of claim 1 of the formula:
- 17. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
- 18. A pharmaceutical composition made by mixing a compound of claim 1 and a pharmaceutically acceptable carrier.
- 19. A process for preparing a pharmaceutical composition comprising mixing a compound of claim 1 and a pharmaceutically acceptable carrier.
- 20. A method for treating a serine protease or dual-serine protease mediated disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound of claim 1.
- 21. The method of claim 20 wherein the disorder is mediated by selective inhibition of a serine protease.
- 22. The method of claim 21 wherein the serine protease is selected from the group consisting of Factor Xa and tryptase.
- 23. The method of claim 20 wherein the disorder is mediated by dual inhibition of at least two serine proteases.
- 24. The method of claim 23 wherein the serine protease is selected from the group consisting of at least Factor Xa and tryptase.
- 25. The method of claim 20 wherein the serine protease or dual-serine protease mediated disorder is selected from the group consisting of thrombotic disorders, arterial thrombosis, venous thrombosis, restenosis, hypertension, heart failure, arrhythmia, myocardial infarction, acute myocardial infarction, reocclusion following thrombolytic therapy, reocclusion following angioplasty, inflammation, angina, unstable angina, stroke, atherosclerosis, ischemic conditions, neurodegenerative disorders (associated with thrombotic or ischemic conditions), asthma and inflammatory bowel syndrome.
- 26. The method of claim 20 wherein the therapeutically effective amount of the compound of claim 1 is from about 0.001 mg/kg/day to about 300 mg/kg/day.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is a divisional of Ser. No. 10/090,872 filed Mar. 5, 2002, which claims benefit of provisional application Serial No. 60/274,845, filed 9 Mar. 2001, which are hereby incorporated by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60274845 |
Mar 2001 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
10090872 |
Mar 2002 |
US |
Child |
10303229 |
Nov 2002 |
US |