Claims
- 1. A compound having the formula I:
- 2. A compound having the formula II:
- 3. The compound as defined in claim 2, wherein R1 is chosen from C6-12 aryl or C3-10 heterocycle.
- 4. The compound as defined in claim 2, wherein R1 is C3-6 heterocycle.
- 5. The compound as defined in claim 2, wherein R1 is chosen from thienyl, furanyl, pyridyl, oxazolyl, thiazolyl, pyrrolyl, benzofuranyl, indolyl, benzoxazolyl, benzothienyl, benzothiazolyl or quinolinyl.
- 6. The compound as defined in claim 2, wherein R1 is phenyl substituted by at least one substituent chosen from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-10 heterocycle, halogen, nitro, amido amino, amidino, guanido, CN, COOC1-12 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-12 alkynyloxy, or C6-12 aryloxy.
- 7. The compound as defined in claim 2, wherein R1 is phenyl substituted by one or two substituents chosen from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-10 heterocycle, halogen, nitro, amido, amino, amidino, guanido, CN, COOC1-6 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-12 alkynyloxy, or C6-12 aryloxy.
- 8. The compound as defined in claim 2, wherein R1 is phenyl substituted by one or two substituents chosen from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 heterocycle, halogen, nitro, amido, amino, amidino, guanido, CN, COOC1-6 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-6 alkynyloxy, or C6-12 aryloxy.
- 9. The compound as defined in claim 2, wherein R1 is phenyl substituted by one or two substituents chosen from C1-12 alkyl, amino, halogen, nitro, amido, CN, COOC1-12 alkyl, or C1-12 alkyloxy.
- 10. The compound as defined in claim 2, wherein R1 is phenyl substituted by one or two substituents chosen from C1-6 alkyl, amino, halogen, nitro, amido, CN, COOC1-6 alkyl, or C1-6 alkyloxy.
- 11. The compound as defined in claim 2, wherein R1 is phenyl.
- 12. The compound as defined in claim 2, wherein X is chosen from:
- 13. The compound as defined in claim 2, wherein X is chosen from:
- 14. The compound as defined in claim 2, wherein X is:
- 15. The compound as defined in claim 2, wherein X is
- 16. The compound as defined in claim 2, wherein Y is chosen from COOR5, tetrazole, CO-(amino acid) or CONRcRd.
- 17. The compound as defined in claim 2, wherein Y is COOR5.
- 18. The compound as defined in claim 15, wherein R5 is C1-12 alkyl.
- 19. The compound as defined in claim 2, wherein Y is CO-(amino acid).
- 20. The compound as defined in claim 2, wherein Y is tetrazole.
- 21. The compound as defined in claim 2, wherein Y is CONRcRd.
- 22. The compound as defined in claim 2, wherein Y is COOH.
- 23. The compound as defined in claim 2, wherein R3 is H.
- 24. The compound as defined in claim 2, wherein R3 is C1-3 alkyl.
- 25. The compound as defined in claim 2, wherein R3 is chosen from methyl, ethyl, n-propyl, isopropyl and cyclopropyl.
- 26. The compound as defined in claim 2, wherein R2 is C3-10 heterocycle.
- 27. The compound as defined in claim 2, wherein R2 is C3-6 heterocycle.
- 28. The compound as defined in claim 2, wherein R2 is chosen from thienyl, furanyl, pyridyl, oxazolyl, thiazolyl, pyrrolyl, benzofuranyl, indolyl, benzoxazolyl, benzothienyl, benzothiazolyl or quinolinyl.
- 29. The compound as defined in claim 2, wherein R2 is C1-12 alkyl.
- 30. The compound as defined in claim 2, wherein R2 is chosen from cyclopentyl, cyclohexyl or t-butyl.
- 31. The compound as defined in claim 2, wherein R2 is C6-12 aryl.
- 32. The compound as defined in claim 2, wherein R2 is chosen from indenyl, naphthyl or biphenyl.
- 33. The compound as defined in claim 2, wherein R2 is phenyl substituted by at least one substituent chosen from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-10 heterocycle, halogen, nitro, amido, amino, amidino, guanido, CN, COOC1-12 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-12 alkynyloxy, or C6-12 aryloxy.
- 34. The compound as defined in claim 2, wherein R2 is phenyl substituted by one or two substituents chosen from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C3-10 heterocycle, halogen, nitro, amido, amino, amidino, guanido, CN, COOC1-12 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-12 alkynyloxy, or C6-12 aryloxy.
- 35. The compound as defined in claim 2, wherein R2 is phenyl substituted by one or two substituents chosen from C1-12 alkyl, amino, halogen, nitro, amido, CN, COOC1-12 alkyl, or C1-12 alkyloxy.
- 36. The compound as defined in claim 2, wherein R2 is phenyl substituted by one or two substituents chosen from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 heterocycle, halogen, nitro, amido, amino, amidino, guanido, CN, COOC1-6 alkyl, C1-12 alkyloxy, C2-12 alkenyloxy, C2-12 alkynyloxy, or C6-12 aryloxy.
- 37. The compound as defined in claim 2, wherein R2 is phenyl substituted by one or two substituents chosen from C1-16 alkyl, amino, halogen, nitro, amido, CN, COOC1-6 alkyl, or C1-6 alkyloxy.
- 38. The compound as defined in claim 2, wherein R2 is methylphenyl.
- 39. The compound as defined in claim 2, wherein R2 is dichlorophenyl.
- 40. The compound as defined in claim 2, wherein R2 is chlorophenyl.
- 41. A compound chosen from or pharmaceutically acceptable salts:
4-[Methyl-(4-methyl-benzoyl)-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(2,4-Dichloro-benzoyl)-methyl-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(2,4-Dichloro-benzoyl)-isopropyl-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(2,4-Dichloro-benzoyl)-ethyl-amino]-2-phenyl-thiazole-5-carboxylic acid; 2-Phenyl-4-(toluene-2-sulfonylamino)-thiazole-5-carboxylic acid; 4-[Isopropyl-(4-methyl-benzoyl)-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-(4-Chloro-benzoylamino)-2-phenyl-thiazole-5-carboxylic acid; 4-(2,4-Dimethyl-benzoylamino)-2-phenyl-thiazole-5-carboxylic acid; 4-(2,4-Dimethyl-benzenesulfonylamino)-2-phenyl-thiazole-5-carboxylic acid; 2-Phenyl-4-(toluene-4-sulfonylamino)-thiazole-5-carboxylic acid; 4-(2,4-Dichloro-benzoylamino)-2-phenyl-thiazole-5-carboxylic acid 4-(3-Methyl-benzoylamino)-2-phenyl-thiazole-5-carboxylic acid4-[(2-Chloro-benzoyl)-methyl-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(4-Chloro-benzoyl)-methyl-amino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(4-Chloro-benzoylamino]-2-phenyl-thiazole-5-carboxylic acid; 4-[(2,4-DIMETHYL-BENZOYL)-METHYL-AMINO]-2-MORPHOLIN-4-YL-THIAZOLE-5-CARBOXYLIC ACID; and pharmaceutical acceptable salts thereof.
- 42. A method for treating or preventing Flaviridae viral infection in a host comprising administering to the host a therapeutically effective amount of at least one compound according to claim 1.
- 43. The method according to claim 42 wherein said Flaviridae infection is hepatitis C(HCV).
- 44. A method for treating or preventing Flaviridae viral infection in a host comprising administering to the host a therapeutically effective amount of at least one compound according to claim 1 and at least one additional agent chosen from antiviral agent, immunomodulating agent, antioxydant agent, antibacterial agent or antisense agent.
- 45. The method according to claim 44 wherein said antiviral agent is chosen from a viral serine protease inhibitor, viral polymerase inhibitor and viral helicase inhibitor.
- 46. The method according to claim 44, wherein said additional agent is chosen from interferon-α, silybum marianum, interleukine-12, amantadine, ribozyme, ursodeoxycholic acid, hypericin, thymosin, N-acetyl cystein, ofloxacin, pentoxifylline, cyclosporin or ribavirin.
- 47. The method according to claim 44, wherein said additional agent is chosen from interferon-α or ribavirin.
- 48. The method as defined in claim 44, wherein said Flaviridea infection is hepatitis C(HCV).
- 49. A pharmaceutical composition for treating or preventing a preventing a Flaviridae viral infection comprising administering at least one compound according to claim 1 together with at least one pharmaceutically acceptable carrier or excipient.
- 50. A composition as defined in claim 49, wherein said Flaviviridea infection is hepatitis C(HCV).
- 51. The use of a compound according to claim 1, for the manufacture of a medicament for treating or preventing a viral Flaviridea infection in a host.
- 52. The use as defined in claim 51, wherein said Flaviridea infection is hepatitis C(HCV).
- 53. A method for inhibiting or reducing the activity of viral polymerase in a host comprising administering a therapeutically effective amount of a compound of claim 1.
- 54. The method of claim 53, wherein said viral polymerase is a Flaviridae viral polymerase.
- 55. The method of claim 53, wherein said viral polymerase is a RNA-dependant RNA polymerase.
- 56. The method of claim 53, wherein said viral polymerase is HCV polymerase.
Parent Case Info
[0001] This application claims the benefit of priority from U.S. Provisional Application No. 60/341,879, filed Dec. 21, 2002, hereby incorporated by refernce.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60341879 |
Dec 2001 |
US |