Claims
- 1. A compound having the formula:
- 2. The compound of claim 1, wherein each of R1 and R2 is directly attached or through a linker, and is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, 9-purine-6-amine, thiazoleamino group, hydroxyl, branched or unbranched alkyl; alkenyl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group.
- 3. The compound of claim 2 wherein the linker is an amide moiety, —O—, —S—, —NH—, or —CH2—.
- 4. The compound of claim 1 having the formula:
- 5. The compound of claim 4, wherein R2 is -amide-R5,
wherein R5 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, 9-purine-6-amine, thiazoleamino group, hydroxyl, branched or unbranched alkyl, alkenyl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group.
- 6. A compound having the formula:
- 7. The compound of claim 6 having the formula:
- 8. The compound of claim 6 having the formula:
- 9. The compound of claim 6 having the formula:
- 10. The compound of claim 9 wherein the aryl or cycloalkyl group is substituted with a methyl, cyano, nitro, trifluoromethyl, amino, aminocarbonyl, methylcyano, chloro, fluoro, bromo, iodo, 2,3-difluoro, 2,4-difluoro, 2,5-difluoro, 3,4-difluoro, 3,5-difluoro, 2,6-difluoro, 1,2,3-trifluoro, 2,3,6-trifluoro, 2,4,6-trifluoro, 3,4,5-trifluoro, 2,3,5,6-tetrafluoro, 2,3,4,5,6-pentafluoro, azido, hexyl, t-butyl, phenyl, carboxyl, hydroxyl, methoxy, phenyloxy, benzyloxy, phenylaminooxy, phenylaminocarbonyl, methyoxycarbonyl, methylaminocarbonyl, dimethylamino, dimethylaminocarbonyl, or hydroxylaminocarbonyl group.
- 11. The compound of claim 6 having the formula:
- 12. The compound of claim 11, wherein n=5.
- 13. The compound of claim 6 having the formula:
- 14. The compound of claim 13, wherein n=5.
- 15. The compound of claim 6 having the formula:
- 16. The compound of claim 15, wherein n=5.
- 17. The compound of claim 6 having the formula:
- 18. The compound of claim 17, wherein n=5.
- 19. The compound of claim 6 having the formula:
- 20. The compound of claim 19, wherein n=5.
- 21. The compound of claim 6 having the formula:
- 22. The compound of claim 21, wherein n=5.
- 23. The compound of claim 6 having the formula:
- 24. The compound of claim 23, wherein n-5.
- 25. The compound of claim 6 having the formula:
- 26. The compound of claim 25, wherein n=5.
- 27. The compound of claim 6 having the formula:
- 28. The compound of claim 27, wherein n=5.
- 29. The compound of claim 6 having the formula:
- 30. The compound of claim 29, wherein n=5.
- 31. The compound of claim 6 having the formula:
- 32. The compound of claim 31, wherein n=5.
- 33. A pharmaceutical composition comprising a pharmaceutically effective amount of the compound of any one of claims 1-9 and a pharmaceutically acceptable carrier.
- 34. A method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable conditions with an effective amount of the compound of any one of claims 1-9.
- 35. A method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an effective amount of the compound of any one of claims 1-9.
- 36. A compound having the formula:
- 37. The compound of claim 36, wherein each of R1 and R2 is directly attached or through a linker, and is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, 9-purine-6-amine, thiazoleamino group, hydroxyl, branched or unbranched alkyl, alkenyl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group.
- 38. The compound of claim 37, wherein the linker is an amide moiety, —O—, —S—, —NH—, or —CH2—.
- 39. The compound of claim 36 having the formula:
- 40. The compound of claim 39, wherein R2 is -sulfonamide-R8, or -amide-R8, wherein R8 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, 9-purine-6-amine, thiazoleamino group, hydroxyl, branched or unbranched alkyl, alkenyl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group.
- 41. The compound of claim 39, wherein R2 is —NH—C(O)—Y, —NH—SO2—Y, wherein Y is selected from the group consisting of:
- 42. The compound of claim 39, wherein R7 is selected from the group consisting of:
- 43. A compound having the formula:
- 44. The compound of claim 43, wherein n is from 4-7, and m is from 1-3.
- 45. The compound of claim 43, wherein each of R1 and R2 is directly attached or through a linker, and is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, 9-purine-6-amine, thiazoleamino group, hydroxyl, branched or unbranched alkyl, alkenyl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group.
- 46. The compound of claim 43, wherein the linker is an amide moiety, —O—, —S—, —NH—, or —CH2—.
- 47. The compound of claim 43, having the formula:
- 48. The compound of claim 47, wherein the linker L comprises the moiety
- 49. The compound of claim 43, having the formula:
- 50. A pharmaceutical composition comprising the compound of claim 1, 36 or 43 and a pharmaceutically acceptable carrier.
- 51. A pharmaceutically acceptable salt of the compound of claim 1, 36, or 43.
- 52. A prodrug of the compound of claim 1, 36 or 43.
- 53. A method of inducing differentiation of tumor cells in a tumor comprising contacting the cells with an effective amount of the compound of claim 1, 36 or 43 so as to thereby differentiate the tumor cells.
- 54. A method of inhibiting the activity of histone deacetylase comprising contacting the histone deacetylase with an effective amount of the compound of claim 1, 36 or 43 so as to thereby inhibit the activity of histone deacetylase.
RELATED APPLICATION
[0001] This application is a continuation of U.S. application Ser. No. 09/645,430, filed Aug. 24, 2000 which claims the benefit of U.S. Provisional Application No. 60/208,688 filed Jun. 1, 2000 and U.S. Provisional Application No. 60/152,755, filed Sep. 8, 1999.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60208688 |
Jun 2000 |
US |
|
60152755 |
Sep 1999 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09645430 |
Aug 2000 |
US |
Child |
10281875 |
Oct 2002 |
US |