Claims
- 1. A compound having of Formula 1
- 2. A compound having Formula 2
- 3. A compound having Formula 3:
- 4. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-[3-(8-methyl amino-imidazo [1,2-a]pyrazin-6-yl)-phenyl]-urea.
- 5. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-[3-(8-phenylamino-imidazo[1,2-a]pyrazin-6-yl)-phenyl]-urea.
- 6. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-{3-[8-(4-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 7. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-{3-[8-(3-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 8. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-{3-[8-(2-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 9. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chloro-phenyl)-3-{3-[8-(pyridin-3-ylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 10. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{3-[8-(4-chlorobenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(4-chloro-phenyl)-urea.
- 11. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{3-[8-(3-chlorobenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(4-chloro-phenyl)-urea.
- 12. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{4-[8-(4-chlorobenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(4-chloro-phenyl)-urea.
- 13. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{4-[8-(3-chlorobenzylamino)-imidazo [1,2-a]pyrazin-6-yl]-phenyl }-3-(4-chloro-phenyl)-urea.
- 14. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 4-(6-{3-[3-(4-chlorophenyl)-ureido]-phenyl}-imidazo[1,2-a]pyrazin-8-ylamino)-benzoic acid ethyl ester.
- 15. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is cyclopropylmethyl-[6-(4-phenoxyphenyl)-imidazo[1,2-a]pyrazin-8-yl]-amine.
- 16. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is (2-methoxybenzyl)-[6-(4-phenoxyphenyl)-imidazo[1,2-a]pyrazin-8-yl]-amine.
- 17. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is benzo[1,3]dioxol-5-ylmethyl-[6-(4-phenoxyphenyl)-imidazo[1,2-a]pyrazin-8-yl]-amine.
- 18. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is [6-(4-(chloromethyl)phenyl)-imidazo[1,2-a]pyrazin-8-yl]-(2-methoxy-benzyl)-amine.
- 19. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{4-[8-(2-methoxybenzylamino)-imidazo [1,2-a]pyrazin-6-yl]-phenyl }-3-phenyl-urea.
- 20. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is (2-methoxy-benzyl)-{6-[4-(4-methoxybenzylamino)-phenyl]-imidazo[1,2-a]pyrazin-8-yl}-amine.
- 21. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is (2-methoxy-benzyl)-{6-[3-(4-methoxybenzylamino)-phenyl]-imidazo[1,2-a]pyrazin-8-yl}-amine.
- 22. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{3-[8-(2-methoxybenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-phenyl-urea.
- 23. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(2-chloro-phenyl)-3-{4-[8-(2-methoxybenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 24. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{4-[8-(2-methoxybenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(2-methoxy-phenyl)-urea.
- 25. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{4-[8-(2-ethoxybenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(3-methoxy-phenyl)-urea.
- 26. A compound according to claim embodiment 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compounds is 4-{6-[4-(piperidine-1-carbonyl)-phenyl]-imidazo[1,2-a]pyrazin-8-ylamino}-benzoic acid ethyl ester.
- 27. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 4-(6-{3-[3-(4-chlorophenyl)-ureido]-phenyl}-imidazo[1,2-a]pyrazin-8-ylamino)-benzoic acid ethyl ester.
- 28. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 4-(6-{3-[3-(2-methylsulfanyl-phenyl)-ureido]-phenyl}-imidazo[1,2-a]pyrazin-8-ylamino)-benzoic acid ethyl ester.
- 29. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is {4-[8-(4-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-piperidin-1-yl-methanone.
- 30. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is {4-[8-(2-chlorophenylamino)-imidazo [1,2-a]pyrazin-6-yl]-phenyl }-piperidin-1-yl-methanone.
- 31. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 3-methoxy-N-{4-[8-(2-methoxybenzylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-benzamide.
- 32. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(3-chloro-4-fluorophenyl)-3-[3-(8-phenylamino-imidazo[1,2-a]pyrazin-6-yl)-phenyl]-urea.
- 33. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chlorophenyl)-3-[3-(8-phenylamino-imidazo[1,2-a]pyrazin-6-yl)-phenyl]-urea.
- 34. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-[3-(8-phenylamino-imidazo[1,2-a]pyrazin-6-yl)-phenyl]-3-(3-trifluoromethyl-phenyl)-urea.
- 35. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(2-chloro-5-trifluoromethyl-phenyl)-3-[3-(8-phenylamino-imidazo[1,2-a]pyrazin-6-yl)-phenyl]-urea.
- 36. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chlorophenyl)-3-{3-[8-(4-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 37. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{3-[8-(4-chloro-phenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(3-trifluoromethylphenyl)-urea.
- 38. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(3-chloro-4-fluorophenyl)-3-{3-[8-(3-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 39. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(4-chlorophenyl)-3-{3-[8-(3-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 40. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-{3-[8-(3-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-3-(3-trifluoromethylphenyl)-urea.
- 41. A compound as in claim 1, or a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug thereof, wherein the compound is 1-(3-chloro-4-fluorophenyl)-3-{3-[8-(2-chlorophenylamino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea.
- 42. A compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug as in claims 1 to 41, wherein in an in vitro assay of kinase modulation, the compound exhibits a IC50 value less than or equal to 25 micromolar.
- 43. A compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug as in claims 1 to 41, wherein in an in vitro assay of modulation of soft agar growth, the compound exhibits a IC50 value less than or equal to 25 micromolar.
- 44. A compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug as in claims 1 to 41, wherein in an in vitro assay of modulation of soft agar growth, wherein the cells are HCT-15, MiaPaca-2, MCF-7, OVCAR-4, or A549 cells, the compound exhibits a IC50 value less than or equal to 25 micromolar.
- 45. A pharmaceutical composition comprising
a compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug as in claims 1 to 41; and at least one pharmaceutically acceptable carrier or excipient.
- 46. A method of treating a kinase-implicated condition in a mammal, comprising administering to the mammal a therapeutically effective amount of a compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug claims 1 to 41.
- 47. The method of claim 46, wherein the mammal is a human.
- 48. The method of claim 46, wherein the mammal is a dog or cat.
- 49. A method of treating cancer, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug of claims 1 to 41.
- 50. A method of treating cancer, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug of claims 1 to 41 and a therapeutically effective amount of an antitumor therapeutic.
- 51. The method of claim 50, wherein treatment with the antitumor therapeutic follows treatment with the compound, pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, or prodrug of claims 1 to 41.
- 52. The method of claim 50, wherein the antitumor therapeutic is a chemotherapeutic agent.
- 53. The method of claim 52, wherein the chemotherapeutic agent is mitomycin C, carboplatin, taxol, cisplatin, paclitaxel, etoposide, doxorubicin, or a combination comprising at least one of the foregoing chemotherapeutic agents.
- 54. The method of claim 50, wherein the antitumor therapeutic is a radiotherapeutic agent.
- 55. The method of claim 50, wherein the mammal is a human.
- 56. The method of claim 50, wherein the mammal is a dog or cat.
- 57. A method for identifying a kinase, comprising contacting an organism, cell, or preparation comprising the kinase with a compound or salt according to claim 1, and detecting modulation of an activity of the kinase.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefits of U.S. Provisional Patent Application Serial No. 60/374,213 filed Apr. 19, 2002, which is fully incorporated herein by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60374213 |
Apr 2002 |
US |