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Details for Patent: 6,420,414

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Details for Patent: 6,420,414

Title: Amino derivatives of EM-138 and methods of treating angiogenesis with same
Abstract:The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.
Inventor(s): D'Amato; Robert (Lancaster, PA)
Assignee: The Children's Medical Center Corporation (Boston, MA)
Filing Date:Nov 09, 2000
Application Number:09/710,533
Claims:1. A compound selected from the group consisting of ##STR19##

wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of H and NH.sub.2, with the provisio that at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are NH.sub.2.

2. The compound of claim 1 which is ##STR20##

3. The compound of claim 1 which is ##STR21##

4. The compound of claim 1 which is ##STR22##

5. The compound of claim 1 which is ##STR23##

6. The compound of claim 1 which is ##STR24##

7. The compound of claim 1 which is ##STR25##

8. The compound of claim 1 which is ##STR26##

9. The compound of claim 1 which is ##STR27##

10. The compound of claim 1 which is ##STR28##

11. The compound of claim 1 which is ##STR29##

12. The compound of claim 1 which is ##STR30##

13. The compound of claim 1 which is ##STR31##

14. A composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

15. The composition of claim 14 wherein the compound is ##STR32##

16. The composition of claim 14 wherein the compound is ##STR33##

17. The composition of claim 14 wherein the compound is ##STR34##

18. The composition of claim 14 wherein the compound is ##STR35##

19. The composition of claim 14 wherein the compound is ##STR36##

20. The composition of claim 14 wherein the compound is ##STR37##

21. The composition of claim 14 wherein the compound is ##STR38##

22. The composition of claim 14 wherein the compound is ##STR39##

23. The composition of claim 14 wherein the compound is ##STR40##

24. The composition of claim 14 wherein the compound is ##STR41##

25. The composition of claim 14 wherein the compound is ##STR42##

26. The composition of claim 14 wherein the compound is ##STR43##

27. A method of inhibiting angiogenesis in a human or animal comprising administering to the human or animal an angiogenesis inhibiting amount of a compound of claim 1 or a pharmaceutical composition thereof.

28. The method of claim 27 wherein the compound is ##STR44##

29. The method of claim 27 wherein the compound is ##STR45##

30. The method of claim 27 wherein the compound is ##STR46##

31. The method of claim 27 wherein the compound is ##STR47##

32. The method of claim 27 wherein the compound is ##STR48##

33. The method of claim 27 wherein the compound is ##STR49##

34. The method of claim 27 wherein the compound is ##STR50##

35. The method of claim 27 wherein the compound is ##STR51##

36. The method of claim 27 wherein the compound is ##STR52##

37. The method of claim 27 wherein the compound is ##STR53##

38. The method of claim 27 wherein the compound is ##STR54##

39. The method of claim 27 wherein the compound is ##STR55##

40. A method of treating an angiogenesis-dependent disease in a human or animal comprising administering to the human or animal an effective amount of a compound of claim 1 or a pharmaceutical composition thereof.

41. The method of claim 40 wherein the compound is ##STR56##

42. The method of claim 40 wherein the compound is ##STR57##

43. The method of claim 40 wherein the compound is ##STR58##

44. The method of claim 40 wherein the compound is ##STR59##

45. The method of claim 40 wherein the compound is ##STR60##

46. The method of claim 40 wherein the compound is ##STR61##

47. The method of claim 40 wherein the compound is ##STR62##

48. The method of claim 40 wherein the compound is ##STR63##

49. The method of claim 40 wherein the compound is ##STR64##

50. The method of claim 40 wherein the compound is ##STR65##

51. The method of claim 40 wherein the compound is ##STR66##

52. The method of claim 40 wherein the compound is ##STR67##

wherein each of R.sub.12 -R.sub.17 is (independently) the same as defined above for R.sub.5 and where R.sub.11 is (independently) the same as defined above for R.sub.8 In the above formula H), R.sub.18, R.sub.19, and R.sub.20 are independently selected from ##STR68## and n=1 to 4.
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