IP Library Granted Patent US 7,884,100
Granted Patent B2
US 7,884,100 · App. 11/811,823 · Granted Feb 8, 2011

Substituted 8-[6-amino-3-pyridyl]xanthines

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Quick Facts
Patent No.
US 7,884,100
App. No.
11/811,823
Granted
Feb 8, 2011
Kind
B2
Abstract

The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A 2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Claims (84)

1. A compound selected from the group:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 1 ; and

(b) a pharmaceutically acceptable excipient.

3. A method for treating asthma comprising administering an effective amount of a compound claim 1 to a mammal in need of such treatment.

4. A method for treating diabetic retinopathy, comprising administering an effective amount of a compound claim 1 or a pharmaceutically acceptable salt thereof to a mammal in need of such treatment.

5. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

6. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

7. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

8. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. A con-mound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

10. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

13. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

14. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

15. A compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 5 ; and

(b) a pharmaceutically acceptable excipient.

17. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 6 ; and

(b) a pharmaceutically acceptable excipient.

18. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 7 ; and

(b) a pharmaceutically acceptable excipient.

19. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 8 ; and

(b) a pharmaceutically acceptable excipient.

20. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 9 ; and

(b) a pharmaceutically acceptable excipient.

21. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 10 ; and

(b) a pharmaceutically acceptable excipient.

22. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 11 ; and

(b) a pharmaceutically acceptable excipient.

23. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 12 ; and

(b) a pharmaceutically acceptable excipient.

24. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 13 ; and

(b) a pharmaceutically acceptable excipient.

25. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 14 ; and

(b) a pharmaceutically acceptable excipient.

26. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a compound of claim 15 ; and

(b) a pharmaceutically acceptable excipient.

27. A method for treating asthma, comprising: administering an effective amount of a compound claim 5 to a mammal in need of such treatment.

28. A method for treating asthma, comprising: administering an effective amount of a compound claim 6 to a mammal in need of such treatment.

29. A method for treating asthma, comprising: administering an effective amount of a compound claim 7 to a mammal in need of such treatment.

30. A method for treating asthma, comprising: administering an effective amount of a compound claim 8 to a mammal in need of such treatment.

31. A method for treating asthma, comprising: administering an effective amount of a compound claim 9 to a mammal in need of such treatment.

32. A method for treating asthma, comprising: administering an effective amount of a compound claim 10 to a mammal in need of such treatment.

33. A method for treating asthma, comprising: administering an effective amount of a compound claim 11 to a mammal in need of such treatment.

34. A method for treating asthma, comprising: administering an effective amount of a compound claim 12 to a mammal in need of such treatment.

35. A method for treating asthma, comprising: administering an effective amount of a compound claim 13 to a mammal in need of such treatment.

36. A method for treating asthma, comprising: administering an effective amount of a compound claim 14 to a mammal in need of such treatment.

37. A method for treating asthma, comprising: administering an effective amount of a compound claim 15 to a mammal in need of such treatment.

38. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 5 to a mammal in need of such treatment.

39. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 6 to a mammal in need of such treatment.

40. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 7 to a mammal in need of such treatment.

41. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 8 to a mammal in need of such treatment.

42. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 9 to a mammal in need of such treatment.

43. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 10 to a mammal in need of such treatment.

44. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 11 to a mammal in need of such treatment.

45. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 12 to a mammal in need of such treatment.

46. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 13 to a mammal in need of such treatment.

47. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 14 to a mammal in need of such treatment.

48. A method for treating diabetic retinopathy, comprising: administering an effective amount of a compound claim 15 to a mammal in need of such treatment.

Assignments (12)
MERGER Recorded Jun 26, 2018
From: DOGWOOD PHARMACEUTICALS, INC.
To: ALLERGAN SALES, LLC
Reel/Frame 046208/0691 →
CORRECTIVE ASSIGNMENT TO CORRECT THE EXECUTION DATE OF THE PREVIOUSLY RECORDED ASSIGNMENT FROM DECEMBER 31, 2011 TO MARCH 15, 2013 PREVIOUSLY RECORDED ON REEL 029737 FRAME 0569. ASSIGNOR(S) HEREBY CONFIRMS THE EXECUTION DATE OF THE ORIGINAL ASSIGNMENT DATED ON DECEMBER 31, 2011 WAS INCORRECT. Recorded Mar 19, 2013
From: FOREST LABORATORIES HOLDINGS LIMITED
To: DOGWOOD PHARMACEUTICALS, INC.
Reel/Frame 030045/0899 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2013
From: CLINICAL DATA, INC.
To: DOGWOOD PHARMACEUTICALS, INC.
Reel/Frame 029737/0389 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2013
From: DOGWOOD PHARMACEUTICALS, INC.
To: FOREST LABORATORIES HOLDINGS LIMITED
Reel/Frame 029737/0498 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2013
From: FOREST LABORATORIES HOLDINGS LIMITED
To: DOGWOOD PHARMACEUTICALS, INC.
Reel/Frame 029737/0569 →
MERGER Recorded Jan 31, 2013
From: TROVIS PHARMACEUTICALS HOLDINGS, INC.
To: CLINICAL DATA, INC.
Reel/Frame 029728/0445 →
MERGER Recorded Jan 31, 2013
From: TROVIS PHARMACEUTICALS LLC
To: TROVIS PHARMACEUTICALS HOLDINGS, INC.
Reel/Frame 029728/0400 →
CHANGE OF NAME Recorded Jan 28, 2011
From: PGXHEALTH, LLC
To: TROVIS PHARMACEUTICALS, LLC
Reel/Frame 025709/0994 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 8, 2009
From: ADENOSINE THERAPEUTICS, LLC
To: PGXHEALTH, LLC
Reel/Frame 022075/0734 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 20, 2008
From: ADENOSINE THERAPEUTICS, LLC
To: PGXHEALTH, LLC
Reel/Frame 021867/0071 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 2, 2008
From: BEAUGLEHOLE, ANTHONY; SCHMIDTMANN, FRANK W.; RIEGER, JAYSON M.; WATKINS, LINDA; LORAM, LISA C.; HUTCHINSON, MARK; THOMPSON, ROBERT D.
To: ADENOSINE THERAPEUTICS, LLC
Reel/Frame 020896/0198 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2008
From: WANG, GUOQUAN; RIEGER, JAYSON M.; THOMPSON, ROBERT D.
To: ADENOSINE THERAPEUTICS, LLC
Reel/Frame 020729/0289 →