IP Library Granted Patent US 9,932,341
Granted Patent B2
US 9,932,341 · App. 14/193,481 · Granted Apr 3, 2018

Use of pyrazolopyrimidine derivatives for the treatment of PI3K-delta related disorders

Inventors: Yun-Long Li (Chadds Ford, PA); Andrew P. Combs (Kennett Square, PA); Eddy W. Yue (Landenberg, PA); Song Mei (Wilmington, DE); Brent Douty (Fallowfield, PA)
Assignees: Incyte Corporation; Incyte Holdings Corporation
C07D487/04A61K31/519A61K31/5377
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Quick Facts
Patent No.
US 9,932,341
App. No.
14/193,481
Granted
Apr 3, 2018
Kind
B2
Abstract

The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.

Claims (50)

1. A method of treating chronic lymphocytic leukemia (CLL), hairy cell leukemia, Mantle cell lymphoma, small lymphocytic lymphoma, follicular lymphoma, lymphoplasmacytic lymphoma, extranodal marginal zone lymphoma, activated B-cell like (ABC) diffuse large B cell lymphoma, or germinal center B cell (GCB) diffuse large B cell lymphoma in a patient, comprising administering to said patient a therapeutically effective amount of a compound of a compound, which is a 4-{3-[1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is (S)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is (S)-4-(3-((R)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the compound is (R)-4-(3-((R)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , which is a method of treating chronic lymphocytic leukemia (CLL).

7. The method of claim 1 , which is a method of treating hairy cell leukemia.

8. The method of claim 1 , which is a method of treating Mantle cell lymphoma.

9. The method of claim 1 , which is a method of treating small lymphocytic lymphoma.

10. The method of claim 1 , which is a method of treating follicular lymphoma.

11. The method of claim 1 , which is a method of treating lymphoplasmacytic lymphoma.

12. The method of claim 1 , which is a method of treating extranodal marginal zone lymphoma.

13. The method of claim 1 , which is a method of treating activated B-cell like (ABC) diffuse large B cell lymphoma.

14. The method of claim 1 , which is a method of treating germinal center B cell (GCB) diffuse large B cell lymphoma.

15. The method of claim 2 , which is a method of treating chronic lymphocytic leukemia (CLL).

16. The method of claim 2 , which is a method of treating hairy cell leukemia.

17. The method of claim 2 , which is a method of treating Mantle cell lymphoma.

18. The method of claim 2 , which is a method of treating small lymphocytic lymphoma.

19. The method of claim 2 , which is a method of treating follicular lymphoma.

20. The method of claim 2 , which is a method of treating lymphoplasmacytic lymphoma.

21. The method of claim 2 , which is a method of treating extranodal marginal zone lymphoma.

22. The method of claim 2 , which is a method of treating activated B-cell like (ABC) diffuse large B cell lymphoma.

23. The method of claim 2 , which is a method of treating germinal center B cell (GCB) diffuse large B cell lymphoma.

24. The method of claim 3 , which is a method of treating chronic lymphocytic leukemia (CLL).

25. The method of claim 3 , which is a method of treating hairy cell leukemia.

26. The method of claim 3 , which is a method of treating Mantle cell lymphoma.

27. The method of claim 3 , which is a method of treating small lymphocytic lymphoma.

28. The method of claim 3 , which is a method of treating follicular lymphoma.

29. The method of claim 3 , which is a method of treating lymphoplasmacytic lymphoma.

30. The method of claim 3 , which is a method of treating extranodal marginal zone lymphoma.

31. The method of claim 3 , which is a method of treating activated B-cell like (ABC) diffuse large B cell lymphoma.

32. The method of claim 3 , which is a method of treating germinal center B cell (GCB) diffuse large B cell lymphoma.

33. The method of claim 4 , which is a method of treating chronic lymphocytic leukemia (CLL).

34. The method of claim 4 , which is a method of treating hairy cell leukemia.

35. The method of claim 4 , which is a method of treating Mantle cell lymphoma.

36. The method of claim 4 , which is a method of treating small lymphocytic lymphoma.

37. The method of claim 4 , which is a method of treating follicular lymphoma.

38. The method of claim 4 , which is a method of treating lymphoplasmacytic lymphoma.

39. The method of claim 4 , which is a method of treating extranodal marginal zone lymphoma.

40. The method of claim 4 , which is a method of treating activated B-cell like (ABC) diffuse large B cell lymphoma.

41. The method of claim 4 , which is a method of treating germinal center B cell (GCB) diffuse large B cell lymphoma.

42. The method of claim 5 , which is a method of treating chronic lymphocytic leukemia (CLL).

43. The method of claim 5 , which is a method of treating hairy cell leukemia.

44. The method of claim 5 , which is a method of treating Mantle cell lymphoma.

45. The method of claim 5 , which is a method of treating small lymphocytic lymphoma.

46. The method of claim 5 , which is a method of treating follicular lymphoma.

47. The method of claim 5 , which is a method of treating lymphoplasmacytic lymphoma.

48. The method of claim 5 , which is a method of treating extranodal marginal zone lymphoma.

49. The method of claim 5 , which is a method of treating activated B-cell like (ABC) diffuse large B cell lymphoma.

50. The method of claim 5 , which is a method of treating germinal center B cell (GCB) diffuse large B cell lymphoma.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE OMMISSION OF SECOND RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 035292 FRAME: 0004. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 2, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 036054/0696 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION AND INCYTE CORPORATION
Reel/Frame 035924/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2014
From: LI, YUN-LONG; YAO, WENQING; COMBS, ANDREW P.; YUE, EDDY W.; MEI, SONG; ZHU, WENYU; GLENN, JOSEPH; MADUSKUIE, THOMAS P., JR.; SPARKS, RICHARD B.; DOUTY, BRENT; HE, CHUNHONG
To: INCYTE CORPORATION
Reel/Frame 033407/0492 →
Continuity (2)
Provisional Application 61771480 · Mar 1, 2013
Related Publication 20140249132A1 · Sep 4, 2014