IP Library Granted Patent US 8,822,481
Granted Patent B1
US 8,822,481 · App. 14/256,383 · Granted Sep 2, 2014

Salts of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Inventors: James D. Rodgers (Landenberg, PA); Hui-Yin Li (Hockessin, DE)
Assignee: Incyte Corporation
C07D487/04
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Quick Facts
Patent No.
US 8,822,481
App. No.
14/256,383
Granted
Sep 2, 2014
Kind
B1
Abstract

The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Claims (28)

1. A method of inhibiting JAK1 and/or JAK2 in a patient in need thereof, comprising administering to said patient an effective amount of a compound that is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt.

2. The method of claim 1 , wherein JAK1 is inhibited.

3. The method of claim 1 , wherein JAK2 is inhibited.

4. The method of claim 1 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt.

5. The method of claim 4 , wherein JAK1 is inhibited.

6. The method of claim 4 , wherein JAK2 is inhibited.

7. The method of claim 4 , wherein said crystalline salt is 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

8. A method of inhibiting JAK1 and/or JAK2 in a patient in need thereof, comprising administering to said patient an effective amount of a pharmaceutical composition comprising (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt and a pharmaceutically acceptable carrier.

9. The method of claim 8 , wherein JAK1 is inhibited.

10. The method of claim 8 , wherein JAK2 is inhibited.

11. The method of claim 8 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt.

12. The method of claim 11 , wherein JAK1 is inhibited.

13. The method of claim 11 , wherein JAK2 is inhibited.

14. The method of claim 11 , wherein said crystalline salt is 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

15. A method of modulating an activity of JAK1 and/or JAK2 in a patient in need thereof, comprising administering to said patient an effective amount of a compound that is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt.

16. The method of claim 15 , wherein JAK1 is inhibited.

17. The method of claim 15 , wherein JAK2 is inhibited.

18. The method of claim 15 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt.

19. The method of claim 18 , wherein JAK1 is inhibited.

20. The method of claim 18 , wherein JAK2 is inhibited.

21. The method of claim 18 , wherein said crystalline salt is 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

22. A method of modulating an activity of JAK1 and/or JAK2 in a patient in need thereof, comprising administering to said patient an effective amount of a pharmaceutical composition comprising (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt and a pharmaceutically acceptable carrier.

23. The method of claim 22 , wherein JAK1 is inhibited.

24. The method of claim 22 , wherein JAK2 is inhibited.

25. The method of claim 22 , wherein (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphoric acid salt is a crystalline salt.

26. The method of claim 25 , wherein JAK1 is inhibited.

27. The method of claim 25 , wherein JAK2 is inhibited.

28. The method of claim 25 , wherein said crystalline salt is 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

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 Jun 3, 2014
From: RODGERS, JAMES D.; LI, HUI-YIN
To: INCYTE CORPORATION
Reel/Frame 033016/0103 →
Continuity (3)
Continuation 14097588 · Dec 5, 2013
Continuation 12137892 · Jun 12, 2008
Provisional Application 60943705 · Jun 13, 2007