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Claims for Patent: 8,822,481

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Claims for Patent: 8,822,481

Title:Salts of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentyl- propanenitrile 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.
Inventor(s): Rodgers; James D. (Landenberg, PA), Li; Hui-Yin (Hockessin, DE)
Assignee: Incyte Corporation (Wilmington, DE)
Application Number:14/256,383
Patent Claims: 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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile: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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile: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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile: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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile 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-cyclopentyl- propanenitrile:phosphoric acid salt.
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