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Details for Patent: 9,376,439

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Details for Patent: 9,376,439

Title:Salts of the janus kinase inhibitor (R)-3(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylp- ropanenitrile
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) Incyte Holdings Corporation (Wilmington, DE)
Filing Date:May 06, 2014
Application Number:14/270,915
Claims:1. A method of treating a cancer selected from the group consisting of breast cancer, Castleman's disease, pancreatic cancer, and leukemia in a patient in need thereof, comprising administering to said patient a therapeutically 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, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

2. The method of claim 1, wherein the cancer is pancreatic cancer.

3. The method of claim 1, wherein the cancer is breast cancer.

4. The method of claim 1, wherein the cancer is leukemia.

5. The method of claim 4, wherein the cancer is chronic myelogenous leukemia (CML).

6. The method of claim 4, wherein the cancer is acute myelogenous leukemia (AML).

7. The method of claim 4, wherein the cancer is acute lymphoblastic leukemia (ALL).

8. The method of claim 4, wherein the cancer is chronic myelomonocytic leukemia (CMML).

9. 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.

10. The method of claim 9, 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.

11. A method of treating a cancer selected from the group consisting of breast cancer, Castleman's disease, pancreatic cancer, and leukemia in a patient in need thereof, comprising administering to said patient a therapeutically 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, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

12. The method of claim 11, wherein the cancer is pancreatic cancer.

13. The method of claim 11, wherein the cancer is breast cancer.

14. The method of claim 11, wherein the cancer is leukemia.

15. The method of claim 14, wherein the cancer is chronic myelogenous leukemia (CML).

16. The method of claim 14, wherein the cancer is acute myelogenous leukemia (AML).

17. The method of claim 14, wherein the cancer is acute lymphoblastic leukemia (ALL).

18. The method of claim 14, wherein the cancer is chronic myelomonocytic leukemia (CMML).

19. The method of claim 11, wherein the pharmaceutical composition is suitable for oral administration.

20. The method of claim 11, wherein the pharmaceutical composition is in tablet form.

21. The method of claim 11, 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.

22. The method of claim 21, 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.

23. A method of treating cachexia in a patient in need thereof, comprising administering to said patient a therapeutically 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, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

24. The method of claim 23, wherein the cachexia results from or is associated with cancer.

25. The method of claim 23, 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 23, 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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