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Last Updated: December 13, 2025

Claims for Patent: 10,610,530


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Summary for Patent: 10,610,530
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-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.
Inventor(s):Hui-Yin Li, James D. Rodgers
Assignee: Incyte Corp , Incyte Holdings Corp
Application Number:US16/003,210
Patent Claims: 1. A method of inhibiting JAK1 and/or JAK2 in a patient suffering from an autoimmune skin disease, 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-cyclopentylpropanenitrile phosphoric acid salt.

2. The method of claim 1, wherein said autoimmune skin disease is bullous skin disorder.

3. The method of claim 2, wherein said bullous skin disorder is pemphigus vulgaris (PV) or bullous pemphigoid (BP).

4. The method of claim 3, wherein said bullous skin disorder is pemphigus vulgaris (PV).

5. The method of claim 1, wherein the autoimmune skin disease is atopic dermatitis, psoriasis, skin sensitization, skin irritation, skin rash, contact dermatitis, or allergic contact sensitization.

6. The method of claim 5, wherein the autoimmune skin disease is psoriasis.

7. The method of claim 5, wherein the autoimmune skin disease is atopic dermatitis.

8. 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.

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

10. A method of treating an autoimmune skin disease selected from pemphigus vulgaris (PV), bullous pemphigoid (BP), atopic dermatitis, and psoriasis in a patient, 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-cyclopentylpropanenitrile phosphoric acid salt, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

11. The method of claim 10, wherein the autoimmune skin disorder is pemphigus vulgaris (PV) or bullous pemphigoid (BP).

12. The method of claim 10, wherein the autoimmune skin disorder is pemphigus vulgaris (PV).

13. The method of claim 10, wherein the autoimmune skin disease is psoriasis.

14. The method of claim 10, wherein the autoimmune skin disease is atopic dermatitis.

15. The method of claim 10, 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.

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

17. A method of treating an autoimmune skin disease selected from pemphigus vulgaris (PV), bullous pemphigoid (BP), atopic dermatitis, and psoriasis in a patient, 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-cyclopentylpropanenitrile phosphoric acid salt and a pharmaceutically acceptable carrier, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

18. The method of claim 17, wherein the autoimmune skin disorder is pemphigus vulgaris (PV).

19. The method of claim 17, wherein the autoimmune skin disease is psoriasis.

20. The method of claim 17, wherein the autoimmune skin disease is atopic dermatitis.

21. The method of claim 17, wherein the pharmaceutical composition is suitable for oral administration.

22. The method of claim 17, wherein the pharmaceutical composition is suitable for topical administration.

23. The method of claim 17, 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.

24. The method of claim 23, wherein said crystalline salt is a 1:1 (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile:phosphoric acid salt.

25. A method of treating atopic dermatitis in a patient, comprising topically 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-cyclopentylpropanenitrile phosphoric acid salt and a pharmaceutically acceptable carrier, wherein said treating refers to ameliorating or inhibiting the disease in a patient.

26. The method of claim 1, wherein said salt is administered topically.

27. The method of claim 10, wherein said salt is administered topically.

28. The method of claim 17, wherein said pharmaceutical composition is administered topically.

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