IP Library Granted Patent US 9,814,722
Granted Patent B2
US 9,814,722 · App. 15/233,652 · Granted Nov 14, 2017

Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as janus kinase inhibitors

Inventors: James D. Rodgers (Landenberg, PA); Stacey Shepard (Wilmington, DE)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/519A61K9/0014A61K9/0053A61K9/20A61K31/573A61K45/06C07B59/002C07D417/04C07D471/04C07D487/04C07B2200/05
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Quick Facts
Patent No.
US 9,814,722
App. No.
15/233,652
Granted
Nov 14, 2017
Kind
B2
Abstract

The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases 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 (30)

1. A method of treating a disease selected from allograft rejection and graft versus host disease in a patient in need thereof, comprising administering to the patient a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.

3. The method of claim 2 , wherein the disease is graft versus host disease.

4. The method of claim 3 , wherein about 5 to about 1000 mg of the compound, or pharmaceutically acceptable salt thereof, is administered to the patient.

5. The method of claim 3 , further comprising administering to the patient at least one additional therapeutic agent.

6. The method of claim 5 , wherein the therapeutic agent is administered to a patient simultaneously or sequentially.

7. The method of claim 5 , wherein said therapeutic agent is an immunosuppressant.

8. The method of claim 5 , wherein said therapeutic agent is a steroid.

9. The method of claim 5 , wherein said therapeutic agent is a corticosteroid.

10. The method of claim 9 , wherein said corticosteroid is dexamethasone or prednisone.

11. The method of claim 9 , wherein said corticosteroid is dexamethasone.

12. The method of claim 9 , wherein said corticosteroid is prednisone.

13. The method of claim 2 , wherein the disease is allograft rejection.

14. The method of claim 13 , wherein about 5 to about 1000 mg of the compound, or pharmaceutically acceptable salt thereof, is administered to the patient.

15. The method of claim 13 , further comprising administering to the patient at least one additional therapeutic agent.

16. The method of claim 15 , wherein the therapeutic agent is administered to a patient simultaneously or sequentially.

17. The method of claim 15 , wherein said therapeutic agent is an immunosuppressant.

18. The method of claim 15 , wherein said therapeutic agent is a steroid.

19. The method of claim 15 , wherein said therapeutic agent is a corticosteroid.

20. The method of claim 19 , wherein said corticosteroid is dexamethasone or prednisone.

21. The method of claim 19 , wherein said corticosteroid is dexamethasone.

22. The method of claim 19 , wherein said corticosteroid is prednisone.

23. A method of treating a disease selected from allograft rejection and graft versus host disease in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a therapeutically effective amount of a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.

24. The method of claim 23 , wherein the compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.

25. The method of claim 24 , wherein the pharmaceutical composition is suitable for oral administration.

26. The method of claim 25 , wherein the pharmaceutical composition is in tablet form.

27. The method of claim 26 , wherein the disease is graft versus host disease.

28. The method of claim 26 , wherein the disease is allograft rejection.

29. The method of claim 24 , wherein the disease is graft versus host disease.

30. The method of claim 24 , wherein the disease is allograft rejection.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 15, 2016
From: RODGERS, JAMES D.; SHEPARD, STACEY
To: INCYTE CORPORATION
Reel/Frame 039434/0803 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 15, 2016
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 039434/0910 →
Continuity (13)
Continuation 15173057 · Jun 3, 2016
Continuation 14711576 · May 13, 2015
Continuation 14274948 · May 12, 2014
Continuation 14020505 · Sep 6, 2013
Division 13076220 · Mar 30, 2011
Continuation 12549170 · Aug 27, 2009
Continuation 11637545 · Dec 12, 2006
Provisional Application 60859404 · Nov 16, 2006
Provisional Application 60856872 · Nov 3, 2006
Provisional Application 60850625 · Oct 10, 2006
Provisional Application 60810231 · Jun 2, 2006
Provisional Application 60749905 · Dec 13, 2005
Related Publication 20160346286A1 · Dec 1, 2016