IP Library Granted Patent US 10,513,522
Granted Patent B2
US 10,513,522 · App. 15/435,735 · Granted Dec 24, 2019

Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors

Inventors: Wenqing Yao (Chadds Ford, PA); David M. Burns (Plymouth Meeting, PA); Jincong Zhuo (Garnet Valley, PA)
Assignees: Incyte Corporation; Incyte Holdings Corporation
C07D487/04C07D471/04
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Quick Facts
Patent No.
US 10,513,522
App. No.
15/435,735
Granted
Dec 24, 2019
Kind
B2
Abstract

The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Claims (25)

1. A compound, which is 5-{3-(cyanomethyl)-3-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]azetidin-1-yl}-N-isopropylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

2. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method of inhibiting an activity of JAK1 comprising contacting JAK1 with a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

4. The method according to claim 3 , wherein said compound, or pharmaceutically acceptable salt thereof, is selective for JAK1 over JAK2.

5. A method of ameliorating or inhibiting an autoimmune diseas in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

6. The method according to claim 5 , wherein the autoimmune disease is a skin disorder.

7. The method according to claim 6 , wherein the skin disorder is atopic dermatitis.

8. The method according to claim 5 , wherein the autoimmune disease is multiple sclerosis.

9. The method according to claim 5 , wherein the autoimmune disease is rheumatoid arthritis.

10. The method according to claim 5 , wherein the autoimmune disease is type I diabetes.

11. The method according to claim 5 , wherein the autoimmune disease is lupus.

12. The method according to claim 5 , wherein the autoimmune disease is inflammatory bowel disease.

13. The method according to claim 5 , wherein the autoimmune disease is Crohn's disease.

14. The method according to claim 5 , wherein the autoimmune disease is myasthenia gravis.

15. The method according to claim 5 , wherein the autoimmune disease is immunoglobulin nephropathies.

16. The method according to claim 5 , wherein the autoimmune disease is myocarditis.

17. The method according to claim 5 , wherein the autoimmune disease is autoimmune thyroid disorder.

18. The method according to claim 6 , wherein the skin disorder is psoriasis.

19. The method according to claim 6 , wherein the skin disorder is skin sensitization.

20. The method according to claim 6 , wherein the skin disorder is skin irritation.

21. The method according to claim 6 , wherein the skin disorder is skin rash.

22. The method according to claim 6 , wherein the skin disorder is contact dermatitis.

23. The method according to claim 6 , wherein the skin disorder is allergic contact sensitization.

24. The method according to claim 5 , wherein the autoimmune disease is psoriatic arthritis.

25. The method according to claim 5 , wherein the autoimmune disease is juvenile arthritis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 13, 2017
From: YAO, WENQING; BURNS, DAVID M.; ZHUO, JINCONG
To: INCYTE CORPORATION
Reel/Frame 042694/0393 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 13, 2017
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 042694/0468 →
Continuity (6)
Continuation 14697236 · Apr 27, 2015
Continuation 14186338 · Feb 21, 2014
Continuation 13526957 · Jun 19, 2012
Provisional Application 61591094 · Jan 26, 2012
Provisional Application 61498942 · Jun 20, 2011
Related Publication 20170253598A1 · Sep 7, 2017
Cited By (4)
US 12,280,054 US 12,428,426 US 12,440,495 US 12,479,851