IP Library Granted Patent US 9,856,261
Granted Patent B2
US 9,856,261 · App. 15/229,267 · Granted Jan 2, 2018

Piperidine inhibitors of Janus kinase 3

Inventors: Tadimeti Rao (San Diego, CA); Chengzhi Zhang (San Diego, CA)
Assignee: Auspex Pharmaceuticals, Inc.
C07D487/04A61K31/519C07B2200/05Y02P20/55
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Quick Facts
Patent No.
US 9,856,261
App. No.
15/229,267
Granted
Jan 2, 2018
Kind
B2
Abstract

The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

Claims (38)

1. A compound that is

or a pharmaceutically acceptable salt thereof;

wherein each position represented as D has deuterium enrichment of no less than about 10%.

2. The compound of claim 1 , wherein each position represented as D has deuterium enrichment of no less than about 50%.

3. The compound of claim 1 , wherein each position represented as D has deuterium enrichment of no less than about 90%.

4. The compound of claim 1 , wherein each position represented as D has deuterium enrichment of no less than about 98%.

5. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

6. The compound of claim 1 that is

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 6 , wherein each position represented as D has deuterium enrichment of no less than about 50%.

8. The compound of claim 6 , wherein each position represented as D has deuterium enrichment of no less than about 90%.

9. The compound of claim 6 , wherein each position represented as D has deuterium enrichment of no less than about 98%.

10. A pharmaceutical composition comprising a compound of claim 6 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

11. The compound of claim 1 that is

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 11 , wherein each position represented as D has deuterium enrichment of no less than about 50%.

13. The compound of claim 11 , wherein each position represented as D has deuterium enrichment of no less than about 90%.

14. The compound of claim 11 , wherein each position represented as D has deuterium enrichment of no less than about 98%.

15. A pharmaceutical composition comprising a compound of claim 11 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

16. The compound of claim 1 that is

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 16 , wherein each position represented as D has deuterium enrichment of no less than about 50%.

18. The compound of claim 16 , wherein each position represented as D has deuterium enrichment of no less than about 90%.

19. The compound of claim 16 , wherein each position represented as D has deuterium enrichment of no less than about 98%.

20. A pharmaceutical composition comprising a compound of claim 16 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

21. A pharmaceutical composition comprising a compound that is

or a combination thereof;

or a pharmaceutically acceptable salt thereof;

together with a pharmaceutically acceptable carrier;

wherein each position represented as D has deuterium enrichment of no less than about 10%.

22. A method of treating a disorder in a patient wherein the disorder is renal transplant rejection, rheumatoid arthritis, psoriasis, inflammatory bowel disease, dry eye syndrome, asthma, or transplant rejection comprising administering to the patient therapeutically effective amount of a compound of claim 1 .

23. The method of claim 22 , wherein the disorder is renal transplant rejection.

24. The method of claim 22 , wherein the disorder is rheumatoid arthritis.

25. The method of claim 22 , wherein the disorder is psoriasis.

26. The method of claim 22 , wherein the disorder is inflammatory bowel disease.

27. The method of claim 22 , wherein the disorder is dry eye syndrome.

28. The method of claim 22 , wherein the disorder is asthma.

29. The method of claim 22 , wherein the disorder is transplant rejection.

Assignments (1)
CHANGE OF ASSIGNEE ADDRESS Recorded Feb 2, 2021
From: AUSPEX PHARMACEUTICALS, INC.
To: AUSPEX PHARMACEUTICALS, INC.
Reel/Frame 055193/0866 →
Continuity (6)
Continuation 14596784 · Jan 14, 2015
Division 13627747 · Sep 26, 2012
Division 12763858 · Apr 20, 2010
Provisional Application 61170858 · Apr 20, 2009
Provisional Application 61300887 · Feb 3, 2010
Related Publication 20160340361A1 · Nov 24, 2016