IP Library Granted Patent US 8,604,043
Granted Patent B2
US 8,604,043 · App. 12/785,057 · Granted Dec 10, 2013

3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); James D. Rodgers (Landenberg, PA)
Assignee: Incyte Corporation
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,604,043
App. No.
12/785,057
Granted
Dec 10, 2013
Kind
B2
Abstract

The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.

Claims (20)

1. A compound, which is 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile, or a pharmaceutically acceptable salt thereof.

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

3. The compound of claim 1 , which is (3S)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile, or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , which is 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile phosphoric acid salt.

5. The compound of claim 1 , which is (3R)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile phosphoric acid salt.

6. The compound of claim 1 , which is (3S)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile phosphoric acid salt.

7. A compound, which is 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, or a pharmaceutically acceptable salt thereof.

8. The compound of claim 7 , which is (3R)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, or a pharmaceutically acceptable salt thereof.

9. The compound of claim 7 , which is (3S)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, or a pharmaceutically acceptable salt thereof.

10. The compound of claim 7 , which is 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile phosphoric acid salt.

11. The compound of claim 7 , which is (3R)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile phosphoric acid salt.

12. The compound of claim 7 , which is (3S)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile phosphoric acid salt.

13. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

14. The composition of claim 13 which is suitable for topical administration.

15. The composition of claim 13 which is suitable for transdermal administration.

16. The composition of claim 14 which is in the form of a transdermal patch, ointment, lotion, cream, or gel.

17. A composition comprising a compound according to claim 7 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

18. The composition of claim 17 which is suitable for topical administration.

19. The composition of claim 17 which is suitable for transdermal administration.

20. The composition of claim 19 which is in the form of a transdermal patch, ointment, lotion, cream, or gel.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE OMMISSION OF SECOND RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 035292 FRAME: 0004. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 2, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 036054/0696 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION AND INCYTE CORPORATION
Reel/Frame 035924/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 9, 2010
From: LI, YUN-LONG; RODGERS, JAMES D.
To: INCYTE CORPORATION
Reel/Frame 024510/0830 →
Continuity (2)
Provisional Application 61180582 · May 22, 2009
Related Publication 20100298355A1 · Nov 25, 2010