IP Library Granted Patent US 10,695,337
Granted Patent B2
US 10,695,337 · App. 15/995,323 · Granted Jun 30, 2020

Piperidin-4-yl azetidine derivatives as JAK1 inhibitors

Inventors: Taisheng Huang (Wilmington, DE); Chu-Biao Xue (Hockessin, DE)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/4545A61K9/0014A61K9/0019A61K9/0024A61K9/0048A61K31/519A61P1/00A61P11/00A61P11/06A61P17/04A61P27/02A61P35/00C07D401/14C07D405/14C07D487/04C07B2200/13C07D471/04C07D519/00
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Quick Facts
Patent No.
US 10,695,337
App. No.
15/995,323
Granted
Jun 30, 2020
Kind
B2
Abstract

The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Claims (14)

1. A method of ameliorating or inhibiting a skin disorder in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound, which is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, wherein said skin disorder is selected from atopic dermatitis, skin sensitization, skin irritation, skin rash, contact dermatitis, and allergic contact sensitization.

2. The method of claim 1 , wherein said pharmaceutically acceptable salt is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

3. The method of claim 1 , wherein the skin disorder is atopic dermatitis.

4. The method of claim 1 , wherein the skin disorder is skin sensitization.

5. The method of claim 1 , wherein the skin disorder is skin irritation.

6. The method of claim 1 , wherein the skin disorder is skin rash.

7. The method of claim 1 , wherein the skin disorder is contact dermatitis.

8. The method of claim 1 , wherein the skin disorder is allergic contact sensitization.

9. The method of claim 2 , wherein the skin disorder is atopic dermatitis.

10. The method of claim 2 , wherein the skin disorder is skin sensitization.

11. The method of claim 2 , wherein the skin disorder is skin irritation.

12. The method of claim 2 , wherein the skin disorder is skin rash.

13. The method of claim 2 , wherein the skin disorder is contact dermatitis.

14. The method of claim 2 , wherein the skin disorder is allergic contact sensitization.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2019
From: HUANG, TAISHENG; XUE, CHU-BIAO; LI, HUI-YIN; LI, QUN; WANG, ANLAI; KONG, LINGQUAN; YE, HAI FEN; YAO, WENQING; RODGERS, JAMES D.; SHEPARD, STACEY; WANG, HAISHENG; SHAO, LIXIN
To: INCYTE CORPORATION
Reel/Frame 048675/0576 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2019
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 048675/0791 →
Continuity (6)
Continuation 15288641 · Oct 7, 2016
Continuation 14289121 · May 28, 2014
Division 13043986 · Mar 9, 2011
Provisional Application 61312588 · Mar 10, 2010
Provisional Application 61415602 · Nov 19, 2010
Related Publication 20180353499A1 · Dec 13, 2018
Cited By (4)
US 12,428,426 US 12,440,495 US 12,473,272 US 12,479,851