IP Library Granted Patent US 11,214,573
Granted Patent B2
US 11,214,573 · App. 16/682,523 · Granted Jan 4, 2022

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 Holdings Corporation; Incyte Corporation
C07D487/04A61K31/506A61P29/00A61P35/00A61P35/02A61P35/04A61P37/06C07D471/04
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Quick Facts
Patent No.
US 11,214,573
App. No.
16/682,523
Granted
Jan 4, 2022
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 (23)

1. A method of inhibiting or ameliorating a disorder selected from myelofibrosis, polycythemia vera (PV), essential thrombocythemia (ET), multiple myeloma, pancreatic cancer, breast cancer, lung cancer, colorectal cancer, rheumatoid arthritis, lymphoma, leukemia, cachexia, Castleman's disease, graft versus host disease and allograft rejection in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of 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. The method of claim 1 , wherein the disorder is myelofibrosis.

3. The method of claim 1 , wherein the disorder is polycythemia vera (PV).

4. The method of claim 1 , wherein the disorder is essential thrombocythemia (ET).

5. The method of claim 2 , wherein the myelofibrosis is post polycythemia vera myelofibrosis (Post-PV MF).

6. The method of claim 2 , wherein the myelofibrosis is post essential thrombocythemia myelofibrosis (Post-ET MF).

7. The method of claim 1 , wherein the disorder is multiple myeloma.

8. The method of claim 1 , wherein the disorder is pancreatic cancer.

9. The method of claim 1 , wherein the disorder is breast cancer.

10. The method of claim 1 , wherein the disorder is lung cancer.

11. The method of claim 1 , wherein the disorder is colorectal cancer.

12. The method of claim 1 , wherein the disorder is rheumatoid arthritis.

13. The method of claim 1 , wherein the disorder is lymphoma.

14. The method of claim 1 , wherein the disorder is leukemia.

15. The method of claim 14 , wherein the leukemia is acute myelogenous leukemia.

16. The method of claim 14 , wherein the leukemia is acute lymphoblastic leukemia.

17. The method of claim 14 , wherein the leukemia is chronic myelogenous leukemia (CML).

18. The method of claim 14 , wherein the leukemia is chronic myelomonocytic leukemia (CMML).

19. The method of claim 1 , wherein the disorder is cachexia.

20. The method of claim 19 , wherein the cachexia results from or is associated with cancer.

21. The method of claim 1 , wherein the disorder is Castleman's disease.

22. The method of claim 1 , wherein the disorder is allograft rejection.

23. The method of claim 1 , wherein the disorder is graft versus host disease.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2020
From: YAO, WENQING; BURNS, DAVID M.; ZHUO, JINCONG
To: INCYTE CORPORATION
Reel/Frame 053341/0956 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2020
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 053342/0001 →
Continuity (7)
Continuation 15435735 · Feb 17, 2017
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 20200079783A1 · Mar 12, 2020
Cited By (3)
US 12,428,426 US 12,440,495 US 12,479,851