IP Library Granted Patent US 10,370,387
Granted Patent B2
US 10,370,387 · App. 15/874,140 · Granted Aug 6, 2019

Tricyclic fused thiophene derivatives as JAK inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); Wenyu Zhu (Media, PA); Song Mei (Wilmington, DE)
Assignees: Incyte Holdings Corporation; Incyte Corporation
C07D495/14A61K31/437C07D495/12
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Quick Facts
Patent No.
US 10,370,387
App. No.
15/874,140
Granted
Aug 6, 2019
Kind
B2
Abstract

The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) 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 (15)

1. A method of ameliorating or inhibiting an autoimmune disease in a patient, comprising administering to said patient a compound, which is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile monohydrate.

3. The method of claim 1 , wherein the autoimmune disease is multiple sclerosis.

4. The method of claim 1 , wherein the autoimmune disease is rheumatoid arthritis.

5. The method of claim 1 , wherein the autoimmune disease is type I diabetes.

6. The method of claim 1 , wherein the autoimmune disease is lupus.

7. The method of claim 6 , wherein the lupus is systemic lupus erythematosus.

8. The method of claim 1 , wherein the autoimmune disease is Crohn's disease.

9. The method of claim 1 , wherein the autoimmune disease is ulcerative colitis.

10. The method of claim 1 , wherein the autoimmune disease is myasthenia gravis.

11. The method of claim 1 , wherein the autoimmune disease is psoriasis.

12. The method of claim 1 , wherein the autoimmune disease is pemphigus vulgaris.

13. The method of claim 1 , wherein the autoimmune disease is asthma.

14. A method of ameliorating or inhibiting allograft rejection or graft versus host disease in a patient, comprising administering to said patient a compound, which is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl }tetrahydro-2H-pyran-2-yl)acetonitrile, or a pharmaceutically acceptable salt thereof.

15. The method of claim 14 , wherein the compound is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile monohydrate.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 4, 2018
From: LI, YUN-LONG; ZHU, WENYU; MEI, SONG; GLENN, JOSEPH
To: INCYTE CORPORATION
Reel/Frame 045972/0969 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 4, 2018
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 045973/0096 →
Continuity (5)
Continuation 14873078 · Oct 1, 2015
Continuation 14068796 · Oct 31, 2013
Provisional Application 61783850 · Mar 14, 2013
Provisional Application 61721308 · Nov 1, 2012
Related Publication 20180148460A1 · May 31, 2018
Cited By (1)
US 12,280,054