IP Library Granted Patent US 11,851,442
Granted Patent B2
US 11,851,442 · App. 17/400,861 · Granted Dec 26, 2023

Tricyclic fused thiophene derivatives as JAK inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); Wenyu Zhu (Media, PA); Song Mei (Wilmington, DE); Joseph Glenn (Mount Royal, NJ)
Assignees: Incyte Corporation; Incyte Holdings Corporation
C07D495/14A61K31/437C07D495/12
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Quick Facts
Patent No.
US 11,851,442
App. No.
17/400,861
Granted
Dec 26, 2023
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 (12)

1. A method of ameliorating or inhibiting a myeloproliferative disorder 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, wherein the myeloproliferative disorder is polycythemia vera (PV), myelofibrosis, primary myelofibrosis (PMF), post polycythemia vera myelofibrosis (Post-PV MF), post-essential thrombocythemia myelofibrosis (Post-ET MF), essential thrombocythemia (ET), myelofibrosis with myeloid metaplasia (MMM), hypereosinophilic syndrome (HES), idiopathic myelofibrosis (IMF), or systemic mast cell disease (SMCD).

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 hydrate.

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

4. The method of claim 1 , wherein the myeloproliferative disorder is myelofibrosis.

5. The method of claim 1 , wherein the myeloproliferative disorder is primary myelofibrosis (PMF).

6. The method of claim 1 , wherein the myeloproliferative disorder is post polycythemia vera myelofibrosis (Post-PV MF).

7. The method of claim 1 , wherein said myeloproliferative disorder is post-essential thrombocythemia myelofibrosis (Post-ET MF).

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

9. The method of claim 1 , wherein the myeloproliferative disorder is myelofibrosis with myeloid metaplasia (MMM).

10. The method of claim 1 , wherein the myeloproliferative disorder is hypereosinophilic syndrome (RES).

11. The method of claim 1 , wherein the myeloproliferative disorder is idiopathic myelofibrosis (IMF).

12. The method of claim 1 , wherein the myeloproliferative disorder is systemic mast cell disease (SMCD).

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 26, 2021
From: LI, YUN-LONG; ZHU, WENYU; MEI, SONG; GLENN, JOSEPH
To: INCYTE CORPORATION
Reel/Frame 057298/0819 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 26, 2021
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 057298/0930 →
Continuity (7)
Continuation 16454830 · Jun 27, 2019
Continuation 15874140 · Jan 18, 2018
Continuation 14873078 · Oct 1, 2015
Continuation 14068796 · Oct 31, 2013
Provisional Application 61783850 · Mar 14, 2013
Provisional Application 61721308 · Nov 1, 2012
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