IP Library Granted Patent US 11,040,980
Granted Patent B2
US 11,040,980 · App. 16/708,340 · Granted Jun 22, 2021

Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors

Inventors: Tim Owens (San Carlos, CA); Erik Verner (Belmont, CA)
Assignee: Principia Biopharma Inc.
C07D487/04A61K9/0053A61K31/495A61K31/506A61K31/519A61K31/5377A61K45/06C07D401/14C07D403/12C07D405/12C07D519/00
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Quick Facts
Patent No.
US 11,040,980
App. No.
16/708,340
Granted
Jun 22, 2021
Kind
B2
Abstract

The present disclosure provides compounds of Formula (IA), such as, e.g., (R)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile having the chemical structure and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

Claims (20)

1. A method for treating a disease in a patient in recognized need thereof, wherein the disease is selected from the group consisting of autoimmune hepatitis, Behcet's disease, Graves' disease, multiple sclerosis, nephritis, pancreatitis, primary biliary cirrhosis, and ulcerative colitis, comprising administering to the patient in recognized need thereof a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of a compound selected from the group consisting of:

and/or a pharmaceutically acceptable salt and/or individual (E)-stereoisomer or (Z)-stereoisomer of any of the above compounds.

2. The method of claim 1 , wherein the disease is autoimmune hepatitis.

3. The method of claim 1 , wherein the disease is Behcet's disease.

4. The method of claim 1 , wherein the disease is Graves' disease.

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

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

7. The method of claim 1 , wherein the disease is pancreatitis.

8. The method of claim 1 , wherein the disease is primary biliary cirrhosis.

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

10. A method for treating a disease in a patient in recognized need thereof, wherein the disease is selected from the group consisting of autoimmune hepatitis, Behcet's disease, Graves' disease, multiple sclerosis, nephritis, pancreatitis, primary biliary cirrhosis, and ulcerative colitis, comprising administering to the patient in recognized need thereof a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of:

and/or a pharmaceutically acceptable salt thereof.

11. The method of claim 10 , wherein the disease is autoimmune hepatitis.

12. The method of claim 10 , wherein the disease is Behcet's disease.

13. The method of claim 10 , wherein the disease is Graves' disease.

14. The method of claim 10 , wherein the disease is multiple sclerosis.

15. The method of claim 10 , wherein the disease is nephritis.

16. The method of claim 10 , wherein the disease is pancreatitis.

17. The method of claim 10 , wherein the disease is primary biliary cirrhosis.

18. The method of claim 10 , wherein the disease is ulcerative colitis.

Assignments (2)
ASSIGNEE CHANGE OF ADDRESS Recorded Sep 16, 2025
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 072881/0270 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2021
From: OWENS, TIM; VERNER, ERIK
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 056241/0931 →
Continuity (7)
Continuation 15978041 · May 11, 2018
Continuation 14997330 · Jan 15, 2016
Continuation 14374788
Provisional Application 61782605 · Mar 14, 2013
Provisional Application 61728693 · Nov 20, 2012
Provisional Application 61699038 · Sep 10, 2012
Related Publication 20200190092A1 · Jun 18, 2020
Cited By (3)
US 12,336,999 US 12,410,176 US 12,673,953