IP Library Granted Patent US 11,117,905
Granted Patent B2
US 11,117,905 · App. 16/467,193 · Granted Sep 14, 2021

Bisaryl heterocycles as NRF2 activators

Inventors: James Francis Callahan (King of Prussia, PA); Roderick S. Davis (King of Prussia, PA); Nicole Cathleen Goodwin (King of Prussia, PA); Jeffrey K. Kerns (King of Prussia, PA)
Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
C07D515/04A61K9/0019A61K9/0053A61K9/0073C07D243/08C07D285/36C07D291/08C07D409/14C07D513/04
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Quick Facts
Patent No.
US 11,117,905
App. No.
16/467,193
Granted
Sep 14, 2021
Kind
B2
Abstract

The present invention relates to bisaryl heterocycle compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to bisaryl heterocycles of Formula (I),

Claims (11)

1. A compound which is (S)-3-(4-(((R)-4-Ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[4,3-b][1,4,5]oxathiazepin-2-yl)methyl)-5-methylthiophen-2-yl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

3. A method of treating COPD which comprises administering to a human in need thereof, a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, according to claim 1 .

4. The method according to claim 3 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered orally.

5. The method according to claim 3 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered intravenously.

6. The method according to claim 3 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered by inhalation.

7. A method of treating heart failure which comprises administering to a human in need thereof, a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, according to claim 1 .

8. The method according to claim 7 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered orally.

9. The method according to claim 7 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered intravenously.

10. The method according to claim 7 wherein the compound, or a pharmaceutically acceptable salt thereof, is administered by inhalation.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2024
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
To: ASTEX THERAPEUTICS LIMITED
Reel/Frame 067952/0915 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 6, 2019
From: KERNS, JEFFREY K.; DAVIS, RODERICK S.; CALLAHAN, JAMES FRANCIS; GOODWIN, NICOLE CATHLEEN
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 049393/0376 →
Continuity (2)
Provisional Application 62434013 · Dec 14, 2016
Related Publication 20200062781A1 · Feb 27, 2020