Nrf2 regulators

Patent metadata

Field	Value
Publication number	US-10144731-B2
Application number	US-201415105306-A
Country	US
Kind code	B2
Filing date	Dec 17, 2014
Priority date	Dec 18, 2013
Publication date	Dec 4, 2018
Grant date	Dec 4, 2018

Abstract

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

First claim

The invention claimed is:

1. A compound which is 3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or a pharmaceutically acceptable salt thereof.

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

3. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 1 .

4. A compound which is (R)-3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 4 and a pharmaceutically acceptable excipient.

6. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 4 .

7. A compound which is (S)-3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or a pharmaceutically acceptable salt thereof.

8. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 7 .

9. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 7 and a pharmaceutically acceptable carrier or excipient.

10. A compound which is (S)-3-(3-(((R)-4-ethyl-1, 1-dioxide-3,4-dihyrdro-2H-pyrido [2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl) -3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid.

11. A pharmaceutical composition comprising the compound according to claim 10 and a pharmaceutically acceptable excipient.

12. A method of activating Nrf2 in a human in need thererof comprising administering to said human a therapeutically effective amount of the compound according to claim 10 .

Assignees

• Glaxosmithkline Ip Dev Ltd
• Astex Therapeutics Ltd

Inventors

• Davies Thomas Glanmor
• Woolford Alison Jo-Anne
• Willems Hendrika Maria Gerarda
• Norton David
• Heightman Thomas Daniel
• Kerns Jeffrey K

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title