Cot modulators and methods of use thereof

Patent metadata

Field	Value
Publication number	US-9878995-B2
Application number	US-201715429086-A
Country	US
Kind code	B2
Filing date	Feb 9, 2017
Priority date	Jul 6, 2015
Publication date	Jan 30, 2018
Grant date	Jan 30, 2018

Abstract

The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

First claim

The invention claimed is:

1. A compound having the formula:

or a pharmaceutically acceptable salt thereof.

2. A composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method of treating a disease or condition selected from diversion colitis, ischemic colitis, infectious colitis, chemical colitis, microscopic colitis, atypical colitis, pseudomembranous colitis, fulminant colitis, autistic enterocolitis, indeterminate colitis, Behçet's disease, gastroduodenal Crohn's disease, jejunoileitis, ileitis, ileocolitis, Crohn's (granulomatous) colitis, irritable bowel syndrome, mucositis, radiation induced enteritis, short bowel syndrome, celiac disease, stomach ulcers, diverticulitis, pouchitis, proctitis, and chronic diarrhea, in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 2 .

4. A method of treating inflammatory bowel disease in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 2 .

5. A compound having the formula:

or a pharmaceutically acceptable salt thereof.

6. A composition comprising a compound according to claim 5 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

7. A method of treating a disease or condition selected from diversion colitis, ischemic colitis, infectious colitis, chemical colitis, microscopic colitis, atypical colitis, pseudomembranous colitis, fulminant colitis, autistic enterocolitis, indeterminate colitis, Behçet's disease, gastroduodenal Crohn's disease, jejunoileitis, ileitis, ileocolitis, Crohn's (granulomatous) colitis, irritable bowel syndrome, mucositis, radiation induced enteritis, short bowel syndrome, celiac disease, stomach ulcers, diverticulitis, pouchitis, proctitis, and chronic diarrhea, in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 6 .

8. A method of treating inflammatory bowel disease in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 6 .

9. A compound having the formula:

or a pharmaceutically acceptable salt thereof.

10. A composition comprising a compound according to claim 9 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

11. A method of treating a disease or condition selected from diversion colitis, ischemic colitis, infectious colitis, chemical colitis, microscopic colitis, atypical colitis, pseudomembranous colitis, fulminant colitis, autistic enterocolitis, indeterminate colitis, Behçet's disease, gastroduodenal Crohn's disease, jejunoileitis, ileitis, ileocolitis, Crohn's (granulomatous) colitis, irritable bowel syndrome, mucositis, radiation induced enteritis, short bowel syndrome, celiac disease, stomach ulcers, diverticulitis, pouchitis, proctitis, and chronic diarrhea, in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 10 .

12. A method of treating inflammatory bowel disease in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 10 .

13. A compound having the formula:

or a pharmaceutically acceptable salt thereof.

14. A composition comprising a compound according to claim 13 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

15. A method of treating a disease or condition selected from diversion colitis, ischemic colitis, infectious colitis, chemical colitis, microscopic colitis, atypical colitis, pseudomembranous colitis, fulminant colitis, autistic enterocolitis, indeterminate colitis, Behçet's disease, gastroduodenal Crohn's disease, jejunoileitis, ileitis, ileocolitis, Crohn's (granulomatous) colitis, irritable bowel syndrome, mucositis, radiation induced enteritis, short bowel syndrome, celiac disease, stomach ulcers, diverticulitis, pouchitis, proctitis, and chronic diarrhea, in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 14 .

16. A method of treating inflammatory bowel disease in a human patient in need thereof, comprising administering to the patient an effective amount of the composition of claim 14 .

Assignees

• Gilead Sciences Inc

Inventors

• Bacon Elizabeth M
• Balan Gayatri
• Chou Chien-Hung
• Clark Christopher T
• Cottell Jeromy J
• Kim Musong
• Kirschberg Thorsten A
• Link John O
• Phillips Gary
• Schroeder Scott D
• Squires Neil H
• Stevens Kirk L
• Taylor James G
• Watkins William J
• Wright Nathan E
• Zipfel Sheila M

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P9/06

  Antiarrhythmics · CPC title

• A61P43/00

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

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title