Novel compounds as diacylglycerol acyltransferase inhibitors

Patent metadata

Field	Value
Publication number	US-2016200736-A1
Application number	US-201614996318-A
Country	US
Kind code	A1
Filing date	Jan 15, 2016
Priority date	May 20, 2011
Publication date	Jul 14, 2016
Grant date	—

Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.

First claim

1 . A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2 . The compound according to claim 1 in free base form.

3 . A pharmaceutical composition comprising the compound or salt according to claim 1 , and a pharmaceutically acceptable carrier.

4 . A pharmaceutical composition comprising the compound according to claim 2 , and a pharmaceutically acceptable carrier.

5 . A method of treating obesity comprising administering to a human in need thereof an effective amount of the compound or salt according to claim 1 .

6 . A method of treating obesity comprising administering to a human in need thereof an effective amount of the compound according to claim 2 .

7 . A method of treating acne comprising administering to a human in need thereof an effective amount of the compound or salt according to claim 1 .

8 . A method of treating acne comprising administering to a human in need thereof an effective amount of the compound according to claim 2 .

9 . The method according to claim 7 wherein the compound is:

10 . The method according to claim 7 wherein the compound is:

11 . The method according to claim 8 wherein the compound is:

12 . The method according to claim 8 wherein the compound is:

13 . A method of treating obesity comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 3 .

14 . A method of treating obesity comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 4 .

15 . A method of treating acne comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 3 .

16 . A method of treating acne comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 4 .

Assignees

• Glaxosmithkline Ip No 2 Ltd

Inventors

• Qin Donghui
• Cheung Mui
• Joshi Hemant
• Tangirala Raghuram
• Bethi Sridhar Reddy

Classifications

• A61P43/00

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

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• C07D519/00 Primary

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title