Benzo-fused heterocyclic derivatives useful as agonists of GPR120

Patent metadata

Field	Value
Publication number	US-10155737-B2
Application number	US-201615372884-A
Country	US
Kind code	B2
Filing date	Dec 8, 2016
Priority date	Mar 14, 2013
Publication date	Dec 18, 2018
Grant date	Dec 18, 2018

Abstract

The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

First claim

We claim:

1. A method of treating a disorder modulated by a GPR120 receptor, comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of:
3-{4-[(5-Chloro-2-ethyl-1-benzofuran-7-yl)methoxyl]-2,3-dimethylphenyl}propanoic acid;
3-(2,3-Dimethyl-4-{[2-methyl-5-(trifluoromethoxy)-1-benzofuran-7-yl]methoxy}phenyl)propanoic acid;
3-(7-{[2-Methyl-5-(trifluoromethoxy)-1-benzofuran-7-yl]methoxy}-2,3-dihydro-1H-inden-4-yl)propanoic acid;
3-{4-[(5-Chloro-2-methyl-1-benzofuran-7-yl)methoxyl]-2,3-dimethylphenyl}propanoic acid;
3-{4-[(5-Chloro-2,6-dimethyl-1-benzofuran-7-yl)methoxyl]-2,3-dimethylphenyl}propanoic acid;
3-(4-{[2-(2-Fluoroethenyl)-5-(trifluoromethoxy)-1-benzofuran-7-yl]methoxy}-2,3-dimethylphenyl)propanoic acid;
3-{4-[(6-Chloro-2-methyl-1,3-benzothiazol-4-yl]methoxyl-2,3-dimethylphenyl}propanoic acid;
and pharmaceutically acceptable salts thereof.

2. The method of claim 1 , wherein the disorder modulated by the GPR120 receptor is selected from the group consisting of obesity, obesity related disorders, impaired oral glucose tolerance, insulin resistance, Type II diabetes mellitus, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, and osteoporosis.

3. The method of claim 2 , wherein the disorder modulated by the GPR120 receptor is Type II diabetes mellitus.

4. The method of claim 2 , wherein the disorder modulated by the GPR120 receptor is selected from the group consisting of obesity and dyslipidemia.

5. The method of claim 2 , wherein the disorder modulated by the GPR120 receptor is metabolic syndrome.

6. The method of claim 2 , wherein the disorder modulated by the GPR120 receptor is selected from the group consisting of elevated LDL, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.

7. The method of claim 2 , wherein the obesity related disorder is an obesity related cardiovascular disorder.

8. A method of treating a disorder modulated by a GPR120 receptor, comprising administering to a subject in need thereof a therapeutically effective amount of 3-(2,3-Dimethyl-4-{[2-methyl-5-(trifluoromethoxy)-1-benzofuran-7-yl]methoxy}phenyl)propanoic acid or pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the disorder modulated by the GPR120 receptor is selected from the group consisting of obesity, obesity related disorders, impaired oral glucose tolerance, insulin resistance, Type II diabetes mellitus, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, and osteoporosis.

10. The method of claim 9 , wherein the disorder modulated by the GPR120 receptor is Type II diabetes mellitus.

11. The method of claim 9 , wherein the disorder modulated by the GPR120 receptor is obesity or dyslipidemia.

12. The method of claim 9 , wherein the disorder modulated by the GPR120 receptor is impaired oral glucose tolerance or insulin resistance.

13. The method of claim 9 , wherein the disorder modulated by the GPR120 receptor is selected from the group consisting of obesity related disorders, elevated LDL, elevated triglycerides, obesity induced inflammation, and osteoporosis.

14. The method of claim 9 , wherein the obesity related disorder is an obesity related cardiovascular disorder.

Assignees

• Janssen Pharmaceutica Nv

Inventors

• Sui Zhihua
• Subasinghe Nalin

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P5/50

  for increasing or potentiating the activity of insulin · CPC title

• A61P43/00

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