IP Library Granted Patent US 10,155,737
Granted Patent B2
US 10,155,737 · App. 15/372,884 · Granted Dec 18, 2018

Benzo-fused heterocyclic derivatives useful as agonists of GPR120

Inventors: Zhihua Sui (Norristown, PA); Nalin Subasinghe (Exton, PA)
Assignee: JANSSEN PHARMACEUTICA NV
C07D307/80C07D231/56C07D263/56C07D277/64C07D307/79C07D307/81C07D307/82C07D307/84C07D333/54C07D333/56C07D401/12C07D405/12C07D493/02C07D493/04
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Quick Facts
Patent No.
US 10,155,737
App. No.
15/372,884
Granted
Dec 18, 2018
Kind
B2
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.

Claims (22)

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2020
From: SUI, ZHIHUA; SUBASINGHE, NALIN
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 054041/0160 →
Continuity (3)
Continuation 14200093 · Mar 7, 2014
Provisional Application 61783118 · Mar 14, 2013
Related Publication 20170088531A1 · Mar 30, 2017