Gpr120 agonists for the treatment of inflammatory bowel disease

Patent metadata

Field	Value
Publication number	US-2025177329-A1
Application number	US-202318843373-A
Country	US
Kind code	A1
Filing date	Mar 3, 2023
Priority date	Mar 3, 2022
Publication date	Jun 5, 2025
Grant date	—

Abstract

The present invention relates to GPR120 agonists for use in the treatment of inflammatory bowel disease, in particular ulcerative colitis or Crohn's disease.

First claim

1 . A method for preventing or treating inflammatory bowel disease in an individual, the method comprising administering to the individual a GPR120 agonist of formula (I):

wherein:
R 1 is CH 3 ,
R 2 is H,
R 3 is selected from F, Cl and CF 3 ,
or
R 1 and R 2 are independently selected from substituted or unsubstituted phenyl or thiophen and H, provided that at least one of R 1 or R 2 is H, and
R 3 is F.

2 . The method of claim 1 , wherein the GPR120 agonist is selected from:
7-(3-(N-(4-fluoro-2,6-dimethylphenyl)sulfamoyl)phenyl)heptanoic acid, 7-(3-(N-(4-chloro-2,6-dimethylphenyl)sulfamoyl)phenyl)heptanoic acid, 7-(3-(N-(4-trifluoromethyl-2,6-dimethyl-phenyl)sulfamoyl)phenyl)heptanoic acid, 7-(3-(N-(6-fluoro-4-methyl-[1,1′-biphenyl]-3-yl)sulfamoyl)phenyl)heptanoic acid, 7-(3-{[4-fluoro-2-methyl-5-(thiophen-2-yl)phenyl]sulfamoyl}phenyl)heptanoic acid, and 7-(3-(N-(5-fluoro-3-methyl-[1,1′-biphenyl]-2-yl)sulfamoyl)phenyl)heptanoic acid.

3 . The method of claim 1 , wherein the GPR120 agonist, is 7-(3-(N-(4-chloro-2,6-dimethylphenyl)sulfamoyl)phenyl)heptanoic acid.

4 . The method of claim 1 , wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease.

5 . The method of any one of claim 1 , wherein said GPR120 agonist is administered orally.

6 . The method of claim 1 , wherein said GPR120 agonist is administered in a pharmaceutical composition that is not a controlled release formulation and/or gastro-resistant formulation.

7 . The method of claim 1 , wherein said GPR120 agonist is comprised within a pharmaceutical composition that further comprises at least one inert pharmaceutically acceptable excipient.

8 . The method of claim 7 , wherein the pharmaceutical composition is administered orally.

9 . A GPR120 agonist which is 7-(3-{[4-fluoro-2-methyl-5-(thiophen-2-yl)phenyl]sulfamoyl}phenyl)heptanoic acid.

10 . A pharmaceutical composition comprising the GPR120 agonist of claim 9 and at least one inert pharmaceutically acceptable excipient.

11 . The method of claim 1 , wherein when said phenyl or thiophen is substituted, the substituent is selected from Cl, F, and CH3.

12 . The method of claim 1 , wherein when said phenyl or thiophen is substituted, the substituent is present in position 2, 3, or 4 of the phenyl or is present in position 3, 4, or 5 on the thiophen.

Assignees

• Dompe Farm Spa

Inventors

• Allegretti Marcello
• Aramini Andrea
• Bianchini Gianluca
• D'Alessio Silvia
• Cypriano Dutra Rafael

Classifications

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61P1/00

  Drugs for disorders of the alimentary tract or the digestive system · CPC title

• C07D333/02

  not condensed with other rings · CPC title

• A61K31/381

  having five-membered rings · CPC title

• A61K31/145 Primary

  having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2) (isothiourea A61K31/155) · CPC title