Intestine-specific partial agonists of farnesoid X receptor and uses thereof
AssigneeEWHA DrugDesignHouse Co.,Ltd.
InventorsDae-Kee Kim, Soyeon Shim
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Abstract
An intestine-specific partial agonists of farnesoid X receptor (FXR) is disclosed, along with methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with FXR activity.
Claims6
A compound of the formula (I):
- wherein:
- R1 is H or F;
- R2 is CN;
- R3 is F;
- and R4 is Me, Et, i-Pr, or cyclopropyl;
- or a pharmaceutically acceptable salt or a solvate thereof.
(E)-3-(3-((2-cyano-4′-dimethylaminobiphenyl-4-ylmethyl)cyclohexanecarbonylamino)-5-fluorophenyl)acrylic acid methyl ester, or a pharmaceutically acceptable salt or a solvate thereof.
A method for treating, preventing, or reducing a disease in human selected from the group consisting of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), cholestasis, nonalcoholic steatohepatitis (NASH), nonalcoholic fatty liver disease (NAFLD), necrotizing enterocolitis, gastritis, ulcerative colitis, Crohn's disease, inflammatory bowel disease, irritable bowel syndrome, gastroenteritis, radiation-induced enteritis, pseudomembranous colitis, chemotherapy-induced enteritis, gastro-esophageal reflux disease (GERD), non-ulcer dyspepsia (NUD), celiac disease, intestinal celiac disease, post-surgical inflammation, gastric carcinogenesis, or any combination thereof.
Dependencies are inferred from the claim text.