BENZOTHIA(DI)AZEPINE COMPOUNDS AND USE THEREOF AS BILE ACID MODULATORS Russian patent published in 2025 - IPC C07D281/10 A61K31/554 A61P1/16 A61P3/06 A61P5/00 A61P9/00 

Abstract RU 2841263 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a compound selected from the group consisting of (S)-3-(((S)-3-butyl-5-(4-fluorophenyl)-3-methyl-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2-hydroxypropanoic acid; (S)-3-(((R)-3-butyl-5-(4-fluorophenyl)-3-methyl-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2-hydroxypropanoic acid; (R)-3-(((S)-3-butyl-5-(4-fluorophenyl)-3-methyl-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2-hydroxypropanoic acid; (R)-3-(((R)-3-butyl-5-(4-fluorophenyl)-3-methyl-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2-hydroxypropanoic acid; 1-(((3-butyl-3-ethyl-5-(4-fluorophenyl)-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)methyl)cyclopropane-1-carboxylic acid; (S)-1-(((3-butyl-3-ethyl-5-(4-fluorophenyl)-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)methyl)cyclopropane-1-carboxylic acid; (R)-1-(((3-butyl-3-ethyl-5-(4-fluorophenyl)-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)methyl)cyclopropane-1-carboxylic acid; 3-((3-butyl-3-ethyl-5-(4-fluorophenyl)-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2,2-dimethylpropanoic acid; (S)-3-((3-butyl-3-ethyl-5-(4-fluorophenyl)-7-(methylthio)-1,1-dioxido-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)-2,2-dimethylpropanoic acid, and so forth, or a pharmaceutically acceptable salt thereof, which are modulators of bile acids and have the activity of inhibiting apical sodium-dependent bile acid transporter (ASBT) and/or hepatic bile acid transporter (LBAT). Invention also relates to a pharmaceutical composition containing said compounds, and to the use of said compounds as a medicinal agent having apical sodium-dependent bile acid transporter (ASBT) inhibition activity and/or liver bile acid transporter (LBAT), for the treatment of cardiovascular diseases, fatty acid metabolism disorders, gastrointestinal diseases and liver diseases.

EFFECT: benzothia(di)azepine compounds and use thereof as bile acid modulators are disclosed.

7 cl, 8 tbl, 14 ex

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RU 2 841 263 C1

Authors

Gillberg, Per-Goran

Starke Ingemar

Kulkarni Santosh S.

Dates

2025-06-05Published

2021-08-03Filed