BENZOTHIAZEPINE COMPOUNDS AND USE THEREOF AS BILE ACID MODULATORS Russian patent published in 2024 - IPC C07D281/10 A61K31/554 A61P1/16 A61P3/06 A61P3/08 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to 1,5-benzothiazepine derivatives of formula (I). In formula (I): each of R¹ and R² is independently C_1-4 alkyl; R³ is independently selected from the group consisting of hydrogen, halogen, hydroxy, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 alkoxy, C_1-4 haloalkoxy, cyano, nitro, amino, N-(C_1-4 alkyl) amino, N, N-di(C_1-4 alkyl)amino and N-(aryl-C_1-4alkyl)amino; n is integer 1, 2 or 3; R⁴ is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, C_1-4 alkyl, C_3-6 cycloalkyl, C_1-4 alkoxy, C_3-6 cycloalkyloxy, C_1-4 alkylthio, C_3-6 cycloalkylthio, amino, N-(C_1-4 alkyl) amino and N, N-di(C_1-4 alkyl) amino; and each of R^5A, R^5B, R^5C and R^5D is independently selected from the group consisting of hydrogen, halogen, hydroxy, amino, C_1-4 alkyl and C_1-4 alkoxy; or a pharmaceutically acceptable salt thereof, provided that the compound is not racemic 3-((7-bromo-3-butyl-3-ethyl-1,1-dioxide-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepine-8-yl)oxy)propanoic acid. Invention also relates to a pharmaceutical composition containing said compounds and to use of said compounds as a medicinal agent.

EFFECT: disclosed compounds are bile acid modulators having activity of inhibiting apical sodium-dependent bile acid transporter (ASBT) and/or hepatic bile acid transport (LBAT) and can be used in the treatment of cardiovascular diseases, disorders of fatty acid metabolism and glucose utilization, gastrointestinal diseases, and liver diseases.

14 cl, 8 tbl, 52 ex