CARBOXYL- OR HYDROXYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES Russian patent published in 2013 - IPC C07D401/14 C07D401/04 C07D235/12 C07D401/12 A61K31/4184 A61K31/4427 A61P3/10 A61P25/16 A61P25/28 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I), or pharmaceutically acceptable salts thereof, where R¹ is selected from and , R² is hydrogen; R³ is cyclohexyl or bicyclo[2.2.1]heptyl; R⁴ is phenyl, which is substituted in the 4th position with a halogen or a lower fluoroalkyl, or a pyridyl, which is substituted with 1 or 2 substitutes independently selected from halogen and a lower alkoxy group; R⁵ and R⁶ independently denote hydrogen or fluorine; R⁷ and R⁹ are independently selected from a group consisting of hydrogen, lower alkyl, halogen, lower alkoxy group, lower fluoroalkyl, lower fluoroalkoxy group and cyano group; R⁸ is -(CR¹²R¹³)_n-COOH, where n equals 0, 1 or 2, and R¹² and R¹³ are independently hydrogen or lower alkyl, or -O-(CR¹⁴R¹⁵)_p-COOH, where p equals 1 or 2, and R¹⁴ and R¹⁵ are independently hydrogen or lower alkyl, or R¹⁴ and R¹⁵ together with the carbon atom with which they are bonded form a cycloalkyl ring, or R⁸ is tetrazole; R¹⁰ is a hydroxy group or -(CH₂)_p-COOH, where p equals 0 or 1; m equals 0 or 1; R¹¹ is -COOH. The invention also relates to specific carboxyl- or hydroxyl-substituted benzimidazole derivatives and a pharmaceutical composition based on a compound of formula (I).

EFFECT: novel carboxyl- or hydroxyl-substituted benzimidazole derivatives, having selective activity with respect to farnesoid X receptor, are obtained.

26 cl, 126 ex