4-PHENOXY-NICOTANIMIDES OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDES Russian patent published in 2015 - IPC C07D401/06 C07D401/12 C07D401/14 C07D213/82 C07D403/06 C07D417/14 A61K31/44 A61K31/4709 A61K31/498 A61K31/444 A61K31/4545 A61K31/506 A61P3/00 A61P9/00 A61P25/18 A61P25/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I wherein A¹ represents CR¹³; A² represents CR¹⁴ or N; R¹ and R² are independently specified in hydrogen, halogen, and halogen-C_1-7-alkyl; R¹³ and R¹⁴ are independently specified in hydrogen, C_1-7-alkyl, halogen, halogen-C_1-7-alkyl and C_1-7-alkoxy; R³ is specified in hydrogen, C_1-7-alkyl, halogen, C_1-7-alkoxy, piperidinyl and -NR¹⁵R¹⁶, wherein R¹⁵ and R¹⁶ are independently specified in hydrogen, C_1-7-alkyl and C_3-7-cycloalkyl; R⁴ is specified in hydrogen and C_1-7-alkyl; or R³ and R⁴ or R³ and R¹⁴ together represent -X-(CR¹⁷R¹⁸)_n- and form a part of the ring, wherein X is specified in -CR¹⁹R²⁰- and -NR²¹-; R¹⁷, R¹⁸, R¹⁹, R²⁰ are hydrogen; R²¹ is specified in hydrogen, C_1-7-alkyl, C_3-7-cycloalkyl or C_3-7-cycloalkyl-C_1-7-alkyl, wherein C_3-7-cycloalkyl is substituted or not by C_1-7-alkoxycarbonyl, and C_1-7-alkylsulphonyl; and n represents 1, 2 or 3; B¹ represents N or N⁺-O^-; B² represents CR⁷ or N; R⁵, R⁶ and R⁷ are independently specified in hydrogen, halogen and C_1-7-alkyl; and R⁸, R⁹, R¹⁰, R¹¹ and R¹² are those as presented in the patent claim. The compound also refers to pharmaceutically acceptable salts of the compounds of formula I and to pharmaceutical compositions possessing GPBAR1 receptor agonist activity.

EFFECT: compounds of formula I as GPBAR1 agonists.

20 cl, 85 ex