3-AMINOPYRIDINES AS GPBAR1 AGONISTS Russian patent published in 2016 - IPC C07D213/75 C07D213/82 C07D401/04 C07D401/12 C07D401/14 C07D405/04 C07D405/12 C07D413/04 C07D413/12 C07D417/04 C07D417/12 C07D491/107 A61K31/4418 A61K31/4433 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

,

where B¹ represents CR⁷ or N; B² is CR⁸ or N; R¹ is selected from group consisting of phenyl, which is unsubstituted or substituted by one, two or three groups; heteroaryl, which is 5-6-member ring, which may include one or two nitrogen atoms, which is unsubstituted or substituted; 3,6-dihydro-2H-pyran-4-yl, and piperidinyl substituted with C_1-7-alkyl groups in amount of one to four; R² is selected from group consisting of hydrogen atom, C_1-7-alkyl, halogen atoms, cyano, C_1-7-alkoxy, amino, C_1-7-alkylamino, C_1-7-alkoxy-C_1-7-alkyl-(C_1-7-alkyl)amino, and heteroaryl; R^2a is selected from group consisting of hydrogen atom, methyl and halogen atom; R³ is selected from group consisting of C_1-7-alkyl, halogen-C-_1-7-alkyl, hydroxy-C-_1-7-alkyl, C_1-7-alkoxy-C_1-7-alkyl, C_1-7-alkylcarbonyl-C_1-7-alkyl, carboxyl-C-_1-7-alkyl, C_1-7-alkoxycarbonyl-C-_1-7-alkyl, cyano-C-_1-7-alkyl, aminocarbonyl-C-_1-7 ^_alkyl, C_1-7-alkylaminokarbonyl-C-_1-7-alkyl, di-C_1-7-alkylaminokarbonyl-C-_1-7-alkyl, C_1-7-alkylsulphonyl-C-_1-7-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C-_1-7-alkyl, unsubstituted heterocyclyl, heterocyclyl-C-_1-7-alkyl, where heterocyclyl is unsubstituted or substituted with one or two groups, selected from C_1-7-alkyl, and represents 4-6-member ring which can contain one oxygen atom, heteroaryl-C-_1-7-alkyl, where heteroaryl is unsubstituted or substituted with one or two groups, selected from C_1-7-alkyl, and phenyl-C-_1-7-alkoxycarbonylamino-C-_1-7-alkyl; R⁴ is selected from group consisting of hydrogen atom and halogen atom; R⁵ and R⁶ are selected independently from each other from group consisting of hydrogen atom, C_1-7-alkyl, C_1-7-cycloalkyl, halogen atom, halogen-C-_1-7-alkyl, halogen-C-_1-7-alkoxy, hydroxy, hydroxy-C-_1-7-alkyl, C_1-7-alkoxy, cyano, carboxyl, C_1-7-alkoxycarbonyl, C_1-7-alkoxycarbonyl-C-_1-7-alkyl, hydroxy-C-_1-7-alkoxy, C_1-7-alkoxy-C_1-7-alkoxy, C_1-7-alkylsulfonyl, hydroxy-C-_1-7-alkylsulfonyl, C_1-7-alkoxy-C_1-7-alkylsulfonyl, C_1-7-alkylsulfonyl, hydroxy-C-_1-7-alkylsulfonyl, C_1-7-alkoxy-C_1-7-alkylsulfonyl, carboxyl-C-_1-7-alkylsulfonyl, carboxyl-C-_1-7-alkylsulfonyl, C_1-7-alkoxycarbonyl-C-_1-7-alkylsulfonyl, C_1-7-alkoxycarbonyl-C-_1-7-alkylsulfonyl, C_1-7-alkoxykarbonylamino-C-_1-7-alkylsulfonyl, carboxyl-C-_1-7-alkyl-aminocarbonyl-C-_1-7-alkylsulfonyl, carboxyl-C-_1-7-alkyl-aminocarbonyl-C-_1-7alkylsulfonyl, heterocyclilsulfonyl, where it is unsubstituted or substituted by C_1-7-alkoxycarbonyl, heterocyclilsulfonyl, besides R⁸ is selected from group consisting of hydrogen atom, C_1-7-alkyl, halogen atom, halogen-C-_1-7-alkyl and C_1-7-alkoxy; as well as to their pharmaceutically acceptable salts.

EFFECT: said compounds are agonists of 1 bile acid receptor interfaced with G protein (GPBAR1; G protein coupled bile acid receptor), and can be used as medicinal agents for treating diabetes, in particular diabetes type 2.

22 cl, 5 tbl, 323 ex