NEW PHENYLAMIDE OR PYRIDYLAMIDE DERIVATIVES AND USING THEM AS GPBAR1 AGONISTS Russian patent published in 2014 - IPC C07D401/06 C07D401/12 C07D401/14 C07D403/06 C07D405/14 C07D413/06 C07D417/06 C07D471/04 C07D215/08 C07D215/18 C07D213/643 C07D213/65 C07D213/82 C07C233/75 A61K31/455 A61K31/4709 A61P3/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new phenylamide or pyridylamide derivatives of formula

or their acceptable salts, wherein A¹ is CR¹² or N; A² is CR¹³ or N; R¹ and R² are independently specified in hydrogen, C_1-7-alkyl, halogen and C_1-7-alkoxygroup; R¹² and R¹³ are independently specified in hydrogen, C_1-7-alkyl, halogen, C_1-7-alkoxygroup, amino group and C_1-7-alkylsulphanyl; R³ is specified in hydrogen, C_1-7-alkyl, halogen, C_1-7-alkoxygroup, cyano group, C_3-7-cycloalkyl, five-merous heteroaryl and phenyl; R⁴ is specified in methyl and ethyl; or R³ and R⁴ together represent -X-(CR¹⁴R¹⁵)_n- and form a part of the ring, wherein X is specified in -CR¹⁶R¹⁷-, O, S, C=O; R¹⁴ and R¹⁵ are independently specified in hydrogen or C_1-7-alkyl; R¹⁶ and R¹⁷ are independently specified in hydrogen, C_1-7-alkoxycarbonyl, heterocyclyl substituted by two groups specified in a halogen, or R₁₆ and R₁₇ together with an atom C, which they are attached to, form =CH₂ group; or X is specified in a group NR¹⁸; R¹⁴ and R¹⁵ are hydrogen; R¹⁸ is specified in hydrogen, C_1-7-alkyl, halogen-C_1-7-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_1-7-alkyl, heterocyclyl, heteroaryl-C_1-7-alkyl, carboxyl-C_1-7-alkyl, C_1-7-alkoxycarbonyl-C_1-7-alkyl, C_1-7-alkylcarbonyloxy-C_1-7-alkyl, phenyl, wherein phenyl is unsubstituted, phenylcarbonyl, wherein phenyl is substituted by C_1-7-alkoxycarbonyl, and phenylsulphonyl, wherein phenyl is substituted by carboxyl-C_1-7-alkyl, or R¹⁸ and R¹⁴ together represent -(CH₂)₃- and form a part of the ring, or R¹⁸ together with R¹⁴ and R¹⁵ represent -CH=CH-CH= and form a part of the ring; and n has the value of 1, 2 or 3; B¹ represents N or CR¹⁹ and B² represents N or CR²⁰, provided no more than one of B¹ and B² represents N; and R¹⁹ and R²⁰ are independently specified in a group consisting of hydrogen and halogen-C_1-7-alkyl; R⁵ and R⁶ are independently specified in a group consisting of hydrogen, halogen and cyano group; and one-three, provided R⁴ represents methyl or ethyl, two of the residues R⁷, R⁸, R⁹, R¹⁰ and R¹¹ are specified in C_1-7-alkyl, halogen, halogen-C_1-7-alkyl, halogen-C_1-7-alkoxygroup, cyano group, C_1-7-alkoxycarbonyl, hydroxy-C_3-7-alkynyl, carboxyl-C_1-7-alkyl, carboxyl-C_2-7-alkenyl, C_1-7-alkoxycarbonyl-C_2-7-alkenyl, C_1-7-alkoxycarbonyl-C_2-7-alkynyl, C_1-7-alkoxycarbonyl-C_1-7-alkylaminocarbonyl, carboxyl-C_1-7-alkylaminocarbonyl-C_1-7-alkyl, carboxyl-C_1-7-alkyl-(C_1-7-alkylamino)-carbonyl-C_1-7-alkyl, phenyl-carbonyl, wherein phenyl is unsubstituted, phenyl-C_1-7-alkyl, wherein phenyl is substituted by 1-2 groups specified in a halogen, C_1-7-alkoxygroup, carboxyl, phenyl-C_2-7-alkynyl, wherein phenyl is substituted by 2 groups specified in halogen, carboxyl or C_1-7-alkoxycarbonyl, and pyrrolidine carbonyl-C_1-7-alkyl, wherein pyrrolidinyl is substituted by carboxyl, and the other R⁷, R⁸, R⁹, R¹⁰ and R¹¹ represent hydrogen; the term 'heteroaryl' means an aromatic 5-merous ring containing one or two atoms specified in nitrogen or oxygen; the term 'heterocyclyl' means a saturated 4-merous ring, which can contain one atom specified in nitrogen or oxygen. Besides, the invention refers to a pharmaceutical composition based on the compound of formula I.

EFFECT: there are prepared new compounds possessing the GPBAR1 agonist activity.

21 cl, 1 tbl, 190 ex