PYPERIDIN-4-YLAMIDE DERIVATIVES AND THEIR APPLICATION AS ANTAGONISTS OF SST RECEPTOR SUBTUPE 5 Russian patent published in 2010 - IPC C07D401/14 C07D401/10 C07D401/12 C07D407/12 C07D413/14 A61K31/4468 A61K31/506 A61K31/5375 A61P3/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula: I, where R¹ is selected from group, consisting of ethyl, 2-fluorethyl and isopropyl; R² is selected from group, consisting of hydrogen, C_1-7-alkyl, hydroxy, C_1-7-alkoxy, C_3-7-cycloalkyl, halogen, -C(O)OR⁶, where R⁶ represents C_1-7-alkyl, amino, phenyl, phenyl, substituted with 1-3 substituents, selected from group, consisting of halogen, halogen-C_1-7-alkyl and halogen-C_1-7-alkoxy, pyridyl, imidazolyl, triazolyl and pyrrolyl; R³ is selected from group, consisting of hydrogen, C_1-7-alkoxy, amino, -O-benzyl and -o-tetrahydropyranyl; or R² and R³ are bound to each other with formation of cycle together with carbon atoms to which they are bound, and R² and R³ together represent -CH=CH-NH-; R⁴ is selected from group, consisting of hydrogen, halogen, pyridyl and pyrimidyl; R⁵ and R^5' independently on each other are selected from hydrogen or methyl; A is selected from group, consisting of isphenyl; phenyl, substituted with 1-3 substituents, selected from group, consisting of C_1-7-alkyl, C_3-7-cycloalkyl, C_1-7-alkylsulfonyl, -O-C_1-7-alkylsulfonyl, hydroxy, C_1-7-alkoxy, hydroxy-C_1-7-alkyl, hydroxy-C_2-7-alkoxy, dihydroxy-C_3-7-alkoxy, C_1-7-alkylamino, di-C_1-7-alkylamino, amino-C_2-7-alkoxy, amino-C_1-7-alkyl, -C(O)NR¹⁰R¹¹, -O-C_1-7-alkylene-C(O)NR¹⁰R¹¹, -C(O)OR¹⁰, -C_1-7-alkylene-C(O)OR¹⁰, -O-C_1-7-alkylene-C(O)OR¹⁰, halogen, halogen-C_1-7-alkoxy, cyano- C_1-7-alkoxy, fluorphenyl, pyridyl, tetrazolyl and tetrazolyl- C_1-7-alkoxy; 1,3-benzodioxolyl; naphtyl; pyrimidinyl; pyridyl, substituted with one or two substituents, selected from group, consisting of C_1-7-alkyl, C_1-7-alkoxy, amino, C_1-7-alkylamino, di-C_1-7-alkylamino, C_3-7-cycloalkylamino, halogen, cyano, morpholinyl, imidazolyl and -NH-C(O)-R⁹, where R⁹ represents C_1-7-alkyl or C_3-7-cycloalkyl, and indolyl; R¹⁰ and R¹¹ independently on each other represent hydrogen or C_1-7-alkyl; and to their pharmaceutically accdeptable salts. Invention also relates to pharmaceutical compositions.

EFFECT: obtaining novel biologically active compounds, which are antagonists of somatostatin receptor subtype 5 (SSTR5).

26 cl, 266 ex