3-SUBSTITUTED-1,4-DIAZEPAN-2-ONE ANTAGONISTS OF MELANOCORTIN 5-RECEPTOR Russian patent published in 2014 - IPC C07D243/08 C07D401/06 C07D401/12 C07D403/06 A61K31/551 A61P17/08 A61P17/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I)

where Y represents a group of formula -(CR⁹R¹⁰)_n-; X represents -C(=O)-; Z represents a group of formula -(CR¹³R¹⁴)_q-; R¹ is selected from a group, consisting of (a) C₂-C₁₂alkenyl, substituted with 4-chlorophenyl; or (b) C₆-C₁₀aryl, optionally substituted with one or two halogen atoms; R² and R³ represent H; R⁴ is selected from a group, consisting of H, C₁-C₁₂alkyl, optionally substituted with hydroxyl, methoxy or benzyloxy, C₃-C₁₂cycloalkyl, C₆aryl, optionally substituted with an amino group or pyperidine, C-bound C₁-C₁₈heteroaryl, selected from pyridine and imidazole, C(=O)R¹⁵, C(=O)NR¹⁶R¹⁷ and ONR¹⁶C(=NR¹⁷)NR¹⁸R¹⁹; each R^5a and R^5b represents H, each R⁶, R⁷ and R⁸ is independently selected from a group, consisting of H, C₁-C₁₂alkyl and C₆-C₁₈aryl, each R⁹ and R¹⁰ represents H; each R¹³ and R¹⁴ represents H; R¹⁵ represents H, each R¹⁶, R¹⁷, R¹⁸, R¹⁹ and R²⁰ is independently selected from a group, consisting of H, C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl, C₆aryl and pyridyl, or any two of R¹⁶, R¹⁷, taken together with atoms, to which they are bound, form a cyclic group, containing 5 carbon atoms, or n equals to 1; q represents an integer number, selected from a group, consisting of 1, 2, 3, 4 and 5; r equals to 1; or its pharmaceutically acceptable salt.

EFFECT: invention relates to a pharmaceutical composition for treatment of MC5R-associated conditions, which contains a formula (I) compound and a pharmaceutically acceptable carrier, a diluent or a filling agent.

23 cl, 6 tbl, 53 ex