AZOLE DERIVATIVES Russian patent published in 2017 - IPC C07D207/444 C07D231/12 C07D233/64 C07D233/70 C07D249/08 C07D249/10 C07D263/32 C07D277/20 C07D277/30 C07D401/04 C07D401/10 C07D403/04 C07D403/06 C07D403/10 C07D413/10 C07D451/06 C07D491/107 C07D498/08 A61K31/4164 A61K31/4178 A61K31/4196 A61K31/4439 A61K31/444 A61K31/454 A61K31/4545 A61K31/46 A61K31/4725 A61K31/496 A61K31/537 A61K31/5377 A61K31/541 A61K31/5386 A61K31/553 A61P1/04 

FIELD: pharmacology.

SUBSTANCE: invention relates to azole derivative of formula (I) or its pharmaceutically acceptable salt, wherein R¹ is hydrogen atom or C_1-5alkyl; R² is hydrogen atom or C_1-5alkyl; R³ is phenyl or pyridyl (where phenyl or pyridyl is optionally substituted with one or two fragments selected from the group consisting of C_1-5alkoxy, halogen and trifluoromethyl atoms); each of R⁴ and R⁵, which can be the same or different, represent hydrogen atom or C_1-5alkyl (where C_1-5alkyl is optionally substituted with one fragment selected from the group consisting of hydroxy and C_1-5alkoxy), or R⁴ and R⁵ together with nitrogen atom joining them form 4-7-membered saturated or unsaturated heterocycle, optionally compirsing one cyclic nitrogen, oxygen or sulfur atom, aside from the mentioned above joining nitrogen atom (where 4-7-membered saturated and unsaturated heterocycle is optionally substituted with one or two fragments, selected from the group consisting of hydroxy C_1-5alkyl (where C_1-5 alkyl is optionally substitued with one or two hydroxyl group), C_1-5alkoxy, halogen atoms, cyano, C_2-5alkanoyl, aminocarbonyl, mono-C_1-5alkylaminocarbonyl, di-C_1-5 alkylaminocarbonyl, trifluoromethyl, amino, mono-C_1-5alkylamino, di-C_1-5alkylamino and C_2-5alkylamino, wherein the mentioned 4-7-membered saturated or unsaturated heterocycle optionally has C_1-5alkylene fragment, joining two different cyclic carbon atoms), or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; azole cycle represented by formula (α) has any structure of group (II) formula, contained in invention formula, and wherein R^y is hydrogen atom or C_1-5alkyl; X¹ and X² are such that: (i) if X¹ means an ordinary link or fragment -CO-, X² means -C_1-5alkylene- or -O-C_1-5alkylene-; and (ii) if X¹ means a fragment -CONR^x1-, X²means an ordinary link; R^x1 is hydrogen atom or C_1-5alkyl; and cycle A is benzol cycle, pyridine cycle (where benzol cycle is optionally substituted with one or two fragments, selected from the group consisting of halogen atoms and C_1-5alkoxy), 5-6-membered saturated or partly unsaturated heterocycle, containing one or two nitrogen atoms (where 5-6-membered saturated or unsaturated heterocycle is optionally substituted with one oxo group) or C_3-7cycloalkane. The invention also relates to a pharmaceutical composition having antagonistic effect against V1b arginine-vasopressin receptor, and to agent for treating or preventing mood disorders, anxiety disorders or drug addiction, comprising azole derivative of formula (I) or its pharmaceutically acceptable salt as an active agent.

EFFECT: azole derivative having antagonistic effect against V1b arginine-vasopressin receptor.

12 cl, 22 tbl, 361 ex