1,2,4-TRIAZOLONE DERIVATIVE Russian patent published in 2015 - IPC C07D249/12 C07D401/10 C07D401/12 C07D401/14 C07D403/10 C07D413/10 C07D413/14 C07D417/10 C07D451/06 C07D491/107 C07D498/08 A61K31/41 A61K31/454 A61K31/46 A61K31/5377 A61K31/5386 A61P17/14 A61P25/08 A61P25/16 A61P25/18 A61P25/28 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to 1,2,4-triazolone derivatives and pharmaceutically acceptable salts thereof. The disclosed compounds have antagonistic activity with respect to the arginine vasopressin V1b receptor. In formula (IA): R¹ is C_1-5 alkyl (the C_1-5 alkyl is optionally substituted with 1-3 groups selected from a group consisting of hydroxy, halogen atoms, and C_3-7 cycloalkyl), C_3-7 cycloalkyl or a 4-8-member saturated heterocycle, containing one heteroatom selected from an oxygen atom; R² is a hydrogen atom; R³ is a phenyl or pyridyl (the phenyl or pyridyl is optionally substituted with 1 or 2 groups selected from a group consisting of C_1-5 alkoxy, halogen atoms, cyano and C_1-5 alkylsulphonyl); R⁴ and R⁵ can be identical or different, and each is a hydrogen atom or C_1-5 alkyl (the C_1-5 alkyl is optionally substituted with one hydroxy), or R⁴ and R⁵ optionally, together with a nitrogen atom with which they are bonded, form a 4-8-member saturated or unsaturated heterocycle, optionally containing one nitrogen, oxygen or sulphur atom, in addition to the nitrogen atom with which they are bonded, in a ring (the 4-8-member saturated or unsaturated heterocycle is optionally substituted with one or two groups selected from a group consisting of hydroxy, C_1-5 alkyl ( the C_1-5 alkyl is optionally substituted with one hydroxy), C_1-5 alkoxy, halogen atoms, cyano, C_2-5 alkanoyl, aminocarbonyl, trifluoromethyl and amino (the amino is optionally substituted with one or two groups selected from a group consisting of C_1-5 alkyl and C_2-5 alkanoyl), and the 4-8-member saturated heterocycle optionally has a C_1-5 alkylene group which crosslinks two different carbon atoms in the ring, or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; A is phenylene, pyridinediyl or pyrimidinediyl (the phenylene, pyridinediyl and pyrimidinediyl are optionally substituted with one group selected from halogen atoms and C_1-5 alkoxy); X is a single bond or -O-; R^a is a hydrogen atom or a C_1-5 alkyl and n equals 0 or 1. The invention also relates to 1,2,4-triazolone derivatives, the structural formulae and values of radicals of which are given in the claim, to a pharmaceutical composition and to a therapeutic or preventive agent containing a 1,2,4-triazolone derivative or a pharmaceutically acceptable salt thereof.

EFFECT: improved properties.

12 cl, 16 tbl, 250 ex