BENZAZEPIN DERIVATIVES APPLICABLE AS VASOPRESSIN ANTAGONISTS Russian patent published in 2013 - IPC C07D223/16 C07D405/12 A61K31/55 A61P7/00 A61P9/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a benzazepin compound of general formula (1) possessing the property of vasopressin antagonist, and to a based pharmaceutical composition. In general formula (1) R¹ means a group (1-1) or (1-3) to (1-7): (1-1) represents a group -CO-(CH₂)_n-COR² wherein n means an integer 1 to 4, R² means (2-1) hydroxyl group; (2-2) lower alkoxy group if necessary substituted by hydroxyl group, lower alkanoyl group, lower alkanoyloxy group, lower alkoxycarbonyloxy group, cycloalkyloxycarbonyloxy group or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) amino group if necessary substituted by hydroxyl lower alkyl; (1-3) represents a group -CO-(CH₂)_p-O-CO-NR⁵R⁶ wherein p means an integer 1 to 4, R⁵ means lower alkyl group, and R⁶ means a group of lower alkoxycarbonyl lower alkyl; (1-4) represents a group -CO-(CH₂)_q-X-R⁷ wherein q means an integer 1 to 4, X means an oxygen atom, a sulphur atom or a sulphonyl group, and R⁷ means a group of carboxy lower alkyl or a group of lower alkoxycarbonyl lower alkyl; (1-5) represents a group -CO-R⁸, (wherein R⁸ means (8-1) alkyl group if necessary substituted by a halogen atom, lower alkanoyloxy group or phenyl group (substituted by dihydroxyphosphoryloxy group wherein hydroxyl groups may be substituted by benzyl groups, and lower alkyl group), a (8-2) lower alkoxy group substituted by a halogen atom, lower alkanoyloxy group or dihydroxyphosphoryloxy group, (8-3) pyridyl group or (8-4) lower alkoxyphenyl group; (1-6) represents a lower alkyl group substituted by a group consisting of a lower alkylthio group, a dihydroxyphosphoryloxy group and a lower alkanoyloxy group; and (1-7) represents a peptide residue if necessary substituted by one or more protective groups.

EFFECT: compound of formula (1) is able to maintain the blood tolvaptan level for a long period of time that enables providing the desired pharmaceutical effects.