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.Изобретение относится к соединению бензазепина общей формулы (1), обла
