BENZAZEPIN DERIVATIVES APPLICABLE AS VASOPRESSIN ANTAGONISTS

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)Rmeans a group (1-1) or (1-3) to (1-7): (1-1) represents a group -CO-(CH)-CORwherein n means an integer 1 to 4, Rmeans (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-(CH)-O-CO-NRRwherein p means an integer 1 to 4, Rmeans lower alkyl group, and Rmeans a group of lower alkoxycarbonyl lower alkyl; (1-4) represents a group -CO-(CH)-X-Rwherein q means an integer 1 to 4, X means an oxygen atom, a sulphur atom or a sulphonyl group, and Rmeans a group of carboxy lower alkyl or a group of lower alkoxycarbonyl lower alkyl; (1-5) represents a group -CO-R, (wherein Rmeans (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), обладающего свойством антагониста вазопрессина, и к фармацевтическому препарату на его основе. Соединение формулы (1) может поддерживать уровень толваптана в крови в течение длительного периода времени, что позволяет обеспечить желаемые фармацевтические эффекты. В общей формуле (1)Rобозначает группу (1-1) или с (1-3) по (1-7): (1-1) представляет собой группу -CO-(CH)-COR, в которой п обозначает целое число от 1 до 4, Rобозначает (2-1) гидроксильную группу; (2-2) низшую алкокси-группу, в случае необходимости замещенную гидроксил