WATER-SOLUBLE COMPOUND OF BENZOAZEPINE AND PHARMACEUTICAL COMPOSITION CONTAINING IT Russian patent published in 2011 - IPC C07F9/553 A61K31/675 A61P7/02 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to benzoazepine compound represented by the following general formula (1): or to ita salt, where R represents a hydrogen atom, hydroxy-group, optionally protected by protective group, selected from lower alkyl group, phenyl(lower)alkyl group, mercapto-group or amino-group, optionally protected by one or two protective groups, selected from lower alkyl group, optionally containing hydroxy-group, R¹ represents a hydrogen atom or hydroxy-protective group, where protective group includes lower alkyl group, phenyl(lower)alkyl group, cyano lower alkyl group and lower alkyloxicarbonyl lower alkyl group, and X represents an oxygen atom, or a sulphur atom. Invention also relates to pharmaceutical composition, which possesses antagonistic activity to vasopressin, on the basis of said compound.

EFFECT: benzoazepine compounds possess high water solubility and can be used as vasodilating, hypotensive, aquaretic agent, inhibitor of platelet aggregation or for treatment of polycystic kidney disease (PKD).

13 cl, 2 dwg, 6 tbl, 30 ex