INDOL-3-YL-CARBONYL-ASASPIRO DERIVATIVES AS VASOPRESSIN RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D471/10 C07D491/10 A61K31/437 A61K31/4355 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel indol-3-yl-carbonyl-asaspiro-derivatives of formula I: where R¹ represents H,-(CH₂)_m-R^a, where R^a represents NRⁱRⁱⁱ, phenyl, possibly substituted by one or more than one B, -(CH₂)_n-(CO)-R^b , where R^b represents NRⁱRⁱⁱ; there exists one or more than one R² , where each R² is the same or different and represents one or more than one H, in halogen way; R³ represents H, C_1-6-alkyl; B represents in halogen way; Rⁱ and Rⁱⁱ each independently represents H, C_1-6-alkyl, C_1-6alkyl-NRⁱⁱⁱR^iv; Rⁱⁱⁱ and R^iv each independently represents C_1-6alkyl; m equals 1-6; n equals 1-4; A represents group : where R⁴ represents H or C_1-6alkyl; R⁵ represents phenyl, possibly substituted in halogen way; or its pharmaceutically acceptable salt; on condition that 1-(1H-indol-3-yl-carbonyl)-4-(1,3-dioxolan-2-yl)pyperidine is excluded.

EFFECT: compounds demonstrate antagonistic activity with respect to Via vasopressin receptor, which makes it possible to apply them for obtaining pharmaceutical composition.

22 cl, 4 dwg, 16 ex