INDOLE DERIVATIVES AS HISTAMINE H-RECEPTOR INHIBITORS FOR TREATING COGNITIVE DISORDERS AND SLEEP DISTURBANCES, OBESITY AND OTHER DISORDERS OF CENTRAL NERVOUS SYSTEM Russian patent published in 2011 - IPC C07D403/12 A61K31/404 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula: where a spacer represents Y represents N; R¹ and R² together with nitrogen atom whereto attached form a 5-6-members heterocyclic ring system which is optionally substituted by 1-3 (C₁-C₅)alkyl groups; n is equal to 2-4; R represents 0-2 groups selected from halogen atom, (C₁-C₆)alkyl, (C₁-C₆)alkoxy groups; R⁴ and R⁵ are independently selected from H, (C₁-C₅)alkyl, (C₁-C₈)alkoxy groups, halogen atom; R⁶ represents H, CONR⁷R⁸, -(CH₂)_x-O-R⁹, (C₁-C₄)alkyl group, COOC₂H₅, cyclopropyl; x is equal to 1-4; R⁷ and R⁸ independently represent hydrogen, (C₁-C₅)alkyl group, (C₃-C₇)-cycloalkyl group, -CH₂-cyclohexyl, or R⁷ and R⁸ together with nitrogen atom whereto attached form a 5-6-members heterocyclic ring system with 0-1 additional heteroatom selected from O; R⁹ represents hydrogen, (C₁-C₅)alkyl, (C₃-C₇)cycloalkyl group; and its pharmaceutically acceptable salt, and its individual stereoisomers.

EFFECT: compounds inhibit histamine H₃-receptor that allows to use them for preparing pharmaceutical compositions.

6 cl, 10 dwg, 1 tbl, 44 ex