BENZIMIDAZOLE AND INDOLE DERIVATIVES AS SELECTIVE 5-HT6 AND/OR 5-HT2A RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D403/12 C07D403/04 C07D209/34 C07D209/38 C07D235/26 A61K31/496 A61K31/454 A61P25/16 A61P25/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel benzimidazole and indole derivatives or pharmaceutically acceptable salts of general formula 1, where m assumes values from 0 to 2; n equals 1, X denotes: -NR^a-; -CR^bR^c-; or -C(O)-; where: R^a is hydrogen or C_1-6alkyl; R^b is hydrogen or C_1-6alkyl; R^c is hydrogen, C_1-6alkyl, hydroxy; or Ar denotes: phenyl, possibly substituted with 1-2 halogens; or isoxazole, possibly substituted with C_1-6alkyl; R¹ is a group of formula p assumes values from 1 to 3; Y denotes: -O-; -NR^d-; or -CR^eR^f-; where R^d, R^e and R^f each independently denotes hydrogen or C_1-6alkyl; each R² independently denotes: halogen; C_1-6alkyl; R³ and R⁴ each independently denotes hydrogen or C_1-6alkyl; R⁵ and R⁶ each independently denotes; and R⁷ and R⁸ each independently denotes hydrogen or C_1-6alkyl; or one of R⁷ and R⁸ and one of R⁵ and R⁶ together with atoms to which they are bonded can form a 4-6-member ring; or one of R⁷ and R⁸ together with R^d and atoms to which they are bonded can form a 6-7-member ring; or one of R⁷ and R⁸ and one of R^e and R^f together with atoms to which they are bonded can form a 5-6-member ring. The invention also relates to a pharmaceutical composition based on compounds of formula I-VI and use of the compounds of formula I-VI.

EFFECT: obtaining novel benzimidazole and indole derivatives with selective 5-and/or 6-HT_2A receptor antagonist properties.

27 cl, 1 tbl, 13 ex