5-HT RECEPTOR MODULATORS AND METHODS FOR USING THEM Russian patent published in 2015 - IPC C07D487/04 C07D491/04 C07D495/12 A61P25/00 A61K31/554 A61K31/553 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in general formula , fragment A is specified in a group consisting of , or , R¹, R³, R⁴ and R⁵ mean hydrogen or alkyl; each of R^4a and R^5a represents hydrogen; G¹ represents aryl or heteroaryl, which can by unsubstituted or substituted by 1, 2, 3, 4 or 5 substitutes specified in a group consisting of alkyl, halogen, cyano, -OR^1b, -S(O)R^2b, -C(O)R^1b, -C(O)OR^1b, -OC(O)N(R^b)(R^3b), -(CR^4bR^5b)_m-OR^1b, -C(OH)[(CR^4bR^5b)_m-R^4b]₂, and halogenalkyl; G² means cycloalkyl, cycloalkenyl or heterocycle unsubstituted or substituted by 1, 2, 3, 4 or 5 substitutes specified in a group consisting of alkyl; R^b represents hydrogen or alkyl; R^1b and R^3b represents hydrogen, alkyl or halogenalkyl; R^2b represents alkyl; R^4b and R^5b represents hydrogen, halogen, alkyl or halogenalkyl; m represents 1, 2, 3, 4 or 5; R² is specified in a group consisting of hydrogen, alkyl, -(CR^4aR^5a)_m-G¹ and -S(O)₂R⁶, R⁶ represents G¹, X¹ means N or CR⁹; X² means N or CR¹⁰; X³ means CR¹¹; X⁴ means N or CR¹²; provided one fragment of X¹, X² or X⁴ can represent N; each of R⁹, R¹⁰, R¹¹, R¹², R¹³ and R¹⁴ independently represents hydrogen, alkyl, alkenyl, halogen, -G¹, -G², -OR^1a, -C(O)G³, -C(O)OR^1a, -C(O)N(R^b)(R^3a), -N(R^b)(R^3a), -(CR^4aR^5a)_m-G¹, -CR^4a=CR^5a-G¹, -(CR^4aR^5a)_m-G², -CR^6a=C(R^7a)₂, halogenalkyl and fragment ; R^1a and R^3a represents hydrogen, alkyl, haloalkyl, G¹, -(CR^4aR^5a)_m-G¹, G² or -(CR^4aR^5a)_m-G²; R^6a is alkyl or halogenalkyl; R^7a represents hydrogen, alkyl or helogenalkyl; G³ represents heterocycle attached to an adjoining carbonyl fragment through a nitrogen atom being a part of heterocycle; or R¹⁰ and R¹¹ or R¹³ and R¹⁴ together with carbon atoms which they are attached to, form unsubstituted phenyl or cycloalkyl; Y¹ means NR¹⁷, CR¹⁸R¹⁹, C(O), S(O)_n or O; Y² means NR²⁰, CR¹⁸R¹⁹ or C(O); Y³ means NR¹⁷, CR¹⁸R¹⁹ or C(O); or Y¹ and Y² together represent CR¹⁸=CR¹⁹, n means 2; R¹⁷ represents hydrogen; R¹⁸ and R¹⁹ represents hydrogen; and R²⁰ is specified in a group consisting of hydrogen, alkyl and -S(O)_n-G¹.

EFFECT: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts possessing the properties of a 5-HT_2C and/or 5-HT₆ receptor modulator, to a based pharmaceutical composition and to methods for preparing them.

33 cl, 7 tbl, 20 dwg, 278 ex