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 R4a and R5a 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, -OR1b, -S(O)R2b, -C(O)R1b, -C(O)OR1b, -OC(O)N(Rb)(R3b), -(CR4bR5b)m-OR1b, -C(OH)[(CR4bR5b)m-R4b]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; Rb represents hydrogen or alkyl; R1b and R3b represents hydrogen, alkyl or halogenalkyl; R2b represents alkyl; R4b and R5b represents hydrogen, halogen, alkyl or halogenalkyl; m represents 1, 2, 3, 4 or 5; R2 is specified in a group consisting of hydrogen, alkyl, -(CR4aR5a)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, -OR1a, -C(O)G3, -C(O)OR1a, -C(O)N(Rb)(R3a), -N(Rb)(R3a), -(CR4aR5a)m-G1, -CR4a=CR5a-G1, -(CR4aR5a)m-G2, -CR6a=C(R7a)2, halogenalkyl and fragment
; R1a and R3a represents hydrogen, alkyl, haloalkyl, G1, -(CR4aR5a)m-G1, G2 or -(CR4aR5a)m-G2; R6a is alkyl or halogenalkyl; R7a 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-HT2C 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
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Authors
Dates
2015-02-20—Published
2010-05-20—Filed