ACYLAMINOALKENYLENEAMIDE DERIVATIVES, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to acylaminoalkenylene-amide derivatives of the formula (I) where R means unsubstituted phenyl or phenyl that can be substituted with halogen atom, alkyl, trifluoromethyl, hydroxy- and alkoxy-group; R₁ means hydrogen atom, alkyl; R₂ means hydrogen atom, alkyl, unsubstituted phenyl or phenyl that can be substituted with halogen atom, trifluoromethyl, hydroxy- and alkoxy-group; R₃ means unsubstituted phenyl or phenyl that can be substituted with halogen atom, alkyl, trifluoromethyl, hydroxy- and alkoxy-group, or it means naphthyl, 1H-indole-3-yl or 1-alkylindole-3-yl; and mean hydrogen atom, alkyl being one of radicals and means hydrogen atom; R₅ - means cycloalkyl, D-azacycloheptane-2-one-3-yl or L-azacycloheptane-2-one-3-yl or its salt. Compounds of the formula (I) show antagonistic activity and can be used therefore in the pharmaceutical composition as an active substance. Invention relates also to methods of synthesis of novel compounds of the formula (I), for example, by N-acylation of compound of the formula (II) with carboxylic acid R-C(=O)-OH or by condensation of carboxylic acid of the formula (III) with cycloalkylamine or with D-(+)- or L-(-)-3-amino--ε--caprolactam. EFFECT: improved method of synthesis. 14 cl, 1 tbl