CYCLOALKYL-SUBSTITUTED IMIDAZOLE DERIVATIVE, POSSESSING INHIBITING ACTIVITY WITH RESPECT TO TAFIa Russian patent published in 2016 - IPC C07D233/64 C07D233/70 C07D403/12 C07D405/12 C07C229/24 A61K31/4164 A61K31/4178 A61K31/4427 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to novel imidazole derivative of general formula , or to its pharmacologically acceptable salt, where A represents group: , where * represents position for substitution; R¹, R² and R³, each represents hydrogen atom; R⁴ represents hydrogen atom or prodrug group; and Y represents group: -CH₂-CHR⁵-CH₂-NHR⁶ (where R⁵ represents hydrogen atom or C1-C6alkyl group, and R⁶ represents hydrogen atom or prodrug group), -O-CHR⁷-CH₂-NHR⁸ (where R⁷ represents hydrogen atom C1-C6alkyl group, and R⁸ represents hydrogen atom) or , (where R⁹ represents hydrogen atom, and * represents position for substitution); where prodrug group, represented by R⁴, represents [(isopropoxycarbonyl)oxy]ethyl group or C1-C6alkyl group, which is substituted with one phenyl group; and where prodrug group, represented by R⁶, represents C1-C6alkanoyl group, which is substituted with one or two similar or different groups, selected from aminogroup and phenyl group; (C1-C6alcoxy)carbonyl group; substituted with one group, selected from C2-C6alkanoyloxy group and (C3-C6cycloalkyl)carbonyloxy group; or 1,3-dioxol-methoxycarbonyl group, substituted with two different groups, selected from oxogroup and C1-C6alkyl group. Invention also relates to particular compounds and salts, TAFIa inhibitor, fibrinolysis promoter, pharmaceutical composition and preventive or therapeutic medication based on formula (I) compound, as well as to intermediate compounds of formulae , and .

EFFECT: novel imidazole derivatives, possessing TAFIa-inhibiting activity have been obtained.

59 cl, 4 dwg, 4 tbl, 50 ex