发明名称 CYCLOALKYL-SUBSTITUTED IMIDAZOLE DERIVATIVE, POSSESSING INHIBITING ACTIVITY WITH RESPECT TO TAFIa
摘要 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; R, Rand R, each represents hydrogen atom; Rrepresents hydrogen atom or prodrug group; and Y represents group: -CH-CHR-CH-NHR(where Rrepresents hydrogen atom or C1-C6alkyl group, and Rrepresents hydrogen atom or prodrug group), -O-CHR-CH-NHR(where Rrepresents hydrogen atom C1-C6alkyl group, and Rrepresents hydrogen atom) or, (where Rrepresents hydrogen atom, and * represents position for substitution); where prodrug group, represented by R, represents [(isopropoxycarbonyl)oxy]ethyl group or C1-C6alkyl group, which is substituted with one phenyl group; and where prodrug group, represented by R, 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
申请公布号 RU2572814(C2) 申请公布日期 2016.01.20
申请号 RU20120144332 申请日期 2011.03.14
申请人 DAJITI SANKIO KOMPANI, LIMITED 发明人 NAGATA TSUTOMU;INOUE MASAKHIRO;ASIDA JUKA;NOGUTI KENGO;ONO MAKOTO
分类号 C07D233/64;A61K31/4164;A61K31/4178;A61K31/4427;A61P9/00;C07C229/24;C07D233/70;C07D403/12;C07D405/12 主分类号 C07D233/64
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