发明名称 ASPARTYL DERIVATIVES OF HISTAMINE, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND THEIR USING AS MODULATORS OF ENZYME ACTIVITY OF ANTIOXIDANT PROTECTION
摘要 FIELD: bioorganic chemistry, biochemistry, pharmacy. ^ SUBSTANCE: invention relates to novel aspartyl derivatives of histamine of the general formula (I): , wherein R means hydrogen atom (H), or , or that are able to modulate activity of enzymes of antioxidant protection - superoxide dismutase (SOD) and catalase. Also, invention relates to using the known compounds of the general formula (I) for the same designation wherein at the same values of X the value R represents acetyl group, and to their pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition possessing capacity to modulate activity of SOD and catalase and comprising the effective amount of compound of the general formula (I), and to a method for synthesis of compounds of the general formula (I). Method involves interaction of pentafluorophenyl ester Nalpha-Z-, beta- or alpha-benzyl ester of aspartic acid with histamine followed by hydrogenolysis without isolation of intermediated protected derivatives of aspartyl histamine. ^ EFFECT: improved method of synthesis, valuable biochemical properties of derivatives. ^ 12 cl, 3 tbl, 2 sch, 2 dwg, 8 ex
申请公布号 RU2287524(C1) 申请公布日期 2006.11.20
申请号 RU20050109241 申请日期 2005.03.31
申请人 OOO "FARMINTERPRAJSEZ" 发明人 NEBOL'SIN VLADIMIR EVGEN'EVICH;ZHELTUKHINA GALINA ALEKSANDROVNA;KROMOVA TAT'JANA ALEKSANDROVNA
分类号 C07D233/64;A61K31/417;A61K38/05;C07D233/00;C07D233/54 主分类号 C07D233/64
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