发明名称 NOVEL 1H-INDOLE-3-ACETAMIDES AS INHIBITORS OF SPLA2 AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF
摘要 organic chemistry, pharmacy. SUBSTANCE: invention relates to 1H-indole- -3-acetamides of the general formula (I) where X means oxygen atom; R1 is taken among the group (i), (iii) where: (i) means C6-C20-alkyl, C4-C12-cycloalkyl; (iii) means -(CH2)n-(R80) where n = 1-8 and R80 is the group indicated in (i); R2 means hydrogen, halogen atom, C1-C3-alkyl, C1-C2-alkylthio-, C1-C2-alkoxy- -group; each of R3 means independently hydrogen atom or methyl group; R4,R5,R6,R7 each means independently C1-C10-alkyl, C2-C10-alkenyl, C3-C8-cycloalkyl, C1-C10-alkoxy-, C4-C8-cycloalkoxy-, phenoxy-group, halogen atom, hydroxy-group, carboxyl, -C(O)O(C1-C10)- -alkyl), hydrazide, hydrazino-group, NH2,NO2,-C(O)NR82R83 where R82 and R83 means independently hydrogen atom, C1-C10-alkyl or the group of the formula: a) where R84 and R85 mean independently hydrogen atom, C1-C10-alkyl; p = 1-5; Z means a bond, -O-, -NH-; Q means , phenyl, group of the formula: b) , c) , d) is taken independently among hydrogen atom, R86-alkyl and its pharmaceutically acceptable salts, esters or amides. Compounds of the formula (I) show inhibitory activity with respect to fatty acids release mediated by C1-C10, phospholipase and they can be used for preparing the pharmaceutical composition. Invention describes intermediate compounds used for synthesis of compounds of the formula (I). EFFECT: new compounds indicated above, valuable pharmacological properties. 15 cl, 2 tbl, 101 ex
申请公布号 RU2162463(C2) 申请公布日期 2001.01.27
申请号 RU19940012930 申请日期 1994.04.15
申请人 EHLI LILLI EHND KOMPANI 发明人 NIKOLAS DZHEJMS BAKH;ROBERT DILEJN DILLARD;SJUZAN EHLIZABET DRAKHAJM;ROBERT BELL KHERMANN;RICHARD UOLTER SHEVITS
分类号 A61K31/40;A61K31/403;A61K31/404;A61K31/405;A61K31/44;A61K31/675;A61P1/00;A61P3/02;A61P11/00;A61P11/08;A61P11/16;A61P17/00;A61P31/04;A61P43/00;C07D209/14;C07D209/18;C07D209/22;C07D209/24;C07D209/30;C07D209/34;C07D209/42;C07D401/06;C07D403/12;C07D417/12;C07F9/40;C07F9/572;(IPC1-7):C07D209/30 主分类号 A61K31/40
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