NOVEL 1H-INDOLE-3-ACETAMIDES AS INHIBITORS OF SPLA AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2001 - IPC

FIELD: 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