CYCLOPEPTOLIDES Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes cyclopeptolides of the formula (I) as a free form or as salt or ester where A means glycolic acid residue optionally α--substituted with methyl, ethyl optionally substituted with thiazole; B means α-amino-γ- methyl-substituted octanoic acid residue; R₁ means methyl; C means N-methyltryptophane residue of the formula: means alkoxy-group; R₃ means methyl; R₄ means methyl; R₅ symbol means a double bond; X means residue of α-amino-substituted (C₂-C₁₄)-carboxylic acid and Y means residue of N-methyl-α-amino- substituted (C₂-C₁₀)-carboxylic acid. These compounds are inhibitors of expression of adhesion molecules and tumor necrosis factor release and therefore they are useful for treatment of inflammatory and other diseases determined by enhanced level of adhesion molecules expression and/or mediated by tumor necrosis factor. Invention describes also therapeutic composition eliciting cytotoxic activity and activity with respect to inhibition of expression of I CAM-1, V CAM-1 and E-selectin, tumor necrosis factor release and proliferation of cells and containing therapeutically effective amount of compound by p. p. 1 or 2. EFFECT: valuable medicinal properties of compounds. 3 cl, 5 dwg, 11 ex