POLYCYCLIC MACROLACTAMS AND PHARMACEUTICAL COMPOSITION BASED ON THEM Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes polycyclic macrolactams of formulas (I) , (II) and (III) where means a simple bond or if R_2a is absent - a double bond; optionally protected hydroxyl group and R_1a-H; or R₁ and R_1a together mean oxo-group; R₂ means optionally protected hydroxyl group or together with R₄ forms -OC(=O)O-; R_2a is H or absent; when symbol means a simple bond then R₂ together with R_2a mean optionally protected hydroxyl group or together with R₂ forms -OC(=O)O-; R_4a is H, or R₄ together with R_4a mean oxo-group; R₅ means, halogen, alkoxycarbonylhydroxy-group, optionally protected hydroxyl, lower alkoxyl, acyloxyl or a group OC(x)N(R₁₀)R₁₁; or R₅ together with R_6a form a group ; or R₅ together with R_8a means hydroxy- -group and then R₈ means hydroxyl; R₆ means hydroxyl, and R_6a or together with R₅ forms a group -OC(=X)-N-; or R₆ and R_6a together form oxo-group; means optionally protected hydroxyl, lower alkoxyl or acyloxyl, and means hydroxyl; or and together form -OC(= O)O-; means hydroxyl or lower alkoxyl, and means hydroxyl; or and together form a group -OC(=O)O; R₇ means methoxyl or hydroxyl; R₈ means optionally protected hydroxyl-group, acyloxyl, imidazolyl- -carbonyl or alkoxycarbonyloxyl and R_8a means hydrogen; or R₈ means hydroxyl and R_8a together with R₅ mean hydroxy-group; or R₈ together with R_8a mean oxo-group; n = 1 or 2 in free state or as salt. Synthesized compounds show pharmacological activity and can be used in pharmaceutical composition showing antiinflammatory, immunosuppressant and antiproliferative activities. EFFECT: improved method of synthesis, enhanced effectiveness. 6 cl, 73 ex, 14 tbl