BICYCLIC CARBOXAMIDES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel bicyclic carboxamides of the formula (i) where: (1) X means N and (a) Z means =CR₁-CR₂ and Y means N; (b) Z means =CR₁ and Y means O, S or NR₄,; or (c) Z means =CR₁-N= and Y means CR₂; or (2) X means NR₄,; Z means -CR₁= and Y means N; Q means O; R₁ and R₂ mean COR₆, C(=NOR₆)R₁₃, alkyl-C-(=NOR₆)R₁₃, NR₈R₉, CF₃ or R₆; R₃ means C_1-6-alkoxy-group; R₄ means H or alkyl; R₅ means heteroaryl optionally substituted with halogen atom, alkyl, CON-R₁₁R₁₂, CF₃ or CN, aryl substituted with halogen atom; R₆ means H, alkyl, cycloalkyl, aryl, heteroaryl, heterocycle, arylalkyl, hetero-arylalkyl or heterocycloalkyl; R₇ means alkyl, hydroxy-group, O-R₁₀, N-R₈R₉, CN, CO₂H, CO₂R₁₀, CONR₁₁R₁₂; R₈ and R₉ means H or alkyl or NR₈R₉ means heterocyclc ring optionally substituted with R₁₄; R₁₀ means alkyl, heterocycle; R₁₁ and R₁₂ means H or alkyl; R₁₃,R₁₄,R₁₅ mean alkyl; Y means O and n = 2-4, and their pharmaceutically acceptable salts. Compounds of the formula (i) show inhibitory effect on activity of phosphodiesterase and tumor necrosis factor and can be used in medicine as an agent for inhibition of phosphodiesterase and tumor necrosis factor. EFFECT: new compounds indicated above, valuable medicinal and biochemical properties. 13 cl, 2 tbl