QUINOLINE CARBOXAMIDES AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel quinolines of the formula (I) where X means CO; R means H, halogen atom; R₁ means H, lower alkoxy-group optionally substituted with halogen atoms; R₂, R₃, R₄ mean H, R₇, OR₁₁, COR₇, C(=NOR₇)R₇, CF₃, lower alkyl-C(= NOH)R₇, CN, NR₉R₁₀ or CON-R₁₂R₁₃ where N-R₁₂R₁₃ is six-membered heterocycle containing one or two N atoms as a heteroatom optionally substituted with one or more R₁₅; R₅ means H; R₆ means phenyl, six-membered heterocycle containing one or two similar or different heteroatoms taken among nitrogen and oxygen atom substituted with R₁₄; R₇ means R₁₁ optionally substituted with R₁₆; R₈ means alkyl; R₉ means H, aklylcarbonyl, lower alkoxycarbonyl, heteroarylcarbonyl; R₁₀ means H, lower alkyl; R₁₁ means lower alkyl, C₃-C₇- cycloalkyl, six-membered heterocycle containing one or two nitrogen atoms as a heteroatom optionally substituted with R₁₅, phenylalkyl; R₁₂ and R₁₃ mean H or NR₁₂R₁₃ where NR₁₂R₁₃ means six-membered heterocycle containing one or two N atoms as a heteroatom optionally substituted with R₁₅; R₁₄ means CO₂R₈, halogen atom, -CN, lower alkyl optionally substituted with halogen atom, lower alkoxy-group; R₁₅ means lower alkyl; R₁₆ means OR₁₁, NR₉R₁₀, CO₂H, CO₂R₁₁, or its pharmaceutically acceptable salt. Invention relates to also pharmaceutical composition containing compound of the formula (I) and eliciting inhibitory activity with respect to phosphodiesterase-IV and tumor necrosis factor. EFFECT: new compounds indicated above, valuable biochemical and medicinal properties. 26 cl, 64 ex