COUMARIN DERIVATIVES, USE THEREOF AS PLA INHIBITORS, AND DRUG Russian patent published in 1999 - IPC

FIELD: medicine, more particularly use of coumaring and carbostyrenes as PLA₂ inhibitors. SUBSTANCE: described are new coumarin derivatives, method of preparation thereof and drugs containing said compounds, described are coumarin and carbostyryl derivatives of general formula I wherein R₁ is hydrogen or C₁-C₆ alkyl; R₂ is hydrogen or residue OT₁; R₃ is hydrogen or residue OT₂; R₄ is hydrogen or C₁-C₆ alkyl; T₁ and T₂ are identical or different, and each is hydrogen, C₁-C₆ alkyl C₁-C₆ alkanoyl, or T₁ and T₂ combined with atoms to which they are attached, form 5-7 membered heterocyclic ring which is substituted, if desired, by oxo or thioxo; or Q is oxygen atom, X is sulfur atom or NH group or Y valent group, C₁-C₆ alkylene residue which is, if desired, substituted by hydroxy group or amino group; phenylene residue which is if desired mono- or multiple substituted by hydroxyl, halogen, C₁-C₆ alkyl or carboxyl; Z is hydrogen, halogen, carboxyl, hydroxymethyl, C₁-C₆ alkoxycarbonyl, cyano or WR₅R₆; R₅ and R₆ are identical or different and each is hydrogen or C₁-C₆ alkyl, or R₅ and R₆ combined with nitrogen atom to which they are attached, form 3-7 membered heterocyclic ring which is substituted by oxo, hydroxy or C₁-C₆ alkoxy group, tautomers thereof and also salts thereof with non- toxic acids or bases. Also described is method of preparation thereof and also drug based on compounds of formula I having PLA₂-inhibiting activity. EFFECT: improved properties of the drug. 6 cl, 14 ex, 1 tbl