COUMARIN DERIVATIVES, USE THEREOF AS PLA2 INHIBITORS, AND DRUG

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 hydrog...

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Hauptverfasser: VOL'FGANG SHEFER, UL'RIKH TIBES, VAL'TER-GUNAR FRIBE, VERNER SHOJER
Format: Patent
Sprache:eng
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Zusammenfassung: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