Quinoline-N-oxide derivative and pharmaceutical composition

摘要

A quinoline-N-oxide derivative represented by the formula: <IMAGE> wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R1 is alkylene or alkenylene having 3 to 15 carbon atom; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, -CH2NHR2 (wherein R2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH2NR3R4 (wherein R3 and R4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH2N+R5R6R7 (wherein R5, R6, and R7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), -COR8 (wherein R8 is a hydrogen atom, lower alkyl or hydroxy), -CH(OR9)2 (wherein R9 is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.