Quinoline-n-oxide derivative and pharmaceutical composition.

摘要

A quinoline-N-oxide derivative represented by the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="27" wi="35" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>[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; R, is alkylene or alkenylene having 3 to 15 carbon atoms; 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, -CH<Sub>2</Sub>NHR<Sub>2</Sub> (wherein R<Sub>2</Sub> is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH<Sub>2</Sub>NR<Sub>3</Sub>R<Sub>4</Sub>, (wherein R<Sub>3</Sub> and R<Sub>4</Sub> are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH<Sub>2</Sub>N<Sup>+</Sup>R<Sub>5</Sub>R<Sub>6</Sub>R<Sub>7</Sub> (wherein R<Sub>5</Sub>, R<Sub>6</Sub>, and R<Sub>7</Sub> are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), -COR<Sub>8</Sub> (wherein R. is a hydrogen atom, lower alkyl or hydroxy), -CH(OR<Sub>9</Sub>)<Sub>2</Sub> (wherein R. 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.