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    Quinoline-N-oxide derivative and pharmaceutical composition
    5.
    发明授权
    Quinoline-N-oxide derivative and pharmaceutical composition 失效
    喹啉-N-氧化物衍生物和药物组合物

    公开(公告)号：US4657916A

    公开(公告)日：1987-04-14

    申请号：US772693

    申请日：1985-09-05

    申请人： Masayuki Teranishi ,  Koji Suzuki ,  Hiroshi Kase ,  Shigeto Kitamura ,  Katsuichi Shuto ,  Kenji Omori

    发明人： Masayuki Teranishi ,  Koji Suzuki ,  Hiroshi Kase ,  Shigeto Kitamura ,  Katsuichi Shuto ,  Kenji Omori

    IPC分类号： A61K31/47 ,  A61P43/00 ,  C07D215/60 ,  C07D405/12 ,  C07F7/18

    CPC分类号： C07D405/12 ,  C07D215/60

    摘要： A quinoline-N-oxide derivative represented by the formula: ##STR1## 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.sub.1 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, --CH.sub.2 NHR.sub.2 (wherein R.sub.2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 NR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 N.sup.+ R.sub.5 R.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 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 (wherein R.sub.8 is a hydrogen atom, lower alkyl or hydroxy), --CH(OR.sub.9).sub.2 (wherein R.sub.9 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.

    摘要翻译： 由下式表示的喹啉-N-氧化物衍生物：其中X为羟基，低级烷氧基，低级烷硫基，未取代或取代的芳烷氧基，或未取代或取代的芳烷硫基; Y是氢原子或卤素原子; R1是具有3至15个碳原子的亚烷基或亚烯基; Z是羟甲基，低级烷氧基甲基，未取代或取代的芳氧基甲基，四氢吡喃氧基甲基，四氢呋喃氧基甲基，未取代或取代的芳基磺酰氧基甲基，低级烷硫基甲基，未取代或取代的芳基硫代甲基，低级烷基亚磺酰基甲基，未取代或取代的芳基亚磺酰基甲基，低级烷基磺酰基甲基，未取代或取代的芳基磺酰基甲基，氨基甲基，-CH2NHR2（ 其中R 2是低级烷基，未取代或取代的芳烷基或未取代或取代的芳基），-CH 2 NR 3 R 4（其中R 3和R 4是低级烷基，未取代或取代的芳烷基，或未取代或取代的芳基），-CH 2 N + R 5 R 6 R 7（其中R 5，R 6 ，R 7为低级烷基，未取代或取代的芳烷基或未取代或取代的芳基，其中抗衡离子为酸或羟基离子的阴离子），-COR8（其中R8为氢原子，低级烷基或羟基），-CH （OR 9）2（其中R 9为低级烷基），亚氨基甲基，羟基亚氨基甲基或卤素 原子及其盐可以非常强烈地抑制脂氧合酶，并显着抑制其代谢物的产生和释放，因此可用作由脂氧合酶代谢物引起的疾病的预防和治疗剂。