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    Quinoline-n-oxide derivative and pharmaceutical composition
    1.
    发明公开
    Quinoline-n-oxide derivative and pharmaceutical composition 失效
    喹啉N-氧化物衍生物和药物制剂。

    公开(公告)号：EP0177764A1

    公开(公告)日：1986-04-16

    申请号：EP85111243.3

    申请日：1985-09-05

    申请人： KYOWA HAKKO KOGYO CO., LTD.

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

    IPC分类号： C07D215/60 ,  C07D405/12 ,  A61K31/47

    CPC分类号： C07D405/12 ,  C07D215/60

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

    Imidazonaphthyridine derivatives
    5.
    发明公开
    Imidazonaphthyridine derivatives 失效
    咪唑并萘啶衍生物

    公开(公告)号：EP0459505A1

    公开(公告)日：1991-12-04

    申请号：EP91108908.4

    申请日：1991-05-31

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Fumio ,  Kuroda, Takeshi ,  Kitamura, Shigeto ,  Ohmori, Kenji

    IPC分类号： C07D471/14 ,  A61K31/435

    CPC分类号： C07D471/14

    摘要： Disclosed are imidazonaphthyridine derivatives represented by formula (I)

    wherein:
       R¹ represents lower alkyl or substituted or unsubstituted aryl; and
       X-Y-Z represents

    wherein R² represents hydrogen, lower alkyl, alkenyl, aralkenyl, or -C(R⁵)H-(CH₂) n -R⁴ (wherein R⁴ represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR⁶R⁷ wherein R⁶ and R⁷ independently represents hydrogen or lower alkyl; R⁵ represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R³ represents hydrogen, mercapto, hydroxy, lower alkyl, or aryl
    and pharmaceutically acceptable salts thereof.
    The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.

    摘要翻译： 公开了由式（I）表示的咪唑并萘啶衍生物，其中：R 1代表低级烷基或取代或未取代的芳基; XYZ表示其中R 2代表氢，低级烷基，烯基，芳烯基或-C（R 5）H-（CH 2）n -R 4（其中R 4代表取代或未取代的芳基，取代或未取代的吡啶基，取代或未取代的呋喃基， 低级链烷酰基，羧基，低级烷氧基羰基，环烷基，羟基，低级烷氧基，卤素或NR 6 R 8，其中R 6和R 7独立地代表氢或低级烷基; R 5代表氢，低级烷基或苯基;以及n 表示0至3的整数）; 和R 3代表氢，巯基，羟基，低级烷基或芳基及其药学上可接受的盐。 该化合物显示出强效的抗炎，抗过敏和支气管扩张活性。