Pyridine derivatives and intermediates thereof
    3.
    发明公开
    Pyridine derivatives and intermediates thereof 失效
    Pyridinderivate和Zwischenprodukte。

    公开(公告)号:EP0347831A2

    公开(公告)日:1989-12-27

    申请号:EP89111177.5

    申请日:1989-06-20

    摘要: A pyridine derivative of formula

    wherein X¹-X² represents
    wherein
    wherein R⁴ represents hydrogen alkyl or a substituted or unsubstituted aralkyl; R⁵ reoresents a hydrogen, alkoxy or alkylthio and R⁶ and R⁸, which may be the same or different, each represent hydrogen, alkyl or alkenyl, R⁷ represents hydrogen or R⁶ and R⁷ are taken together to form
    wherein R⁹ represents alkyl; and m represents an integer of from 1 to 3; and any one of a, b, and c represents a nitrogen or an N-oxide (N→O), with the other two representing a carbon atom, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A₂ and is useful in the treatment and prevention of a broad range of diseases.

    摘要翻译: 的吡啶衍生物,其中X 1 -X 2表示CHEM> CHEM,其中R 4表示氢烷基或取代或未取代的芳烷基; R 5表示氢,烷氧基或烷硫基,R 6和R 8可以相同或不同,各自表示氢,烷基或烯基,R 7表示氢或R 6,和 R 7一起形成,其中R 9表示烷基; m表示1〜3的整数, a,b和c中的任一个表示氮或N-氧化物(N-> O),另外两个表示碳原子,其表现出对凝血恶烷生物合成的选择性,潜在和持久的抑制活性 A2,可用于治疗和预防广泛的疾病。

    Quinoline-n-oxide derivative and pharmaceutical composition
    5.
    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

    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.