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    • 8. 发明公开
    • Heterocyclic derivatives
    • 杂环衍生物
    • EP0420511A2
    • 1991-04-03
    • EP90310332.3
    • 1990-09-21
    • IMPERIAL CHEMICAL INDUSTRIES PLCICI PHARMA
    • Crawley, Graham CharlesEdwards, Philip Neil
    • C07D405/12C07D409/12C07D401/12A61K31/47A61K31/50
    • C07D409/12C07D401/12C07D405/12
    • The invention concerns a heterocyclic derivative of the formula I
      wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;
      X¹ is oxy, thio, sulphinyl, sulphonyl or imino;
      Ar is phenylene which may optionally bear one or two substituents or
      Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;
      R¹ is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; and
      R² and R³ together form a group of the formula -A²-X²-A³- which, together with the carbon atom to which A² and A³ are attached, defines a ring having 4 to 7 ring atoms, wherein A² and A³, which may be the same or different, each is (1-4C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino;
      or a pharmaceutically-acceptable salt thereof.
      The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    • 本发明涉及式I的杂环衍生物,其中Q是含有一个或两个氮原子的任选取代的6元单环或10元双环杂环部分; X 1是氧,硫,亚磺酰基,磺酰基或亚氨基; Ar为可任选带有一个或两个取代基的亚苯基或Ar为含最多三个氮原子的任选取代的6-元杂环部分; (1-6C)烷基,(3-6C)链烯基或(3-6C)炔基; 并且R 2和R 3一起形成式-A 2 -X 2 -A 3 - 的基团,其与连接A 2和A 3的碳原子一起定义一个具有4-7个环原子的环,其中A 2和A 3可以 各自是(1-4C)亚烷基,X 2是氧,硫,亚磺酰基,磺酰基或亚氨基; 或其药学上可接受的盐。 本发明的化合物是5-脂氧合酶的抑制剂。
    • 10. 发明公开
    • Heterocyclic derivatives
    • 杂环衍生物
    • EP0381375A1
    • 1990-08-08
    • EP90300780.5
    • 1990-01-25
    • IMPERIAL CHEMICAL INDUSTRIES PLCICI PHARMA
    • Crawley, Graham CharlesEdwards, Martin Paul
    • C07D417/12A61K31/435A61K31/495
    • C07D417/12
    • The invention concerns a thiazole of the formula I,
      wherein Q¹ is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;
      X is oxy, thio, sulphinyl, sulphonyl or imino;
      Ar is phenylene which may optionally bear one or two substituents, or Ar is an optionally substituted 6-membered heterocyclene moiety contining up to three nitrogen atoms;
      R¹ is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;
      R² is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R² is optionally substituted benzoyl; and
      Q² is optionally substituted thiazolyl;
      or a pharmaceutically-acceptable salt thereof.
      The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.
    • 本发明涉及式I的噻唑,其中Q 1是含有一个或两个氮原子的任选取代的6元单环或10元双环杂环部分; X是氧基,硫基,亚磺酰基,磺酰基或亚氨基; Ar是可以任选地带有一个或两个取代基的亚苯基,或Ar是连续至多三个氮原子的任选取代的6元杂环烯基团; R 1是氢,(1-6C)烷基,(2-6C)烯基,(2-6C)炔基或取代的(1-4C)烷基; (1-6C)烷基,(3-6C)烯基,(3-6C)炔基或取代的(1-4C)烷基或R 2是任选取代的苯甲酰基; 和Q 2是任选取代的噻唑基; 或其药学上可接受的盐。 本发明还涉及制备式I的噻唑和含有所述噻唑的药物组合物的方法。