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    Lipoxygenase and cyclooxygenase inhibiting compounds
    3.
    发明授权
    Lipoxygenase and cyclooxygenase inhibiting compounds 失效
    脂氧合酶和环加氧酶抑制化合物

    公开(公告)号：US5516789A

    公开(公告)日：1996-05-14

    申请号：US421125

    申请日：1995-04-12

    申请人： Clint D. W. Brooks ,  Andrew O. Stewart ,  Anwer Basha ,  Randy L. Bell

    发明人： Clint D. W. Brooks ,  Andrew O. Stewart ,  Anwer Basha ,  Randy L. Bell

    IPC分类号： C07C275/64 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58 ,  C07D409/12 ,  A61K31/405 ,  C07D209/14

    CPC分类号： C07D409/12 ,  C07C275/64 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58

    摘要： Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z--COOH.

    摘要翻译： 具有结构或其药学上可接受的盐的化合物具有作为环氧合酶和5-脂氧合酶抑制剂的活性，降低白细胞三烯B4，C4，D4和E4以及环加氧酶产物如前列腺素和血栓烷的生物合成，并且可用于 治疗炎症和过敏性疾病状态。 化合物具有上述结构，其中A选自（a）光学取代的碳环芳基，（b）光取代的呋喃基，（c）光取代的苯并[b]呋喃基，（d）最佳取代的噻吩基，（e） 吡啶基氧基，（f）选择性取代的吡啶基烷基，（g）最佳取代的苯并[b]噻吩基，（h）最佳取代的吡啶基，（i）最佳取代的喹啉基和（j） X选自（a）任选取代的烷基，（b）光学取代的烯基和（c）最佳取代的炔基; R 1和R 2独立地选自氢，羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。