LIPOXYGENASE AND CYCLOOXYGENASE INHIBITING COMPOUNDS
    5.
    发明申请
    LIPOXYGENASE AND CYCLOOXYGENASE INHIBITING COMPOUNDS 审中-公开
    LIPOXYGENASE和CYCLOOXYGENASE抑制化合物

    公开(公告)号:WO1996032377A1

    公开(公告)日:1996-10-17

    申请号:PCT/US1996003907

    申请日:1996-03-22

    Abstract: Compounds having the structure of general formula (I) or a pharmaceutically acceptable salt thereof have activity as inhibitors of cyclooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 and cyclooxygenase 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) optionally susbtituted carbocyclic aryl, (b) optionally substituted furyl, (c) optionally substituted benzo[b]furyl, (d) optionally substituted thienyl, (e) optionally substituted pyridyloxy, (f) optionally substituted pyridylalkyl, (g) optionally substituted benzo[b]thienyl, (h) optionally substituted pyridyl, (i) optionally substituted quinolyl, and (j) optionally substituted indolyl; X is selected from (a) optionally susbtituted alkyl, (b) optionally substituted alkenyl, and (c) optionally substituted alkynyl; R and R 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.

    Abstract translation: 具有通式(I)结构的化合物或其药学上可接受的盐具有作为环加氧酶和5-脂氧合酶抑制剂的活性,降低了白三烯B4,C4,D4和E4以及环氧合酶产物如前列腺素和血栓素的生物合成, 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)任选取代的碳环芳基,(b)任选取代的呋喃基,(c)任选取代的苯并[b]呋喃基,(d)任选取代的噻吩基,(e) 吡啶基氧基,(f)任选取代的吡啶基烷基,(g)任选取代的苯并[b]噻吩基,(h)任选取代的吡啶基,(i)任选取代的喹啉基,和(j)任选取代的吲哚基; X选自(a)任选的取代的烷基,(b)任选取代的烯基,和(c)任选取代的炔基; 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。

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