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    Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity
    5.
    发明授权
    Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity 失效
    芳基烷基醚和芳烷基硫醚抑制剂的脂氧合酶活性

    公开(公告)号：US5183818A

    公开(公告)日：1993-02-02

    申请号：US750362

    申请日：1991-08-27

    申请人： Dee W. Brooks ,  Andrew O. Stewart ,  Jonathan G. Martin

    发明人： Dee W. Brooks ,  Andrew O. Stewart ,  Jonathan G. Martin

    IPC分类号： C07D307/38 ,  C07D307/42 ,  C07D333/16 ,  C07D333/34 ,  C07D333/56 ,  C07D495/04

    CPC分类号： C07D307/42 ,  C07D307/38 ,  C07D333/16 ,  C07D333/34 ,  C07D333/56 ,  C07D495/04

    摘要： The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.1 is absent or is divalent alkylene of from one to six carbon atoms, and Q.sub.2 is divalent alkylene from from two to ten carbon atoms.The group Z is N(OR.sub.1)COR.sub.2 where R.sub.1 is selected from hydrogen or a pharmaceutically suitable salt. R.sub.2 is selected from hydrogen; alkyl; cycloalkyl; amino; alkylamino, optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; dialkylamino in which the alkyl groups are independently are optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; cycloalkylamino; 2-hydroxyethylamino; N-morpholino; N-thiomorpholino; N-piperazine; N'-alkyl-N-piperazine and cyclopropylmethylamino.

    摘要翻译： 本发明提供具有抑制脂氧合酶，特别是5-脂氧合酶的催化作用的结构为Y-Het- [Q1] -X- [Q2] -Z的化合物，从而减少白三烯B4，C4，D4的生物合成， 和E4。 在上述通式中，X是氧或硫，Het是选自呋喃基，噻吩基，2-，3-和4-吡啶基，2-和3-苯并[b]呋喃基的杂芳基， 2-和3-苯并[b]噻吩基和噻吩并噻吩基。 Y是一个或两个独立地选自氢，羟基，卤素，氰基，烷基，卤代烷基，烷氧基，烷硫基，烷氧基芳基），烷基硫代芳基，芳基烷氧基，芳基烷硫基，芳氧基，芳硫基，烷基酰氨基，环烷基，烷酰基，烷氧基羰基，氨基，烷基氨基， 二烷基氨基和下列基团，其中R 1在每次出现时独立地选自氢和1至6个碳原子的烷基：-CRROR，-NRC（O）R，-NRC（O）OR和-C（O ）NRR。 基团Q1不存在或为1至6个碳原子的二价亚烷基，Q 2为2至10个碳原子的二价亚烷基。 基团Z是N（OR 1）COR 2，其中R 1选自氢或药学上合适的盐。 R2选自氢; 烷基; 环烷基 氨基; 任选被羟基，卤素，烷氧基或羧基取代的烷基氨基; 其中烷基独立的二烷基氨基任选被羟基，卤素，烷氧基或羧基取代; 环烷基氨基; 2-羟基乙基氨基; N-吗啉代; N-硫代吗啉代 N-哌嗪; N'-烷基-N-哌嗪和环丙基甲基氨基。