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    • 2. 发明授权
    • (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and
aryalkynylarylurea inhibitors of 5-lipoxygenase
    • (4-烷氧基吡喃-4-基)取代的芳基烷基芳基 - 芳烯基芳基和芳氧基炔基芳基脲抑制剂5-脂氧合酶
    • US5432194A
    • 1995-07-11
    • US236001
    • 1994-05-09
    • Joseph F. DellariaAnwer BashaLawrence A. BlackLinda J. CherneskyWendy Lee
    • Joseph F. DellariaAnwer BashaLawrence A. BlackLinda J. CherneskyWendy Lee
    • C07D309/12C07D405/12A61K31/35C07D309/10
    • C07D405/12C07D309/12
    • Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    • 其中W选自其中Q是氧或硫的结构的化合物,R6和R7是氢或烷基,或R6和R7与它们所连接的氮原子一起定义为 烷基,卤代烷基,任选取代的苯基,羟基烷基,氨基烷基,羧基烷基,(烷氧基羰基)烷基和(烷基氨基羰基)烷基; Z是-CH 2 - ,氧,硫或-NR 9,其中R 9是氢或烷基,L 1和L 2选自价键,亚烷基,亚丙烯基和亚丙炔基,R 1,R 2,R 3和R 4独立地选自烷基 卤素,卤素,氰基,氨基,烷氧基羰基和二烷基氨基羰基,Y选自氧,-NR10,其中R10是氢或烷基,和其中n = 0,1或2,R5是烷基,抑制 白三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。