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N-hydroxyureas as 5-lipoxygenase inhibitors and inhibitors of oxidative modification of low density lipoprotein

机译:N-羟基脲作为5-脂氧合酶抑制剂和低密度脂蛋白氧化修饰的抑制剂

摘要

This invention relates to compounds having 5-lipoxygenase inhibiting properties and inhibition of oxidative modification of low density lipoprotein which have the formula: ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C. sub.1 -C. sub.6 alkoxy, trifluoromethyl, or C.sub.1 -C.sub.6 trifluoroalkoxy; PPR.sub.2 is hydrogen or methyl;P PR.sup.4 is hydrogen, methyl or hydroxy;PPR.sup.5 is hydrogen, --NH. sub.2, C.sub.1 -C.sub.6 alkyl, aryl, aralkyl, or -- N═C(CH.sub.3).sub. 2 ;PPX and Y are independently O or S; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. Compounds which inhibit 5- lipoxygenase are useful in the treatment of diseases mediated by leukotrienes such as inflammation or bronchoconstriction. Compounds which inhibit oxidative metabolism of low density lipoprotein are useful in the inhibition of atherosclerotic plaque formation.
机译:本发明涉及具有抑制5-脂氧合酶性能和抑制低密度脂蛋白氧化修饰的化合物,其分子式为:其中R.sup.1和R.sup.3分别是氢,卤素,C 1 -C 6烷基,C 1 -C。 sub.6烷氧基,三氟甲基或C1 -C.sub.6三氟烷氧基;

R.sub.2是氢或甲基;

R.sup.4是氢,甲基或羟基; P 5 R是氢,-NH。 sub.2,Csub.1 -Csub.6烷基,芳基,芳烷基或-N═ C(CH.sub.3).sub。 2;

X和Y独立地为O或S; n为0或1;或其药学上可接受的盐。抑制5-脂氧合酶的化合物可用于治疗由白三烯介导的疾病,例如炎症或支气管收缩。抑制低密度脂蛋白氧化代谢的化合物可用于抑制动脉粥样硬化斑块的形成。

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