申请人:Abbott Laboratories
公开号:US05426111A1
公开(公告)日:1995-06-20
Compounds of formula ##STR1## Ar is selected from (a) phenyl, (b) phenyl substituted with one or more groups selected from halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl, (c) furyl, (d) furyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (e) pyridyl, (f) pyridyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (g) thienyl, and (h) thienyl substituted with one or more groups selected from halogen, alkyl, and alkoxy; L is selected from alkylene of one to three carbon atoms, alkenylene of two to three carbon atoms, and alkynylene of two to three carbon atoms, and ##STR2## wherein p is an integer of 1 to 4, inclusive, and R.sup.4 is selected from the group consisting of hydrogen, alkyl of one to four carbon atoms, halogen, haloalkyl of one to four carbon atoms, and alkoxy of one to six carbon atoms; R.sup.1 is alkyl; R.sup.2 is hydrogen or alkyl; m is 1 or 2; Z is oxygen or CHOR.sup.3, and n is 0 or 1 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
公式为 ##STR1## 的化合物,其中 Ar 选自 (a) 苯基,(b) 被卤素、
氰基、烷基、卤代烷基、烷氧基和烷氧羰基等一种或多种基团取代的苯基,(c)
呋喃基,(d) 被卤素、烷基和烷氧基等一种或多种基团取代的
呋喃基,(e)
吡啶基,(f) 被卤素、烷基和烷氧基等一种或多种基团取代的
吡啶基,(g)
噻吩基,和 (h) 被卤素、烷基和烷氧基等一种或多种基团取代的
噻吩基;L 选自一至三个碳原子的烷基,二至三个碳原子的烯基和二至三个碳原子的炔基,以及 ##STR2## 其中 p 为 1 至 4 的整数,R.sup.4 选自氢、一至四个碳原子的烷基、卤素、一至四个碳原子的卤代烷基和一至六个碳原子的烷氧基;R.sup.1 为烷基;R.sup.2 为氢或烷基;m 为 1 或 2;Z 为氧或 CHOR.sup.3;n 为 0 或 1,这些化合物是脂氧合酶酶的有效
抑制剂,因此抑制了
白三烯的
生物合成。这些化合物在治疗或缓解过敏和炎症疾病状态方面很有用。