申请人:E. R. Squibb & Sons, Inc.
公开号:US04721725A1
公开(公告)日:1988-01-26
Aryl-cyclopenta- and arylcyclohexa[b]pyrrole derivatives are provided having the structure ##STR1## wherein n is 1 or 2; X is --OR.sup.1 or --NR.sup.2 R.sup.3 wherein R.sup.1 is H, lower alkyl, cycloalkyl, aryl, aralkyl or cycloalkylalkyl, and R.sup.2 and R.sup.3 may be the same or different and are H, lower alkyl, cycloalkyl, aryl, aralkyl or cycloalkylalkyl; Y is --OR.sup.4 or --NR.sup.5 R.sup.6 wherein R.sup.4 is H or lower alkyl, and R.sup.5 and R.sup.6 are the same or different and are H or lower alkyl; and Z is aryl. These compounds are useful in inhibiting the 5-lipoxygenation of arachadonic acid in RBL-1 cells and preventing leukotriene formation in macrophages and as such are useful as antiallergy agents and in treating inflammation and psoriasis.
提供了具有结构##STR1##的芳基环戊二烯和芳基环己二烯[b]吡咯衍生物,其中n为1或2;X为--OR.sup.1或--NR.sup.2R.sup.3,其中R.sup.1为H、较低烷基、环烷基、芳基、芳基烷基或环烷基烷基,而R.sup.2和R.sup.3可以相同也可以不同,为H、较低烷基、环烷基、芳基、芳基烷基或环烷基烷基;Y为--OR.sup.4或--NR.sup.5R.sup.6,其中R.sup.4为H或较低烷基,而R.sup.5和R.sup.6可以相同也可以不同,为H或较低烷基;Z为芳基。这些化合物在抑制RBL-1细胞中花生四烯酸的5-脂氧合作用以及在巨噬细胞中预防白三烯形成方面是有用的,因此可用作抗过敏剂,并用于治疗炎症和银屑病。