申请人:Imperial Chemical Industries PLC
公开号:US05225438A1
公开(公告)日:1993-07-06
The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula --X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 -- wherein X.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl; each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene; X.sup.2 is oxy, thio, sulphinyl or sulphonyl; R.sup.1 is (1-4C)alkyl; and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.3 is oxy, thio, sulphinyl or sulphonyl; which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.
这项发明涉及一种公式I的芳基衍生物,其中Ar.sup.1是可选择地取代的苯基、萘基或杂环基,而X.sup.1是氧、硫、砜基、砜酰基、二氟甲基、亚胺、(1-4C)烷基亚胺或可选择地取代的(1-4C)烷基烯,或者X.sup.1是公式--X.sup.4 --CR.sub.2 --或--CR.sub.2 --X.sup.4 --的基团,其中X.sup.4是氧、硫、砜基、砜酰基或羰基,每个R是氢、甲基或乙基;Ar.sup.2和Ar.sup.3中的每一个都是可选择地取代的苯基;X.sup.2是氧、硫、砜基或砜酰基;R.sup.1是(1-4C)烷基;R.sup.2和R.sup.3共同形成公式--A.sup.1 --X.sup.3 --A.sup.2 --的基团,其中与A.sup.1和A.sup.2连接的碳原子一起定义具有5到7个环原子的环,其中每个A.sup.1和A.sup.2是(1-3C)烷基,而X.sup.3是氧、硫、砜基或砜酰基;这些化合物是5-脂氧合酶的抑制剂,并且在治疗炎症或过敏性疾病中有用。