申请人:ZENECA LIMITED
公开号:EP0462830A2
公开(公告)日:1991-12-27
The invention concerns a cyclic ether derivative of the formula I
wherein Ar1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety ;
A1 is a direct link to X1 or (1-3C)alkylene;
X1 is oxy, thio, sulphinyl, sulphonyl or imino;
Ar2 is optionally substituted phenylene or pyridylene ;
R1 includes hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl and (1-4C)alkylthio; and
R2 and R3 together form a group of the formula -A2-X2-A3- which, together with the carbon atom to which A2 and A3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A2 and A3 is (1-3C)alkylene and X2 is oxy, thio, sulphinyl or sulphonyl ; or a pharmaceutically-acceptable salt thereof.
The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
本发明涉及一种式 I 的环醚衍生物
其中 Ar1 是任选取代的苯基、萘基或 9 或 10 元双环杂环分子;
A1 是与 X1 或(1-3C)亚烷基的直接连接;
X1 是氧基、硫代、亚砜基、磺酰基或亚氨基;
Ar2 是任选取代的亚苯基或亚吡啶;
R1 包括氢、(1-4C)烷基、(1-4C)烷氧羰基和(1-4C)烷硫基;以及
R2 和 R3 共同形成一个式-A2-X2-A3-的基团,该基团与 A2 和 A3 所连接的碳原子一起定义一个具有 5 至 7 个环原子的环,其中 A2 和 A3 各为 (1-3C)烷基,X2 为氧基、硫基、亚砜基或磺酰基;或其药学上可接受的盐。
本发明的化合物是 5-脂氧合酶的抑制剂。