申请人:ZENECA LIMITED
公开号:EP0385679A2
公开(公告)日:1990-09-05
The invention concerns a heterocyclic cyclic ether of the formula I
wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;
A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;
X is oxy, thio, sulphinyl, sulphonyl or imino;
Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ and R² together form a group of the formula -A²-X²-A³- which, together with the oxygen atom to which A² is attached and with the carbon atom to which A³ is attached, defines a ring having 5 to 7 ring atoms, wherein A² and A³ each is (1-3C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino, and which ring may bear one, two or three substituents; and
R³ is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;
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 的杂环环醚
其中 Q 是含有一个或两个氮原子的任选取代的 6 元单环或 10 元双环杂环分子;
A是(1-6C)亚烷基、(3-6C)烯基、(3-6C)炔基或环(3-6C)亚烷基;
X 是氧基、硫代、亚砜基、磺酰基或亚氨基;
Ar 是亚苯基,可任选带有一个或两个取代基,或者 Ar 是任选被取代的含有最多三个氮原子的六元杂环分子;
R¹ 和 R² 共同形成一个式 -A²-X²-A³- 的基团,该基团与 A² 所连接的氧原子和 A³ 所连接的碳原子共同定义一个具有 5 至 7 个环原子的环,其中 A² 和 A³ 各为 (1-3C)亚烷基,X² 为氧基、硫基、亚砜基、磺酰基或亚氨基,该环可带有一个、两个或三个取代基;以及
R³ 是氢、(1-6C)烷基、(2-6C)烯基、(2-6C)炔基或取代的(1-4C)烷基;
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。