申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0375404A2
公开(公告)日:1990-06-27
The invention concerns a heterocyclic derivative of the formula I,
wherein Ar¹ is optionally substituted phenyl or naphthyl;
A¹ is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;
Ar² is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;
R¹ is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and
R² and R³ together form a group of the formula -A²-X-A³- wherein each of A² and A³ is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino;
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 的杂环衍生物、
其中 Ar¹ 是任选取代的苯基或萘基;
A¹是(1-6C)亚烷基、(3-6C)烯基、(3-6C)炔基或环(3-6C)亚烷基;
Ar² 是任选取代的亚苯基,或含有最多三个氮原子的 6 位杂环分子;
R¹ 是氢、(1-6C)烷基、(3-6C)烯基、(3-6C)炔基、氰基-(1-4C)烷基或(2-4C)烷酰基,或任选取代的苯甲酰基;和
R² 和 R³ 共同形成式 -A²-X-A³- 的基团,其中 A² 和 A³ 均为 (1-4C)亚烷基,X 为氧基、硫代、亚砜基、磺酰基或亚氨基;
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。