申请人:ZENECA LIMITED
公开号:EP0505122A1
公开(公告)日:1992-09-23
The invention concerns α,α-dialkylbenzyl derivatives of the formula I
wherein Ar¹ is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;
A¹ is a direct link to X¹ or is (1-3C)alkylene;
X¹ is oxy, thio, sulphinyl or sulphonyl;
the phenylene group may optionally bear one or two substituents R³;
each of R¹ and R², which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R¹ and R² are not methyl or fluoromethyl; and
Q is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;
or a pharmaceutically-acceptable salt thereof;
processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
本发明涉及式 I 的 α、α-二烷基苄基衍生物
其中 Ar¹ 是苯基或萘基,或含有一个或两个氮杂原子并可选择含有一个选自氮、氧和硫的杂原子的 10 元双环杂环分子;
A¹ 与 X¹ 直接相连或为(1-3C)亚烷基;
X¹ 是氧基、硫代、亚砜基或磺酰基;
亚苯基可任选带有一个或两个取代基 R³;
R¹和 R²(可以相同或不同)各自是(1-4C)烷基、(2-4C)烯基、(2-4C)炔基、氟-(1-4C)烷基、苯基或苯基-(1-4C)烷基,条件是 R¹ 和 R² 都不是甲基或氟甲基;以及
Q 是氰基、氨基、硝基、甲酰基、(1-4C)烷氧基、噻唑基或 (2-4C)烷酰基;
或其药学上可接受的盐;
它们的制造工艺;含有它们的药物组合物以及它们作为 5-脂氧合酶抑制剂的用途。