申请人:Imperial Chemical Industries
公开号:US05208259A1
公开(公告)日:1993-05-04
The invention concerns a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; X.sup.1 is oxy, thio, sulphinyl or sulphonyl; Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms; R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-4C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino. The invention also concerns processes for the manufacture of a diaryl ether heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said heterocycle. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
本发明涉及式I的二芳基醚杂环化合物或其药学上可接受的盐,其中Ar.sup.1是可选取代的苯基或萘基;X.sup.1是氧、硫、亚磺酰基或磺酰基;Ar.sup.2是可选取代的苯基、或含有最多三个氮原子的6元杂环基;R.sup.1是(1-6C)烷基、(3-6C)烯基、(3-6C)炔基、氰基-(1-4C)烷基或可选取代的苯甲酰基;R.sup.2和R.sup.3共同形成式--A.sup.2--X.sup.2--A.sup.3--的基团,其中A.sup.2和A.sup.3各自是(1-4C)烷基,X.sup.2是氧、硫、亚磺酰基、磺酰基或亚胺基。本发明还涉及制备式I的二芳基醚杂环化合物或其药学上可接受的盐的方法,以及含有该杂环化合物的制药组合物。该化合物是5-脂氧合酶酶的抑制剂。