申请人:Takeda Chemical Industries, Ltd.
公开号:US05491145A1
公开(公告)日:1996-02-13
Novel compound of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R.sup.2 or R.sup.3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O).sub.p (p stands for an integer from 0 to 2; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for a hydrogen atom, an optionally substituted lower lakyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.7 may, taken together with the adjacent nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group; m stands for an integer from 0 to 4; and n stands for an integer from 0 to 4, or a salt thereof, which has excellent anti-PAF activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.
通用公式的新化合物:其中R.sup.1代表氢原子、可选择取代的低烷基基团或卤原子;R.sup.2和R.sup.3分别代表氢原子或可选择取代的低烷基基团,但R.sup.2或R.sup.3中的一个是氢原子,另一个是可选择取代的低烷基基团,或R.sup.2和R.sup.3可以与相邻的--C=C--基团一起形成5-至7-成员环;X代表氧原子或S(O).sub.p(p为0至2的整数);Y代表以下式的基团:其中R.sup.4和R.sup.5分别代表氢原子或可选择取代的低烷基基团,或源自可选择取代的3-至7-成员同环或异环环的双价基团;R.sup.6和R.sup.7分别代表氢原子、可选择取代的低烷基基团、可选择取代的环烷基基团或可选择取代的芳基基团,或R.sup.6和R.sup.7可以与相邻的氮原子一起形成可选择取代的含氮杂环基团;m为0至4的整数;n为0至4的整数,或其盐,具有优异的抗PAF活性,是一种抗哮喘药物,以及其制备、中间体和药物组成。