申请人:KOWA COMPANY, LTD.
公开号:EP0067561A2
公开(公告)日:1982-12-22
Novel piperazine derivatives represented by the following formula:
wherein
R, is an indolyl group which may optionally be substituted by one or more lower alkyl and/or lower alkoxy groups, a naphthyl group which may optionally be partially saturated with 2 or 4 hydrogen atoms, or a phenyl or cyclohexyl group which may optionally be substituted by one or more lower alkyl groups;
A is a single bond or an alkylene group;
P is a single bond or a vinylene group;
Q is an -O-alkylene group or an -NH-alkylene group when P is a single bond, or a single bond when P is a vinylene group; and
R2 is a lower alkyl, morpholino-lower alkyl, morpholinocarbonyl lower alkyl, piperidinocarbonyl lower alkyl, piperazinocarbonyl lower alkyl or lower alkylaminocarbonyl lower alkyl group,
and acid addition salts thereof are described, which are proteolytic enzyme inhibitors. Processes for preparing the novel derivatives are described.
下式所代表的新型哌嗪衍生物:
其中
R,是吲哚基,可任选被一个或多个低级烷基和/或低级烷氧基取代;R,是萘基,可任选被 2 个或 4 个氢原子部分饱和;R,是苯基或环己基,可任选被一个或多个低级烷基取代;
A 是单键或亚烷基;
P 是单键或乙烯基;
Q 是-O-亚烷基或-NH-亚烷基(当 P 为单键时),或单键(当 P 为乙烯基时);以及
R2 是低级烷基、吗啉低级烷基、吗啉羰基低级烷基、哌啶羰基低级烷基、哌嗪羰基低级烷基或低级烷基氨基羰基低级烷基、
及其酸加成盐,它们是蛋白水解酶抑制剂。还介绍了制备这些新型衍生物的工艺。