申请人:ORTHO PHARMACEUTICAL CORPORATION
公开号:EP0176333A2
公开(公告)日:1986-04-02
The synthesis of 5,6-dioxy substituted quinazolinediones is described. The novel quinazolinediones are useful as cardiotonic agents, and have the formula
wherein R, and R2 are the same or different substituents and are hydrogen, lower alkyl or methylenedioxy when taken together; Y and Z are the same or different and are hydrogen, nitro, amino, acetamido, alkylamino,alkyl, cycloalkylamino and cycloalkyldiamino, carboxy, carboalkoxy, cyano, methanesulfonyl, carboxamido and halo; R3 is hydrogen, alkyl, hydroxylakyl, haloalkyl, amino, dialkylamino, dialkylamino alkyl, cycloalkylamino, cycloalkylaminoalkyl, phenyl, substituted phenyl; R4 is hydrogen, lower alkyl, carboalkoxy and wherein R6 is hydrogen or lower alkyl; X is carboxyl, carboalkosy, cyano, carboxamido, methanesulfonyl, formyl, benzoyl and substituted benzoyl and the pharmaceutically acceptable salts thereof; provided that when R3 is amino or alkylamino, Y and Z are not simultaneously hydrogen.
本文描述了 5,6-二氧基取代的
喹唑啉二酮的合成过程。新型
喹唑啉二酮可用作强心剂,其式如下
其中 R 和 R2 是相同或不同的取代基,合在一起时为氢、低级烷基或亚甲基二氧基;Y 和 Z 是相同或不同的取代基,合在一起时为氢、硝基、
氨基、乙酰
氨基、烷基
氨基、烷基、环烷基
氨基和环烷基二
氨基、羧基、羧基烷氧基、
氰基、甲磺酰基、羧酰胺基和卤基;R3 是氢、烷基、羟烷基、卤代烷基、
氨基、二烷基
氨基、二烷基
氨基烷基、环烷基
氨基、环烷基
氨基烷基、苯基、取代苯基; R4 是氢、低级烷基、羧基烷氧基,其中 R6 是氢或低级烷基;X 为羧基、羧基烷氧基、
氰基、羧酰胺基、甲磺酰基、甲酰基、苯甲酰基和取代苯甲酰基及其药学上可接受的盐;但当 R3 为
氨基或烷基
氨基时,Y 和 Z 不能同时为氢。