申请人:Hoffman-La Roche Inc.
公开号:US04711889A1
公开(公告)日:1987-12-08
The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond, A is lower alkylene, R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.
该发明涉及以下结构的苦橙酮衍生物:其中虚线是一个可选键,R.sup.1是氢、卤素或硝基,R.sup.2是氢或较低烷基,R.sup.3和R.sup.4中的一个是氢或较低烷基,另一个与R一起是一个额外的键,A是较低烷基,R.sup.5是一个含氮的5-成员环,可选择地是较低烷基取代的芳香杂环,氨基或该基团,符号是一个5-或6-成员的,可选择地是较低烷基取代的饱和杂环,其中环成员可以是氧或硫,或者是该基团,B是基团--CO--,--COO--或--SO.sub.2--,n是数字0或1,A.sup.1是较低烷基,R.sup.6是氢,氨基,较低烷基氨基或二(较低烷基)氨基,R.sup.7是氢或较低烷基,以及其药学上可接受的酸盐,其制备和基于此的制药组合物。