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.
本发明涉及公式为##STR1##的蒽酮衍生物,其中虚线是可选的键,R.sup.1是氢,卤素或硝基,R.sup.2是氢或较低的烷基,R.sup.3和R.sup.4中的一个是氢或较低的烷基,另一个与R一起形成一个额外的键,A是较低的烷基,R.sup.5是含氮的5-成员芳香杂环,可选择地低烷基取代,氨基或##STR2##组,符号是5-或6-成员,可选择地低烷基取代的饱和杂环,其可以作为环成员包含氧或硫或##N(B).sub.n--A.sup.1--R.sup.6,B是--CO--,--COO--或--SO.sub.2--基团,n是数字0或1,A.sup.1是较低的烷基,R.sup.6是氢,氨基,较低的烷基氨基或二(较低的烷基)氨基,R.sup.7是氢或较低的烷基,以及其制备方法和基于其的制药组合物的医药上可接受的酸盐。