申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US04435322A1
公开(公告)日:1984-03-06
The invention relates to new heterocyclic compound containing an alkoxycarbonyl and a substituted methyl group a process for the preparation of these and analogeous compound and pharmaceutical compositions containing them. More particularly, the invention concerns compounds of the general formula (IVa) ##STR1## wherein R' is hydrogen, 2-ethoxycarbonylethyl, aryl or a group suitable for a temporary protection of amides and Y' represents a group of the formula --COOZ or --CH.sub.2 M, in which Z is lower alkyl and M is hydroxyl, halogen, cyano or a group of the formula --O--SO.sub.2 R.sup.2, in which R.sup.2 is lower alkyl or aryl, with the proviso that if R' is phenyl, Y' cannot stand for the group --COOC.sub.2 H.sub.5. The invention further relates to a process for the preparation of compounds of the general formula (IV) ##STR2## in which R and Y are identical with R' and Y', respectively, except the proviso. According to a further aspect of the invention there are provided pharmaceutical compositions, first of all with antihypoxic activity, comprising compounds of the general formula (IVa) as active ingredient.
该发明涉及一种新的含有烷氧羰基和取代甲基基团的杂环化合物,以及制备这些类似化合物和制药组合物的方法。更具体地,该发明涉及具有一般式(IVa)的化合物,其中R'是氢、2-乙氧羰基乙基、芳基或适用于酰胺的暂时保护基团,Y'表示具有以下结构的基团--COOZ或--CH.sub.2 M,其中Z是较低的烷基,M是羟基、卤素、氰基或具有以下结构的基团--O--SO.sub.2 R.sup.2,其中R.sup.2是较低的烷基或芳基,但如果R'为苯基,则Y'不能表示基团--COOC.sub.2 H.sub.5。该发明还涉及一种制备一般式(IV)化合物的方法,其中R和Y与R'和Y'相同,除了上述规定外。根据该发明的另一个方面,提供了首先具有抗缺氧活性的药物组合物,其包括作为活性成分的一般式(IVa)化合物。