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.
本发明涉及一种新的杂环化合物,其含有一个烷氧羰基和一个取代甲基基团,以及制备这些类似化合物和含有它们的药物组合物的过程。更具体地说,本发明涉及具有下列一般式(IVa)的化合物:##STR1## 其中R'为氢、2-乙氧羰基乙基、芳基或适用于酰胺临时保护的基团,Y'表示公式--COOZ或--CH.sub.2 M的基团,在其中Z为低级烷基,M为羟基、卤素、氰基或公式--O--SO.sub.2R.sup.2的基团,其中R.sup.2为低级烷基或芳基,但是如果R'为苯基,则Y'不能代表--COOC.sub.2H.sub.5基团。本发明还涉及一种制备具有下列一般式(IV)的化合物的方法:##STR2## 其中R和Y与R'和Y'相同,除了上述规定。根据本发明的另一方面,提供了含有一般式(IVa)的化合物作为活性成分的药物组合物,首先具有抗低氧活性。