Novel heterocyclic substituted pyrazinoylguanidines, processes for preparing and a pharmaceutical composition containing the same
申请人:Merck & Co., Inc.
公开号:EP0017152A1
公开(公告)日:1980-10-15
The case involves novel heterocyclic substituted pyrazinoylguanidines, their pharmaceutically acceptable non-toxic addition salts and a process for preparing same. The novel pyrazinoylguanidines have the general formula
wherein
R2 is hydrogen, lower alkyl having from 1 to 5 carbon atoms;
R2 is hydrogen, lower alkyl having 1 to 5 carbon atoms;
R3 is a 5 or 6 membered heterocyclic ring containing from 1 to 3 heterocyclic atoms selected from the elements N. α or S, said ring containing from 0 to 2 substituents selected from lower alkyl having 1 to 5 carbon atoms, halo, oxy or hydroxy;
X is halo.
They are eukalemic agents possessing diuretic and natriuretic properties.
本案涉及新型杂环取代的吡嗪酰胍类化合物、其药学上可接受的无毒加成盐及其制备方法。新型吡嗪酰胍的通式为
其中
R2 是氢、具有 1 至 5 个碳原子的低级烷基;
R2 是氢、具有 1 至 5 个碳原子的低级烷基
R3 是 5 或 6 个成员的杂环,含有 1 至 3 个选自 N、α 或 S 元素的杂环原子,所述环含有 0 至 2 个选自具有 1 至 5 个碳原子的低级烷基、卤代、氧基或羟基的取代基;
X 为卤代。
它们是具有利尿和利钠特性的真核生物制剂。