申请人:Eli Lilly and Company
公开号:US04396619A1
公开(公告)日:1983-08-02
Broad spectrum cephalosporin betaine antibiotics represented by the formula ##STR1## wherein R' is a heterocyclic ring, e.g. 2-aminothiazol-4-yl, 2-amino-1,3,5-thiadiazol-4-yl, or 2-aminopyridin-6-yl; R" is C.sub.1 -C.sub.4 alkyl, especially methyl, a substituted carbamoyl group, or a carboxy-substituted alkyl or cycloalkyl group; and R.sub.1 is isoquinolinium or a substituted isoquinolinium group are provided. Compounds wherein R.sub.1 is isoquinolinium are preferred especially syn-7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(isoquinolinium- 2-ylmethyl)-3-cephem-4-carboxylate. Pharmaceutical formulations and a method for treating infectious diseases comprising the use of the antibiotics are described.
提供了以公式 ##STR1## 代表的广谱头孢菌素甜菜碱抗生素,其中R'是杂环环,例如2-氨基噻唑-4-基,2-氨基-1,3,5-噻二唑-4-基或2-氨基吡啶-6-基; R"是C.sub.1-C.sub.4烷基,特别是甲基,取代的氨基甲酰基团或羧基取代的烷基或环烷基团; R.sub.1是异喹啉或取代的异喹啉基团。首选R.sub.1为异喹啉的化合物,特别是syn-7-[2-(2-氨基噻唑-4-基)-2-甲氧基亚氨基乙酸酰胺]-3-(异喹啉-2-基甲基)-3-头孢烯-4-羧酸酯。描述了含有这些抗生素的制药配方和治疗传染病的方法。