首页> 外国专利> PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ANALYSIS (6 7R) -7 - ((Z) -2- (2-AMINOTIAZOL-4-YL) -2- (2-CARBOXIPROP-2-OXYMNO) -ACETAMIDO) -3- (1 -PYRIDINIUM METHYL) -CEF-3-EM-4-CARBOXYLA T

PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ANALYSIS (6 7R) -7 - ((Z) -2- (2-AMINOTIAZOL-4-YL) -2- (2-CARBOXIPROP-2-OXYMNO) -ACETAMIDO) -3- (1 -PYRIDINIUM METHYL) -CEF-3-EM-4-CARBOXYLA T

机译:治疗性分析的制备程序(6 7R)-7-((Z)-2-(2-氨基噻唑-4-基)-2-(2-羧甲基-2-氧肟基-乙酰氨基)-3-(1 -吡啶基甲基)-CEF-3-EM-4-羧甲基苯丙酸酯

摘要

Cephalosporin antibiotics of the general formula IMAGE (I) (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group or Ra and Rb together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group; and R4 represents hydrogen or a 3- or 4-carbamoyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimono) acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4 carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of such antibiotics.
机译:通式(I)的头孢菌素抗生素(其中Ra和Rb可以相同或不同,分别代表C1-4烷基或Ra和Rb与它们所连接的碳原子一起形成a C3-7亚环烷基;和R4代表氢或3-或4-氨基甲酰基)表现出广谱抗生素活性,该活性对革兰氏阴性生物如假单胞菌生物菌株异常高。 (6R,7R)-7-[(Z)-2-(2-氨基噻唑-4-) yl)-2-(2-羧基丙-2-氧基单)乙酰胺基] -3-(1-吡啶鎓甲基)-ceph-3-em-4羧酸酯。本发明还包括式(I)化合物的无毒盐和无毒代谢不稳定的酯。还描述了含有本发明抗生素的组合物和制备此类抗生素的方法。

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