Cephalosporin compounds, process for their preparation and pharmaceutical compositions
申请人:BEECHAM GROUP PLC
公开号:EP0359536A2
公开(公告)日:1990-03-21
β-Lactam antibiotics of the formula (Ia) or a pharmaceutically acceptable salt or pharmaceutically acceptable in vivo hydrolysable ester thereof are disclosed:
wherein R¹ is hydrogen, methoxy or formamido;
R² is an acyl group, in particular that of an antibacterially active cephalosporin;
CO₂R⁶ is a carboxy group or a carboxylate anion;
R⁴ is a butenolide or butanolide ring, optionally substituted by one or two alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl groups, which may be the same or different, or, wherein two adjacent carbon atoms which are available for substitution define the common bond of an aromatic fused bicyclic system;
X is S,SO,SO₂,O or CH₂; and the dashed line adjacent to R⁴ represents an optional double bond.
Processes for the preparation of compounds together with intermediates for use therein are disclosed.
本发明公开了式(Ia)的β-内酰胺类抗生素或其药学上可接受的盐或药学上可接受的体内可水解酯:
其中 R¹ 是氢、甲氧基或甲酰胺基;
R² 是酰基,特别是抗菌活性头孢菌素的酰基;
CO₂R⁶ 是羧基或羧酸阴离子;
R⁴ 是丁烯内酯或丁内酯环,可选择被一个或两个烷基、二烷基氨基、烷氧基、羟基、卤素或芳基取代,这些基团可以是相同的或不同的,或者,其中两个相邻的碳原子可被取代,它们定义了芳香族融合双环系统的公共键;
X 是 S、SO、SO₂、O 或 CH₂;R⁴ 旁的虚线代表任选双键。
本发明公开了化合物及其中间体的制备方法。