申请人:Basilea Pharmaceutica AG
公开号:US06583133B1
公开(公告)日:2003-06-24
Disclosed are cephalosporin derivatives of the general formula
wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms,
as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.
本发明涉及一般式的头孢菌素衍生物,其中R是有机残基,其分子量不超过400,通过碳与相邻的硫原子相结合,由碳、氢和可选的氧、硫、氮和/或卤素原子组成;R1是氢、较低的烷基或苯基;A是次级、三级或季铵氮原子,直接与丙烯基团结合,并被分子量不超过400的有机残基取代,由碳、氢和可选的氧、硫、氮和/或卤素原子组成,以及其容易水解的酯,所述化合物的药学上可接受的盐和一般式I及其酯和盐的水合物。