申请人:Kyoto Pharmaceutical Industries, Ltd.
公开号:EP0293771A2
公开(公告)日:1988-12-07
Cephalosporin compounds represented by the general formula (I):
wherein R1 and R5 independently represented a hydrogen atom or a protective group for an amino group; R2 represents an alkyl group or a cycloalkyl group; R3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.
Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.
由通式(I)代表的头孢菌素化合物:
其中 R1 和 R5 独立地代表氢原子或氨基的保护基团;R2 代表烷基或环烷基;R3 代表氢原子、低级烯基、烷酰氧基甲基、氨基甲酰氧基甲基、杂环硫代甲基或杂环甲基;R4代表氢原子或酯残基;X代表CH或氮原子,以及药理学上可接受的其加成盐、用于这些化合物合成过程的中间化合物、这些化合物的生产方法和含有这些化合物的药物组合物。
上述化合物或其加成盐甚至对铜绿假单胞菌也有明显的抗菌活性,而已知的头孢菌素化合物对铜绿假单胞菌没有抗菌活性,此外,对普通的革兰氏阳性菌和革兰氏阴性菌也有很好的效果。