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    • 8. 发明授权
    • Cephalosporin compounds
    • 头孢菌素化合物
    • US4616081A
    • 1986-10-07
    • US511183
    • 1983-07-06
    • Joji NishikidoEiji KodamaChisei Shibuya
    • Joji NishikidoEiji KodamaChisei Shibuya
    • C07D213/55C07D233/90C07D501/24C07D501/36C07D501/46C07D505/00A61K31/545
    • C07D233/90C07D213/55C07D505/00Y02P20/55
    • Novel cephalosporin compounds having antibacterial activity, which are represented by the following compounds of the general formula (I), ##STR1## wherein R.sub.1 represents an amino group or a protected amino group; .circle.A represents a 5- or 6-membered heterocyclic ring containing therein 1 to 4 nitrogen, oxygen or sulfur atoms;R.sub.2 represents a normal alkyl group having 1 to 6 carbon atoms, a branched alkyl group having 3 to 6 carbon atoms, an alkoxyalkyl group having 2 to 6 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms; a cycloalkenyl group having 3 to 6 carbon atoms; an aromatic organic residue; a 3- to 6-membered heterocyclic ring containing 1 to 4 nitrogen, sulfur or oxygen atoms or, ##STR2## wherein Ra and Rb each, which may be the same or different, represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms;R.sub.3 represents an organic residue containing an amino group or a protected amino group and a carboxyl group or a protected carboxyl group;X represents a sulfur atom or an oxygen atom; andR.sub.4 represents a hydrogen atom or a protective group of carboxyl group.The general formula (I) described above can also be used as physiologically acceptable addition salts.The compounds exhibit excellent intestinal absorption as well as high blood concentration and longer biological half-life.
    • 具有抗菌活性的新型头孢菌素化合物,其由以下通式(I)的化合物,其中R 1表示氨基或被保护的氨基; &Cir&A表示含有1至4个氮,氧或硫原子的5-或6-元杂环; R2表示碳原子数1〜6的正烷基,碳原子数3〜6的支链烷基,碳原子数2〜6的烷氧基烷基,碳原子数3〜6的环烷基。 具有3〜6个碳原子的环烯基; 芳香族有机残基; 含有1至4个氮,硫或氧原子的3至6元杂环,或者其中每个R a和R b可以相同或不同,表示氢原子或具有1-4个碳原子的烷基 碳原子 R3表示含有氨基或被保护的氨基,羧基或被保护的羧基的有机残基; X表示硫原子或氧原子; R 4表示氢原子或羧基的保护基。 上述通式(I)也可以用作生理上可接受的加成盐。 该化合物显示出优异的肠吸收以及高血液浓度和更长的生物半衰期。