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    • 3. 发明授权
    • Cephalosporin antibiotics and processes for preparation thereof
    • 头孢菌素类抗生素及其制备方法
    • US5605895A
    • 1997-02-25
    • US277629
    • 1994-07-20
    • Chan S. BangYong Z. KimJae H. YeoJong C. LimYoung M. WooHun S. OhDuk H. YangSam S. KimSe H. KimJae H. JeonTae H. LeeSung I. KimMi K. SeoJae W. Lee
    • Chan S. BangYong Z. KimJae H. YeoJong C. LimYoung M. WooHun S. OhDuk H. YangSam S. KimSe H. KimJae H. JeonTae H. LeeSung I. KimMi K. SeoJae W. Lee
    • A61K31/545A61K31/546A61P31/04C07D501/00C07D501/36
    • C07D501/00Y02P20/55
    • The present invention relates to a cephalosporin compound represented by the following general formula (I), its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, which is useful as an antibiotic agent: ##STR1## in which R.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and each represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a diol-protecting cyclic group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5 represents hydrogen, C.sub.1-4 alkyl, alkoxycarbonyl, carboxyl or sulfomethyl,R.sup.6 represents hydrogen, amino or substituted amino, andR.sup.7 represents C.sub.1-4 alkyl, amino or substituted amino, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a 3 to 7-membered cyclic group, orR.sup.6 and R.sup.7 together with the carbon and nitrogen atoms to which they are attached can form a 3 to 7-membered heterocyclic ring which may optionally contain additional heteroatoms such as nitrogen and/or oxygen and which may be substituted with the substituents selected from C.sub.1-4 alkyl, amino and substituted amino, andQ represents CH or N.
    • 本发明涉及以下通式(I)表示的头孢菌素化合物,其药学上可接受的无毒盐,生理上可水解的酯,水合物或溶剂化物或其异构体,其可用作抗生素: I),其中R 1表示氢或氨基保护基,R 2和R 3可以相同或不同,各自表示氢或羟基保护基,或者R 2和R 3一起可以形成二醇保护的环状基团,R 4表示氢 或羧基保护基,R5表示氢,C1-4烷基,烷氧基羰基,羧基或磺基甲基,R6表示氢,氨基或取代的氨基,R7表示C1-4烷基,氨基或取代的氨基,或R5和R6连同 它们连接的碳原子可以形成3至7元环基,或者R6和R7与它们所连接的碳原子和氮原子一起可以形成3至7元杂环,其可以 任选地含有另外的杂原子如氮和/或氧并且可以被选自C 1-4烷基,氨基和取代的氨基的取代基取代,Q代表CH或N.