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1. 发明公开

EP0293771A3 Cephalosporin compound and pharmaceutical composition thereof 失效
标题翻译： CEPHOROSPORIN化合物及其药物组合物
公开(公告)号：EP0293771A3
公开(公告)日：1990-10-17
申请号：EP88108456.0
申请日：1988-05-27
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： Nishizawa, Susumu , Muro, Hiroyuki , Kasai, Masayasu , Hatano, Satoru , Kamiya, Syouzi 202, Nakagawa Co.op 5 , Kakeya, Nobuharu , Kitao, Kazuhiko
IPC分类号： C07D501/20 , C07D277/20 , C07D285/08 , A61K31/545
CPC分类号： C07D277/587 , C07D285/08 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula (I): wherein R 1 and R 5 independently represented a hydrogen atom or a protective group for an amino group; R 2 represents an alkyl group or a cycloalkyl group; R 3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R 4 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.

2. 发明公开

EP0300423A2 Cephalosporin compound, method of its production and composition for prevention and treatment of bacterial infectious diseases 失效
标题翻译：头孢菌素化合物，其制备方法，和制备用于细菌感染性疾病的预防和治疗的方法。
公开(公告)号：EP0300423A2
公开(公告)日：1989-01-25
申请号：EP88111597.6
申请日：1988-07-19
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： Nishizawa, Susumu , Muro, Hiroyuki , Kasai, Masayasu , Hatano, Satoru , Kamiya, Syouzi 202, Nakagawa Co.op. 5 , Kakeya, Nobuharu , Kitao, Kazuhiko
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36
摘要： A cephalosporin compound represented by the formula (I):
wherein R' represents a hydrogen atom or a-amino acid residue (ester bonding), its ester, or its pharmacologically acceptable salt, which is useful as a preventive, therapeutic drug for bacterial infections as well as an intermediate for the synthesis of other cephalosporin compounds, a method of its production, a pharmaceutical composition for prevention and treatment of bacterial infectious diseases and method for the treatment of bacterial infectious diseases.
摘要翻译：由式（I）表示的头孢菌素化合物： worin - [R <1> darstellt氢原子或α-氨基酸残基（酯键），其酯，或其药理学上可接受的盐，所有这些是作为预防是有用的，用于细菌感染的治疗药物，以及在中间其它头孢菌素化合物的合成，其产生的方法，用于预防和治疗细菌感染性疾病的方法和用于细菌感染性疾病的治疗的药物组合物。

3. 发明公开

EP0300423A3 Cephalosporin compound, method of its production and composition for prevention and treatment of bacterial infectious diseases 失效
标题翻译： CEPHOROSPORIN化合物，其生产方法及其用于预防和治疗细菌感染性疾病的组合物
公开(公告)号：EP0300423A3
公开(公告)日：1990-11-14
申请号：EP88111597.6
申请日：1988-07-19
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： Nishizawa, Susumu , Muro, Hiroyuki , Kasai, Masayasu , Hatano, Satoru , Kamiya, Syouzi 202, Nakagawa Co.op. 5 , Kakeya, Nobuharu , Kitao, Kazuhiko
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36
摘要： A cephalosporin compound represented by the formula (I): wherein R' represents a hydrogen atom or a-amino acid residue (ester bonding), its ester, or its pharmacologically acceptable salt, which is useful as a preventive, therapeutic drug for bacterial infections as well as an intermediate for the synthesis of other cephalosporin compounds, a method of its production, a pharmaceutical composition for prevention and treatment of bacterial infectious diseases and method for the treatment of bacterial infectious diseases.
摘要翻译：由式（I）表示的头孢菌素化合物：其中R 1表示氢原子或α-氨基酸残基（酯键合），其酯或其药理学上可接受的盐，其可用作预防，用于细菌感染的治疗药物以及用于合成其它头孢菌素化合物的中间体，其生产方法，用于预防和治疗细菌感染性疾病的药物组合物和用于治疗细菌感染性疾病的方法。

4. 发明公开

EP0293771A2 Cephalosporin compound and pharmaceutical composition thereof 失效
标题翻译： Cephalosporinverbindungen und sie enthaltende pharmazeutischePräparate。
公开(公告)号：EP0293771A2
公开(公告)日：1988-12-07
申请号：EP88108456.0
申请日：1988-05-27
申请人： Kyoto Pharmaceutical Industries, Ltd.
发明人： Nishizawa, Susumu , Muro, Hiroyuki , Kasai, Masayasu , Hatano, Satoru , Kamiya, Syouzi 202, Nakagawa Co.op 5 , Kakeya, Nobuharu , Kitao, Kazuhiko
IPC分类号： C07D501/20 , C07D277/20 , C07D285/08 , A61K31/545
CPC分类号： C07D277/587 , C07D285/08 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula (I):
wherein R 1 and R 5 independently represented a hydrogen atom or a protective group for an amino group; R 2 represents an alkyl group or a cycloalkyl group; R 3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R 4 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.
摘要翻译：由通式（I）表示的头孢菌素化合物：其中R 1和R 5独立地表示氢原子或氨基的保护基; R 2表示烷基或环烷基; R 3表示氢原子，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; R 4表示氢原子或酯残基; X表示CH或氮原子及其药学上可接受的加成盐，这些化合物的合成中使用的中间体化合物，这些化合物的制造方法以及含有这些化合物的药物组合物。所述化合物或其加成盐即使在绿脓假单胞菌上也显示出显着的抗菌活性，其中已知的头孢菌素化合物不具有抗菌活性，而且对普通的革兰氏阳性菌和革兰氏阴性细菌有很好的效果。

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