公开(公告)号：US4840945A

公开(公告)日：1989-06-20

申请号：US838309

申请日：1986-03-10

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D209/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/20 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D519/00

CPC分类号： C07D209/48 ,  C07D277/587 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

摘要翻译： 本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物的合成中的中间体化合物及其制备方法。 本发明基于选择含有缩合杂环，特别是三唑并嘧啶环或噻二唑并嘧啶环作为头孢烯骨架3位上的取代基的基团，以及含有儿茶酚部分，特别是儿茶酚羧甲氧基亚氨基部分的基团 或邻苯二酚羧基亚氨基部分作为头孢烯骨架的7-位上的取代基。 含有上述取代基的本发明化合物对革兰氏阴性菌具有很强的抗菌活性，对抗耐甲氧西林金黄色葡萄球菌的革兰氏阳性菌具有很强的抗菌活性。 这些化合物对治疗感染性疾病非常有用。

公开(公告)号：US5001121A

公开(公告)日：1991-03-19

申请号：US368830

申请日：1989-06-20

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D209/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/20 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D519/00

CPC分类号： C07D209/48 ,  C07D277/587 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

公开(公告)号：US5064953A

公开(公告)日：1991-11-12

申请号：US412992

申请日：1989-09-26

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D239/40 ,  C07D239/46 ,  C07D277/20 ,  C07D417/12 ,  C07D487/04 ,  C07D501/36 ,  C07D513/04

CPC分类号： C07D239/47 ,  C07D239/40 ,  C07D277/587 ,  C07D417/12 ,  C07D487/04 ,  C07D513/04

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

摘要翻译： 本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物合成中的中间体化合物及其制备方法。 根据本发明的新型头孢菌素衍生物含有缩合杂环基团，特别是作为头孢烯骨架3位的取代基的三唑并嘧啶环或噻二唑嘧啶环，作为7-位上的取代基的羟基亚氨基，烷氧基亚氨基或酰氧基亚氨基部分， 头脑骨架的位置。 含有上述取代基的本发明化合物对革兰氏阴性细菌和包括耐甲氧西林金黄色葡萄球菌的革兰氏阳性细菌具有很强的抗菌活性。 这些化合物对治疗感染性疾病非常有用。

公开(公告)号：US4888332A

公开(公告)日：1989-12-19

申请号：US687455

申请日：1984-12-28

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D519/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D239/40 ,  C07D239/46 ,  C07D277/20 ,  C07D417/12 ,  C07D487/04 ,  C07D501/36 ,  C07D513/04 ,  C07D519/06

CPC分类号： C07D239/47 ,  C07D239/40 ,  C07D277/587 ,  C07D417/12 ,  C07D487/04 ,  C07D513/04 ,  Y02P20/55

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

摘要翻译： 本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物合成中的中间体化合物及其制备方法。 根据本发明的新型头孢菌素衍生物含有缩合杂环基团，特别是作为头孢烯骨架3位的取代基的三唑并嘧啶环或噻二唑嘧啶环，作为7-位上的取代基的羟基亚氨基，烷氧基亚氨基或酰氧基亚氨基部分， 头脑骨架的位置。 含有上述取代基的本发明化合物对革兰氏阴性细菌和包括耐甲氧西林金黄色葡萄球菌的革兰氏阳性细菌具有很强的抗菌活性。 这些化合物对治疗感染性疾病非常有用。

公开(公告)号：US4956474A

公开(公告)日：1990-09-11

申请号：US368846

申请日：1989-06-20

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D209/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/20 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D519/00

CPC分类号： C07D209/48 ,  C07D277/587 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

公开(公告)号：US4904791A

公开(公告)日：1990-02-27

申请号：US174518

申请日：1988-03-28

申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

IPC分类号： C07D209/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/20 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D519/00

CPC分类号： C07D209/48 ,  C07D277/587 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.