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    Cephalosporin derivatives
    3.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    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。

    Intermediates cephalosporin derivatives
    5.
    发明授权
    Intermediates cephalosporin derivatives 失效
    中间体CEPHALOSPORIN衍生物

    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。

    Cephalosporin derivatives
    6.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    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。

    Cephalosporin derivatives
    8.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    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.

    7-Diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine and pharmaceutical composition containing same
    9.
    发明授权
    7-Diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine and pharmaceutical composition containing same 失效
    7-二乙基氨基-5-甲基 - 噻唑并[5,4-d]嘧啶和含有它们的药物组合物

    公开(公告)号：US4476127A

    公开(公告)日：1984-10-09

    申请号：US433206

    申请日：1982-09-29

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

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

    IPC分类号： C07D513/04 ,  A61K31/495 ,  C07D417/02

    CPC分类号： C07D513/04

    摘要： The compound related to this invention is 7-diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine.The compound related to this invention possesses vasodilating action, hypotensive action, inhibitory action on platelet aggregation, and lowering action on cholesterol levels in blood, and is useful as a therapeutic agent for cardiovascular diseases.

    摘要翻译： PCT No.PCT / JP82 / 00046 Sec。 371日期：1982年9月29日 102（e）1982年9月29日PCT PCT 1982年9月19日PCT公布。 出版物WO83 / 02945 1983年9月1日。与本发明有关的化合物是7-二乙基氨基-5-甲基 - 噻唑并[5,4-d]嘧啶。 本发明涉及的化合物具有血管舒张作用，降血压作用，对血小板聚集的抑制作用，降低血液中胆固醇水平的作用，可用作心血管疾病的治疗剂。