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    Method for preparation of cephalosporin compounds
    2.
    发明授权
    Method for preparation of cephalosporin compounds 失效
    头孢菌素化合物的制备方法

    公开(公告)号：US4327211A

    公开(公告)日：1982-04-27

    申请号：US210746

    申请日：1980-11-26

    申请人： Masahiro Murakami ,  Masateru Kobayashi ,  Takanori Sone ,  Chisei Shibuya

    发明人： Masahiro Murakami ,  Masateru Kobayashi ,  Takanori Sone ,  Chisei Shibuya

    IPC分类号： C07D501/36 ,  C07D501/56

    CPC分类号： C07D501/36

    摘要： A method for preparing a cephalosporin compound represented by the general formula (III) ##STR1## (wherein R represents hydrogen or methyl group) or a pharmaceutically acceptable salt thereof, which is characterized by reacting 7-amino-3-(benzimidazol-2-yl)-thiomethyl-3-cephem-4-carboxylic acid represented by the general formula (I) ##STR2## or a salt thereof with a compound represented by general formula (II) ##STR3## wherein R represents hydrogen or methyl group.

    摘要翻译： 制备由通式（III）表示的头孢菌素化合物（III）（其中R表示氢或甲基）或其药学上可接受的盐的方法，其特征在于使7-氨基-3-（苯并咪唑 （II）表示的化合物或其盐与通式（II）表示的化合物（II）表示的通式（I）表示的化合物 其中R表示氢或甲基。

    1-Methyltetrazol-5-ylthio ester of cyanomethylthioacetic acid
    6.
    发明授权
    1-Methyltetrazol-5-ylthio ester of cyanomethylthioacetic acid 失效
    氰甲基硫代乙酸1-甲基四唑-5-基硫酯

    公开(公告)号：US4454323A

    公开(公告)日：1984-06-12

    申请号：US545202

    申请日：1983-10-25

    申请人： Masahiro Murakami ,  Masateru Kobayashi ,  Kimiyo Yamamoto ,  Chisei Shibuya

    发明人： Masahiro Murakami ,  Masateru Kobayashi ,  Kimiyo Yamamoto ,  Chisei Shibuya

    IPC分类号： C07D249/04 ,  C07D257/04 ,  C07D285/12 ,  C07D285/125 ,  C07D501/06 ,  C07D501/36

    CPC分类号： C07D257/04 ,  C07D249/04 ,  C07D285/125

    摘要： Novel thioesters effective as acylating agents for amines or hydrazines, especially effective as active esters in synthesis of cephalosporin compounds are disclosed. The novel thioester of the present invention can be prepared by reacting a thiol or a derivative thereof with an acetic acid derivative or a reactive derivative thereof. By reacting the thioester of the present invention with a 7-aminocephalosporin derivative or a salt thereof, cephalosporin derivatives or pharmacologically acceptable salts thereof which are excellent antibiotic substances having a high antimicrobial activity can be obtained in high yield very safely.

    摘要翻译： 公开了作为胺或肼的酰化剂有效的新型硫酯，在合成头孢菌素化合物中作为活性酯特别有效。 本发明的新型硫酯可以通过硫醇或其衍生物与乙酸衍生物或其反应性衍生物反应来制备。 通过使本发明的硫酯与7-氨基头孢菌素衍生物或其盐反应，可以高产率非常安全地获得具有高抗菌活性的优异的抗生素物质的头孢菌素衍生物或其药理学上可接受的盐。

    Cephalosporin compounds
    8.
    发明授权
    Cephalosporin compounds 失效
    头孢菌素化合物

    公开(公告)号：US4616081A

    公开(公告)日：1986-10-07

    申请号：US511183

    申请日：1983-07-06

    申请人： Joji Nishikido ,  Eiji Kodama ,  Chisei Shibuya

    发明人： Joji Nishikido ,  Eiji Kodama ,  Chisei Shibuya

    IPC分类号： C07D213/55 ,  C07D233/90 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07D505/00 ,  A61K31/545

    CPC分类号： C07D233/90 ,  C07D213/55 ,  C07D505/00 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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。