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    PROCESS FOR PRODUCING CARBAPENEM COMPOUND FOR ORAL ADMINISTRATION
    8.
    发明公开
    PROCESS FOR PRODUCING CARBAPENEM COMPOUND FOR ORAL ADMINISTRATION 审中-公开
    用于生产碳青霉烯口服

    公开(公告)号：EP1580191A1

    公开(公告)日：2005-09-28

    申请号：EP03774005.7

    申请日：2003-11-13

    申请人： KANEKA CORPORATION

    发明人： NISHINO, Keita, c/o KANEKA CORPORATION ,  KOGA, Teruyoshi, c/o KANEKA CORPORATION

    IPC分类号： C07D477/06 ,  C07F7/18

    CPC分类号： C07D477/06 ,  C07F7/1892 ,  Y02P20/55

    摘要： The present invention provides a process for efficiently producing a 1β-methylcarbapenem compound for oral administration. The process, which is for producing a 1β-methylcarbapenem compound represented by general formula (2), is characterized by reacting a β-lactam compound represented by general formula (1) as a starting material with a thiol compound (R 3 -SH) in the presence of a base and optionally eliminating the protective group R 1 .
    In the formulae (1) and (2), R 1 denotes a hydrogen atom, a trimethylsilyl group or a triethylsilyl group; R 2 denotes an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; R 3 denotes an organic group; and R 4 denotes hydrogen, a trimethylsilyl group or a triethylsilyl group.

    NOVEL BETA-LACTAM COMPOUNDS AND PROECSS FOR PRODUCING THE SAME
    9.
    发明公开
    NOVEL BETA-LACTAM COMPOUNDS AND PROECSS FOR PRODUCING THE SAME 有权
    新泽西州ZERDEREN HERSTELLUNG的BETA-LACTAMVERBINDUNGEN

    公开(公告)号：EP1340756A1

    公开(公告)日：2003-09-03

    申请号：EP01979010.4

    申请日：2001-11-06

    申请人： Sumitomo Pharmaceuticals Company, Limited

    发明人： SUNAGAWA, Makoto ,  KUBOTA, Katsumi ,  ITOH, Masanori ,  GOETSCHI, Erwin

    IPC分类号： C07D477/20 ,  A61K31/427 ,  A61K31/4545 ,  A61P31/04

    CPC分类号： C07D477/20 ,  C07D477/06

    摘要： 1. A β-lactam compound of the formula [1];
       wherein R 1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R 2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y 1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y 2 is hydrogen, an alkyl, cyano, -C(R 3 )=NR 4 (wherein R 3 and R 4 are hydrogen, an amino, an alkyl, etc., or R 3 and R 4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.

    摘要翻译： 1.式Ä1Ü的β-内酰胺化合物; 其中R 1为低级烷基，被羟基取代的低级烷基; R 2是氢，低级烷基; X是O，S，NH; m和n为0〜4，Y 1为卤素，氰基，羟基，氨基，低级烷氧基，低级烷基氨基，羧基，氨基甲酰基，低级烷基等。 氢，烷基，氰基，-C（R 3）= NR 4（其中R 3和R 4是氢，氨基，烷基等，或R 3和R <4>可以与氮原子一起形成5至7元杂环基）或其药学上可接受的盐或其无毒酯，其对革兰氏阳性菌具有优异的抗菌活性 细菌，特别是针对MRSA和MRCNS。