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    VERFAHREN ZUR HERSTELLUNG VON CEFTOBIPROL MEDOCARIL
    6.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON CEFTOBIPROL MEDOCARIL 有权
    VERFAHREN ZUR HERSTELLUNG VON CEFTOBIPOL MEDOCARIL

    公开(公告)号：EP2435442A1

    公开(公告)日：2012-04-04

    申请号：EP10723985.7

    申请日：2010-05-25

    申请人： Sandoz AG

    发明人： KREMMINGER, Peter ,  LUDESCHER, Johannes ,  STURM, Hubert

    IPC分类号： C07D501/04 ,  C07D501/18 ,  C07D501/56

    CPC分类号： C07D501/56 ,  C07D501/04 ,  C07D501/18

    摘要： The invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazole-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1'-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3']bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2 carboxylate (ceftobiprole medocaril). The invention also relates to a method for the production of compounds of the general formula (1) and of the general formula (2), to the compounds themselves, and to intermediates in the production process according to the invention.

    摘要翻译： 本发明涉及用于制备有机化合物，特别是（6R，7R）-7 - [（Z）-2-（5-氨基 - [1,2,4]噻二唑-3-基） - 2-肟基乙酰氨基] -8-氧代-3 - [（E） - （R）-1' - （5-甲基-2-氧代 - [1,3]二氧杂环戊烯-4-基甲氧羰基）-2-氧代 - [1,3']联吡咯烷-3-亚基甲基] -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2羧酸酯（头孢比罗中药油）。 本发明还涉及通式（1）和通式（2）的化合物的生产方法，化合物本身以及本发明生产方法中的中间体。

    3-PYRIDINIUM METHYLCEPHEM COMPOUND
    7.
    发明公开
    3-PYRIDINIUM METHYLCEPHEM COMPOUND 审中-公开
    3 PYRIDINIUMMETHYLCEPHEMVERBINDUNG

    公开(公告)号：EP1721906A4

    公开(公告)日：2008-02-27

    申请号：EP05719869

    申请日：2005-03-03

    申请人： SHIONOGI & CO

    发明人： NISHITANI YASUHIRO ,  YASUKATA TATSURO ,  YAMAWAKI KENJI

    IPC分类号： C07D501/56 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00

    CPC分类号： C07D501/00

    摘要： A compound represented by the formula [Chemical formula 1] (I) {wherein A is optionally substituted lower alkylene [substituent: mono- or di(lower alkyl), lower alkylidene, or C2 or higher (lower alkylene)]; and Z+ is either of the following groups: [Chemical formula 2] (Z-1) (Z-2) [wherein R1 and R2 each independently is hydrogen, optionally substituted amino(lower alkyl), optionally substituted aminocycloalkyl, optionally substituted cyclic amino, or optionally substituted (cyclic amino)lower alkyl; R9 is hydrogen or lower alkyl, provided that R1 and R9 may form an optionally substituted cyclic amino in cooperation with the adjacent nitrogen atom; R3 is hydrogen or amino; and X is nitrogen or CR4 (R4 is hydrogen or optionally substituted lower alkyl)]}, a pharmaceutically acceptable salt of the compound, or a solvate of either.

    摘要翻译： 由式[化学式1]（I）表示的化合物{其中A是任选取代的低级亚烷基[取代基：单或二（低级烷基），低级亚烷基或C2或更高级（低级亚烷基）]; （Z-2）[其中R 1和R 2各自独立地为氢，任选取代的氨基（低级烷基），任选取代的氨基环烷基，任选取代的环氨基 ，或任选取代的（环状氨基）低级烷基; R9为氢或低级烷基，条件是R1和R9可以与相邻的氮原子配合形成任选取代的环状氨基; R3是氢或氨基; 和X是氮或CR 4（R 4是氢或任选取代的低级烷基）]}，该化合物的药学上可接受的盐或任一种的溶剂化物。

    NOVEL CEPHEM DERIVATIVES
    8.
    发明公开
    NOVEL CEPHEM DERIVATIVES 失效
    新头孢烯衍生物

    公开(公告)号：EP0774466A4

    公开(公告)日：1998-09-02

    申请号：EP96914440

    申请日：1996-05-24

    申请人： MEIJI SEIKA CO

    发明人： UMEMURA EIJIRO ,  ATSUMI KUNIO ,  IWAMATSU KATSUYOSHI ,  TAMURA ATSUSHI

    IPC分类号： A61K31/545 ,  A61P31/04 ,  C07D501/00 ,  C07D501/56 ,  C07D519/06 ,  C07D519/00

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： Compounds represented by general formula (I) and having a β-(optionally substituted imidazo[5,1-b]thiazolyl)vinyl group at the 3-position of the cephem ring, and salts and esters thereof. These compounds have an extremely broad antimicrobial spectrum and exerts potent antimicrobial effects on Gram-positive bacteria, Gram-negative bacteria and even resistant bacteria. In formula (I) X represents CH or N; R1 represents hydrogen or an amino protecting group; R2 represents hydrogen, C¿1-6? alkyl, C3-7 cycloalkyl or a hydroxy protecting group; R?3¿ is not present or represents hydrogen, a cation forming a salt or a carboxy protecting group; R?4, R5 and R6¿ may be the same or different and each represents hydrogen or C¿1-6? alkyl; R?7+¿ is not present or represents a cation of C¿1-6? alkyl; and n is an integer of 0 or 1.

    Cephalosporins
    9.
    发明公开
    Cephalosporins 失效
    头孢菌素。

    公开(公告)号：EP0295341A1

    公开(公告)日：1988-12-21

    申请号：EP87304366.5

    申请日：1987-05-18

    申请人： Pfizer Corporation

    发明人： Nagakura, Isao ,  Nakanishi, Susumu

    IPC分类号： C07D501/56 ,  C07D501/20

    CPC分类号： C07D501/22 ,  C07D501/24 ,  C07D501/56

    摘要： A cephalosporin antibiotic of the formula:-
    or a pharmaceutically-acceptable salt or in vivo hydrolysable ester thereof, wherein Rʹ is C₁-C₆ alkyl substituted by carboxy, cyano, halo, hydroxy or a protected carboxy group; and A is phenyl or thienyl both optionally substituted by C₁-C₆ alkyl, hydroxy or halo.

    摘要翻译： 一种具有下式的头孢菌素抗生素： - 或其药学上可接受的盐或体内可水解的酯，其中R'是被羧基，氰基，卤素，羟基或保护的羧基取代的C 1 -C 6烷基; 并且A是任选被C 1 -C 6烷基，羟基或卤素取代的苯基或噻吩基。