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    METHOD FOR PRODUCING 6-HYDROXYETHYLPENAM COMPOUND
    3.
    发明公开
    METHOD FOR PRODUCING 6-HYDROXYETHYLPENAM COMPOUND 有权
    生产6-羟基乙基苯胺化合物的方法

    公开(公告)号：EP2123657A1

    公开(公告)日：2009-11-25

    申请号：EP08721477.1

    申请日：2008-03-06

    申请人： OTSUKA CHEMICAL COMPANY, LTD.

    发明人： TANAKA, Hideo ,  KUROBOSHI, Manabu ,  TATEYAMA, Syoichi ,  YAMADA, Takae ,  KAMEYAMA, Yutaka

    IPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897

    CPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897 ,  Y02P20/55

    摘要： The present invention provides a method by which a 6-hydroxyethyl penam compound represented by General Formula (2) below can be produced with a high selectivity:

    wherein R represents a hydrogen atom or a protective group for carboxylic acid and X 2 represents a halogen atom;
    the method including the steps of reacting a Grignard reagent with a halogeno penam compound represented by General Formula (1) below:

    wherein R and X 2 are the same as above, and X 1 represents a halogen atom;
    reacting the generated compound with an amine compound; and
    further reacting the generated compound with acetaldehyde.

    摘要翻译： 本发明提供了一种可以以高选择性制备下述通式（2）表示的6-羟乙基青霉素化合物的方法：其中R代表氢原子或羧酸保护基团，并且X 2代表卤素原子; 所述方法包括以下步骤：使格利雅试剂与由以下通式（1）表示的卤代青霉烷化合物反应：其中R和X2与上述相同，并且X1表示卤素原子; 使生成的化合物与胺化合物反应; 并进一步使生成的化合物与乙醛反应。

    BETA-LACTAMASE INHIBITOR PRODRUG
    4.
    发明公开
    BETA-LACTAMASE INHIBITOR PRODRUG 审中-公开
    BETA-LACTAMASEHEMMER PRODRUG

    公开(公告)号：EP1636240A1

    公开(公告)日：2006-03-22

    申请号：EP04734576.4

    申请日：2004-05-24

    申请人： Pfizer Products Inc.

    发明人： MARFAT, Anthony, Pfizer Global R. And D. ,  MCLEOD, Dale, Gordon, Pfizer Global R. and D. ,  O'DONNELL, John, Paul, Pfizer Global R. and D.

    IPC分类号： C07D499/00 ,  A61K31/351 ,  A61K31/357 ,  A61K31/397 ,  A61P31/04

    CPC分类号： C07D499/861 ,  C07D309/12 ,  C07D319/12

    摘要： Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is 0, or wherein R is H, each X is 0 and Y is methylene, and solvates thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in 20 a mammal by administering an effective amount of a beta­lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

    6-(Aminoacyloxymethyl) penicillanic acid 1, 1-dioxides as beta-lactamase inhibitors
    7.
    发明公开
    6-(Aminoacyloxymethyl) penicillanic acid 1, 1-dioxides as beta-lactamase inhibitors 失效
    6-（氨基酰氧基甲基）青霉烷-1,1-二氧化物酶β-内酰胺酶抑制剂。

    公开(公告)号：EP0154444A1

    公开(公告)日：1985-09-11

    申请号：EP85301115.3

    申请日：1985-02-20

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/00 ,  C07D519/00 ,  A61K31/43

    CPC分类号： C07D499/861

    摘要： beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1.1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.

    摘要翻译： β-内酰胺酶抑制剂，其为6-α和6-β-（羟甲基）青霉酸1,1-二氧化物的氨基酸酯; 其药学上可接受的盐; 其在体内可水解的其常规酯; 双甲烷二醇酯; 或与所述β-内酰胺酶抑制剂和舒巴坦混合的甲基二醇酯。 包含所述β-内酰胺酶抑制剂和常规β-内酰胺抗生素的药物组合物，所述组合物可用于治疗细菌感染。 用作合成所述β-内酰胺酶抑制剂的中间体的化合物。 所述氨基酰氧基甲基青霉素酸1,1-二氧化物和氨苄青霉素或阿莫西林的抗菌混合双甲磺酸酯也可用于治疗细菌感染; 及其中间体。