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544 条记录 (耗时 0.019 秒)

    Production of crystalline penem
    81.
    发明公开
    Production of crystalline penem 失效
    Herstellung einer kristallinen Penem-Verbindung。

    公开(公告)号：EP0533149A1

    公开(公告)日：1993-03-24

    申请号：EP92115869.7

    申请日：1992-09-17

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. ,  LEDERLE (JAPAN), Ltd.

    发明人： Kaneko, Masayoshi ,  Yabuno, Shigeo

    IPC分类号： C07D477/00 ,  A61K31/40

    CPC分类号： C07D477/20

    摘要： A method of crystallizing (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate (hereinafter simply referred to as L-627), which is characterized by maintaining an aqueous solution of L-627 at temperatures ranging from the eutectic temperature of the solution to temperatures lower than 0° C.
    The method provides some advantages that loss of L-627 accompanied by crystallization is less, number of steps in the preparation of vial formulations is less and maintenance of these steps under sterile and dust-free conditions can be performed easily, dispensation of the drug can be conducted with quantitative accuracy, and the crystals dissolve in a solvent promptly at the time of use.

    摘要翻译： （1R，5S，6S）-2 - [（6,7-二氢-5H-吡唑并[1,2-a] [1,2,4]三唑鎓-6-基）] - - [（R）-1-羟乙基] -1-甲基 - 碳青霉烯-3-羧酸酯（以下简称为L-627），其特征在于将L-627的水溶液保持在共晶温度 的溶液温度低于0℃。该方法提供了一些优点，即伴随结晶的L-627的损失较少，制备小瓶配方的步骤数量较少，并且在无菌和无粉尘下维持这些步骤 条件可以容易地进行，可以定量精确地进行药物的分配，并且晶体在使用时迅速溶解在溶剂中。

    Antibacterial condensed carbapenemes
    87.
    发明公开
    Antibacterial condensed carbapenemes 失效
    抗菌凝聚碳青霉烯类

    公开(公告)号：EP0502468A1

    公开(公告)日：1992-09-09

    申请号：EP92103598.6

    申请日：1992-03-02

    申请人： GLAXO S.p.A.

    发明人： Perboni, Alcide, Glaxo SpA ,  Donati, Daniele, Glaxo SpA ,  Tarzia, Giorgio, Glaxo SpA

    IPC分类号： C07D477/00 ,  A61K31/40

    CPC分类号： C07D477/00 ,  Y02P20/55

    摘要： Compounds of general formula (I)

    in which
       R₁ represents a hydrogen atom or a hydroxyl protecting group, R₂ represents a hydrogen atom or a carboxyl protecting group, and R₃ represents the group N(R₄)-CH=NR₅ wherein R₄ represents a hydrogen atom and R₅ represents a hydrogen atom; and salts, metabolically labile esters and solvates thereof and a process for their production. The compounds of formula (I) are either antibacterial agents and or useful intermediates for the preparation of antibacterial agents.

    摘要翻译： 通式（Ⅰ）的化合物，其中R 1代表氢原子或羟基保护基，R 2代表氢原子或羧基保护基，R 3代表N（R 4）-CH = NR 5基，其中R 4代表氢原子 和R 5代表氢原子; 和盐，代谢不稳定的酯和溶剂化物以及它们的生产方法。 式（I）化合物是抗菌剂和或用于制备抗菌剂的有用中间体。

    Intermediates and process for preparing carbapenem derivatives
    88.
    发明公开
    Intermediates and process for preparing carbapenem derivatives 失效
    Zwischenprodukte und Verfahren zur Herstellung von Carbapenem-Derivaten。

    公开(公告)号：EP0499196A1

    公开(公告)日：1992-08-19

    申请号：EP92102233.1

    申请日：1992-02-11

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Murata, Masayoshi ,  Kasahara, Chiyoshi ,  Tsutsumi, Hideo ,  Murakami, Yoshihiro

    IPC分类号： C07D205/08 ,  C07D403/12 ,  C07F9/568 ,  C07F9/6558 ,  C07D477/00

    CPC分类号： C07D403/12 ,  C07D205/08 ,  C07D477/20 ,  C07F9/5683

    摘要： New compounds of the formula

    in which

    R² is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,
    R³ is hydrogen or lower alkyl,
    R⁶ is an organic group, and
    R is hydrogen, or certain groups,
    and processes for preparing them. The invention also relates to industrially excellent processes for preparing carbapenem derivatives having the formula

    in which

    R¹ is carboxy or protected carboxy,
    R² is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,
    R³ is hydrogen or lower alkyl, and
    R⁶ is an organic group,
    or salts thereof, which are useful as antimicrobial agents.

    摘要翻译： 式（CHEM）的新化合物，其中R 2是羟基（低级）烷基或保护的羟基（低级）烷基，R 3是氢或低级烷基，R 6是有机基团，R是 氢或某些基团，以及制备它们的方法。 本发明还涉及制备具有式CHEM的碳青霉烯衍生物的工业上优良的方法，其中R 1是羧基或保护的羧基，R 2是羟基（低级）烷基或保护的羟基（低级）烷基， 3>是氢或低级烷基，R 6是可用作抗微生物剂的有机基团或其盐。

    Novel 2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of producing them
    89.
    发明公开
    Novel 2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of producing them 失效
    2-取代基烷基-3-羧基 - 碳青霉烯类抗生素和Verfahren zu deren Herstellung。

    公开(公告)号：EP0478874A2

    公开(公告)日：1992-04-08

    申请号：EP91102512.0

    申请日：1991-02-21

    申请人： AMERICAN CYANAMID COMPANY

    发明人： Ziegler, Carl B., Jr. ,  Curran, William V. ,  Feigelson, Gregg

    IPC分类号： C07D477/00 ,  C07D205/08 ,  A61K31/40

    CPC分类号： C07D477/14 ,  C07D205/08

    摘要： The invention relates to new 2-substituted alkyl-3-carboxy carbapenems having the formula:
    with R 1 , R 2 , R 3 , X and Y defined in the specification as antibiotics and beta lactamase inhibitors produced by a novel Michael addition-elimination reaction of a substituted allyl azetidinone in the reaction shown:
    with Q defined in the specification.

    摘要翻译： 本发明涉及具有下式的新的2-取代烷基-3-羧基碳青霉烯：具有本说明书中定义的R 1，R 2，R 3，X和Y的作为抗生素和β-内酰胺酶抑制剂 在所示的反应中通过取代的烯丙基氮杂环丁酮的新的迈克尔加成 - 消除反应产生：＆lt; CHEM＆gt;与本说明书中定义的Q