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    2-(pyrazol-3-yl)carbapenem derivatives
    3.
    发明授权
    2-(pyrazol-3-yl)carbapenem derivatives 失效
    2-（吡唑-3-基）碳青霉烯衍生物

    公开(公告)号：US07045619B2

    公开(公告)日：2006-05-16

    申请号：US10324593

    申请日：2002-12-19

    申请人： Eric Hunt ,  Steven Coulton ,  Jeremy David Hinks ,  Stephen Frederick Moss ,  Stephen Christopher Martin Fell ,  Alfred John Eglington ,  George Burton

    发明人： Eric Hunt ,  Steven Coulton ,  Jeremy David Hinks ,  Stephen Frederick Moss ,  Stephen Christopher Martin Fell ,  Alfred John Eglington ,  George Burton

    IPC分类号： C07D477/14

    CPC分类号： C07D477/14 ,  C07D477/08 ,  Y02P20/55

    摘要： A compound of formula (I): wherein Rα is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; Rβ is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; or Rα and Rβ together form an optionally substituted 5 or 6 membered heterocyclic ring with or without additional heteroatoms; R1 is (C1-6)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a removable hydroxy protecting group, or by an amino group which is optionally protected by a removable amino protecting group; R2 is hydrogen or methyl; and —CO2R3 is carboxy or a carboxylate anion or the group R3 is a removable carboxy protecting group. This invention also relates to processes for its preparation, intermediates and pharmaceutical compositions comprising compounds of formula (I). Compounds of formula (I) which include pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof have a broad spectrum of anti-bacterial activity and show good stability towards DHP-1.

    摘要翻译： 式（I）的化合物：其中R a为氢，任选取代的（C 1-6 - ）烷基或任选取代的芳基; R 6是氢，任选取代的（C 1-6 - ）烷基或任选取代的芳基; 或R aα和R b一起形成具有或不具有另外的杂原子的任选取代的5或6元杂环; R 1是未被取代或被氟取代的（C 1-6 - ）烷基，任选地被可除去的羟基保护基保护的羟基，或被氨基 任选被可除去的氨基保护基团保护的基团; R 2是氢或甲基; 并且-CO 2 R 3是羧基或羧酸根阴离子或基团R 3是可除去的羧基保护基。 本发明还涉及其制备方法，中间体和包含式（I）化合物的药物组合物。 包括其药学上可接受的盐或其药学上可接受的体内可水解的酯的式（I）化合物具有广谱的抗细菌活性，并显示出对DHP-1的良好的稳定性。