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    Pyridonecarboxylic acid derivatives or salts thereof and antibacterial agents containing the same as the active ingredient
    3.
    发明授权
    Pyridonecarboxylic acid derivatives or salts thereof and antibacterial agents containing the same as the active ingredient 失效
    吡啶酮羧酸衍生物或其盐和含有该活性成分的抗菌剂

    公开(公告)号：US06211375B1

    公开(公告)日：2001-04-03

    申请号：US09171411

    申请日：1999-01-20

    申请人： Akira Yazaki ,  Yoshiko Niino ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Yuzo Hirao ,  Tamae Yamane

    发明人： Akira Yazaki ,  Yoshiko Niino ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Yuzo Hirao ,  Tamae Yamane

    IPC分类号： C07D21556

    CPC分类号： C07D401/04

    摘要： A novel pyridonecarboxylic acid derivative or its salt exhibiting satisfactory antibacterial activities, intestinal absorption, metabolic stability, and reduced side effects, in particular, phototoxicity and cytotoxicity, as well as an antibacterial agent containing such pyridonecarboxylic acid derivative or its salt are provided. For such an object, a pyridonecarboxylic acid derivative represented by the following formula (1): (wherein R1 represents hydrogen atom, a halogen atom or a lower alkyl group; R2 represents hydrogen atom or a lower alkyl group; R3 represents substituted or unsubstituted amino group or hydroxyl group; and R4 represents hydrogen atom, a lower alkyl group, amino group or nitro group) or its salt is provided.

    摘要翻译： 提供了具有令人满意的抗菌活性，肠吸收，代谢稳定性和副作用特别是光毒性和细胞毒性的新型吡啶酮羧酸衍生物或其盐，以及含有这种吡啶酮羧酸衍生物或其盐的抗菌剂。 目的，下述式（1）表示的吡啶酮羧酸衍生物:(其中，R1表示氢原子，卤素原子或低级烷基; R2表示氢原子或低级烷基; R3表示取代或未取代的氨基或 羟基，R4表示氢原子，低级烷基，氨基或硝基）或其盐。

    Process for preparing quinolone antibiotic intermediates
    4.
    发明授权
    Process for preparing quinolone antibiotic intermediates 有权
    制备喹诺酮类抗生素中间体的方法

    公开(公告)号：US06803469B2

    公开(公告)日：2004-10-12

    申请号：US10630608

    申请日：2003-07-30

    申请人： Jared Lynn Randall

    发明人： Jared Lynn Randall

    IPC分类号： C07D21556

    CPC分类号： C07D215/56

    摘要： The present invention relates to a process for preparing a quinolone antibiotic intermediate having the formula: wherein R is C1-C2 alkyl, C1-C2 fluoroalkyl, C2-C4 alkenyl, methoxy, chloro, or bromo; R1 is a unit selected from the group consisting of C1-C2 alkyl, C2-C3 alkenyl, C3-C5 cycloalkyl, and phenyl, each of which can be substituted by one or more fluorine atoms; said process comprising the step of cyclizing an admixture of quinolone precursors, said admixture comprising a 2-ethoxy substituted intermediate having the formula: in the presence of a silylating agent.

    摘要翻译： 本发明涉及制备具有下式的喹诺酮抗生素中间体的方法：其中R是C 1 -C 2烷基，C 1 -C 2氟烷基，C 2 -C 4烯基，甲氧基，氯或溴; R 1是选自C 1 -C 2烷基，C 2 -C 3烯基，C 3 -C 5环烷基和苯基的单元，每个可以被一个或多个氟原子取代; 所述方法包括使喹诺酮前体的混合物环化的步骤，所述混合物包含具有下式的2-乙氧基取代的中间体：在甲硅烷基化剂存在下。

    Process for preparing quinolonecarboxylic acids
    5.
    发明授权
    Process for preparing quinolonecarboxylic acids 失效
    制备喹诺酮羧酸的方法

    公开(公告)号：US06699992B2

    公开(公告)日：2004-03-02

    申请号：US10344643

    申请日：2003-02-12

    申请人： Yuncai Wang ,  Rongye Chen ,  Haijun Nan

    发明人： Yuncai Wang ,  Rongye Chen ,  Haijun Nan

    IPC分类号： C07D21556

    CPC分类号： C07D215/56 ,  C07C49/807

    摘要： The present invention provides a process for preparing quinolonecarboxylic acid derivatives having the formula (I): wherein R1 is H, halogen, or amino; R2 is halogen; R3 is H, halogen, C1-4 alkoxyl, or CN; R4 is selected from the group consisting of C3-6cycloalkyl, C1-4alkyl, C1-4alkoxyC1-4alkyl, and C1-4alkylaminoC1-4alkyl. The invention also provides new acetophenones having the formula (II) that are intermediates for preparing the compound of the formula (I).

    摘要翻译： 本发明提供了制备具有式（I）的喹诺酮羧酸衍生物的方法：其中R1是H，卤素或氨基; R2是卤素; R3是H，卤素，C1-4烷氧基或CN; R 4选自C 3-6环烷基，C 1-4烷基，C 1-4烷氧基C 1-4烷基和C 1-4烷基氨基C 1-4烷基。 本发明还提供了具有式（II）的新的苯乙酮，它是制备式（I）化合物的中间体。