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12 条记录 (耗时 0.029 秒)

    Pyridonecarboxylic acid derivatives or salts thereof and drugs containing the same as the active ingredient
    2.
    发明授权
    Pyridonecarboxylic acid derivatives or salts thereof and drugs containing the same as the active ingredient 失效
    吡啶酮羧酸衍生物或其盐和含有与活性成分相同的药物

    公开(公告)号：US6136823A

    公开(公告)日：2000-10-24

    申请号：US308641

    申请日：1999-05-28

    申请人： Nobuya Sakae ,  Akira Yazaki ,  Yasuhiro Kuramoto ,  Jiro Yoshida ,  Yoshiko Niino ,  Yoshihiro Ohshita ,  Yuzo Hirao ,  Norihiro Hayashi ,  Hirotaka Amano

    发明人： Nobuya Sakae ,  Akira Yazaki ,  Yasuhiro Kuramoto ,  Jiro Yoshida ,  Yoshiko Niino ,  Yoshihiro Ohshita ,  Yuzo Hirao ,  Norihiro Hayashi ,  Hirotaka Amano

    IPC分类号： C07D215/56 ,  C07D401/04 ,  C07D471/04 ,  C07D215/16 ,  A61K31/47

    CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D471/04 ,  Y02P20/55

    摘要： The invention relates to pyridonecarboxylic acid derivatives represented by the general formula (1): ##STR1## wherein R.sup.1 is --OH, a carboxy-protecting group or (alkyl)amino group, R.sup.2 is H, or --NO.sub.2, (protected) amino, (protected) hydroxyl, lower alkyl or lower alkoxyl group, R.sup.3 is a halogen atom, H, or --NO.sub.2, lower alkyl, lower alkoxyl or amino group, R.sup.4 is an azido, (substituted) hydrazino, (substituted) amino, lower alkoxyl or hydroxyl group, R.sup.5, R.sup.6 and R.sup.7 are independently H, --NO.sub.2, halogen atom or lower alkyl group, R.sup.8 is a --NO.sub.2, (substituted) amino, --OH or lower alkoxyl group, A is N or C--R.sup.12, in which R.sup.12 is H, halogen atom, or (substituted) lower alkyl, lower alkenyl, lower alkynyl, lower alkoxyl, lower alkylthio or nitro group, and B is N or C--R.sup.13, in which R.sup.13 is H or halogen atom, or salts thereof, and medicine comprising such a compound as an active ingredient. The derivatives or the salts thereof exhibit excellent antibacterial action and peroral absorbability, scarcely cause side effects, and are easy of synthesis.

    摘要翻译： PCT No.PCT / JP97 / 04326 Sec。 371日期1999年5月28日 102（e）1999年5月28日PCT 1997年11月27日PCT PCT。 公开号WO98 / 23592 日期：1998年6月4日本发明涉及由通式（1）表示的吡啶酮羧酸衍生物：其中R1是-OH，羧基保护基或（烷基）氨基，R2是H或-NO2，（被保护的） 氨基，（被保护的）羟基，低级烷基或低级烷氧基，R3是卤原子，H或-NO2，低级烷基，低级烷氧基或氨基，R4是叠氮基，（取代的）肼基，（取代的）氨基， 低级烷氧基或羟基，R5，R6和R7独立地是H，-NO2，卤原子或低级烷基，R8是-NO2，（取代的）氨基，-OH或低级烷氧基，A是N或C-R12 其中R 12为H，卤素原子或（取代）低级烷基，低级烯基，低级炔基，低级烷氧基，低级烷硫基或硝基，B为N或C-R 13，其中R 13为H或卤素原子， 或其盐，以及包含这种化合物作为活性成分的药物。 其衍生物或其盐表现出优异的抗菌作用和口服吸收性，几乎不引起副作用，并且易于合成。

    Quinolinecarboxylic acid derivative or its salt
    5.
    发明授权
    Quinolinecarboxylic acid derivative or its salt 失效
    喹啉羧酸衍生物或其盐

    公开(公告)号：US06586420B1

    公开(公告)日：2003-07-01

    申请号：US10069514

    申请日：2002-03-04

    申请人： Akira Yazaki ,  Yoshiko Niino ,  Yasuhiro Kuramoto ,  Yuzo Hirao ,  Yoshihiro Oshita ,  Norihiro Hayashi ,  Hirotaka Amano

    发明人： Akira Yazaki ,  Yoshiko Niino ,  Yasuhiro Kuramoto ,  Yuzo Hirao ,  Yoshihiro Oshita ,  Norihiro Hayashi ,  Hirotaka Amano

    IPC分类号： A61K3155

    CPC分类号： C07D401/14

    摘要： The present invention relates a 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-hydroxyazetidin-1-yl)-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or salt thereof; and drugs containing the same as the active ingredient. Since this compound or salt thereof is highly stable to light while sustaining the excellent properties inherent to quinolone antibacterial agents, an antibacterial agent comprising, as an active ingredient, the invention compound or salt thereof can be stored over a long period of time without suffering from any decrease in the drug effect and can therefore be supplied as stable preparations such as injections, eye drops and surgical medicines.

    摘要翻译： 本发明涉及1-（6-氨基-3,5-二氟吡啶-2-基）-6-氟-7-（3-羟基吖丁啶-1-基）-8-甲基-1,4-二氢-4 - 喹啉-3-羧酸或其盐; 和含有与活性成分相同的药物。 由于该化合物或其盐在维持喹诺酮类抗菌剂固有的优异性能的同时高度稳定，所以可以长期储存本发明化合物或其盐作为活性成分的抗菌剂，而不会受到 任何药物作用下降，因此可作为稳定的制剂如注射剂，滴眼剂和外用药物提供。

    Pyridonecarboxylic acid derivatives or salts thereof and antibacterial agents containing the same as the active ingredient
    10.
    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。