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    CAPRAZENE AS A NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS A NOVEL COMPOUND AND DERIVATIVES THEREOF
    5.
    发明申请
    CAPRAZENE AS A NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS A NOVEL COMPOUND AND DERIVATIVES THEREOF 有权
    作为新化合物及其衍生物，和作为新化合物的化合物及其衍生物

    公开(公告)号：US20090131652A1

    公开(公告)日：2009-05-21

    申请号：US12345190

    申请日：2008-12-29

    申请人： Toshiaki MIYAKE ,  Masayuki IGARASHI ,  Tetsuo SHITARA ,  Yoshiaki TAKAHASHI ,  Masa HAMADA

    发明人： Toshiaki MIYAKE ,  Masayuki IGARASHI ,  Tetsuo SHITARA ,  Yoshiaki TAKAHASHI ,  Masa HAMADA

    IPC分类号： C07H19/048

    CPC分类号： C07H19/067 ,  A61K31/7072 ,  C07D403/08 ,  C07D403/14 ,  C07D405/14 ,  C07H15/26 ,  C07H19/06 ,  Y02P20/55

    摘要： Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1′″-amide derivative of the formula (II) and a caprazene-1′″-ester derivative of the formula (III) from caprazene. Further, there could be synthesized a caprazol-1′″-amide derivative of the formula (V) and a caprazol-1′″-amide-3′″-ester derivative and a caprazol-3′″-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol.The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.

    摘要翻译： Caprazene和caprazol可以通过caprazamycin的水解合成。 可以从癸腈合成式（II）的癸酰肼衍生物和式（III）的癸酰基-1“ - 酯衍生物。 此外，可以合成式（V）的十六唑-1“ - 酰胺衍生物和十六唑-1” - 酰胺-3' - 酯衍生物和癸酰唑-3' - 酯衍生物 衍生物等。 此外，咪唑啉酮衍生物可以由四唑的1,4-二氮杂环酮环的开环产物合成。 现在合成的新型caprazene衍生物，新型吡唑衍生物和新型咪唑啉酮衍生物对各种细菌，包括耐酸细菌表现出优异的抗菌活性。

    Antibacterial agent and therapeutic agent for Johne's disease containing the same
    7.
    发明申请
    Antibacterial agent and therapeutic agent for Johne's disease containing the same 有权
    抗菌剂和治疗剂含有相同的约翰氏病

    公开(公告)号：US20090209744A1

    公开(公告)日：2009-08-20

    申请号：US12378172

    申请日：2009-02-11

    申请人： Yoshiaki Takahashi ,  Masayuki Igarashi

    发明人： Yoshiaki Takahashi ,  Masayuki Igarashi

    IPC分类号： C07H19/06

    CPC分类号： A61K31/7072 ,  A01N43/62

    摘要： An antibacterial agent having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is provided. Specifically, the antibacterial agent of the present invention having high antibacterial activity against Mycobacterium avium subsp. paratuberculosis is a caprazamycin derivative represented, for example, by the following general formula (II): wherein Me is a methyl group; and R1 is a straight or substantially straight chain alkyl group having 5 to 21 carbon atoms, a straight or substantially straight chain alkenyl group having 5 to 21 carbon atoms, a cycloalkyl group having 5 to 12 carbon atoms, or a phenyl group substituted at the para-position with a straight chain alkyl group having 1 to 14 carbon atoms, a straight chain alkoxy group having 1 to 9 carbon atoms or a cycloalkyl group having 5 to 12 carbon atoms.

    摘要翻译： 对鸟分枝杆菌亚种具有高抗菌活性的抗菌剂 提供副结核病。 具体地说，本发明的抗菌剂对鸟分枝杆菌属 副结核病是例如由以下通式（II）表示的卡拉霉素衍生物：其中Me是甲基; R1为碳原子数5〜21的直链或直链状的直链状烷基，碳原子数5〜21的直链或直链状的链烯基，碳原子数5〜12的环烷基， 具有1至14个碳原子的直链烷基的对位位置，具有1至9个碳原子的直链烷氧基或具有5至12个碳原子的环烷基。