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    PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF HBV INFECTION
    1.
    发明公开
    PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF HBV INFECTION 审中-公开
    药剂师ZUSAMMENSETZUNG ZUR BEHANDLUNG ODER PRENVENTION VON HBV-INFEKTIONEN

    公开(公告)号：EP2305234A1

    公开(公告)日：2011-04-06

    申请号：EP09766696.0

    申请日：2009-06-18

    申请人： Public University Corporation Nagoya City University ,  Chugai Seiyaku Kabushiki Kaisha

    发明人： MIZOKAMI, Masashi ,  TANAKA, Yasuhito ,  SUGIYAMA, Masaya ,  SUDOH, Masayuki

    IPC分类号： A61K31/165 ,  A61K31/201 ,  A61K31/381 ,  A61K31/405 ,  A61K31/4406 ,  A61K31/4418 ,  A61P1/16 ,  A61P31/14 ,  A61P35/00

    CPC分类号： A61K31/13 ,  A61K31/165 ,  A61K31/201 ,  A61K31/381 ,  A61K31/405 ,  A61K31/4406 ,  A61K31/4418

    摘要： First, the present inventors assessed the effect of the compound represented by formula (III) below on Huh-7 cells infected with HBV, and demonstrated that the compound alone had an anti-HBV effect in vitro.

    Then, the present inventors revealed that the HBV replication-suppressing effect of PEG-IFN is enhanced in chimeric mice having a human liver infected with genotype C or A HBV when PEG-IFN is used in combination with the compound represented by formula (III) above. The present inventors also revealed that the HBV replication-suppressing effect of Entecavir is enhanced in chimeric mice having a human liver infected with genotype C HBV (wild-type and Entecavir-resistant strains) when Entecavir is used in combination with the compound represented by formula (III) above. In addition, the present inventors revealed that the compound represented by formula (III) above exerts the anti-HBV effect not only against wild-type HBV strains but also against Entecavir- and/or Lamivudine-resistant HBV strains.

    摘要翻译： 首先，本发明人评估了下述式（III）表示的化合物对HBV感染的Huh-7细胞的作用，并证明该化合物在体外具有抗HBV作用。 然后，本发明人发现，当将PEG-IFN与式（III）表示的化合物组合使用时，在具有感染基因型C或A HBV的人肝脏的嵌合小鼠中，PEG-IFN的HBV复制抑制作用增强， 以上。 本发明人还发现，当恩替卡韦与式（I）表示的化合物组合使用时，恩替卡韦的HBV复制抑制作用在具有感染基因型C HBV（野生型和恩替卡韦抗性菌株）的人肝脏的嵌合小鼠中得到增强 （三）。 此外，本发明人发现，上述式（III）表示的化合物不仅对野生型HBV株产生抗HBV作用，而且针对恩替卡韦和/或拉米夫定耐药株。