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    ANTAGONIST FOR MUTATED ANDROGEN RECEPTOR
    1.
    发明公开
    ANTAGONIST FOR MUTATED ANDROGEN RECEPTOR 审中-公开
    ANTAGONISTFÜREINEN MUTIERTEN ANDROGENREZEPTOR

    公开(公告)号：EP2631233A1

    公开(公告)日：2013-08-28

    申请号：EP11834469.6

    申请日：2011-10-21

    申请人： Astellas Pharma Inc.

    发明人： IDEYAMA, Yukitaka ,  KUROMITSU, Sadao ,  FURUTANI, Takashi ,  TAKEDA, Masayoshi ,  KONAGAI, Satoshi ,  YAMADA, Tomohiro ,  TANIGUCHI, Nobuaki ,  KONDOH, Yutaka ,  HIRANO, Masaaki ,  WATANABE, Kazushi ,  SUGANE, Takashi ,  KAKEFUDA, Akio

    IPC分类号： C07D401/12 ,  A61K31/496 ,  A61K31/506 ,  A61P5/26 ,  A61P35/00 ,  C07D403/12

    CPC分类号： C07D401/02 ,  A61K31/496 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12

    摘要： [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation [Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.

    摘要翻译： 本发明的目的在于提供一种可用于治疗伴随雄激素受体突变的前列腺癌的新型抗癌药物。本发明人进行了关于突变型雄激素相关疾病的全面研究， 雄激素药物变得无效。 结果发现，作为本发明的药物组合物的活性成分的化合物在人类突变雄激素受体（AR）中表现出抗转录活化的抑制作用，并且在人体中具有优异的抗肿瘤作用 前列腺癌的小鼠，从而完成本发明。 因此，作为本发明的药物组合物的活性成分的化合物可用于一系列与前列腺癌有关的雄激素受体相关疾病。