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    PYRAZINE CARBOXAMIDE COMPOUND
    5.
    发明公开
    PYRAZINE CARBOXAMIDE COMPOUND 有权
    吡嗪羧酰胺化合物

    公开(公告)号：EP2805940A1

    公开(公告)日：2014-11-26

    申请号：EP13738947.4

    申请日：2013-01-15

    申请人： Astellas Pharma Inc.

    发明人： MATSUYA, Takahiro ,  KONDOH, Yutaka ,  SHIMADA, Itsuro ,  KIKUCHI, Shigetoshi ,  IIDA,Maiko ,  ONDA, Kenichi ,  FUKUDOME, Hiroki ,  TAKEMOTO, Yukihiro ,  SHINDOU, Nobuaki ,  SAKAGAMI, Hideki ,  HAMAGUCHI, Hisao

    IPC分类号： C07D241/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10 ,  C07D491/113 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07D241/24 ,  C07D241/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D491/113

    摘要： [Problem]
    A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided.
    [Means for Solution]
    The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention. The pyrazinecarboxamide compound of the present invention has an inhibitory action on an EGFR T790M mutation kinase, and can be used as an agent for preventing and/or treating EGFR T790M mutation positive cancer, in another embodiment, EGFR T790M mutation positive lung cancer, in a still other embodiment, EGFR T790M mutation positive non-small cell lung cancer, in further still another embodiment, EGFR T790M mutation protein positive cancer, in further still another embodiment, EGFR T790M mutation protein positive lung cancer, in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant cancer, in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant lung cancer, and in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant non-small cell lung cancer, or the like.

    摘要翻译： [问题]提供了可用作EGFR T790M突变激酶活性抑制剂的化合物。 [解决手段]本发明人研究了对EGFR T790M突变激酶具有抑制作用的化合物，发现吡嗪甲酰胺化合物对EGFR T790M突变激酶具有抑制作用，从而完成了本发明。 本发明的吡嗪甲酰胺化合物对EGFR T790M突变激酶具有抑制作用，并且可以用作预防和/或治疗EGFR T790M突变阳性癌症的药剂，在另一个实施方案中，EGFR T790M突变阳性肺癌 在又一个实施方案中，EGFR T790M突变阳性非小细胞肺癌，在又一又一个实施方案中，EGFR T790M突变蛋白阳性癌，在又一个实施方案中，EGFR T790M突变蛋白阳性肺癌，在又一个实施方案中，EGFR酪氨酸 在另一又一个实施方案中，EGFR酪氨酸激酶抑制剂抗性癌症，和在又一个实施方案中，EGFR酪氨酸激酶抑制剂抗性非小细胞肺癌等。

    CRYSTALS OF DI(ARYLAMINO)ARYL COMPOUND
    9.
    发明公开
    CRYSTALS OF DI(ARYLAMINO)ARYL COMPOUND 审中-公开
    DI（芳基氨基）芳基化合物晶体

    公开(公告)号：EP2581370A1

    公开(公告)日：2013-04-17

    申请号：EP11783482.0

    申请日：2011-05-16

    申请人： Astellas Pharma Inc.

    发明人： SHIMADA, Itsuro ,  HIRAKURA, Yutaka ,  YAMAZAKI, Kouji ,  TAKEGUCHI, Kazuhiro ,  UEDA, Norihiro

    IPC分类号： C07D401/12 ,  A61K31/53 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07D401/12 ,  A61K31/53

    摘要： PROBLEM
    Provided are crystals of compound A which have properties suitable for industrial production.
    MEANS FOR SOLVING
    As the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04-type crystal of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a drug substance.

    摘要翻译： 问题提供了具有适于工业生产的性质的化合物A的晶体。 解决手段作为提供对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制活性的化合物A的结晶的深入研究的结果，发现了化合物A的结晶。 此外，发现化合物A的A04型晶体在上述化合物A的晶体中出乎意料地具有作为药物的优选性质。