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    PYRAZINE CARBOXAMIDE COMPOUND
    1.
    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。

    MEDICINAL COMPOSITION COMPRISING PYRAZINE CARBOXAMIDE COMPOUND AS ACTIVE INGREDIENT
    2.
    发明公开
    MEDICINAL COMPOSITION COMPRISING PYRAZINE CARBOXAMIDE COMPOUND AS ACTIVE INGREDIENT 审中-公开
    维生素ZSAMMENSETZUNG MIT PYRAZIN-CARBOXAMID-VERBINDUNG ALS WIRKSTOFF

    公开(公告)号：EP3150206A1

    公开(公告)日：2017-04-05

    申请号：EP15799603.4

    申请日：2015-05-27

    申请人： Astellas Pharma Inc.

    发明人： KONAGAI, Satoshi ,  TANAKA, Hiroaki ,  YAMAMOTO, Hiroko ,  SAKAGAMI, Hideki

    IPC分类号： A61K31/497 ,  A61P35/00 ,  A61P35/02

    CPC分类号： A61K31/497

    摘要： [Problem]
    Provided is a pharmaceutical composition for treating cancer in which one or more kinases of BTK, JAK3, and ITK is involved.
    [Means for Solution]
    The present inventors studied compounds having a BTK inhibiting effect, a JAK3 inhibiting effect and an ITK inhibiting effect, and confirmed that a specific pyrazine carboxamide compound has the BTK inhibiting effect, the JAK3 inhibiting effect, and the ITK inhibiting effect, and that a pharmaceutical composition comprising the compound as an active ingredient has a therapeutic effect on cancer in which one or more kinases of BTK, JAK3 and ITK is involved, in another aspect, cancer in which BTK is overexpressed or activated, in another aspect, cancer in which a B cell receptor signal is activated, in still another aspect, cancer in which JAK3 is activation-mutated or activated, and in still another aspect, cancer in which ITK is activated, thereby completing the present invention.

    摘要翻译： [问题]提供一种用于治疗其中涉及一种或多种BTK，JAK3和ITK的激酶的癌症的药物组合物。 [解决方案]本发明人研究了具有BTK抑制作用，JAK3抑制作用和ITK抑制作用的化合物，并证实特异性吡嗪羧酰胺化合物具有BTK抑制作用，JAK3抑制作用和ITK抑制作用 并且包括该化合物作为活性成分的药物组合物在另一方面具有BTK，JAK3和ITK的一种或多种激酶涉及的癌症的治疗效果，在另一方面，在另一方面，BTK过表达或活化的癌症 在另一方面，其中JAK3是活化突变或活化的癌症，另一方面是其中ITK被激活的癌症，从而完成本发明，其中B细胞受体信号被激活的癌症。