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。

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。