公开(公告)号：EP2821402A1

公开(公告)日：2015-01-07

申请号：EP13754501.8

申请日：2013-02-26

申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

发明人： KAMEDA, Minoru ,  KURIWAKI, Ikumi ,  IIKUBO, Kazuhiko ,  HISAMICHI, Hiroyuki ,  KAWAMOTO, Yuichiro ,  MORITOMO, Hiroyuki ,  SUZUKI, Tomoyuki ,  FUTAMI, Takashi ,  SUZUKI, Atsushi ,  TSUNOYAMA, Kazuhisa ,  ASAUMI, Makoto ,  TOMIYAMA, Hiroshi ,  NODA, Atsushi ,  IWAI, Yoshinori ,  TOKUZAKI, Kazuo ,  OKADA, Haruki ,  MIYASAKA, Kozo

IPC分类号： C07D239/42 ,  A61K31/4545 ,  A61K31/506 ,  A61P35/00 ,  A61P43/00 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/10 ,  C07D487/20

CPC分类号： C07D239/47 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D451/04 ,  C07D453/02 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107

摘要： Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer.
As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

摘要翻译： 提供可用作膀胱癌的预防和/或治疗剂的化合物。 本发明人等对具有FGFR抑制作用的化合物进行研究的结果发现，本发明的含氮芳香族杂环化合物对FGFR1，FGFR2和/或FGFR3，特别是FGFR3具有抑制作用， 本发明已经完成。 本发明的含氮芳香族杂环化合物可以用作肺癌，激素治疗耐受性乳腺癌，胃癌，三重阴性乳腺癌等与FGFR1，FGFR2和/或FGFR3有关的各种癌症的治疗剂 癌症，子宫内膜癌，膀胱癌和成胶质细胞瘤，特别是作为突变型FGFR3阳性膀胱癌的预防和/或治疗剂。

公开(公告)号：EP2821402B1

公开(公告)日：2019-08-21

申请号：EP13754501.8

申请日：2013-02-26

申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

发明人： KAMEDA, Minoru ,  KURIWAKI, Ikumi ,  IIKUBO, Kazuhiko ,  HISAMICHI, Hiroyuki ,  KAWAMOTO, Yuichiro ,  MORITOMO, Hiroyuki ,  SUZUKI, Tomoyuki ,  FUTAMI, Takashi ,  SUZUKI, Atsushi ,  TSUNOYAMA, Kazuhisa ,  ASAUMI, Makoto ,  TOMIYAMA, Hiroshi ,  NODA, Atsushi ,  IWAI, Yoshinori ,  TOKUZAKI, Kazuo ,  OKADA, Haruki ,  MIYASAKA, Kozo

IPC分类号： C07D239/42 ,  A61K31/4545 ,  A61K31/506 ,  A61P35/00 ,  A61P43/00 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/10 ,  C07D487/20

公开(公告)号：EP2824181B1

公开(公告)日：2018-11-14

申请号：EP13757006.5

申请日：2013-03-07

申请人： Astellas Pharma Inc.

发明人： SUZUKI, Atsushi ,  ASAUMI, Makoto ,  TSUNOYAMA, Kazuhisa ,  NISHIMURA, Kouichi ,  MORINAKA, Akifumi ,  YAMAUCHI, Tomohiro ,  YOSHINO, Masayasu ,  YOSHIZAKI, Hiroaki

IPC分类号： C12Q1/6886

CPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/496 ,  C07K14/47 ,  C07K14/71 ,  C07K2319/00 ,  C12Q1/6886 ,  C12Q2600/118 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/57407 ,  G01N33/57423 ,  G01N33/74 ,  G01N2333/50

摘要： [Problem] The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. [Means for Solution] The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.

公开(公告)号：EP2824181A1

公开(公告)日：2015-01-14

申请号：EP13757006.5

申请日：2013-03-07

申请人： Astellas Pharma Inc.

发明人： SUZUKI, Atsushi ,  ASAUMI, Makoto ,  TSUNOYAMA, Kazuhisa ,  NISHIMURA, Kouichi ,  MORINAKA, Akifumi ,  YAMAUCHI, Tomohiro ,  YOSHINO, Masayasu ,  YOSHIZAKI, Hiroaki

IPC分类号： C12N15/09 ,  A61K45/00 ,  A61P35/00 ,  C12Q1/68 ,  G01N33/53

CPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/496 ,  C07K14/47 ,  C07K14/71 ,  C07K2319/00 ,  C12Q1/6886 ,  C12Q2600/118 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/57407 ,  G01N33/57423 ,  G01N33/74 ,  G01N2333/50

摘要： [Problem] The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer.
[Means for Solution] The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.

摘要翻译： 本发明旨在阐明多核苷酸作为癌症的新型负责基因，其目的在于提供一种检测多核苷酸的方法和由该多核苷酸编码的多肽以及检测试剂盒，探针组和用于 检测。 本发明还旨在提供一种治疗癌症的药物组合物。 [解决方案]该方法检测由FGFR3基因的一部分和TACC3基因的一部分或融合基因编码的融合蛋白构成的融合基因。 引物组，探针组或检测试剂盒包含有义引物和由编码FGFR3的部分设计的探针组和由编码TACC3的部分设计的反义引物和探针组。 由于多肽的抑制剂表现出抗肿瘤效果，因此提供了用于治疗对融合基因或多肽呈阳性的癌症的药物组合物。