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公开(公告)号:US20130096100A1
公开(公告)日:2013-04-18
申请号:US13618732
申请日:2012-09-14
申请人: Yutaka KONDOH , Kazuhiko Iikubo , Sadao Kuromitsu , Nobuaki Shindo , Takatoshi Soga , Takashi Furutani , Itsuro Shimada , Takahiro Matsuya , Kazuo Kurosawa , Akio Kamikawa , Hiroyuki Mano
发明人: Yutaka KONDOH , Kazuhiko Iikubo , Sadao Kuromitsu , Nobuaki Shindo , Takatoshi Soga , Takashi Furutani , Itsuro Shimada , Takahiro Matsuya , Kazuo Kurosawa , Akio Kamikawa , Hiroyuki Mano
IPC分类号: A61K31/551 , A61K31/541 , A61K31/53 , A61K31/517 , A61K31/5377
CPC分类号: A61K31/551 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D239/95 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D471/10 , C07D487/08 , C07D491/113 , C07D498/10
摘要: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.
摘要翻译: 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果,本发明的发明人已经发现本发明的二(芳基氨基)芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症,肺癌,非小细胞肺癌,小细胞肺癌,EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物, 阳性癌症,EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。