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公开(公告)号：US20100099658A1
公开(公告)日：2010-04-22
申请号：US12448759
申请日：2008-07-04
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： A61K31/397 , C07D239/72 , A61K31/497 , A61K31/517 , C07D413/02 , A61K31/5377 , C07D403/02 , A61K31/53 , C07D279/12 , A61K31/541 , A61P35/00
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。
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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。
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公开(公告)号：US08318702B2
公开(公告)日：2012-11-27
申请号：US12448759
申请日：2008-07-04
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： A01N57/00 , A01N43/00 , A01N43/66 , A61K31/675 , A61K31/00 , A61K31/53 , C07D251/00 , C07D253/00 , C07D251/40 , C07D251/18 , C07D251/48
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。
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公开(公告)号：US07728120B2
公开(公告)日：2010-06-01
申请号：US11845498
申请日：2007-08-27
IPC分类号： C07H21/04
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US09029521B2
公开(公告)日：2015-05-12
申请号：US13468730
申请日：2012-05-10
IPC分类号： C07K14/435 , C12N9/12 , C07K14/47 , A61K31/506 , C12N15/113 , C12Q1/48 , C12Q1/68
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US20130158095A1
公开(公告)日：2013-06-20
申请号：US13468730
申请日：2012-05-10
IPC分类号： C12N9/12 , C12N15/113 , A61K31/506 , C12Q1/68 , C12Q1/48
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US08197818B2
公开(公告)日：2012-06-12
申请号：US13086245
申请日：2011-04-13
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US07964710B2
公开(公告)日：2011-06-21
申请号：US12466920
申请日：2009-05-15
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US20110230545A1
公开(公告)日：2011-09-22
申请号：US13086245
申请日：2011-04-13
IPC分类号： A61K31/713 , C12N9/12 , C12N15/63 , C12N5/10 , C07H21/00 , C12Q1/48 , C12N1/00 , C12Q1/68 , A61K31/506 , A61P35/00
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。
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公开(公告)号：US07605131B2
公开(公告)日：2009-10-20
申请号：US12100595
申请日：2008-04-10
CPC分类号： C12N15/1137 , A61K31/506 , C07K14/47 , C07K2319/00 , C12N9/1205 , C12N2310/14 , C12Q1/485 , C12Q1/6886
摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, and a therapeutic agent for cancer.
摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞和癌症治疗剂。
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