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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
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
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公开(公告)号：EP2428508A1
公开(公告)日：2012-03-14
申请号：EP10772177.1
申请日：2010-05-06
发明人： SHIMADA, Itsuro , KUROSAWA, Kazuo , MATSUYA, Takahiro , IIKUBO, Kazuhiko , KONDOH, Yutaka , KAMIKAWA, Akio , TOMIYAMA, Hiroshi , IWAI, Yoshinori
IPC分类号： C07D239/48 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P35/00 , A61P43/00 , C07D241/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
CPC分类号： C07D239/48 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
摘要： Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.
As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EMLA-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.摘要翻译： 提供了可用作抑制EML4-ALK融合蛋白的激酶活性的化合物。 作为对具有针对EMLA-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入研究的结果，本发明人发现本发明的二氨基杂环羧酰胺化合物对EML4-ALK融合体的激酶活性具有抑制活性 蛋白。 通过这一发现，完成了本发明。 本发明的化合物可以用作预防和/或治疗癌症的药物组合物，例如肺癌，非小细胞肺癌和小细胞肺癌。
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公开(公告)号：EP2428508B1
公开(公告)日：2015-12-16
申请号：EP10772177.1
申请日：2010-05-06
发明人： SHIMADA, Itsuro , KUROSAWA, Kazuo , MATSUYA, Takahiro , IIKUBO, Kazuhiko , KONDOH, Yutaka , KAMIKAWA, Akio , TOMIYAMA, Hiroshi , IWAI, Yoshinori
IPC分类号： C07D239/48 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61P35/00 , C07D241/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
CPC分类号： C07D239/48 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
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公开(公告)号：EP2428508B9
公开(公告)日：2016-04-20
申请号：EP10772177.1
申请日：2010-05-06
发明人： SHIMADA, Itsuro , KUROSAWA, Kazuo , MATSUYA, Takahiro , IIKUBO, Kazuhiko , KONDOH, Yutaka , KAMIKAWA, Akio , TOMIYAMA, Hiroshi , IWAI, Yoshinori
IPC分类号： C07D239/48 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61P35/00 , C07D241/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
CPC分类号： C07D239/48 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
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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
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。
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公开(公告)号：EP2565194A1
公开(公告)日：2013-03-06
申请号：EP11774973.9
申请日：2011-04-26
申请人： Astellas Pharma Inc.
发明人： SAMIZU, Kiyohiro , MASUDA, Naoyuki , IIKUBO, Kazuhiko , KOGANEMARU, Yohei , KAWANO, Noriyuki , OHMORI, Junya , MITANI, Yasuyuki , NI, Keni
IPC分类号： C07D471/04 , A61K31/437 , A61K31/438 , A61K31/4545 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D495/14 , C07D519/00
CPC分类号： C07D471/04 , C07D211/48 , C07D221/04 , C07D471/08 , C07D471/10 , C07D471/14 , C07D491/044 , C07D495/14 , C07D519/00
摘要： [Problem]
To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
[Measures for Solution]
The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.摘要翻译： 本发明提供可用作具有PDE4B抑制活性的药物的化合物，特别是用作治疗或预防精神分裂症，阿尔茨海默氏病，痴呆，抑郁症等的组合物的活性成分。 [解决办法]本发明人研究了具有PDE4B抑制活性的化合物，发现三环或四环咪唑并[1,2-a]吡啶衍生物或其盐具有优异的PDE4B抑制活性，从而完成了本发明。 咪唑并[1,2-a]吡啶衍生物可用作治疗或预防精神分裂症，阿尔茨海默氏病，痴呆，抑郁症等的药剂。
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公开(公告)号：EP2172461A1
公开(公告)日：2010-04-07
申请号：EP08777903.9
申请日：2008-07-04
申请人： Astellas Pharma Inc.
发明人： KONDOH, Yutaka , IIKUBO, Kazuhiko , KUROMITSU, Sadao , SHINDO, Nobuaki , SOGA, Takatoshi , FURUTANI, Takashi , SHIMADA, Itsuro , MATSUYA, Takahiro , KUROSAWA, Kazuo , KAMIKAWA, Akio , MANO, Hiroyuki
IPC分类号： C07D239/95 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P43/00 , C07D251/18 , C07D251/50 , C07D251/52 , C07D251/54 , C07D401/12 , C07D401/14 , C07D403/12
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蛋白激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变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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