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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:US08969336B2
公开(公告)日:2015-03-03
申请号:US13266164
申请日:2010-05-06
申请人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
发明人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
IPC分类号: A61K31/55 , A61K31/497 , A61K31/4965 , A61K31/505 , A61K31/54 , C07D243/08 , C07D413/14 , C07D241/02 , C07D237/02 , C07D401/12 , C07D239/48 , C07D241/26 , C07D241/28 , 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 EML4-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EML4-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入和广泛的研究的结果,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:US20120040968A1
公开(公告)日:2012-02-16
申请号:US13266164
申请日:2010-05-06
申请人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
发明人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
IPC分类号: A61K31/497 , C07D405/14 , C07D401/14 , C07D491/113 , C07D403/12 , A61K31/551 , A61K31/538 , C07D409/14 , C07D417/12 , A61K31/55 , A61K31/541 , C07D471/08 , C07D241/28 , C07D401/12 , A61K31/513 , C07D239/48 , A61P35/00 , A61K31/5377
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 EML4-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EML4-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入和广泛的研究的结果,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:US20070249587A1
公开(公告)日:2007-10-25
申请号:US11576889
申请日:2005-10-05
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/517 , A61K31/519 , A61K31/55 , A61P3/10 , C07D403/02 , C07D471/04 , C07D495/04
CPC分类号: C07D471/04 , C07D495/04 , C07D513/04
摘要: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供已经与选自噻吩,噻唑和吡啶的芳族杂环或其药学上可接受的盐融合的新的嘧啶衍生物; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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公开(公告)号:US07947690B2
公开(公告)日:2011-05-24
申请号:US11577648
申请日:2005-10-17
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/519 , A61K31/497 , C07D495/04 , A61P3/10 , C07D487/04 , C07D471/04 , C07D239/72 , A61K31/517
CPC分类号: C07D239/70 , C07D239/94 , C07D495/04
摘要: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.
摘要翻译: 本发明提供由式(I)表示的稠合嘧啶化合物或其药学上可接受的盐:其中A表示环,其中所述环中至少一个碳原子任选被一个或多个选自以下的基团取代:低级烷基 ,-O-(低级烷基),卤素原子,羧基,-CO 2 - (低级烷基)和氨基甲酰基,R 1表示:(1)被至少三个卤素原子取代的苯基,其可以具有至少一个另外的取代基,或 (2)环丙基,环丁基,环戊基,环己基或环庚基,其各自任选被取代; 并且R 2表示由式(II)表示的基团或任选取代的环状氨基:其中R 21和R 22可以相同或不同,并且各自表示-H,低级烷基,低级烯基,低级炔基,环烷基,苯基,杂芳基, 芳族杂环基或-O-(低级烷基),其各自任选被取代。
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公开(公告)号:US20080070896A1
公开(公告)日:2008-03-20
申请号:US11577648
申请日:2005-10-17
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/519 , A61K31/497 , A61K31/5377 , A61K31/551 , A61P3/00 , C07D285/36 , C07D413/14 , C07D495/04 , C07D487/04 , C07D403/04 , C07D239/70 , A61K31/554 , A61K31/55 , A61K31/517
CPC分类号: C07D239/70 , C07D239/94 , C07D495/04
摘要: There are provided new pyrimidine derivatives condensed with a non-aromatic ring selected from dihydrothiophene, dihydrofuran, cycloalkane moiety, and the like or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供了与选自二氢噻吩,二氢呋喃,环烷烃部分等的非芳香环稠合的新的嘧啶衍生物或其药学上可接受的盐; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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公开(公告)号:US07557112B2
公开(公告)日:2009-07-07
申请号:US11576889
申请日:2005-10-05
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61P3/10 , C07D495/04 , C07D279/12 , C07D417/04 , C07D413/04 , A61K31/541 , A61K31/5355 , A61K31/519
CPC分类号: C07D471/04 , C07D495/04 , C07D513/04
摘要: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供已经与选自噻吩,噻唑和吡啶的芳族杂环或其药学上可接受的盐融合的新的嘧啶衍生物; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖型糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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