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公开(公告)号:US20090197862A1
公开(公告)日:2009-08-06
申请号:US12365325
申请日:2009-02-04
申请人: Arno G. Steinig , Mark J. Mulvihill , Jing Wang , Douglas S. Werner , Qinghua Weng , Julie Kan , Heather Coate , Xin Chen
发明人: Arno G. Steinig , Mark J. Mulvihill , Jing Wang , Douglas S. Werner , Qinghua Weng , Julie Kan , Heather Coate , Xin Chen
IPC分类号: A61K31/4439 , C07D401/14 , C07D417/14 , C07D451/02 , C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , A61K31/4725 , A61K31/5377 , A61K31/4545
CPC分类号: C07D417/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D451/04
摘要: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.
摘要翻译: 具有式I结构的2-氨基吡啶化合物和这些化合物的药学上可接受的盐。 式I的化合物抑制动物(包括人)中酪氨酸激酶的活性,并且可用于治疗和/或预防各种疾病和病症。 特别地,本文公开的化合物是激酶抑制剂,特别是但不限于KDR,Tie-2,Flt3,FGFR3,Ab1,Aurora A,c-Src,IGF-1R,ALK,c-MET,RON, PAK1,PAK2和TAK1,并且可用于治疗增殖性疾病,例如但不限于癌症。 本发明还涉及包含治疗有效量的式I化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物。 本发明还涉及通过向患者施用治疗有效量的上述药物组合物来治疗具有由蛋白激酶活性介导的病症的患者的方法。
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公开(公告)号:US08178668B2
公开(公告)日:2012-05-15
申请号:US12365325
申请日:2009-02-04
申请人: Arno G. Steinig , Mark J. Mulvihill , Jing Wang , Douglas S. Werner , Qinghua Weng , Heather Coate , Xin Chen
发明人: Arno G. Steinig , Mark J. Mulvihill , Jing Wang , Douglas S. Werner , Qinghua Weng , Heather Coate , Xin Chen
IPC分类号: C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D487/04
CPC分类号: C07D417/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D451/04
摘要: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.
摘要翻译: 具有式I结构的2-氨基吡啶化合物和这些化合物的药学上可接受的盐。 式I的化合物抑制动物(包括人)中酪氨酸激酶的活性,并且可用于治疗和/或预防各种疾病和病症。 特别地,本文公开的化合物是激酶抑制剂,特别是但不限于KDR,Tie-2,Flt3,FGFR3,Ab1,Aurora A,c-Src,IGF-1R,ALK,c-MET,RON, PAK1,PAK2和TAK1,并且可用于治疗增殖性疾病,例如但不限于癌症。 本发明还涉及包含治疗有效量的式I化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物。 本发明还涉及通过向患者施用治疗有效量的上述药物组合物来治疗具有由蛋白激酶活性介导的病症的患者的方法。
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公开(公告)号:US20120046267A1
公开(公告)日:2012-02-23
申请号:US13025281
申请日:2011-02-11
申请人: Keith R. Hornberger , Dan M. Berger , Xin Chen , Andrew P. Crew , Hanqing Dong , Andrew Kleinberg , An-Hu Li , Lifu Ma , Mark J. Mulvihill , Bijoy Panicker , Kam W. Siu , Arno G. Steinig , James G. Tarrant , Jing Wang , Qinghua Weng , Rajaram Sangem , Ramesh C. Gupta
发明人: Keith R. Hornberger , Dan M. Berger , Xin Chen , Andrew P. Crew , Hanqing Dong , Andrew Kleinberg , An-Hu Li , Lifu Ma , Mark J. Mulvihill , Bijoy Panicker , Kam W. Siu , Arno G. Steinig , James G. Tarrant , Jing Wang , Qinghua Weng , Rajaram Sangem , Ramesh C. Gupta
IPC分类号: A61K31/4355 , A61K31/4545 , A61K31/4725 , A61K31/4709 , A61K31/5377 , C07D495/04 , A61K31/4365 , A61K31/519 , A61K31/5025 , C07D513/04 , A61K31/437 , C07D487/04 , A61K31/4985 , A61K31/502 , C12N9/99 , A61P35/00 , A61P29/00 , C07D491/048
CPC分类号: C07D491/048
摘要: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
摘要翻译: 式1的化合物,如下文所定义:其药学上可接受的盐,合成,中间体,制剂及其治疗方法,包括治疗癌症,例如至少部分由TAK1驱动的肿瘤,或适合于 TAK1抑制剂有效。 本发明并不限于本发明。
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公开(公告)号:US08378104B2
公开(公告)日:2013-02-19
申请号:US13025281
申请日:2011-02-11
申请人: Keith R. Hornberger , Dan M. Berger , Xin Chen , Andrew P. Crew , Hanqing Dong , Andrew Kleinberg , An-Hu Li , Lifu Ma , Mark J. Mulvihill , Bijoy Panicker , Kam W. Siu , Arno G. Steinig , James G. Tarrant , Jing Wang , Qinghua Weng , Rajaram Sangem , Ramesh C. Gupta
发明人: Keith R. Hornberger , Dan M. Berger , Xin Chen , Andrew P. Crew , Hanqing Dong , Andrew Kleinberg , An-Hu Li , Lifu Ma , Mark J. Mulvihill , Bijoy Panicker , Kam W. Siu , Arno G. Steinig , James G. Tarrant , Jing Wang , Qinghua Weng , Rajaram Sangem , Ramesh C. Gupta
IPC分类号: C07D471/02
CPC分类号: C07D491/048
摘要: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
摘要翻译: 式1的化合物,如下文所定义:其药学上可接受的盐,合成,中间体,制剂及其治疗方法,包括治疗癌症,例如至少部分由TAK1驱动的肿瘤,或适合于 TAK1抑制剂有效。 本发明并不限于本发明。
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公开(公告)号:US20090197864A1
公开(公告)日:2009-08-06
申请号:US12366743
申请日:2009-02-06
申请人: An-Hu Li , Arno G. Steinig , Andrew Kleinberg , Qinghua Weng , Mark J. Mulvihill , Jing Wang , Xin Chen , Ti Wang , Hanqing Dong , Meizhong Jin
发明人: An-Hu Li , Arno G. Steinig , Andrew Kleinberg , Qinghua Weng , Mark J. Mulvihill , Jing Wang , Xin Chen , Ti Wang , Hanqing Dong , Meizhong Jin
IPC分类号: A61K31/4355 , C07D491/048 , A61K31/00 , A61K31/54 , A61K31/5377 , A61K31/506 , A61P35/00
CPC分类号: C07D491/048
摘要: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
摘要翻译: 呋喃并[3,2-c]吡啶和噻吩并[3,2-c]吡啶化合物及其药学上可接受的盐,制剂,中间体,药物组合物和用途,例如疾病治疗包括癌症,包括 涉及EMT的病症,包括蛋白激酶活性介导的病症,如RON和/或MET。
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公开(公告)号:US08022206B2
公开(公告)日:2011-09-20
申请号:US12366743
申请日:2009-02-06
申请人: An-Hu Li , Arno G. Steinig , Andrew Kleinberg , Qinghua Weng , Mark J. Mulvihill , Jing Wang , Xin Chen , Ti Wang , Hanqing Dong , Meizhong Jin
发明人: An-Hu Li , Arno G. Steinig , Andrew Kleinberg , Qinghua Weng , Mark J. Mulvihill , Jing Wang , Xin Chen , Ti Wang , Hanqing Dong , Meizhong Jin
IPC分类号: C07D413/00 , C07D403/00 , C07D471/02
CPC分类号: C07D491/048
摘要: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
摘要翻译: 呋喃并[3,2-c]吡啶和噻吩并[3,2-c]吡啶化合物及其药学上可接受的盐,制剂,中间体,药物组合物和用途,例如疾病治疗包括癌症,包括 涉及EMT的病症,包括蛋白激酶活性介导的病症,如RON和/或MET。
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公开(公告)号:US08796455B2
公开(公告)日:2014-08-05
申请号:US13767947
申请日:2013-02-15
申请人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
发明人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
IPC分类号: C07D487/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , A61K31/5025 , A61P19/02 , A61P35/00
CPC分类号: C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是mTOR的抑制剂,可用于治疗癌症。
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公开(公告)号:US07700594B2
公开(公告)日:2010-04-20
申请号:US11599663
申请日:2006-11-15
申请人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
发明人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A. R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
IPC分类号: C07D487/04 , C07D401/14 , C07D403/04 , A61K31/53 , A61K31/4523 , A61K35/00
CPC分类号: C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是mTOR的抑制剂,可用于治疗癌症。
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公开(公告)号:US20110218183A1
公开(公告)日:2011-09-08
申请号:US13106954
申请日:2011-05-13
申请人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kem W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
发明人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kem W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
IPC分类号: A61K31/4985 , C07D487/04 , A61K31/53 , C07D519/00 , A61K31/5377 , A61P35/00
CPC分类号: C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是mTOR的抑制剂,可用于治疗癌症。
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公开(公告)号:US20090163468A1
公开(公告)日:2009-06-25
申请号:US12326536
申请日:2008-12-02
申请人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joesph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
发明人: Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joesph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Qinghua Weng , James David Beard
IPC分类号: A61K31/397 , C07D487/02 , A61K31/4985 , A61K31/5377 , C07F5/02 , A61P19/02 , A61P37/00 , A61P35/00 , C07D253/06 , C07D413/14 , A61K31/53
CPC分类号: C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是mTOR的抑制剂,可用于治疗癌症。
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