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公开(公告)号:US20130072495A1
公开(公告)日:2013-03-21
申请号:US13697819
申请日:2011-05-16
申请人: An-Hu Li , Mark J. Mulvihill , Arno G. Steinig
发明人: An-Hu Li , Mark J. Mulvihill , Arno G. Steinig
IPC分类号: C07D471/04 , A61K31/4985 , A61P35/00 , A61K31/4545 , A61K31/5025 , C07D487/04 , A61K31/437
CPC分类号: C07D487/04 , C07D471/04
摘要: Compounds of Formula I, 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 but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.
摘要翻译: 式I化合物,如下文所示和定义: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,例如但不限于至少部分至少驱动至少 RON,MET,IR,IGF-1R或ALK之一。 本发明并不限于本发明。
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公开(公告)号:US08367826B2
公开(公告)日:2013-02-05
申请号:US13308694
申请日:2011-12-01
申请人: Radoslaw Laufer , An-Hu Li , Mark J. Mulvihill , Arno G. Steinig
发明人: Radoslaw Laufer , An-Hu Li , Mark J. Mulvihill , Arno G. Steinig
IPC分类号: C07D471/00
CPC分类号: C07F5/025 , C07D471/04 , C07D487/04
摘要: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
摘要翻译: 其中X 1,X 2,X 3,X 4,X 5,X 6,X 7,R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶,并且可用于治疗和/或预防 过度增生性疾病如癌症,炎症,牛皮癣,过敏/哮喘,免疫系统的疾病和状况,中枢神经系统的疾病和状况。
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公开(公告)号:US20140088114A1
公开(公告)日:2014-03-27
申请号:US14117741
申请日:2012-05-15
申请人: Meizhong Jin , Mark J. Mulvihill , Arno G. Steinig , Jing WANG
发明人: Meizhong Jin , Mark J. Mulvihill , Arno G. Steinig , Jing WANG
IPC分类号: C07D471/04
CPC分类号: C07D471/04 , C07D487/04
摘要: Compounds of Formula (I), 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 at least one of MET, RON, ALK, IR, or IGF-1R. This Abstract is not limiting of the invention.
摘要翻译: 式(I)的化合物,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,例如至少部分地由至少一种MET,RON,ALK,IR ,或IGF-1R。 本发明并不限于本发明。
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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: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: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: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:US08592448B2
公开(公告)日:2013-11-26
申请号:US13130113
申请日:2009-11-19
申请人: Xin Chen , Melzhong Jin , Andrew Kleinberg , An-Hu Li , Mark J. Mulvihill , Arno G. Steinig , Jing Wang
发明人: Xin Chen , Melzhong Jin , Andrew Kleinberg , An-Hu Li , Mark J. Mulvihill , Arno G. Steinig , Jing Wang
IPC分类号: A61K31/437
CPC分类号: C07D471/04
摘要: Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
摘要翻译: 式I化合物,如下文所示和定义:(I)药学上可接受的盐,合成,中间体,制剂及其治疗方法,包括至少部分由Ron和/或Met介导的癌症。
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公开(公告)号:US08445510B2
公开(公告)日:2013-05-21
申请号:US13108024
申请日:2011-05-16
申请人: Mark J. Mulvihill , Arno G. Steinig , Andrew Philip Crew , Meizhong Jin , Andrew Kleinberg , An-Hu Li , Jing Wang
发明人: Mark J. Mulvihill , Arno G. Steinig , Andrew Philip Crew , Meizhong Jin , Andrew Kleinberg , An-Hu Li , Jing Wang
IPC分类号: A61K31/437 , C07D471/04
CPC分类号: C07D471/04
摘要: Compounds of Formula I, 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 at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
摘要翻译: 式I化合物,如下文所示和定义: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,例如至少部分地通过至少一种RON, MET或ALK。 本发明并不限于本发明。
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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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