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公开(公告)号：EP1963312B1
公开(公告)日：2014-07-02
申请号：EP06838016.1
申请日：2006-11-17
申请人： Amgen Inc.
发明人： XUE, Qiufen , ALBRECHT, Brian K. , ANDERSEN, Denise Lyn , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HITCHCOCK, Stephen , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod F. , PENNINGTON, Lewis , WEISS, Matthew , YANG, Bryant , ZHONG, Wenge
IPC分类号： C07D405/12 , C07D413/12 , A61K31/44 , A61P25/28
CPC分类号： C07D405/12 , C07D413/12
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公开(公告)号：EP2231601B1
公开(公告)日：2014-06-18
申请号：EP08859859.4
申请日：2008-12-11
申请人： Amgen Inc.
IPC分类号： C07D211/50 , C07D241/06 , A61K31/496 , A61K31/4523 , A61P25/18
CPC分类号： C07D211/50 , C07D241/06
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3.发明公开AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开AMINOHETEROARYLVERBINDUNGEN ALSβ-分泌调节剂和其使用方法
公开(公告)号：EP2504315A1
公开(公告)日：2012-10-03
申请号：EP10782786.7
申请日：2010-11-19
申请人： Amgen Inc.
发明人： CHENG, Yuan , POWERS, Timothy , ASHTON, Kate , BROWN, James , HARRIED, Scott , HITCHCOCK, Stephen , JUDD, Ted , LOPEZ, Patricia , NIXEY, Thomas , PARAS, Nick A, , POON, Steve F. , ST. JEAN JR., David J. , XUE, Qiufen , ZHONG, Wenge
IPC分类号： C07D215/38 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/12 , C07D417/04 , A61K31/4709 , A61P25/28
CPC分类号： C07D215/38 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/12 , C07D417/04
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B
1 , B
2 , B
3 , L, R
1 , R
4 , R
5 and m of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.-
公开(公告)号：EP2231601A2
公开(公告)日：2010-09-29
申请号：EP08859859.4
申请日：2008-12-11
申请人： Amgen, Inc
IPC分类号： C07D211/50 , C07D241/06 , A61K31/496 , A61K31/4523 , A61P25/18
CPC分类号： C07D211/50 , C07D241/06
摘要： The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
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5.发明授权AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权氨基芳基化合物以β-分泌酶调节剂及其使用方法
公开(公告)号：EP2526092B1
公开(公告)日：2014-08-06
申请号：EP11702316.8
申请日：2011-01-14
申请人： Amgen Inc.
发明人： PARAS, Nick A, , BROWN, James , CHENG, Yuan , HITCHCOCK, Stephen , JUDD, Ted , LOPEZ, Patricia , MINATTI, Ana Elena , NIXEY, Thomas , POWERS, Timothy , TEGLEY, Christopher M. , XUE, Qiufen , YANG, Bryant , ZHONG, Wenge
IPC分类号： C07D215/38 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08 , A61K31/47 , A61K31/4709 , A61P25/28
CPC分类号： C07D401/10 , C07D215/38 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08
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6.发明公开AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权氨基芳基化合物以β-分泌酶调节剂及其使用方法
公开(公告)号：EP2526092A1
公开(公告)日：2012-11-28
申请号：EP11702316.8
申请日：2011-01-14
申请人： Amgen Inc.
发明人： PARAS, Nick A, , BROWN, James , CHENG, Yuan , HITCHCOCK, Stephen , JUDD, Ted , LOPEZ, Patricia , MINATTI, Ana Elena , NIXEY, Thomas , POWERS, Timothy , TEGLEY, Christopher M. , XUE, Qiufen , YANG, Bryant , ZHONG, Wenge
IPC分类号： C07D215/38 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08 , A61K31/47 , A61K31/4709 , A61P25/28
CPC分类号： C07D401/10 , C07D215/38 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B
1 , B
2 , B
3 , L, R
1 , R
2 , ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).-
7.发明授权NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS FOR THE TREATMENT OF RAF PROTEIN KINASE-MEDIATED DISEASES 有权含氮二环杂用于疾病治疗由RAF蛋白激酶介导BE
公开(公告)号：EP1976836B1
公开(公告)日：2012-08-22
申请号：EP06848110.0
申请日：2006-12-22
申请人： Amgen Inc.
发明人： DE MORIN, Frenel, F. , CHEN, Jian J. , DOHERTY, Elizabeth M. , HITCHCOCK, Stephen , HUANG, Qi , KIM, Joseph, L. , LIU, Gang , NIXEY, Thomas , PARAS, Nick, A. , PETKUS, Jeffrey , RETZ, Daniel, M. , SMITH, Adrian, L. , TASKER, Andrew , ZHU, Jiawang
IPC分类号： C07D239/84 , C07D239/95 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/435 , A61K31/495 , A61K31/55 , C07D471/04 , C07D487/04 , C07D495/04 , C07D413/04
CPC分类号： C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
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公开(公告)号：EP2041088B1
公开(公告)日：2014-01-08
申请号：EP07796466.6
申请日：2007-06-26
申请人： AMGEN INC.
IPC分类号： C07D213/36 , C07D243/08 , C07D295/14 , C07D333/20 , A61P25/18 , A61K31/495 , C07D241/04
CPC分类号： C07D241/04 , A61K31/495 , A61K31/551 , A61K33/00 , C07D213/36 , C07D241/08 , C07D243/08 , C07D295/15 , C07D333/20
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9.发明授权NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS FOR THE TREATMENT OF RAF PROTEIN KINASE-MEDIATED DISEASES 有权含氮二环杂用于疾病治疗由RAF蛋白激酶介导BE
公开(公告)号：EP1976836B9
公开(公告)日：2013-02-06
申请号：EP06848110.0
申请日：2006-12-22
申请人： Amgen Inc.
发明人： DE MORIN, Frenel, F. , CHEN, Jian J. , DOHERTY, Elizabeth M. , HITCHCOCK, Stephen , HUANG, Qi , KIM, Joseph, L. , LIU, Gang , NIXEY, Thomas , PARAS, Nick, A. , PETKUS, Jeffrey , RETZ, Daniel, M. , SMITH, Adrian, L. , TASKER, Andrew , ZHU, Jiawang
IPC分类号： C07D239/84 , C07D239/95 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/435 , A61K31/495 , A61K31/55 , C07D471/04 , C07D487/04 , C07D495/04 , C07D413/04
CPC分类号： C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
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公开(公告)号：EP2231602A1
公开(公告)日：2010-09-29
申请号：EP08859465.0
申请日：2008-12-12
申请人： Amgen, Inc
发明人： HITCHCOCK, Stephen , CHEN, Jian J. , NCUBE, Mqhele , NIXEY, Thomas , AMEGADZIE, Albert , KUNZ, Roxanne , QIAN, Wenyuan , CHEN, Ning , TEGLEY, Christopher M. , DEMORIN, Frenel , YUAN, Chester Chenguang , LIU, Qingyian , ZHU, Jiawang , PETERKIN, Tanya , ADAMS, Jeffrey A. , HU, Essa , CHAVEZ, JR., Frank
IPC分类号： C07D213/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , A61K31/00 , A61P25/28
CPC分类号： C07D213/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12
摘要： The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译： 本发明提供了为γ分泌酶调节剂的化合物，因此可用于治疗通过调节γ分泌酶例如阿尔茨海默氏病可治疗的疾病。 还提供了含有这些化合物的药物组合物以及制备这些化合物的方法。
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