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1.发明申请公开(公告)号：US20200231601A1
公开(公告)日：2020-07-23
申请号：US16466207
申请日：2017-12-13
申请人： AMGEN INC.
发明人： Jennifer R. ALLEN , Matthew P. BOURBEAU , James A. BROWN , Ning CHEN , Michael J. FROHN , Zice FU , Longbin LIU , Qingyian LIU , Liping H. PETTUS , Wenyuan QIAN , Corey REEVES , Aaron C. SIEGMUND
IPC分类号： C07D513/08 , C07D417/10 , A61P25/28
摘要： The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2′, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
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公开(公告)号：US20170035744A1
公开(公告)日：2017-02-09
申请号：US15298748
申请日：2016-10-20
申请人： AMGEN INC.
发明人： Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC分类号： A61K31/4439 , C07D239/30 , C07D241/18 , C07D213/61 , A61K31/695 , A61K31/444 , A61K31/497 , A61K31/437 , A61K31/501 , A61K45/06 , C07C311/13 , C07D241/12 , C07D239/34 , C07D295/16 , A61K31/506 , C07D239/26
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号：US20170144971A1
公开(公告)日：2017-05-25
申请号：US15412804
申请日：2017-01-23
申请人： AMGEN INC.
发明人： Michael D. BARTBERGER , Ana GONZALEZ BUENROSTRO , Hilary Plake BECK , Xiaoqi CHEN , Richard Victor CONNORS , Jeffrey DEIGNAN , Jason A. DUQUETTE , John EKSTEROWICZ , Benjamin FISHER , Brian M. FOX , Jiasheng FU , Zice FU , Felix GONZALEZ LOPEZ DE TURISO , Michael W. GRIBBLE, Jr. , Darin J. GUSTIN , Julie A. HEATH , Xin HUANG , XianYun JIAO , Michael G. JOHNSON , Frank KAYSER , David John KOPECKY , SuJen LAI , Yihong LI , Zhihong LI , Jiwen LIU , Jonathan D. LOW , Brian S. LUCAS , Zhihua MA , Lawrence R. MCGEE , Joel MCINTOSH , Dustin L. MCMINN , Julio C. MEDINA , Jeffrey Thomas MIHALIC , Steven H. OLSON , Yosup REW , Phillip M. ROVETO , Daqing SUN , Xiaodong WANG , Yingcai WANG , Xuelei YAN , Ming YU , Jiang ZHU
IPC分类号： C07D211/76 , C07D417/12 , C07D413/06 , C07D471/10 , C07D409/04 , C07D417/06 , C07D405/04 , C07D401/04 , C07D279/02 , C07D401/12 , C07D491/08 , C07D498/08 , C07D409/12 , C07D405/12 , C07D417/14 , C07D498/20 , C07D401/06
CPC分类号： C07D211/76 , C07D221/20 , C07D279/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/06 , C07D409/04 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/10 , C07D491/08 , C07D491/153 , C07D498/08 , C07D498/14 , C07D498/20
摘要： The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
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4.发明申请公开(公告)号：US20160137667A1
公开(公告)日：2016-05-19
申请号：US15008342
申请日：2016-01-27
申请人： AMGEN INC.
发明人： Michael D. BARTBERGER , Ana GONZALEZ BUENROSTRO , Hilary Plake BECK , Xiaoqi CHEN , Richard Victor CONNORS , Jeffrey DEIGNAN , Jason A. DUQUETTE , John EKSTEROWICZ , Benjamin FISHER , Brian M. FOX , Jiasheng FU , Zice FU , Felix GONZALEZ LOPEZ DE TURISO , Michael W. GRIBBLE, JR. , Darin J. GUSTIN , Julie A. HEATH , Xin HUANG , XianYun JIAO , Michael G. JOHNSON , Frank KAYSER , David John KOPECKY , SuJen LAI , Yihong LI , Zhihong LI , Jiwen LIU , Jonathan D. LOW , Brian S. LUCAS , Zhihua MA , Lawrence R. MCGEE , Joel MCINTOSH , Dustin L. MCMINN , Julio C. MEDINA , Jeffrey Thomas MIHALIC , Steven H. OLSON , Yosup REW , Phillip M. ROVETO , Daqing SUN , Xiaodong WANG , Yingcai WANG , Xuelei YAN , Ming YU , Jiang ZHU
IPC分类号： C07D498/14 , C07D221/20 , C07D471/10
CPC分类号： C07D211/76 , C07D221/20 , C07D279/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/06 , C07D409/04 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/10 , C07D491/08 , C07D491/153 , C07D498/08 , C07D498/14 , C07D498/20
摘要： The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
摘要翻译： 本发明提供了式I的MDM2抑制剂化合物，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。
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公开(公告)号：US20180319773A1
公开(公告)日：2018-11-08
申请号：US16033632
申请日：2018-07-12
申请人： AMGEN INC.
发明人： Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC分类号： C07D401/14 , C07D401/12 , A61K31/437 , C07D417/14 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D471/04 , C07D413/14 , C07D413/04 , C07D401/04 , C07D213/61 , C07D239/34 , C07D241/18 , C07F7/08 , C07D295/16 , C07C311/13 , A61K31/695 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , C07D405/14
CPC分类号： C07D401/14 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号：US20170281625A1
公开(公告)日：2017-10-05
申请号：US15629567
申请日：2017-06-21
申请人： AMGEN INC.
发明人： Ning Chen , Xiaoqi CHEN , Yinhong CHEN , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Zhihua MA , Jeffrey T. MIHALIC , Gayathri SWAMINATH , Xiaodong WANG , Wen-Chen YEH
IPC分类号： A61K31/506 , A61K45/06 , A61K31/497
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.
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公开(公告)号：US20170044131A1
公开(公告)日：2017-02-16
申请号：US15298434
申请日：2016-10-20
申请人： AMGEN INC.
发明人： Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC分类号： C07D401/04 , A61K45/06 , C07D401/14 , A61K31/506 , C07D417/14 , A61K31/444 , A61K31/497 , A61K31/513 , C07D471/04 , A61K31/4439 , C07D413/14
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号：US20190275008A1
公开(公告)日：2019-09-12
申请号：US16347903
申请日：2017-11-03
申请人： AMGEN INC.
发明人： Matthew BROWN , Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , James S. HARVEY , Julie Anne HEATH , Lars V. HEUMANN , Jonathan HOUZE , Frank KAYSER , Aarif Yusuf KHAKOO , David j. KOPECKY , Su-Jen LAI , Zhihua MA , Julio C. MEDINA , Jeffrey T. MIHALIC , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Malgorzata WANSKA , Wen-Chen YEH
IPC分类号： A61K31/4196 , C07D405/14 , C07D405/04 , A61K31/506 , C07D405/12 , C07D471/04 , A61K31/437 , C07F7/08 , A61K31/4439 , A61K31/501 , C07D413/12 , A61K31/421 , C07D239/26 , C07D403/12
摘要： Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
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公开(公告)号：US20170320860A1
公开(公告)日：2017-11-09
申请号：US15584109
申请日：2017-05-02
申请人： AMGEN INC.
发明人： Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Mikkel V. DEBENEDETTO , Paul John DRANSFIELD , Zice FU , James S. HARVEY , Julie Anne HEATH , Simon J. HEDLEY , Jonathan HOUZE , Ted C. JUDD , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Wen-Chen YEH
IPC分类号： C07D405/14 , C07D471/04 , C07D405/04 , A61K31/5383 , A61K31/437 , A61K31/506 , A61K31/497 , A61K31/4439 , C07D498/04 , A61K45/06
CPC分类号： C07D405/14 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D409/14 , C07D471/04 , C07D498/04
摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号：US20170042872A1
公开(公告)日：2017-02-16
申请号：US15297940
申请日：2016-10-19
申请人： AMGEN INC.
发明人： Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua Ma , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. Judd , Frank KAYSER
IPC分类号： A61K31/4439 , A61K31/695 , A61K31/501 , A61K31/497 , A61K31/444 , A61K45/06 , A61K31/506
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
摘要翻译： 其中在这里提供变量的定义。
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