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公开(公告)号：US11306107B2
公开(公告)日：2022-04-19
申请号：US16078152
申请日：2017-02-24
申请人： AMGEN INC.
发明人： Sean P. Brown , David Karl Bedke , Michael R. Degraffenreid , Jiasheng Fu , Zhihong Li , Felix Gonzalez Lopez De Turiso , Ana Gonzalez Buenrostro , Michael W. Gribble, Jr. , Michael G. Johnson , Todd J. Kohn , Kexue Li , Yunxiao Li , Mike Elias Lizarzaburu , Yosup Rew , Joshua Taygerly , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu , Manuel Zancanella , Xian Yun Jiao , Liusheng Zhu , Xianghong Wang , Julio C. Medina , Jason A. Duquette , Jonathan B. Houze , Marc Vimolratana , Mario G. Cardozo , Alan C. Cheng
IPC分类号： C07D513/10 , C07D513/20 , C07D515/10
摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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公开(公告)号：US09868721B2
公开(公告)日：2018-01-16
申请号：US15297272
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： C07D401/14 , C07D401/04 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/12 , A61K31/695 , C07F7/08 , A61K31/437 , C07C311/13 , C07D213/61 , C07D239/34 , C07D241/18 , C07D295/16
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：US09845310B2
公开(公告)日：2017-12-19
申请号：US15298748
申请日：2016-10-20
申请人： AMGEN INC.
发明人： Ning Chen , Xiaoqi 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 , David John Kopecky , Su-Jen Lai , Zhihua Ma , Lawrence R. McGee , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Xiaodong Wang , Kevin Yang , Mikkel V. Debenedetto , Simon J. Hedley
IPC分类号： A61K31/4439 , C07D239/30 , C07D401/14 , C07D401/04 , C07D413/04 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D241/12 , C07D241/24 , C07D249/08 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/12 , A61K31/695 , C07F7/08 , A61K31/437 , C07C311/13 , C07D213/61 , C07D239/34 , C07D241/18 , C07D295/16
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 VII, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula VII have the following structure: where the definitions of the variables are provided herein.
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4.发明授权公开(公告)号：US09593129B2
公开(公告)日：2017-03-14
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 , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu
IPC分类号： C07D498/14 , C07D221/20 , C07D471/10 , C07D211/76 , C07D279/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D407/04 , C07D407/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D498/08 , C07D498/20 , C07D405/04 , C07D417/12 , C07D417/14 , C07D491/08 , C07D491/153
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： 本发明提供式IE的MDM2抑制剂化合物，该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：US09573936B2
公开(公告)日：2017-02-21
申请号：US15158174
申请日：2016-05-18
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 , A61K45/06 , C07D213/82 , C07D241/24 , C07D239/30 , C07D239/26 , C07D401/04 , A61K31/4439 , A61K31/506 , C07D413/14 , C07B59/00 , A61K31/497 , A61K31/513 , C07D471/04 , A61K31/444 , C07D417/14 , C07B57/00 , C07D405/14 , A61K31/501 , C07D249/08 , C07D241/12 , C07D213/71 , C07D211/54
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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公开(公告)号：US09296736B2
公开(公告)日：2016-03-29
申请号：US14316586
申请日：2014-06-26
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 , 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 , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu
IPC分类号： C07D279/02 , C07D417/12 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D407/04 , C07D407/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D471/10 , C07D498/08 , C07D498/20 , C07D405/04 , C07D417/14 , C07D491/08 , C07D491/153
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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公开(公告)号：US20220169611A1
公开(公告)日：2022-06-02
申请号：US17672660
申请日：2022-02-15
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. Dequette, I , John Eksterowicz , Benjamin Fisher , Brian M. Fox , Jiasheng Fu , Zice Fu , Felix Gonzalez Lopez De Turiso , Michael W. Gribble , 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 , Josel McIntosh , Dustin L. McMinn , Julio C. Medina , Jeffrey Thomas Mihalic , Steven H. Olson , Yossup Rew , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu
IPC分类号： C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D407/04 , C07D407/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D471/10 , C07D498/08 , C07D498/20 , C07D279/02 , C07D405/04 , C07D417/12 , C07D417/14 , C07D491/08 , C07D491/153 , C07D221/20 , C07D498/14 , C07D405/12 , C07D409/12
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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公开(公告)号：US20190062276A1
公开(公告)日：2019-02-28
申请号：US15927426
申请日：2018-03-21
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 , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu
IPC分类号： C07D211/76 , C07D279/02 , C07D405/12 , C07D405/04 , C07D491/153 , C07D407/04 , C07D401/12 , C07D401/06 , C07D417/06 , C07D413/06 , C07D491/08 , C07D401/04 , C07D471/10 , C07D221/20 , C07D417/14 , C07D498/08 , C07D409/04 , C07D407/06 , C07D417/12 , C07D498/14 , C07D409/12 , 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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公开(公告)号：US20160340336A1
公开(公告)日：2016-11-24
申请号：US15158174
申请日：2016-05-18
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 , C07D213/82 , C07D241/24 , C07D239/30 , C07D239/26 , C07D401/04 , A61K31/4439 , A61K31/506 , C07D413/14 , C07B59/00 , A61K31/497 , A61K31/513 , C07D471/04 , A61K31/444 , C07D417/14 , C07B57/00 , C07D405/14 , A61K31/501 , C07D249/08 , C07D241/12 , C07D213/71 , C07D211/54 , A61K45/06
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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公开(公告)号：US11046680B1
公开(公告)日：2021-06-29
申请号：US16347910
申请日：2017-11-03
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 , James S. Harvey , Julie Anne Heath , Lars V. Heumann , Daniel B. Horne , Jonathan Houze , Matthew R. Kaller , Frank Kayser , Aarif Yusuf Khakoo , David J. Kopecky , Su-Jen Lai , Zhihua Ma , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Gayathri Swaminath , Xiaodong Wang , Malgorzata Wanska , Kevin Yang , Wen-Chen Yeh
IPC分类号： C07D417/14 , A61P9/00 , C07D401/14 , C07D403/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
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 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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