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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
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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.
Abstract translation: 其中在这里提供变量的定义。
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公开(公告)号:US20140011796A1
公开(公告)日:2014-01-09
申请号:US14025688
申请日:2013-09-12
Applicant: AMGEN INC.
Inventor: Michael David BARTBERGER , Ana Gonzalez Buenrostro , Hilary Plake Beck , Xiaoqi Chen , Richard Victor Connors , Jeffrey Deignan , Jason Duquette , John Eksterwicz , Benjamin Fisher , Brian Matthew Fox , Jiasheng Fu , Zice Fu , Felix Gonzalez Lopez De Turiso , Michael William Gribble , Dann James Gustin , Julie Anne Heath , Xin Huang , Xianyun Jiao , Michael Johnson , Frank Kayser , David John Kopecky , Sujen Lai , Yihong Li , Zhihong Li , Jiwen Liu , Jonathan Dante Low , Brian Stuart Lucas , Zhihua Ma , Lawrence R. McGee , Joel McIntosh , Dustin McMinn , Julio Cesar Medina , Jeffrey Thomas Mihalic , Steven Howard Olson , Yosup Rew , Philip Marley Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu
IPC: C07D211/76 , C07D417/12 , C07D413/06 , C07D471/10 , C07D409/04 , C07D401/04 , C07D279/02 , C07D491/08 , C07D498/08 , C07D417/14 , C07D491/153 , C07D417/06 , C07D401/06 , C07D405/04
CPC classification number: 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
Abstract: 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:US11285135B2
公开(公告)日:2022-03-29
申请号:US16675121
申请日:2019-11-05
Applicant: AMGEN INC.
Inventor: Brian Alan Lanman , Victor J. Cee , Alexander J. Pickrell , Anthony B. Reed , Kevin C. Yang , David John Kopecky , Hui-Ling Wang , Patricia Lopez , Kate Ashton , Shon Booker , Christopher M. Tegley
IPC: C07D417/04 , C07D417/14 , C07D513/04 , A61K31/428 , A61K31/496 , A61K31/519 , A61P35/00 , A61K31/5025 , A61K31/502 , A61K31/517 , C07D275/04 , C07D471/08 , C07D403/04 , C07D401/04 , C07D487/04 , C07D239/80 , C07D487/10 , C07D471/04
Abstract: Provided herein are methods of treating cancer with KRAS G12C inhibitors of Formula I and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号:US11090304B2
公开(公告)日:2021-08-17
申请号:US16402538
申请日:2019-05-03
Applicant: Amgen Inc.
Inventor: John Gordon Allen , Jennifer Rebecca Allen , Ana Elena Minatti , Qiufen Xue , Ryan Paul Wurz , Christopher M. Tegley , Alexander J. Pickrell , Thomas T. Nguyen , Vu Van Ma , Patricia Lopez , Longbin Liu , David John Kopecky , Michael J. Frohn , Ning Chen , Jian Jeffrey Chen , Aaron C. Siegmund , Albert Amegadzie , Nuria A. Tamayo , Shon Booker , Clifford Goodman , Mary Walton , Nobuko Nishimura , Youngsook Shin , Jonathan D. Low , Victor J. Cee , Anthony B. Reed , Hui-Ling Wang , Brian Alan Lanman
IPC: A61K31/517 , A61P35/00 , A61K31/4985 , A61K39/395 , C07D403/04 , C07D471/04
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号:US10519146B2
公开(公告)日:2019-12-31
申请号:US15984855
申请日:2018-05-21
Applicant: Amgen Inc.
Inventor: Brian Alan Lanman , Jian Chen , Anthony B. Reed , Victor J. Cee , Longbin Liu , David John Kopecky , Patricia Lopez , Ryan Paul Wurz , Thomas T. Nguyen , Shon Booker , Nobuko Nishimura , Youngsook Shin , Nuria A. Tamayo , John Gordon Allen , Jennifer Rebecca Allen
IPC: C07D471/04 , C07D487/04 , C07D403/04 , C07D401/04 , C07D475/00 , A61K31/496 , A61K31/519 , A61P35/00 , C07D417/04 , A61K38/07 , C07D487/08 , C07D417/12 , C07D513/04 , C07D487/10 , C07D239/80 , C07D401/14 , C07D237/34 , A61K31/416 , A61K31/55 , A61K31/454 , A61K31/517 , A61K31/502 , A61K31/5025 , A61K31/7068 , C07D275/04
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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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
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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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28.Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer 有权
Title translation: 哌啶酮衍生物作为治疗癌症的MDM2抑制剂公开(公告)号:US09593129B2
公开(公告)日:2017-03-14
申请号:US15008342
申请日:2016-01-27
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: AMGEN INC.
Inventor: 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: 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 classification number: 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
Abstract: 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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