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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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3.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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5.
公开(公告)号:US09359355B2
公开(公告)日:2016-06-07
申请号:US14088796
申请日:2013-11-25
Applicant: AMGEN INC.
Inventor: Xiaoqi Chen , Kang Dai , Jason Duquette , Michael W. Gribble, Jr. , Justin N. Huard , Kathleen S. Keegan , Zhihong Li , Sarah E. Lively , Lawrence R. McGee , Mark L. Ragains , Xianghong Wang , Margaret F. Weidner , Jian Zhang
IPC: C07D471/14 , C07D519/00
CPC classification number: C07D519/00 , C07D471/14
Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.
Abstract translation: 式I化合物是CDK 4,CDK 6和FLT 3的有用抑制剂。 这些化合物可用于治疗癌症和各种其他疾病状况。 式I的化合物具有以下结构:其中R1是式IA,式IB,式IC或式ID的基团,并且本文提供了其它变量的定义。
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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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公开(公告)号:US11046680B1
公开(公告)日:2021-06-29
申请号:US16347910
申请日:2017-11-03
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 , 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: C07D417/14 , A61P9/00 , C07D401/14 , C07D403/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
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 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:US20210179560A1
公开(公告)日:2021-06-17
申请号:US16983027
申请日:2020-08-03
Applicant: Amgen Inc.
Inventor: Michael D. Bartberger , Ana Gonzalez Buenrostro , Hilary Plake Beck , Xiaoqi Chen , Richard Victor Connors , Jeffrey Deignan , Jason A. Duquette, 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 , Joel 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: C07D211/76 , C07D401/12 , C07D498/14 , C07D409/04 , C07D407/04 , C07D471/10 , C07D401/06 , C07D279/02 , C07D405/04 , C07D417/12 , C07D405/12 , C07D417/06 , C07D221/20 , C07D498/08 , C07D491/153 , C07D498/20 , C07D409/12 , C07D491/08 , C07D417/14 , C07D413/06 , C07D407/06 , C07D401/04
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:US10150760B2
公开(公告)日:2018-12-11
申请号:US15945852
申请日:2018-04-05
Applicant: AMGEN INC.
Inventor: Xiaoqi Chen , Alan C. Cheng , Richard V. Connors , Mikkel V. Debenedetto , Paul John Dransfield , Zice Fu , James S. Harvey , Julie Anne Heath , Jonathan Houze , Ted C. Judd , David John Kopecky , Su-Jen Lai , Zhihua Ma , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Xiaodong Wang
IPC: C07D405/14 , C07D403/14 , C07D409/14 , C07D401/14 , C07D403/04 , A61K45/06 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5383 , C07D498/04 , C07D405/04 , C07D471/04 , A61K31/437
Abstract: Compounds of Formula V, salts thereof, tautomers thereof, and salts of the tautomers have the following structure and are useful compounds in preparing small molecule agonists of the APJ Receptor: where the definitions of the variables are provided herein.
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公开(公告)号:US09656998B2
公开(公告)日:2017-05-23
申请号:US15298686
申请日:2016-10-20
Applicant: AMGEN INC.
Inventor: Ning Chen , Xiaoqi Chen , 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 , Robert P. Farrell , Simon J. Hedley , Ted C. Judd
IPC: C07D213/82 , C07D241/24 , C07D401/12 , 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 , C07D239/26 , C07D239/30 , C07D241/12 , C07D249/08 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/695
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 V, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula V have the following structure: where the definitions of the variables are provided herein.
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