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11.发明授权公开(公告)号：US09376425B2
公开(公告)日：2016-06-28
申请号：US14347628
申请日：2012-09-26
Applicant: AMGEN INC.
Inventor： Michael D. Bartberger , Hilary Plake Beck , Xiaoqi Chen , Richard Victor Connors , Jeffrey Deignan , Jason A. Duquette , John Eksterowicz , Brian M. Fox , Jiasheng Fu , Ana Gonzalez Buenrostro , Felix Gonzalez Lopez De Turiso , Darin J. Gustin , Julie A. Heath , Michael G. Johnson , Frank Kayser , David John Kopecky , Yihong Li , Zhihong Li , Zhihua Ma , Joel McIntosh , Julio C. Medina , Jeffrey Thomas Mihalic , Steven H. Olson , Yosup Rew , Philip M. Roveto , Michael J. Schmitt , Daqing Sun , Xiaodong Wang , Malgorzata Wanska , Christine Weathers , Xuelei Yan
IPC: C07D265/06 , C07D413/04 , C07D413/10 , C07D417/04 , C07D413/12 , C07D265/32
CPC classification number: C07D413/04 , C07D265/06 , C07D265/32 , C07D413/10 , C07D413/12 , C07D417/04
Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, 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I或II的MDM2抑制剂化合物或其药学上可接受的盐，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：US20140163052A1
公开(公告)日：2014-06-12
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
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：US20240300892A1
公开(公告)日：2024-09-12
申请号：US18484675
申请日：2023-10-11
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 , 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
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.-
公开(公告)号：US10058550B2
公开(公告)日：2018-08-28
申请号：US15629567
申请日：2017-06-21
Applicant: AMGEN INC.
Inventor： 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: A61K31/506 , A61K31/497 , A61K45/06
CPC classification number: 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
Abstract: 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：US09751864B2
公开(公告)日：2017-09-05
申请号：US15298434
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: C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , C07D413/14 , 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 , 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: Methods of preparing compounds of Formula VI, salts thereof, tautomers thereof, or salts of the tautomers include cyclizing compounds of Formula V, salts thereof, tautomers thereof, or salts of the tautomers. Compounds of Formula VI and Formula V have the following structures: where the definitions of the variables are provided herein.
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Patent Agency Ranking
16.发明申请公开(公告)号：US20140235629A1
公开(公告)日：2014-08-21
申请号：US14347628
申请日：2012-09-26
Applicant: AMGEN INC.
Inventor： Michael D. Bartberger , Hilary Plake Beck , Xiaoqi Chen , Richard Victor Connors , Jeffrey Deignan , Jason A. Duquette , John Eksterowicz , Brian M. Fox , Jiasheng Fu , Ana Gonzalez Buenrostro , Felix Gonzalez Lopez De Turiso , Darin J. Gustin , Julie A. Heath , Michael G. Johnson , Frank Kayser , David John Kopecky , Yihong Li , Zhihong Li , Zhihua Ma , Joel Micintosh , Julio C. Medina , Jeffrey Thomas Mihalic , Steven H. Olson , Yosup Rew , Philip M. Roveto , Michael J. Schmitt , Daqing Sun , Xiaodong Wang , Malgorzata Wanska , Christine Weathers , Xuelei Yan
IPC: C07D413/04 , C07D265/32 , C07D413/10 , C07D417/04
CPC classification number: C07D413/04 , C07D265/06 , C07D265/32 , C07D413/10 , C07D413/12 , C07D417/04
Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, 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I或II的MDM2抑制剂化合物或其药学上可接受的盐，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：US10736883B2
公开(公告)日：2020-08-11
申请号：US16347903
申请日：2017-11-03
Applicant: AMGEN INC.
Inventor： 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: A61K31/4196 , A61K31/341 , C07D405/04 , C07D405/14 , A61K31/421 , A61K31/437 , A61K31/4439 , A61K31/501 , A61K31/506 , C07D239/26 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07F7/08 , A61P9/00 , A61P9/02 , C07D307/54
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: (I); (II). Intermediates (V) are also claimed.
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公开(公告)号：US10221162B2
公开(公告)日：2019-03-05
申请号：US16033632
申请日：2018-07-12
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: C07D401/12 , C07D401/14 , C07D405/14 , 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 , A61K31/437
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：US09988369B2
公开(公告)日：2018-06-05
申请号：US15584109
申请日：2017-05-02
Applicant: AMGEN INC.
Inventor： 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: C07D405/14 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D405/04 , C07D471/04 , C07D498/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
CPC classification number: 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
Abstract: 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：US09745286B2
公开(公告)日：2017-08-29
申请号：US15297487
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: A61K31/4439 , A61K31/501 , A61K31/444 , A61K31/506 , A61K31/497 , C07D401/14 , A61K31/437 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/00 , 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
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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