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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
Applicant: Amgen Inc.
Inventor： 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: 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
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：US20190062276A1
公开(公告)日：2019-02-28
申请号：US15927426
申请日：2018-03-21
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: 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
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：US20180222895A1
公开(公告)日：2018-08-09
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 , C07D409/14 , C07D403/14 , C07D403/04 , C07D401/14 , A61K45/06 , A61K31/4439 , A61K31/437 , A61K31/506 , A61K31/5383 , C07D498/04 , C07D405/04 , C07D471/04 , A61K31/497
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 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：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：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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Patent Agency Ranking
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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7.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
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：US09365522B2
公开(公告)日：2016-06-14
申请号：US14633936
申请日：2015-02-27
Applicant: AMGEN INC. , TEIJIN PHARMA LIMITED
Inventor： Hilary Plake Beck , Shon Keith Booker , Howard Bregman , Victor J. Cee , Nagasree Chakka , Timothy D. Cushing , Oleg Epstein , Brian M. Fox , Stephanie Geuns-Meyer , Xiaolin Hao , Kenta Hibiya , Jun Hirata , Zihao Hua , Jason Human , Shinji Kakuda , Patricia Lopez , Ryota Nakajima , Kazuhisa Okada , Steven H. Olson , Hiroyuki Oono , Lewis D. Pennington , Kosuke Sasaki , Keiko Shimada , Youngsook Shin , Ryan D. White , Ryan P. Wurz , Shuyan Yi , Xiao Mei Zheng
IPC: C07D231/14 , C07D403/12 , C07D401/14 , C07D405/14 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/14 , C07D493/08 , C07D413/12 , A61K31/4155 , A61K31/44 , A61K31/4427 , A61K31/422
CPC classification number: C07D231/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14 , C07D493/08
Abstract: The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
Abstract translation: 本发明涉及具有抑制RORγ活性的新型化合物。 本发明还涉及包含该化合物的药物组合物，该化合物在治疗或预防自身免疫疾病，炎性疾病，代谢疾病或癌症疾病中的用途。
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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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