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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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公开(公告)号:US20240360147A1
公开(公告)日:2024-10-31
申请号:US18687347
申请日:2022-08-30
Applicant: AMGEN INC.
Inventor: Athimoolam Arunachalampillai , Richard David Crockett , Robert P. Farrell , Ted Charles Judd , Adrian Ortiz , Joanna Robinson , Carolyn S. Wei , Kumiko Yamamoto , Diana Catherine Fager , Heather Claire Johnson , Neil Fred Langille , Liang Zhang
IPC: C07D491/147
CPC classification number: C07D491/147
Abstract: The disclosure provides processes for preparing Compound A, Compound E, Compound I, salts thereof, and/or stereoisomers thereof, as described 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: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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公开(公告)号:US20250115622A1
公开(公告)日:2025-04-10
申请号:US18730357
申请日:2023-02-03
Applicant: AMGEN INC.
Inventor: Ron C. Kelly , Mary Chaves , Jing Teng , Stephan Parent , Markian Stec , Van Luu , Robert P. Farrell , James E. Huckle , Michal Achmatowicz , Tian Wu , Darren Leonard Reid , Lingyun Xiao
IPC: C07D519/00 , A61K31/553
Abstract: Disclosed herein are crystalline forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-1616-cyclobuta[i] [1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-4,1′-naphthalene]-16,16,18(7H,17H)-trione (AMG 397): (AMG 397), hydrates, and solvates thereof. Also disclosed are methods of making the crystalline forms, and methods of treating diseases and disorders with the crystalline forms.
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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: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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公开(公告)号:US09656997B2
公开(公告)日:2017-05-23
申请号:US15297940
申请日:2016-10-19
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 , Gayathri Swaminath , Xiaodong Wang , Kevin Yang , Mikkel V. Debenedetto , Robert P. Farrell , Simon J. Hedley , Ted C. Judd , Frank Kayser
IPC: A61K31/4439 , A61K31/695 , A61K31/501 , A61K31/497 , A61K31/444 , A61K45/06 , A61K31/506 , C07D401/14 , C07D401/04 , C07D413/04 , A61K31/513 , 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 , 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:US20170042897A1
公开(公告)日:2017-02-16
申请号:US15298686
申请日:2016-10-20
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: A61K31/506 , C07D213/82 , A61K31/497 , C07D241/24 , C07D401/12 , A61K45/06 , A61K31/4439
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:US20250122224A1
公开(公告)日:2025-04-17
申请号:US18730353
申请日:2023-02-03
Applicant: AMGEN INC.
Inventor: Ron C. Kelly , Mary Chaves , Jing Teng , Stephan Parent , Van Luu , Robert P. Farrell , James E. Huckle , Michal Achmatowicz , Tian Wu , Darren Leonard Reid , Lingyun Xiao
IPC: C07D519/00 , A61K31/553
Abstract: Disclosed herein are salt and solvate forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-16,16-cyclobuta[i][1,4]oxazepino[3,4-f][1,2,7]thiadlazacyclohexadecine-4,1 naphthalene]-16,16,18 (7H,17H)-trione (AMG 397): (AMG 397), such as crystalline salt and solvate forms thereof. Also disclosed are methods of making the salt and solvate forms, and methods of treating diseases and disorders with the salt and solvate forms.
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