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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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22.发明授权公开(公告)号：US10246429B2
公开(公告)日：2019-04-02
申请号：US15749895
申请日：2016-08-04
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Albert Amegadzie , Matthew P. Bourbeau , James A. Brown , Ning Chen , Michael J. Frohn , Longbin Liu , Qingyian Liu , Liping H. Pettus , Wenyuan Qian , Corey M. Reeves , Aaron C. Siegmund
IPC: C07D417/10 , C07D279/08 , C07D417/14 , C07D471/04 , C07D491/056 , A61P25/28 , A61P25/00 , A61P25/16 , C07D491/08 , C07D491/107 , C07D498/10 , C07F7/08
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.
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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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Patent Agency Ranking
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：US20250059205A1
公开(公告)日：2025-02-20
申请号：US18696946
申请日：2022-04-28
Applicant: AMGEN INC.
Inventor： Brian Alan Lanman , Ryan Paul Wurz , Wei Zhao , Xiaofen Li , Michael M. Yamano , Yunxiao Li , Ning Chen , Birgitte Weinreich Husemoen , Sebastian Leth-Petersen , Jose M. Medina , Kexue Li , Liping Pettus , Rene Rahimoff , Primali Vasundera Navaratne , Huan Rui , Christopher P. Mohr
IPC: C07D519/00 , A61K31/4995 , A61K31/517 , C07D487/08
Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: (I) wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.
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公开(公告)号：US20240417412A1
公开(公告)日：2024-12-19
申请号：US18695688
申请日：2022-08-10
Applicant: AMGEN INC.
Inventor： Brian Alan Lanman , Wei Zhao , Ryan Paul Wurz , Primali Vasundera NAVARATNE , Liping PETTUS , Michael M. YAMANO , Ning Chen , Rene RAHIMOFF , Francesco MANONI , John STELLWAGEN
IPC: C07D519/00 , A61K31/519 , A61K31/5377 , A61K31/553
Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.
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29.发明授权公开(公告)号：US11548903B2
公开(公告)日：2023-01-10
申请号：US16466202
申请日：2017-12-13
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Matthew P. Bourbeau , Ning Chen , Qingyian Liu , Liping H. Pettus , Aaron C. Siegmund
IPC: C07D513/04 , C07D498/04 , A61P25/28
Abstract: The present disclosure provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I): (Formula (I)) wherein variables X, Y, R2, R3, R4, R5, R6, and n of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
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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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