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公开(公告)号：US20170275327A1
公开(公告)日：2017-09-28
申请号：US15503776
申请日：2015-08-14
Applicant: John Simon EDWARDS , Peter Richard MULLENS , Edward CLEATOR , Bryon L. SIMMONS , Courtney K. MAGUIRE , Jeremy Peter SCOTT , Nobuyoshi YASUDA , Yong ZHONG , Lisa F. FREY , Peter G. DORMER , Andrew BRUNSKILL , Artis KLAPARS , Eric ASHLEY , Pu QIAN , Yi ZHANG , Baoqiang WAN , MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED
Inventor： John Edwards , Peter Richard Mullens , Ed Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Puneet Qian , Yi Zhang , Baoqiang Wan
CPC classification number: C07H19/10 , C07F9/242 , C07F9/2458 , C07F9/2487 , C07F9/58 , C07F9/65586 , C07H19/06
Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
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公开(公告)号：US10214554B2
公开(公告)日：2019-02-26
申请号：US15427674
申请日：2017-02-08
Applicant: Merck Sharp & Dohme Corp.
Inventor： John Y. L. Chung , Amude Kassim , John Limanto , Michael Shevlin , Peter E. Maligres , Daniel A. DiRocco , James F. Dropinski , Rose Mathew , Yi Ning Ji Chen , Edward C. Sherer , Mikhail Reibarkh , Artis Klapars , Alan Hyde , Susan L. Zultanski , Aaron Moment , Bryon Simmons , Tyler A. Davis , Timothy James Wright , Ralph Calabria , Louis charles Campeau
IPC: C07H19/00 , C07H19/048 , C07H19/10 , C07H19/06 , C07H19/24 , C07D487/04
Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
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公开(公告)号：US10202401B2
公开(公告)日：2019-02-12
申请号：US15807992
申请日：2017-11-09
Inventor： Hongming Li , Jingjun Yin , Kevin M. Belyk , Kevin R. Campos , Qinghao Chen , Alan M. Hyde , Tetsuji Itoh , Artis Klapars , Matthew Thomas Tudge , Edward Cleator , Aaron M. Dumas , Louis-Charles Campeau , Yonggang Chen , Ji Qi , Wensong Xiao
IPC: C07D265/14 , C07D498/04 , C07C251/24 , C07F9/6509 , C07F17/02 , C07D413/14 , C07D239/74 , C07D413/04 , C07D417/04 , C07D265/36
Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.
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![PROCESS FOR THE PREPARATION OF TERT-BUTYL 4-((2S,5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDO)PIPERIDINE-1-CARBOXYLATE AND ANALOGS THEREOF](/abs-image/US/2017/12/21/US20170362233A1/abs.jpg.150x150.jpg)
公开(公告)号：US20170362233A1
公开(公告)日：2017-12-21
申请号：US15532788
申请日：2015-11-30
Applicant: Merck Sharp & Dohme Corp.
Inventor： Zhijian Liu , Nobuyoshi Yasuda , Lu Yang , Artis Klapars , Kevin R. Campos , Mikhail Reibarkh
IPC: C07D471/08 , C07F7/18 , C07F7/10
CPC classification number: C07D471/08 , C07F7/10 , C07F7/1804
Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include intermediates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US10251903B2
公开(公告)日：2019-04-09
申请号：US15519846
申请日：2015-10-20
Applicant: MERCK SHARP & DOHME CORP. , IDENIX Pharmaceuticals LLC , Bryon L. Simmons , Kevin R. Campos , Artis Klapars , Alistair J. Stewart , Benjamin A. Mayes , Peter E. Maligres , Alan Hyde , Steven Mark Silverman , Yong-Li Zhong , Adel M. Moussa , Kenneth Baker , Kara Van Valkenburg
Inventor： Bryon L. Simmons , Kevin R. Campos , Artis Klapars , Alistair J. Stewart , Benjamin A. Mayes , Peter E. Maligres , Alan Hyde , Steven Mark Silverman , Yong-Li Zhong , Adel M. Moussa , Kenneth Baker , Kara Van Valkenburg
IPC: C07H19/10 , A61K31/7052 , C07H1/00 , C08K3/08
Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
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Patent Agency Ranking
公开(公告)号：US10597422B2
公开(公告)日：2020-03-24
申请号：US16248273
申请日：2019-01-15
Applicant: Merck Sharp & Dohme Corp.
Inventor： Daniel DiRocco , Artis Klapars , Edward C. Sherer
IPC: C07D239/00 , C07D421/00 , C07D517/00 , C07H19/10 , C07H19/06 , C07H19/24 , C07D487/04 , C07H9/06 , C07H1/00 , C07H1/02
Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
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公开(公告)号：US10526363B2
公开(公告)日：2020-01-07
申请号：US15503776
申请日：2015-08-14
Applicant: Merck Sharp & Dohme Corp. , Merck Sharp & Dohme Limited , John Simon Edwards , Peter Richard Mullens , Edward Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Pu Qian , Yi Zhang , Baoqiang Wan , Eric Ashley
Inventor： John Simon Edwards , Peter Richard Mullens , Edward Cleator , Bryon L. Simmons , Courtney K. Maguire , Jeremy Peter Scott , Nobuyoshi Yasuda , Yong-Li Zhong , Lisa F. Frey , Peter G. Dormer , Andrew Brunskill , Artis Klapars , Pu Qian , Yi Zhang , Baoqiang Wan , Eric Ashley
IPC: C07H19/10 , C07F9/58 , C07H19/06 , C07F9/24 , C07F9/6558
Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
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公开(公告)号：US20180111954A1
公开(公告)日：2018-04-26
申请号：US15562973
申请日：2016-03-28
Applicant: Steven M. SILVERMAN , Bryon Ladd SIMMONS , Zhuqing LIU , Jing LIAO , Artis KLAPARS , Kevin R. CAMPOS , Ana Ines BELLOMO PERAZA , MERCK SHARP & DOHME CORP.
Inventor： Steven M. Silverman , Bryon Ladd Simmons , Zhuqing Liu , Jing Liao , Artis Klapars , Kevin R. Campos , Ana Inés Bellomo Peraza
Abstract: The present invention is directed to process for making Compounds of Formula (II): (II), and salts thereof, wherein B, X, R2, R3, R4 R7, R8 and R9 are defined herein.
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![Process for the preparation of tert-butyl 4-((2S ,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carboxylate and analogs thereof](/abs-image/US/2018/08/21/US10053460B2/abs.jpg.150x150.jpg)
公开(公告)号：US10053460B2
公开(公告)日：2018-08-21
申请号：US15532788
申请日：2015-11-30
Applicant: Merck Sharp & Dohme Corp.
Inventor： Zhijian Liu , Nobuyoshi Yasuda , Lu Yang , Artis Klapars , Kevin R. Campos , Mikhail Reibarkh
IPC: C07D471/08 , C07F7/02 , C07F7/10 , C07F7/18
CPC classification number: C07D471/08 , C07F7/10 , C07F7/1804
Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include interme-diates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1 ]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20180065985A1
公开(公告)日：2018-03-08
申请号：US15807992
申请日：2017-11-09
Inventor： Hongming Li , Jingjun Yin , Kevin M. Belyk , Kevin R. Campos , Qinghao Chen , Alan M. Hyde , Tetsuji Itoh , Artis Klapars , Matthew Thomas Tudge , Edward Cleator , Aaron M. Dumas , Louis-Charles Campeau , Yonggang Chen , Ji Qi , Wensong Xiao
IPC: C07D498/04 , C07F9/6509 , C07D413/04 , C07D417/04 , C07C251/24 , C07D265/14
CPC classification number: C07D498/04 , C07C251/24 , C07D239/74 , C07D265/14 , C07D265/36 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/650994 , C07F17/02
Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.
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