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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
申请人： 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
发明人： 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分类号： C07H19/10 , C07F9/58 , C07H19/06 , C07F9/24 , C07F9/6558
摘要： 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：US20170275327A1
公开(公告)日：2017-09-28
申请号：US15503776
申请日：2015-08-14
申请人： 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
发明人： 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分类号： C07H19/10 , C07F9/242 , C07F9/2458 , C07F9/2487 , C07F9/58 , C07F9/65586 , C07H19/06
摘要： 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：US20170166586A1
公开(公告)日：2017-06-15
申请号：US15325392
申请日：2015-07-10
申请人： Hongming LI , Jingjun YIN , Kevin M. BELYK , Kevin R. CAMPOS , Qinghao CHEN , Alan M. HYDE , Tetsuji ITOH , Artis KLAPARS , Mathew Thomas TUDGE , Edward CLEATOR , Aaron M. DUMAS , Louis-Charles CAMPEAU , Yonggang CHEN , Ji QI , Wensong XIAO , MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED , MSD R&D (CHINA) CO., LTD
发明人： 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分类号： C07D498/04 , C07F9/6509 , C07D265/14 , C07D413/04 , C07C251/24 , C07D417/04
CPC分类号： C07D498/04 , C07C251/24 , C07D239/74 , C07D265/14 , C07D265/36 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/650994 , C07F17/02
摘要： 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 are useful as synthetic intermediates in the process of the invention.
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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
申请人： 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
发明人： 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分类号： C07H19/10 , A61K31/7052 , C07H1/00 , C08K3/08
摘要： 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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公开(公告)号：US10202401B2
公开(公告)日：2019-02-12
申请号：US15807992
申请日：2017-11-09
发明人： 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分类号： C07D265/14 , C07D498/04 , C07C251/24 , C07F9/6509 , C07F17/02 , C07D413/14 , C07D239/74 , C07D413/04 , C07D417/04 , C07D265/36
摘要： 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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公开(公告)号：US20180065985A1
公开(公告)日：2018-03-08
申请号：US15807992
申请日：2017-11-09
发明人： 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分类号： C07D498/04 , C07F9/6509 , C07D413/04 , C07D417/04 , C07C251/24 , C07D265/14
CPC分类号： C07D498/04 , C07C251/24 , C07D239/74 , C07D265/14 , C07D265/36 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/650994 , C07F17/02
摘要： 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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公开(公告)号：US20180111954A1
公开(公告)日：2018-04-26
申请号：US15562973
申请日：2016-03-28
申请人： Steven M. SILVERMAN , Bryon Ladd SIMMONS , Zhuqing LIU , Jing LIAO , Artis KLAPARS , Kevin R. CAMPOS , Ana Ines BELLOMO PERAZA , MERCK SHARP & DOHME CORP.
发明人： Steven M. Silverman , Bryon Ladd Simmons , Zhuqing Liu , Jing Liao , Artis Klapars , Kevin R. Campos , Ana Inés Bellomo Peraza
摘要： 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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8.发明授权公开(公告)号：US07629470B2
公开(公告)日：2009-12-08
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/63
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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9.发明申请公开(公告)号：US20090018340A1
公开(公告)日：2009-01-15
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/64 , C07C255/50
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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10.发明申请FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF 审中-公开四唑替代方法的形成及其选择性减少公开(公告)号：US20100041893A1
公开(公告)日：2010-02-18
申请号：US12603901
申请日：2009-10-22
申请人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D211/72 , C07C233/00
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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