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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：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：US08168799B2
公开(公告)日：2012-05-01
申请号：US11919309
申请日：2006-04-20
申请人： Michael Stewart Ashwood , Matthew Bio , Edward Cleator , David Hands , Faye Julia Sheen , Robert Darrin Wilson
发明人： Michael Stewart Ashwood , Matthew Bio , Edward Cleator , David Hands , Faye Julia Sheen , Robert Darrin Wilson
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R1 and R2 are each independently hydrogen, or C1-6 alkyl groups or R1 and R2 are linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring.
摘要翻译： 一种制备式（I）化合物或其盐，水合物或溶剂合物的方法; 其中R 1和R 2各自独立地为氢，或C 1-6烷基或R 1和R 2连接，并与其连接的环戊烷碳原子一起形成环丙基环。
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公开(公告)号：US09108959B2
公开(公告)日：2015-08-18
申请号：US14002221
申请日：2012-02-27
申请人： Carl A. Baxter , Edward Cleator , Faye Sheen , Shane W. Krska , Gavin Stewart , Neil Strotman , Debra J. Wallace , Timothy Wright
发明人： Carl A. Baxter , Edward Cleator , Faye Sheen , Shane W. Krska , Gavin Stewart , Neil Strotman , Debra J. Wallace , Timothy Wright
IPC分类号： A61K31/551 , C07D413/04 , C07D413/14 , C07D249/06 , A61K31/55
CPC分类号： C07D413/14 , A61K31/55 , C07D249/06 , C07D413/04
摘要： The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
摘要翻译： 本发明涉及制备食欲肽受体拮抗剂的二氮杂环丁烷化合物的方法，其可用于治疗或预防涉及食欲素受体的神经和精神疾病及疾病。 本发明进一步涉及该二氮杂环丁烷化合物的结晶形式及其药物组合物。
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公开(公告)号：US09073825B2
公开(公告)日：2015-07-07
申请号：US14239391
申请日：2012-08-16
申请人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
发明人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
IPC分类号： A01N43/04 , A01N43/42 , C07C35/04 , C07K5/083 , C07D403/12 , C07D498/16 , C07K5/12 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , A61K38/00
CPC分类号： C07C35/04 , A61K38/00 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , C07D403/12 , C07D498/16 , C07K5/0808 , C07K5/126
摘要： A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound A
摘要翻译： 本发明的第一方面描述了选自下组的化合物：其中R是H，C（O）RA或C（O）NHCH（X）COOH; 条件是X是C 2 -C 6烷基或C 3 -C 8环烷基，RA是C 1-6烷基或芳基; 这些化合物用于制备化合物A.
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公开(公告)号：US20100174091A1
公开(公告)日：2010-07-08
申请号：US11919309
申请日：2006-04-20
申请人： Michael Stewart Ashwood , Matthew Bio , Edward Cleator , David Hands , Faye Julia Sheen , Robert Darrin Wilson
发明人： Michael Stewart Ashwood , Matthew Bio , Edward Cleator , David Hands , Faye Julia Sheen , Robert Darrin Wilson
IPC分类号： C07D403/04 , C07D403/06
CPC分类号： C07D403/04
摘要： A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R1 and R2 are each independently hydrogen, or C1-6 alkyl groups or R1 and R2 are linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring.
摘要翻译： 一种制备式（I）化合物或其盐，水合物或溶剂合物的方法; 其中R 1和R 2各自独立地为氢，或C 1-6烷基或R 1和R 2连接，并与其连接的环戊烷碳原子一起形成环丙基环。
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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：US20140243519A1
公开(公告)日：2014-08-28
申请号：US14239391
申请日：2012-08-16
申请人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
发明人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
IPC分类号： C07D498/16 , C07D403/12 , C07C269/04 , C07C271/34 , C07C69/013 , C07C67/14 , C07C35/04 , C07C69/12
CPC分类号： C07C35/04 , A61K38/00 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , C07D403/12 , C07D498/16 , C07K5/0808 , C07K5/126
摘要： The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applica
摘要翻译： 本发明包括可用作制备大内酰胺的中间体的化合物，制备中间体的方法和制备大新戊酰胺的方法。 本文描述的方法和中间体的一个用途是制备能够抑制HCV NS3蛋白酶活性的大环内酰胺化合物。 HCV NS3抑制化合物具有治疗和研究应用
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公开(公告)号：US20140242645A1
公开(公告)日：2014-08-28
申请号：US14354161
申请日：2012-10-22
申请人： John Y.L. Chung , Kevin Campos , Edward Cleator , Robert F. Dunn , Andrew Gibson , R Scott Hoerrner , Stephen Keen , Dave Lieberman , Zhuqing Liu , Joseph Lynch , Kevin M. Maloney , Feng Xu , Nobuyoshi Yasuda , Naoki Yoshikawa , Yong-Li Zhong
发明人： John Y.L. Chung , Kevin Campos , Edward Cleator , Robert F. Dunn , Andrew Gibson , R Scott Hoerrner , Stephen Keen , Dave Lieberman , Zhuqing Liu , Joseph Lynch , Kevin M. Maloney , Feng Xu , Nobuyoshi Yasuda , Naoki Yoshikawa , Yong-Li Zhong
IPC分类号： C07D207/09 , C12P17/10
CPC分类号： C07D207/09 , C07D207/08 , C12P17/10
摘要： The present invention is directed to a process for preparing a compound of formula I-11 through multiple-step reactions.
摘要翻译： 本发明涉及通过多步反应制备式I-11化合物的方法。
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公开(公告)号：US20130331379A1
公开(公告)日：2013-12-12
申请号：US14002221
申请日：2012-02-27
申请人： Carl A. Baxter , Edward Cleator , Faye Sheen , Shane W. Krska , Gavin Stewart , Neil Strotman , Debra J. Wallace , Timothy Wright
发明人： Carl A. Baxter , Edward Cleator , Faye Sheen , Shane W. Krska , Gavin Stewart , Neil Strotman , Debra J. Wallace , Timothy Wright
IPC分类号： C07D413/14 , C07D413/04
CPC分类号： C07D413/14 , A61K31/55 , C07D249/06 , C07D413/04
摘要： The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
摘要翻译： 本发明涉及制备食欲肽受体拮抗剂的二氮杂环丁烷化合物的方法，其可用于治疗或预防涉及食欲素受体的神经和精神疾病及疾病。 本发明还涉及该二氮杂环丁烷化合物的结晶形式及其药物组合物。
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