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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：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：US20180179223A1
公开(公告)日：2018-06-28
申请号：US15578777
申请日：2016-06-03
申请人： Jingjun Yin , Tetsuji Itoh , Jianguo Yin , Bangping Xiang , Kevin R. Campos , Alexei Kalinin , Zhuqing Liu , Melodie Deniz Christensen , Kevin M. Belyk , Richard J. Varsolona , Andrew Brunskill
发明人： Jingjun Yin , Tetsuji Itoh , Jianguo Yin , Bangping Xiang , Kevin R. Campos , Alexei Kalinin , Zhuqing Liu , Melodie Deniz Christensen , Kevin M. Belyk , Richard J. Varsolona , Andrew Brunskill
IPC分类号： C07D498/04 , C07F5/02 , C07D403/04 , B01J31/04
CPC分类号： C07D498/04 , B01J31/04 , C07D403/04 , C07F5/025
摘要： The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
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公开(公告)号：US20150329521A1
公开(公告)日：2015-11-19
申请号：US14649837
申请日：2013-12-04
申请人： Tetsuji ITOH , Ingyu JEON , Ian MANGION , Gang QIAN , Benjamin D. SHERRY , Donald R. GAUTHIER , Yang CAO , MERCK SHARP & DOHME CORP.
发明人： Tetsuji Itoh , Ingyu Jeon , Ian Mangion , Gang QIAN , Benjamin D. Sherry , Donald R. Gauthier , Yang CAO
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.
摘要翻译： 本发明涉及一种合成3-（取代的苯氧基）-1 - [（5-氧代-4,5-二氢-1H-1,2,4-三唑-3-基）甲基]] - 吡啶-2（1H） - 酮衍生物。 通过本发明的方法合成的化合物是可用于抑制逆转录酶，HIV复制和人类免疫缺陷病毒感染治疗的HIV逆转录酶抑制剂。
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公开(公告)号：US09663490B2
公开(公告)日：2017-05-30
申请号：US14649837
申请日：2013-12-04
发明人： Tetsuji Itoh , Ingyu Jeon , Ian Mangion , Gang Qian , Benjamin D. Sherry , Donald R. Gauthier , Yang Cao
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.
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![PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR MAKING (2S,5R)-7-OXO-N-PIPERIDIN-4-YL-6-(SULFOXY)-l,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDE](/abs-image/US/2022/06/23/US20220194941A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220194941A1
公开(公告)日：2022-06-23
申请号：US17604525
申请日：2020-04-21
发明人： John Y.L. Chung , Tetsuji Itoh , Jungchul Kim , Jacob Henry Waldman , Debra J. Wallace , Andrew Wood , Feng Xu , Andrew Gibson , Jeremy Peter Scott
IPC分类号： C07D471/08 , C07D211/96
摘要： The invention is related to the preparation of protected piperidine carboxylates suitable for use as intermediates that lead, via a series of additional process steps, including a sulfation of a hydroxy urea compound, to the preparation of the beta lactamase inhibitor (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide.
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公开(公告)号：US20160297794A1
公开(公告)日：2016-10-13
申请号：US15100940
申请日：2014-12-02
发明人： Yang Cao , Donald R. Gauthier, Jr. , Guy R. Humphrey , Tetsuji Itoh , Michel Journet , Gang Qian , Benjamin D. Sherry , David M. Tschaen
IPC分类号： C07D401/06 , C07D213/69
CPC分类号： C07D401/06 , C07D213/69 , C07D213/78
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
摘要翻译： 本发明涉及一种合成3-（取代的苯氧基）-1 - [（5-氧代-4,5-二氢-1H-1,2,4-三唑-3-基）甲基]] - 吡啶-2（1H） - 酮衍生物。 通过本发明的方法合成的化合物是用于抑制逆转录酶和HIV复制的HIV逆转录酶抑制剂以及人类免疫缺陷病毒感染的治疗。
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公开(公告)号：US10457690B2
公开(公告)日：2019-10-29
申请号：US15578777
申请日：2016-06-03
发明人： Jingjun Yin , Tetsuji Itoh , Jianguo Yin , Bangping Xiang , Kevin R. Campos , Alexei Kalinin , Zhuqing Liu , Melodie Deniz Christensen , Kevin M. Belyk , Richard J. Varsolona , Andrew Brunskill
IPC分类号： C07D498/04 , C07D403/04 , C07F5/02 , B01J31/04
摘要： The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
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公开(公告)号：US09598397B2
公开(公告)日：2017-03-21
申请号：US15100940
申请日：2014-12-02
发明人： Yang Cao , Donald R. Gauthier, Jr. , Guy R. Humphrey , Tetsuji Itoh , Michel Journet , Gang Qian , Benjamin D. Sherry , David M. Tschaen
IPC分类号： C07D401/06 , C07D213/69 , C07D213/78
CPC分类号： C07D401/06 , C07D213/69 , C07D213/78
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
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