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公开(公告)号:US20210154221A1
公开(公告)日:2021-05-27
申请号:US17166512
申请日:2021-02-03
发明人: Mark McLaughlin , Edward Cleator , Jongrock Kong , Andrew William Gibson , David R. Lieberman , Alejandro Diequez Vazquez , Stephen Philip Keen , Michael J. Williams , Jeffrey C. Moore , Erika M. Milczek , Feng Peng , Kevin M. Belyk , Zhiguo Jake Song
IPC分类号: A61K31/7064 , C07D307/33 , A61K45/06 , C07H1/00 , C07H19/14 , C07H23/00 , C07H19/16 , A61P31/18
摘要: The present invention is directed to 4′-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula I and derivatives thereof.
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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:US20190022115A1
公开(公告)日:2019-01-24
申请号:US15761742
申请日:2016-09-16
发明人: Vinay M. Girijavallabhan , Mark McLaughlin , Edward Cleator , Jongrock Kong , Andrew William Gibson , David R. Lieberman , Alejandro Dieguez Vazquez , Stephen Philip Keen , Michael J. Williams , Jeffrey C. Moore , Erika M. Milczek , Feng Peng , Kevin M. Belyk , Zhiguo Jake Song
IPC分类号: A61K31/7064 , C07D307/33 , A61P31/18
摘要: The present invention is directed to 4′-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula (I) and derivatives 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
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: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:US20140309213A1
公开(公告)日:2014-10-16
申请号:US14353804
申请日:2012-10-25
发明人: Shawn P. Walsh , Alexander Pasternak , Reynalda K. DeJesus , Haifeng Tang , Barbara Pio , Aurash Shahripour , Kevin M. Belyk , Harry R. Chobanian , Yan Guo , Jessica L. Frie , Zhi-Cai Shi , Helen Chen , Timothy A. Blizzard , Brian Cato
IPC分类号: C07D471/08 , C07D498/08 , C07D487/18 , C07D405/12 , C07D405/14 , C07D487/08
CPC分类号: C07D471/08 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D487/08 , C07D487/18 , C07D491/08 , C07D498/08
摘要: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译: 本发明涉及具有以下一般结构的式I-VI化合物:Z1-Y1-(CH2)n1-R-(CH2)n2-Y2-Z2其中R是具有2个氮原子的6-8元饱和杂环 分别与 - (CH2)n1-和 - (CH2)n2-连接,以及作为肾外膜(ROMK)通道(Kir1.1)的抑制剂的药学上可接受的盐。 这些化合物可用作利尿剂和利尿钠,因此可用于治疗和预防由过度的盐和水分滞留引起的疾病,包括心血管疾病如高血压和慢性和急性心力衰竭。
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公开(公告)号:US20200010449A1
公开(公告)日:2020-01-09
申请号:US16576133
申请日:2019-09-19
发明人: Cheol K. Chung , Mark E. Scott , Paul G. Bulger , Kevin M. Belyk , John Limanto , Guy R. Humphrey
IPC分类号: C07D401/10
摘要: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
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公开(公告)号:US10815214B2
公开(公告)日:2020-10-27
申请号:US16576133
申请日:2019-09-19
发明人: Cheol K. Chung , Mark E. Scott , Paul G. Bulger , Kevin M. Belyk , John Limanto , Guy R. Humphrey
IPC分类号: C07D401/10
摘要: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
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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:US20150038707A1
公开(公告)日:2015-02-05
申请号:US14384624
申请日:2013-09-19
发明人: Kevin M. Belyk , Edward Cleator , Shen-Chun Kuo , Peter Emmanuel Maligres , Bangping Xiang , Nobuyoshi Yasuda , Jianguo Yin
IPC分类号: C07D487/04 , C07F7/18 , C07D471/04 , C07D471/20 , C07D405/06
CPC分类号: C07D487/04 , A01N53/00 , C07D405/06 , C07D471/04 , C07D471/20 , C07F7/1804 , A01N25/34
摘要: Methods for preventing pest infestations are disclosed. In some embodiments, the methods for preventing infestations involve use of pyrethroid insecticides or the stereoisomers or salts thereof.
摘要翻译: 公开了预防害虫侵害的方法。 在一些实施方案中,预防感染的方法涉及使用拟除虫菊酯类杀虫剂或其立体异构体或其盐。
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