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公开(公告)号：WO2016100101A1
公开(公告)日：2016-06-23
申请号：PCT/US2015/065142
申请日：2015-12-11
IPC分类号： B01J23/46 , C07D233/12 , C07D241/00
CPC分类号： B01J23/46 , C07F15/0046
摘要： The present disclosure relates to ruthenium pre-catalyst compounds of the structure of Formula I or the structure of Formula II, which are recyclable, highly reactive for olefin metathesis reactions and have a novel activation mechanism.
摘要翻译： 本公开涉及式I结构的钌预催化剂化合物或式II结构，其可再循环，对于烯烃复分解反应具有高反应性并具有新的活化机理。
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公开(公告)号：WO2022133205A1
公开(公告)日：2022-06-23
申请号：PCT/US2021/064021
申请日：2021-12-17
申请人： MERCK SHARP & DOHME CORP. , BENKOVICS, Tamas , FIER, Patrick, S. , FRYSZKOWSKA, Anna , HUFFMAN, Mark, A. , ITOH, Tetsuji , KONG, Jongrock , MALIGRES, Peter, E. , MALONEY, Kevin, M. , MCINTOSH, John , MURPHY, Grant, S. , SILVERMAN, Steven, M. , YANG, Hao
发明人： BENKOVICS, Tamas , FIER, Patrick, S. , FRYSZKOWSKA, Anna , HUFFMAN, Mark, A. , ITOH, Tetsuji , KONG, Jongrock , MALIGRES, Peter, E. , MALONEY, Kevin, M. , MCINTOSH, John , MURPHY, Grant, S. , SILVERMAN, Steven, M. , YANG, Hao
IPC分类号： A61K31/7068 , A61K31/7072 , A61K31/14 , C07H1/00 , C07H19/067 , C07H19/10
摘要： The present invention relates to efficient synthetic processes useful in the preparation of antiviral nucleosides, particularly uridine 4-oxime 5'-(2-methylpropanoate) {(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]oxolan-2-yl}methyl 2-methylpropanoate and pharmaceutically acceptable salts, derivatives, tautomers, isomers, and prodrugs of, which may be active as antiviral agents, as well as compositions and methods thereof. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
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公开(公告)号：WO2015095437A1
公开(公告)日：2015-06-25
申请号：PCT/US2014/071014
申请日：2014-12-18
申请人： MERCK SHARP & DOHME CORP. , KONG, Jongrock , MCLAUGHLIN, Mark , WILLIAMS, Michael , SONG, Zhiguo Jake , CHEN, Yonggang , JIN, Yan
发明人： KONG, Jongrock , MCLAUGHLIN, Mark , WILLIAMS, Michael , SONG, Zhiguo Jake , CHEN, Yonggang , JIN, Yan
IPC分类号： A61K31/70
CPC分类号： C07D498/18
摘要： The present invention relates to synthetic processes useful in the preparation of macrolactams that inhibit hepatitis C virus (HCV), specifically macrolactam compounds that inhibit the HCV NS3 protease activity and have application in the treatment of conditions caused by HCV. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及用于制备抑制丙型肝炎病毒（HCV）的大内酰胺的合成方法，特别是抑制HCV NS3蛋白酶活性的大内酰胺化合物，并且可用于治疗由 HCV。 本发明还包括可用于所公开的合成方法及其制备方法的中间体。
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公开(公告)号：WO2015095430A1
公开(公告)日：2015-06-25
申请号：PCT/US2014/071007
申请日：2014-12-18
发明人： WILLIAMS, Michael , MCLAUGHLIN, Mark , KONG, Jongrock , JIN, Yan
IPC分类号： A61K31/395
CPC分类号： C07D498/22 , C07D498/08 , C07D498/18
摘要： The present invention relates to synthetic processes useful in the preparation of macrolactams that inhibit hepatitis C virus (HCV), specifically macrolactam compounds that inhibit the HCV NS3 protease activity and have application in the treatment of conditions caused by HCV. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及可用于制备抑制丙型肝炎病毒（HCV）的大新戊酰胺的合成方法，特别是抑制HCV NS3蛋白酶活性的大环内酰胺化合物，并且可用于治疗由HCV引起的病症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。
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公开(公告)号：WO2015095437A8
公开(公告)日：2016-02-04
申请号：PCT/US2014071014
申请日：2014-12-18
申请人： MERCK SHARP & DOHME , KONG JONGROCK , MCLAUGHLIN MARK , WILLIAMS MICHAEL , SONG ZHIGUO JAKE , CHEN YONGGANG , JIN YAN
发明人： KONG JONGROCK , MCLAUGHLIN MARK , WILLIAMS MICHAEL , SONG ZHIGUO JAKE , CHEN YONGGANG , JIN YAN
CPC分类号： C07D498/18
摘要： The present invention relates to synthetic processes useful in the preparation of macrolactams that inhibit hepatitis C virus (HCV), specifically macrolactam compounds that inhibit the HCV NS3 protease activity and have application in the treatment of conditions caused by HCV. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及可用于制备抑制丙型肝炎病毒（HCV）的大新戊酰胺的合成方法，特别是抑制HCV NS3蛋白酶活性的大环内酰胺化合物，并且可用于治疗由HCV引起的病症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。
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公开(公告)号：WO2012082672A3
公开(公告)日：2013-12-27
申请号：PCT/US2011064521
申请日：2011-12-13
申请人： MERCK SHARP & DOHME , CHEN CHENG , KONG JONGROCK , HUMPHREY GUY , DOLMAN SARAH , LI HONGMEI , TUDGE MATTHEW T , YONG KELVIN , XIANG BANGPING , ZACUTO MICHAEL
发明人： CHEN CHENG , KONG JONGROCK , HUMPHREY GUY , DOLMAN SARAH , LI HONGMEI , TUDGE MATTHEW T , YONG KELVIN , XIANG BANGPING , ZACUTO MICHAEL
CPC分类号： C07D498/16 , C07C271/22 , C07C271/24 , C07C271/56 , C07C309/80 , C07C309/85 , C07C311/47 , C07C311/51 , C07C2601/02 , C07D207/16 , C07D209/44 , C07D403/12 , C07D498/18 , C07K5/06034
摘要： The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.
摘要翻译： 本发明涉及大分子内酰胺化合物，可用于制备大内酰胺的中间体，制备中间体的方法以及制备和改性大环内酯的方法。 本文所述的化合物和方法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。 可以使用本文所述方法合成的HCV抑制化合物的实例是化合物A及其衍生物。
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7.发明申请4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF 审中-公开4'-取代的核苷反义转录酶抑制剂及其制备
公开(公告)号：WO2017053216A3
公开(公告)日：2017-05-18
申请号：PCT/US2016052409
申请日：2016-09-19
申请人： MERCK SHARP & DOHME , MERCK SHARP & DOHME , GIRIJAVALLABHAN VINAY M , MCLAUGHLIN MARK , CLEATOR EDWARD , KONG JONGROCK , GIBSON ANDREW WILLIAM , LIEBERMAN DAVID R , DIEGUEZ VAZQUEZ ALEJANDRO , KEEN STEPHEN PHILIP , WILLIAMS MICHAEL J , MOORE JEFFREY C , MILCZEK ERIKA M , PENG FENG , BELYK KEVIN M , SONG ZHIGUO JAKE
发明人： GIRIJAVALLABHAN VINAY M , MCLAUGHLIN MARK , CLEATOR EDWARD , KONG JONGROCK , GIBSON ANDREW WILLIAM , LIEBERMAN DAVID R , DIEGUEZ VAZQUEZ ALEJANDRO , KEEN STEPHEN PHILIP , WILLIAMS MICHAEL J , MOORE JEFFREY C , MILCZEK ERIKA M , PENG FENG , BELYK KEVIN M , SONG ZHIGUO JAKE
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.
摘要翻译： 本发明涉及式（I）的4'-取代的核苷衍生物及其在抑制HIV逆转录酶，预防HIV感染，HIV感染治疗以及预防，治疗和延迟 在艾滋病和/或ARC的发病或进展中。 本发明还提供了制备式（I）的4'-取代的核苷衍生物及其衍生物的方法。
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8.发明申请4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF 审中-公开4'-取代的核苷酸逆转录酶抑制剂及其制备
公开(公告)号：WO2017053216A2
公开(公告)日：2017-03-30
申请号：PCT/US2016/052409
申请日：2016-09-19
申请人： MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED , GIRIJAVALLABHAN, Vinay, M. , MCLAUGHLIN, Mark , CLEATOR, Edward , KONG, Jongrock , GIBSON, Andrew William , LIEBERMAN, David, R. , DIEGUEZ VAZQUEZ, Alejandro , KEEN, Stephen Philip , WILLIAMS, Michael, J. , MOORE, Jeffrey, C. , MILCZEK, Erika, M. , PENG, Feng , BELYK, Kevin, M. , SONG, Zhiguo Jake
发明人： GIRIJAVALLABHAN, Vinay, M. , MCLAUGHLIN, Mark , CLEATOR, Edward , KONG, Jongrock , GIBSON, Andrew William , LIEBERMAN, David, R. , DIEGUEZ VAZQUEZ, Alejandro , KEEN, Stephen Philip , WILLIAMS, Michael, J. , MOORE, Jeffrey, C. , MILCZEK, Erika, M. , PENG, Feng , BELYK, Kevin, M. , SONG, Zhiguo Jake
IPC分类号： A61K31/7064 , C07H19/14
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.
摘要翻译： 本发明涉及式（I）的4'-取代的核苷衍生物及其在抑制HIV逆转录酶中的用途，HIV的感染预防，HIV感染的治疗以及预防，治疗和延迟 在AIDS和/或ARC的发病或进展中。 本发明还提供制备式（I）的4'-取代的核苷衍生物及其衍生物的方法。
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公开(公告)号：WO2012082672A2
公开(公告)日：2012-06-21
申请号：PCT/US2011/064521
申请日：2011-12-13
申请人： MERCK SHARP & DOHME CORP. , CHEN, Cheng , KONG, Jongrock , HUMPHREY, Guy , DOLMAN, Sarah , LI, Hongmei , TUDGE, Matthew, T. , YONG, Kelvin , XIANG, Bangping , ZACUTO, Michael
发明人： CHEN, Cheng , KONG, Jongrock , HUMPHREY, Guy , DOLMAN, Sarah , LI, Hongmei , TUDGE, Matthew, T. , YONG, Kelvin , XIANG, Bangping , ZACUTO, Michael
CPC分类号： C07D498/16 , C07C271/22 , C07C271/24 , C07C271/56 , C07C309/80 , C07C309/85 , C07C311/47 , C07C311/51 , C07C2601/02 , C07D207/16 , C07D209/44 , C07D403/12 , C07D498/18 , C07K5/06034
摘要： The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.
摘要翻译： 本发明涉及大分子内酰胺化合物，可用于制备大内酰胺的中间体，制备中间体的方法以及制备和改性大环内酯的方法。 本文所述的化合物和方法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。 可以使用本文所述方法合成的HCV抑制化合物的实例是化合物A及其衍生物。
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