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1. 发明申请

WO2017091453A1 NOVEL PROCESSES FOR MAKING SUBSTITUTED QUINAZOLINE COMPOUNDS USING HYDROGEN BONDING CATALYSTS 审中-公开
标题翻译：用氢键连接催化剂制备取代喹唑啉化合物的新工艺
公开(公告)号：WO2017091453A1
公开(公告)日：2017-06-01
申请号：PCT/US2016/062654
申请日：2016-11-18
申请人： MERCK SHARP & DOHME CORP. , CHUNG, Cheol, K. , HUMPHREY, Guy, R. , LIU, Zhijian , MCLAUGHLIN, Mark , XU, Yingju , YU, Younong
发明人： CHUNG, Cheol, K. , HUMPHREY, Guy, R. , LIU, Zhijian , MCLAUGHLIN, Mark , XU, Yingju , YU, Younong
IPC分类号： A61K31/517 , A61P31/12 , C07C309/30 , C07D239/72 , C07D239/84
CPC分类号： A61K31/517 , C07D239/84
摘要： Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.
摘要翻译：本文公开了一种使用氢键催化剂制备式（I）的取代喹唑啉化合物的新方法。

2. 发明申请

WO2011005731A2 PROCESS FOR MAKING CGRP RECEPTOR ANTAGONIST 审中-公开
标题翻译：制备CGRP受体拮抗剂的方法
公开(公告)号：WO2011005731A2
公开(公告)日：2011-01-13
申请号：PCT/US2010/041023
申请日：2010-07-06
申请人： MERCK SHARP & DOHME CORP. , BELYK, Kevin, M. , BULGER, Paul, G. , LINGHU, Xin , MALONEY, Kevin, M. , MCLAUGHLIN, Mark , PAN, Jun , XIANG, Bangping , XU, Yingju , YIN, Jingjun
发明人： BELYK, Kevin, M. , BULGER, Paul, G. , LINGHU, Xin , MALONEY, Kevin, M. , MCLAUGHLIN, Mark , PAN, Jun , XIANG, Bangping , XU, Yingju , YIN, Jingjun
IPC分类号： C07D241/38 , C07D291/04 , C07D471/04
CPC分类号： C07D471/04 , C07D241/38 , C07D291/04
摘要： The invention encompasses a novel process for making 2-[(8R)-8-(3,5-Difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3- b ]pyridin]-5-yl]acetamide, which is a CGRP receptor antagonist useful for the treatment of migraine, using an asymmetric phase-transfer catalysis route. The invention also encompasses an efficient and practical synthesis of the (R)-acid intermediate, and generates the benzylic stereocenter in an enantioselective manner.
摘要翻译：本发明包括制备2 - [（8R）-8-（3,5-二氟苯基）-10-氧代-6,9-二氮杂螺[4.5]癸-9-基 ] -N - [（2R）-2'-氧代-1,1' ，2' ，3-四氢螺[茚-2,3'-吡咯并[2,3的 b'/ I>]吡啶] -5-基]乙酰胺，它是用于治疗偏头痛的CGRP受体拮抗剂，采用不对称相转移催化途径。本发明还包括有效和实用的（R） - 酸中间体的合成，并以对映选择性方式产生苄型立构中心。

3. 发明申请

WO2016073659A1 PROCESS FOR PREPARING SUBSTITUTED INDOLE COMPOUNDS 审中-公开
标题翻译：制备取代的吲哚化合物的方法
公开(公告)号：WO2016073659A1
公开(公告)日：2016-05-12
申请号：PCT/US2015/059129
申请日：2015-11-05
申请人： MERCK SHARP & DOHME CORP. , DIROCCO, Daniel, A. , DAVIES, Ian , PENG, Feng , MCLAUGHLIN, Mark , CAMPEAU, Louis-Charles , XU, Yingju
发明人： DIROCCO, Daniel, A. , DAVIES, Ian , PENG, Feng , MCLAUGHLIN, Mark , CAMPEAU, Louis-Charles , XU, Yingju
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/405
CPC分类号： C07D498/04 , B01J31/00 , B01J31/181 , B01J35/004 , B01J2231/766 , B01J2531/827
摘要： The present invention is directed to a process for preparing Substituted Indole Compounds of Formula (I): wherein R 1 , R 2 , R 3 and R 4 are as defined herein. These indole compounds are useful as synthetic intermediates for making inhibitors of HCV NS5A.
摘要翻译：本发明涉及制备式（I）的取代吲哚化合物的方法：其中R 1，R 2，R 3和R 4如本文所定义。这些吲哚化合物可用作制备HCV NS5A抑制剂的合成中间体。

4. 发明申请

WO2013066734A1 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF 3-AMINO-4-CYCLOBUTYL-2-HYDROXYBUTANAMIDE AND SALTS THEREOF 审中-公开
标题翻译：制备3-氨基-4-环丙基-2-羟基丁酰胺及其盐的方法和中间体
公开(公告)号：WO2013066734A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/062025
申请日：2012-10-26
申请人： MERCK SHARP & DOHME CORP. , WU, George, G. , ITOH, Tetsuji , MCLAUGHLIN, Mark , LIU, Zhijian , QIAN, Gang
发明人： WU, George, G. , ITOH, Tetsuji , MCLAUGHLIN, Mark , LIU, Zhijian , QIAN, Gang
IPC分类号： C07C69/74
CPC分类号： C07C67/11 , C07C67/307 , C07C69/716 , C07C69/92 , C07C227/08 , C07C229/28 , C07C231/12 , C07C253/16 , C07C269/04 , C07C269/06 , C07C271/22 , C07C303/28 , C07C2601/04 , C07C309/66 , C07C255/31 , C07C237/14
摘要： The present invention relates to synthetic processes useful in the preparation of a compound of Formula (I), and salts thereof. Compounds of Formula (I) and salts thereof have application in the preparation of inhibitors of the hepatitis C virus, such as (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6, 6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide. 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式（I）化合物及其盐的合成方法。式（I）化合物及其盐可用于制备丙型肝炎病毒的抑制剂，例如（1R，5S）-N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] - 3- [2（S） - [[[（1,1-二甲基乙基）氨基]羰基]氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基-3-氮杂双环[3.1.0] 己基-2（S） - 甲酰胺。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。

5. 发明申请

WO2016014324A1 PROCESS FOR PREPARING CHIRAL DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译：制备精氨酸肽酶IV抑制剂的方法
公开(公告)号：WO2016014324A1
公开(公告)日：2016-01-28
申请号：PCT/US2015/040674
申请日：2015-07-16
申请人： MERCK SHARP & DOHME CORP. , CHUNG, John, Y. L. , PENG, Feng , CHEN, Yonggang , KASSIM, Amude Mahmoud , CHEN, Cheng-yi , MAUST, Mathew , MCLAUGHLIN, Mark , ZACUTO, Michael, J. , CHEN, Qinghao , TAN, Lushi , SONG, Zhiguo Jake , CAO, Yang , XU, Feng
发明人： CHUNG, John, Y. L. , PENG, Feng , CHEN, Yonggang , KASSIM, Amude Mahmoud , CHEN, Cheng-yi , MAUST, Mathew , MCLAUGHLIN, Mark , ZACUTO, Michael, J. , CHEN, Qinghao , TAN, Lushi , SONG, Zhiguo Jake , CAO, Yang , XU, Feng
IPC分类号： A61K31/4162 , A01N43/56 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , C07D309/30
摘要： A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:.
摘要翻译：制备结构式Ia化合物的方法：包括用Boc还原胺化的Boc去保护。

6. 发明申请

WO2015095437A1 METHODS AND INTERMEDIATES FOR THE PREPARATION OF MACROLACTAMS 审中-公开
标题翻译：制备大环内酯的方法和中间体
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。

7. 发明申请

WO2015095430A1 METHODS AND INTERMEDIATES FOR THE PREPARATION OF MACROLACTAMS 审中-公开
标题翻译：制备MACROLACTAMS的方法和中间体
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
申请人： MERCK SHARP & DOHME CORP. , WILLIAMS, Michael , MCLAUGHLIN, Mark , KONG, Jongrock , JIN, Yan
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。

8. 发明申请

WO2017053216A2 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF 审中-公开
标题翻译： 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
CPC分类号： A61K45/06 , C07D307/33 , C07H1/00 , C07H19/14 , C07H19/16 , C07H23/00
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。

9. 发明公开

EP3352781A2 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF 有权转让
公开(公告)号：EP3352781A2
公开(公告)日：2018-08-01
申请号：EP16849385.6
申请日：2016-09-19
申请人： Merck Sharp & Dohme Corp. , Merck Sharp & Dohme Limited
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： A61K38/44 , C12N1/20
CPC分类号： A61K45/06 , C07D307/33 , C07H1/00 , C07H19/14 , C07H19/16 , C07H23/00
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.

10. 发明申请

WO2011069016A1 INTEGRATED ELECTRONIC HEALTH RECORD (EHR) SYSTEM WITH TRANSCRIPTION, SPEECH RECOGNITION AND AUTOMATED DATA EXTRACTION 审中-公开
标题翻译：具有转录，语音识别和自动数据提取的综合电子健康记录（EHR）系统
公开(公告)号：WO2011069016A1
公开(公告)日：2011-06-09
申请号：PCT/US2010/058798
申请日：2010-12-02
申请人： MXSECURE, INC. , MCLAUGHLIN, Mark
发明人： MCLAUGHLIN, Mark
IPC分类号： A61B5/00
CPC分类号： A61B5/00 , A61B5/411 , A61B5/4528 , G06F19/00 , G06Q50/24 , G16H10/20 , G16H10/60
摘要： An integrated health record system comprises a platform including a processor coupled to a medical application. The system includes at least one input device coupled to the processor. The input device receives patient information of a patient via an electronic form and receives vital signs of the patient. The medical application integrates the patient information and the vital signs into an electronic health record (EHR) that corresponds to the patient. The medical application receives a sound file that includes information resulting from an examination of the patient, and translates the sound file into a document that comprises a clinical document architecture (CDA). The medical application parses the document and identifies a plurality of data components based on a correspondence to a plurality of data fields of the HER. The medical application populates each of the plurality of data fields with each of the data components.
摘要翻译：综合的健康记录系统包括一个平台，它包括耦合到医疗应用的处理器。该系统包括耦合到处理器的至少一个输入设备。输入装置通过电子形式接收患者的患者信息并接收患者的生命体征。医疗应用将患者信息和生命体征整合到与患者对应的电子健康记录（EHR）中。医疗应用程序接收包括由患者检查产生的信息的声音文件，并将声音文件翻译成包括临床文档架构（CDA）的文档。医疗应用程序基于与HER的多个数据字段的对应关系来分析文档并识别多个数据组件。医疗应用程序使用每个数据组件填充多个数据字段中的每一个。

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