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公开(公告)号：US09932350B2
公开(公告)日：2018-04-03
申请号：US15515377
申请日：2015-09-25
申请人： MERCK SHARP & DOHME CORP. , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
发明人： Michael D. Altman , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
IPC分类号： C07D491/08 , C07D239/94 , A61K31/517 , A61K45/06 , C07D239/88 , A61K31/5377 , C07D403/12 , C07D401/12 , C07D413/12 , A61K31/538 , C07D491/052 , A61K31/5386 , C07D491/048 , A61K31/55 , C07D405/12
CPC分类号： C07D491/08 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D491/048 , C07D491/052 , C07D498/08 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：US08614229B2
公开(公告)日：2013-12-24
申请号：US12675891
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/47 , A61K31/4402 , A61K31/426 , A61K31/428 , A61K31/4184 , A61K31/404 , C07D239/96 , C07D239/88 , C07D241/44 , C07D471/04 , C07D215/18 , C07D401/04 , C07D211/88 , C07D277/18 , C07D487/04 , C07D275/04 , C07D249/18
CPC分类号： C07D403/04 , C07D401/04
摘要： The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译： 本发明涉及取代的吲哚衍生物，包含至少一种取代的吲哚衍生物的组合物，以及使用这些取代的吲哚衍生物来治疗或预防患者的病毒感染或病毒相关病症的方法。
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13.发明授权4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections 有权用于治疗或预防HCV和相关病毒感染的4,5环环状吲哚衍生物公开(公告)号：US08557848B2
公开(公告)日：2013-10-15
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K31/497 , A61K31/4353 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/498 , A61K31/517 , C07D215/12 , C07D401/14 , C07D241/44 , C07D239/88
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译： 本发明涉及4,5-环环状吲哚衍生物，包含至少一种4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防病毒感染或 患者病毒相关疾病。 其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。
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14.发明申请4,5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS 有权用于治疗或预防HCV和相关病毒感染的4,5环结构吲哚类衍生物公开(公告)号：US20100098661A1
公开(公告)日：2010-04-22
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K38/21 , C07D401/02 , A61K31/4439 , C07D417/14 , A61K31/4436 , C07D215/00 , A61K31/47 , C07D241/36 , A61K31/498 , C07D401/14 , A61K31/517 , A61K31/444 , A61K39/00 , A61K39/395 , A61P31/12
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译： 本发明涉及4,5-环环状吲哚衍生物，包含至少一个4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防病毒感染或 患者病毒相关疾病。 其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。
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15.发明授权Compositions of hepatitis C virus NS5B polymerase and methods for crystallizing same 失效丙型肝炎病毒NS5B聚合酶的组合物及其结晶方法公开(公告)号：US06434489B1
公开(公告)日：2002-08-13
申请号：US09541990
申请日：2000-04-03
IPC分类号： G01N3348
CPC分类号： C07K14/005 , C07K2299/00 , C12N9/127 , C12N2770/24222
摘要： The invention relates to the purification, crystallization of and structure of hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. Also, crystallization conditions for NS5B are provided. Further, the atomic coordinates for the NS5B protein are disclosed. Examples of its use for the determination of the three-dimensional atomic structures of HCV NS5B or HCV NS5B in complex with substrates or substrate analogs or inhibitors are also provided.
摘要翻译： 本发明涉及丙型肝炎病毒（HCV）NS5B RNA依赖性RNA聚合酶的纯化，结晶和结构。 此外，提供NS5B的结晶条件。 此外，公开了NS5B蛋白质的原子坐标。 还提供了其用于确定与底物或底物类似物或抑制剂复合的HCV NS5B或HCV NS5B的三维原子结构的用途。
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公开(公告)号：US20240246937A1
公开(公告)日：2024-07-25
申请号：US18556196
申请日：2022-04-28
申请人： George Madalin GIAMBASU , Andrew M. HAIDLE , Brett A. HOPKINS , James P. JEWELL , Matthew A. LARSEN , Charles A. LESBURG , Ping LIU , Qinglin PU , Sulagna SANYAL , Phieng SILIPHAIVANH , Matthew TUDOR , Catherine M. WHITE , Xin YAN , Lianyun ZHAO , Xiao Mei ZHENG , William P. KAPLAN , Michaelyn Claire LUX , Derun LI , Rebecca JOHNSON , MERCK SHARP & DOHME LLC , MSD R&D (CHINA) CO., LTD.
发明人： George Madalin GIAMBASU , Andrew M. HAIDLE , Brett A. HOPKINS , James P. JEWELL , Matthew A. LARSEN , Charles A. LESBURG , Ping LIU , Qinglin PU , Sulagna SANYAL , Phieng SILIPHAIVANH , Matthew TUDOR , Catherine M. WHITE , Xin YAN , Lianyun ZHAO , Xiao Mei ZHENG , William P. KAPLAN , Michaelyn Claire LUX , Derun LI , Rebecca JOHNSON
IPC分类号： C07D403/06 , C07D401/06 , C07D401/14 , C07D403/10 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D487/04
CPC分类号： C07D403/06 , C07D401/06 , C07D401/14 , C07D403/10 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D487/04
摘要： The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.
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公开(公告)号：US20220056051A1
公开(公告)日：2022-02-24
申请号：US17312480
申请日：2019-12-13
申请人： Abdelghani Abe ACHAB , Matthew L. CHILDERS , Jared N. CUMMING , Symon GATHIAKA , Charles A. LESBURG , Derun LI , Min LU , Matthew J. MITCHELTREE , Anandan PALANI , Rachel L. PALTE , Hongjun ZHANG , Merck Sharp & Dohme Corp.
发明人： Abdelghani Abe Achab , Matthew L. Childers , Jared N. Cumming , Symon Gathiaka , Charles A. Lesburg , Derun Li , Min Lu , Matthew J. Mitcheltree , Anandan Palani , Rachel L. Palte , Hongjun Zhang
IPC分类号： C07F5/02
摘要： Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
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公开(公告)号：US20160347757A1
公开(公告)日：2016-12-01
申请号：US15116659
申请日：2015-02-06
申请人： Santhosh F. NEELAMKAVIL , Scott D. EDMONDSON , Zhuyan GUO , Alan W. HRUZA , Zahid HUSSAIN , Charles A. LESBURG , Remond MONINGKA , Anthony K. OGAWA , Rudrajit MAL , MERCK SHARP & DOHME CORP
发明人： Santhosh F. Neelamkavil , Scott D. Edmondson , Zhuyan Guo , Alan W. Hruza , Zahid Hussain , Charles A. Lesburg , Remond Moningka , Anthony K. Ogawa , Rudrajit Mal
IPC分类号： C07D487/08 , C07D471/08
CPC分类号： C07D487/08 , C07D471/08
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
摘要翻译： 本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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19.发明授权公开(公告)号：US08048663B2
公开(公告)日：2011-11-01
申请号：US12815817
申请日：2010-06-15
申请人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
发明人： Wenyan Wang , Shahriar Shane Taremi , Winifred Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
CPC分类号： C07K14/70567 , C07K14/4705 , C07K2319/31
摘要： The present invention relates to Pregnane X receptor (PXR) polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明涉及可用于例如结晶和用于鉴定PXR调节剂的测定中的孕烷X受体（PXR）多肽和晶体。
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20.发明申请公开(公告)号：US20110165118A1
公开(公告)日：2011-07-07
申请号：US12743016
申请日：2008-11-13
申请人： Tin-Yau Chan , Jose S. Duca , Liwu Hong , Charles A. Lesburg , Brian A. McKittrick , Haiyan Pu , Li Wang , Henry M. Vaccaro
发明人： Tin-Yau Chan , Jose S. Duca , Liwu Hong , Charles A. Lesburg , Brian A. McKittrick , Haiyan Pu , Li Wang , Henry M. Vaccaro
IPC分类号： A61K31/519 , C07D495/04 , C07D403/04 , A61K31/517 , C07D487/04 , C07D473/04 , A61K31/522 , C07D471/04 , A61K31/513 , A61K31/5377 , A61K31/4178 , A61K38/21 , A61K31/7088 , A61K39/395 , A61P31/14
CPC分类号： C07D403/04 , C07D401/04 , C07D403/14 , C07D487/04 , C07D495/04
摘要： The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译： 本发明涉及3-杂环取代的吲哚衍生物，包含至少一种3-杂环取代的吲哚衍生物的组合物，以及使用3-杂环取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关病症的方法 患者。
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