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公开(公告)号：US07785879B1
公开(公告)日：2010-08-31
申请号：US11522698
申请日：2006-09-18
申请人： Wenyan Wang , Shahriar Shane Taremi , Winifred W. Prosise , Paul Reichert , Charles A. Lesburg , Vincent S. Madison , Kuo-Chi Cheng
发明人： Wenyan Wang , Shahriar Shane Taremi , Winifred W. 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, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明尤其涉及PXR多肽和晶体，其可用于例如结晶和用于鉴定PXR调节剂的测定。
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公开(公告)号：US20210052573A1
公开(公告)日：2021-02-25
申请号：US16980594
申请日：2019-03-15
申请人： Michael D. NEEDHAM , Matthew L. CHILDERS , James P. JEWELL , Charles A. LESBURG , Tony SIU , Merck Sharp & Dohme Corp.
IPC分类号： A61K31/4725 , C07D405/10 , C07D413/14 , C07D405/14 , C07D417/14 , C07D413/04 , C07D409/04 , C07D411/04 , A61K31/5377 , A61K31/497 , A61K31/538
摘要： The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
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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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14.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：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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17.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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公开(公告)号：US20100286372A1
公开(公告)日：2010-11-11
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
IPC分类号： C07K14/00
CPC分类号： C07K14/70567 , C07K14/4705 , C07K2319/31
摘要： The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.
摘要翻译： 本发明尤其涉及PXR多肽和晶体，其可用于例如结晶和用于鉴定PXR调节剂的测定。
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