公开(公告)号：US09938299B2

公开(公告)日：2018-04-10

申请号：US14655222

申请日：2013-12-20

申请人： MERCK SHARP & DOHME CORP. ,  ALECTOS THERAPEUTICS, INC.

发明人： Harold G. Selnick ,  Kun Liu ,  Ernest J. McEachern ,  Ramesh Kaul ,  Zhongyong Wei ,  Yaode Wang ,  Jiang Chang

IPC分类号： C07D513/04 ,  B65D71/14 ,  B65D71/16 ,  B65D5/00 ,  B65D5/20

CPC分类号： C07D513/04 ,  B65D5/005 ,  B65D5/2057 ,  B65D71/14 ,  B65D71/16 ,  B65D2571/0016 ,  B65D2571/0029 ,  B65D2571/0066 ,  B65D2571/00716

摘要： The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US11053243B2

公开(公告)日：2021-07-06

申请号：US16829878

申请日：2020-03-25

申请人： Merck Sharp & Dohme Corp.

发明人： Craig A. Coburn ,  Steven W. Ludmerer ,  Kun Liu ,  Hao Wu ,  Richard Soil ,  Bin Zhong ,  Jian Zhu

IPC分类号： C07D471/04 ,  C07D407/14 ,  C07D487/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D413/14 ,  C07D405/14 ,  C07D405/12 ,  C07D417/14 ,  C07D409/14 ,  A61K31/4985 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4025 ,  A61K31/519 ,  A61K31/404 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/475 ,  A61K31/536 ,  A61K31/4178 ,  A61K31/517 ,  A61K31/5386 ,  A61K31/553 ,  A61K31/437

摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

公开(公告)号：US10995085B2

公开(公告)日：2021-05-04

申请号：US16819325

申请日：2020-03-16

申请人： Merck Sharp & Dohme Corp.

发明人： Yongxin Han ,  Abdelghani Achab ,  Yongqi Deng ,  Xavier Fradera ,  Craig Gibeau ,  Brett A. Hopkins ,  Derun Li ,  Kun Liu ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David Sloman ,  Catherine White ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D405/10 ,  A61K31/4523 ,  A61K45/06 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/4155 ,  C07D305/08 ,  A61K31/337 ,  C07D417/10 ,  A61K31/427 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/4184 ,  C07D405/14 ,  A61K31/444 ,  A61K31/513 ,  C07D413/04 ,  C07D401/04 ,  C07D213/56 ,  A61K31/4418 ,  C07D417/14 ,  A61K31/501 ,  C07D241/12 ,  A61K31/4965 ,  A61K31/4427 ,  C07D263/32 ,  A61P37/00 ,  C07D231/12 ,  A61P35/00 ,  C07D413/10 ,  C07D401/12 ,  C07D405/04 ,  A61P31/00 ,  C07D209/46 ,  C07D413/14

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10745364B2

公开(公告)日：2020-08-18

申请号：US16270882

申请日：2019-02-08

申请人： Merck Sharp & Dohme Corp. ,  Lycera Corporation

发明人： Thomas D. Aicher ,  Chad A. VanHuis ,  William D. Thomas ,  John K. MacLean ,  Brian M. Andresen ,  Kenneth J. Barr ,  Corey E. Bienstock ,  Neville J. Anthony ,  Matthew Daniels ,  Kun Liu ,  Yuan Liu ,  Catherine M. White ,  Blair T. Lapointe ,  Nunzio Sciammetta ,  Vladimir Simov

IPC分类号： C07D265/36 ,  C07D413/14 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/04 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/538 ,  A61K45/06 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D487/04

摘要： The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

公开(公告)号：US20200231606A1

公开(公告)日：2020-07-23

申请号：US16326408

申请日：2017-08-24

申请人： Merck Sharp & Dohme Corp.

发明人： Kun Liu ,  Abdelghani Achab ,  Purakkattle Biju ,  Timothy A. Cernak ,  Yongqi Deng ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Guoqing Li ,  Qinglin Pu ,  Zhi-Cai Shi ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07F5/02 ,  C07D271/08 ,  C07D413/12

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10689369B2

公开(公告)日：2020-06-23

申请号：US16356172

申请日：2019-03-18

申请人： Merck Sharp & Dohme Corp.

发明人： Blair T. Lapointe ,  Peter H. Fuller ,  Hakan Gunaydin ,  Kun Liu ,  Mark E. Scott ,  B. Wesley Trotter ,  Hongjun Zhang

IPC分类号： C07D403/08 ,  C07D401/12 ,  C07D401/06 ,  C07D491/107 ,  C07D491/048 ,  C07D487/10 ,  C07D487/04 ,  C07D405/12 ,  C07D403/14 ,  C07D403/06 ,  C07D231/56 ,  C07D403/12 ,  A61P19/02

摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

公开(公告)号：US10647705B2

公开(公告)日：2020-05-12

申请号：US16186769

申请日：2018-11-12

申请人： Merck Sharp & Dohme Corp.

发明人： Yongxin Han ,  Abdelghani Achab ,  Yongqi Deng ,  Xavier Fradera ,  Craig Gibeau ,  Brett A. Hopkins ,  Derun Li ,  Kun Liu ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David Sloman ,  Catherine White ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D405/10 ,  A61K31/4523 ,  A61K45/06 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/4155 ,  C07D305/08 ,  A61K31/337 ,  C07D417/10 ,  A61K31/427 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/4184 ,  C07D405/14 ,  A61K31/444 ,  A61K31/513 ,  C07D413/04 ,  C07D401/04 ,  C07D213/56 ,  A61K31/4418 ,  C07D417/14 ,  A61K31/501 ,  C07D241/12 ,  A61K31/4965 ,  A61K31/4427 ,  C07D263/32 ,  A61P37/00 ,  C07D231/12 ,  A61P35/00 ,  C07D413/10 ,  C07D401/12 ,  C07D405/04 ,  A61P31/00 ,  C07D209/46 ,  C07D413/14

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10584121B2

公开(公告)日：2020-03-10

申请号：US15770257

申请日：2016-10-27

申请人： Merck Sharp & Dohme Corp.

发明人： Hongjun Zhang ,  Kenneth Jay Barr ,  Blair T. Lapointe ,  Hakan Gunaydin ,  Kun Liu ,  B. Wesley Trotter

IPC分类号： C07D471/04 ,  A61K31/4353 ,  A61P37/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00

摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

公开(公告)号：US09611275B2

公开(公告)日：2017-04-04

申请号：US14399146

申请日：2013-05-03

申请人： Merck Sharp & Dohme Corp.

发明人： Harold G. Selnick ,  Wenping Li ,  Eric Hostetler ,  Kun Liu ,  Ernest J. McEachern ,  Yuanxi Zhou ,  Zhongyong Wei ,  Changwei Mu ,  Yaode Wang ,  Jiang Chang

IPC分类号： C07D513/04 ,  C07B59/00 ,  C07H9/06

CPC分类号： C07D513/04 ,  C07B59/005 ,  C07B2200/05 ,  C07H9/06

摘要： The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.

公开(公告)号：US20160304505A1

公开(公告)日：2016-10-20

申请号：US15103407

申请日：2014-12-19

申请人： MERCK SHARP & DOHME CORP. ,  LYCERA CORPORATION

发明人： Thomas D. Aicher ,  Chad A. VanHuis ,  John MacLean ,  Brian M. Andresen ,  Kenneth J. Barr ,  Corey Bienstock ,  Neville J. Anthony ,  Matthew Daniels ,  Yuan Liu ,  Catherine White ,  Blair T. Lapointe ,  Nunzio Sciammetta ,  Vladimir Simov ,  Wesley B. Trotter ,  Kun Liu

IPC分类号： C07D413/12 ,  A61K31/538 ,  C07D265/36 ,  C07D413/14 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  C07D417/12 ,  A61K45/06 ,  C07D471/04

CPC分类号： C07D413/12 ,  A61K31/538 ,  A61K45/06 ,  C07D265/36 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra, Rb, Rc, Rd, Rg, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.