公开(公告)号：US20190144433A1

公开(公告)日：2019-05-16

申请号：US16186769

申请日：2018-11-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D405/10 ,  A61K31/4427 ,  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 ,  A61K31/4523

Abstract: 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：US20190127365A1

公开(公告)日：2019-05-02

申请号：US15800172

申请日：2017-11-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Craig A. Coburn ,  Steven W. Ludmerer ,  Kun Liu ,  Hao Wu ,  Richard Soll ,  Bin Zhong ,  Jian Zhu

IPC: C07D471/04 ,  A61K31/437 ,  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 ,  C07D487/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D413/14 ,  C07D405/14 ,  C07D405/12 ,  C07D417/14 ,  C07D409/14 ,  C07D407/14

Abstract: 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：US20180030005A1

公开(公告)日：2018-02-01

申请号：US15730997

申请日：2017-10-12

Applicant: Merck Sharp & Dohme Corp. ,  Lycera Corporation

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

CPC classification number: C07D265/36 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/538 ,  A61K45/06 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  Y02A50/409

Abstract: 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：US09868738B2

公开(公告)日：2018-01-16

申请号：US15512081

申请日：2015-09-14

Applicant: Merck Sharp & Dohme Corp. ,  Kun Liu ,  Shuwen He ,  Jared N. Cumming ,  Andrew W. Stamford

Inventor： Kun Liu ,  Shuwen He ,  Jared N. Cumming ,  Andrew W. Stamford

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K45/06 ,  A61P25/00

Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

公开(公告)号：US09783511B2

公开(公告)日：2017-10-10

申请号：US15103409

申请日：2014-12-19

Applicant: Merck Sharp & Dohme Corp. ,  Lycera Corporation

Inventor： Thomas D. Aicher ,  Chad A. VanHuis ,  John MacLean ,  Brian M. Andresen ,  Kenneth J. Barr ,  Corey Bienstock ,  Matthew Daniels ,  Kun Liu ,  Yuan Liu ,  Catherine White ,  Nunzio Sciammetta ,  Vladimir Simov

IPC: C07D265/36 ,  A61K31/538 ,  C07D413/12 ,  C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D265/36 ,  A61K31/538 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, 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：US09663502B2

公开(公告)日：2017-05-30

申请号：US15103407

申请日：2014-12-19

Applicant: Merck Sharp & Dohme Corp. ,  Lycera Corporation

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

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

Abstract: 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.

公开(公告)号：US09511052B2

公开(公告)日：2016-12-06

申请号：US14415210

申请日：2013-07-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Timothy A. Cernak ,  Kevin D. Dykstra ,  Dong-Ming Shen ,  Kun Liu ,  Andrew Stamford ,  John Qiang Tan

IPC: C07D231/56 ,  A61K31/416 ,  A61K45/06

CPC classification number: A61K31/416 ,  A61K45/06 ,  C07D231/56 ,  A61K2300/00

Abstract: The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

公开(公告)号：US20160304476A1

公开(公告)日：2016-10-20

申请号：US15103414

申请日：2014-12-19

Applicant: MERCK SHARP & DOHME CORP. ,  LYCERA CORPORATION

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

CPC classification number: C07D265/36 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/538 ,  A61K45/06 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04

Abstract: 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：US20150038490A1

公开(公告)日：2015-02-05

申请号：US14518825

申请日：2014-10-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kun Liu ,  Shawn J. Stachel ,  Craig A. Coburn ,  Thomas G. Steele ,  Richard Soll ,  Hao Wu ,  Xuanjin Peng ,  Yaxian Cai ,  Xiaoxiang Du ,  Jian Li

IPC: C07D401/06 ,  C07D513/10 ,  C07D495/10 ,  C07D491/107 ,  C07D471/10

CPC classification number: C07D401/06 ,  C07D209/96 ,  C07D471/10 ,  C07D471/20 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D495/10 ,  C07D513/10 ,  C07D513/20

Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract translation: 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的螺吡咯烷化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20230054411A1

公开(公告)日：2023-02-23

申请号：US17294836

申请日：2019-11-26

Applicant: Yonglian ZHANG ,  Amjad ALI ,  Jared CUMMING ,  Duane DEMONG ,  Qiaolin DENG ,  Thomas H. GRAHAM ,  Elisabeth HENNESSY ,  Matthew A. LARSEN ,  Kun LIU ,  Ping LIU ,  Umar Faruk MANSOOR ,  Jianping PAN ,  Christopher W. PLUMMER ,  Aaron SATHER ,  Uma SWAMINATHAN ,  Huijun WANG ,  Merck Sharp & Dohme Corp.

Inventor： Yonglian Zhang ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Matthew A. Larsen ,  Kun Liu ,  Ping Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang

IPC: A61K31/519 ,  A61K39/395 ,  C07D471/04 ,  C07D519/00 ,  A61K31/55

Abstract: In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.