公开(公告)号：US20230416227A1

公开(公告)日：2023-12-28

申请号：US18043357

申请日：2021-09-09

申请人： Merck Sharp & Dohme LLC ,  Anthony Ken OGAWA ,  Christopher J. SINZ ,  Jacqueline D. HICKS ,  Alan C. CHENG ,  Song YANG ,  Jianming BAO ,  Donna A. A. W. HAYES ,  Simon B. LANG ,  Maoqun TIAN ,  Salman JABRI ,  Galen Paul SHEARN-NANCE ,  Rongze KUANG ,  Zhiqiang ZHAO ,  Zhicai WU

发明人： Anthony Ken Ogawa ,  Christopher J. Sinz ,  Jacqueline D. Hicks ,  Alan C. Cheng ,  Song Yang ,  Jianming Bao ,  Donna A. A. W. Hayes ,  Simon B. Lang ,  Maoqun Tian ,  Salman Jabri ,  Galen Paul Shearn-Nance ,  Rongze Kuang ,  Zhiqiang Zhao ,  Zhicai Wu

IPC分类号： C07D401/14 ,  A61K45/06 ,  A61P9/10

CPC分类号： C07D401/14 ,  A61P9/10 ,  A61K45/06

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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US20230167085A1

公开(公告)日：2023-06-01

申请号：US17920943

申请日：2021-05-07

申请人： Wei LAN ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian ,  Merck Sharp & Dohme LLC

发明人： Jacqueline D. HICKS ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian

IPC分类号： C07D401/14 ,  C07D417/14

CPC分类号： C07D401/14 ,  C07D417/14

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 XI activation inhibitors.

公开(公告)号：US20140088124A1

公开(公告)日：2014-03-27

申请号：US14123246

申请日：2012-06-01

申请人： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

发明人： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

IPC分类号： C07D401/14 ,  C07D417/14 ,  C07D493/04 ,  C07D471/04

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04

摘要： Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

摘要翻译： 本文描述的是式（I）的化合物。式I化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：US20240076297A1

公开(公告)日：2024-03-07

申请号：US18015364

申请日：2021-07-22

申请人： Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Jared N. Cumming ,  Manuel De Lera Ruiz ,  Duane DeMong ,  Thomas H. Graham ,  Elisabeth T. Hennessy ,  Joseph M. Kelly ,  Rongze Kuang ,  Michael Man-Chu Lo ,  Umar Faruk Mansoor ,  Jesus Moreno ,  Uma Swaminathan ,  Heping Wu ,  Yingchun Ye ,  Younong Yu

IPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/28

CPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/2818

摘要： The present invention provides compounds of the structural Formula (I), and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active 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 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.

公开(公告)号：US20230348428A1

公开(公告)日：2023-11-02

申请号：US18014787

申请日：2021-07-06

申请人： Merck Sharp & Dohme LLC

发明人： Jacqueline D. HICKS ,  Rongze Kuang ,  Christopher J. Sinz ,  Matthew J. Lombardo ,  Jovan Alexander Lopez ,  Rohan Rajiv Merchant ,  Phillip Patrick Sharp ,  Zhicai Wu ,  Zhiqiang Zhao ,  Alan C. Cheng ,  Song Yang ,  Jianming Bao ,  Maoqun Tian ,  Galen Paul Shearn-Nance

IPC分类号： C07D401/14 ,  C07D413/14 ,  A61P27/02 ,  A61K45/06 ,  C07D403/14

CPC分类号： C07D401/14 ,  A61K45/06 ,  A61P27/02 ,  C07D403/14 ,  C07D413/14 ,  C07B2200/05

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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US20230322785A1

公开(公告)日：2023-10-12

申请号：US18015387

申请日：2022-07-21

申请人： Christopher W. BOYCE ,  Thomas H. GRAHAM ,  Andrew J. HOOVER ,  Xianhai HUANG ,  Rognze KUANG ,  Jae-Hun KIM ,  Joseph M. KELLY ,  Michael Man-Chu LO ,  Jing SU ,  Dong XIAO ,  Xiaohong ZHU ,  Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Christopher W. Boyce ,  Jared N. Cumming ,  Duane DeMong ,  Thomas H. Graham ,  Subrahmanyam Gudipati ,  Andrew J. Hoover ,  Xianhai Huang ,  Rongze Kuang ,  Jae-Hun Kim ,  Joseph M. Kelly ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Jesus Moreno ,  Jing Su ,  Heping Wu ,  Dong Xiao ,  Younong Yu ,  Xiaohong Zhu

IPC分类号： C07D487/04 ,  C07K16/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07K16/2896

摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active 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 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.

公开(公告)号：US20230286958A1

公开(公告)日：2023-09-14

申请号：US18007787

申请日：2021-06-10

申请人： Merck Sharp & Dohme LLC

发明人： Salman Jabri ,  Anthony Ken Ogawa ,  Christopher J. Sinz ,  Jacqueline D. Hicks ,  Alan C. Cheng ,  Ying-Duo Gao ,  Song Yang ,  Jianming Bao ,  Donna A. A. W. Hayes ,  Simon B. Lang ,  Brandon M. Taoka ,  Maoqun Tian ,  Galen Paul Shearn-Nance ,  Rongze Kuang ,  Matthew J. Lombardo ,  Zhicai Wu ,  Zhiqiang Zhao

IPC分类号： C07D403/14 ,  A61P27/00 ,  C07D471/04

CPC分类号： C07D403/14 ,  A61P27/00 ,  C07D471/04

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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

申请人： Amjad ALI ,  Michael Man-Chu LO ,  Yeon-Hee LIM ,  Andrew STAMFORD ,  Rongze KUANG ,  Paul TEMPEST ,  Younong YU ,  Michael BERLIN ,  Pauline TING ,  Gang ZHOU ,  Tao YU ,  Christopher BOYCE ,  Joseph Michael KELLY ,  Jayaram TAGAT ,  Junying ZHENG ,  Xianhai HUANG ,  Wei ZHOU ,  Jae-Hun KIM ,  Nicolas ZORN ,  Dong XIAO ,  Gioconda V. GALLO ,  Walter WON ,  Heping WU ,  Rajan ANAND ,  MERCK SHARP & DOHME CORP.

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC分类号： C07D487/04 ,  C07D487/18 ,  C07D487/08 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

摘要翻译： 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US09676780B2

公开(公告)日：2017-06-13

申请号：US14655572

申请日：2013-12-20

申请人： MERCK SHARP & DOHME CORP. ,  Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：US08232274B2

公开(公告)日：2012-07-31

申请号：US12046755

申请日：2008-03-12

申请人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

发明人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

IPC分类号： A61K31/501 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  A61P31/00

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D515/22

摘要： Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.

摘要翻译： 公开了一组可用作具有式I的通式结构的葡聚糖合酶抑制剂的化合物：其中各个部分A，D，R 6等如说明书中所定义。 这些化合物可用于治疗或预防患者的真菌感染。