公开(公告)号：US20240190892A1

公开(公告)日：2024-06-13

申请号：US18550332

申请日：2022-03-16

申请人： Natalija Cernaka ,  Anthony K. OGAWA ,  Alan C. CHENG ,  Jianming BAO ,  Phillip Patrick SHARP ,  Jovan Alexander LOPEZ ,  Dong XIAO ,  Haiqun TANG ,  Merck Sharp & Dohme LLC

发明人： Natalija Cernaka ,  Anthony K. Ogawa ,  Alan C. Cheng ,  Jianming Bao ,  Phillip Patrick Sharp ,  Jovan Alexander Lopez ,  Dong Xiao ,  Haiqun Tang

IPC分类号： C07D498/20 ,  A61K31/5386 ,  A61K45/06 ,  C07D519/00

CPC分类号： C07D498/20 ,  A61K31/5386 ,  A61K45/06 ,  C07D519/00

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 degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US20230219962A1

公开(公告)日：2023-07-13

申请号：US17927222

申请日：2021-06-03

申请人： Jianming BAO ,  Natalija CERNAKA ,  Scott D. HOLLINGSWORTH ,  Madeleine Eileen KIEFFER ,  Simon B. LANG ,  Akash M. PATEL ,  W. Michael SEGANISH ,  Merck Sharp & Dohme LLC

发明人： Jianming Bao ,  Natalija Cernaka ,  Scott A. Hollingsworth ,  Madeleine Eileen Kieffer ,  Simon B. Lang ,  Akash M. Patel ,  W. Michael Seganish

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K39/395 ,  A61K31/519

CPC分类号： C07D487/04 ,  C07D519/00 ,  A61K39/3955 ,  A61K31/519

摘要： The present invention relates to novel Pyrazolo[4,3 -d]Pyrimidine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Pyrazolo[4,3-d]Pyrimidine Derivative, and methods of using the Pyrazolo[4,3-d]Pyrimidine Derivatives for treating or preventing a cellular proliferative disorder in a patient.

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：US20240140938A1

公开(公告)日：2024-05-02

申请号：US18257133

申请日：2021-12-17

申请人： MERCK SHARP & DOHME LLC

发明人： Jianming Bao ,  Chen Cheng ,  Faben A. Cruz ,  Yeon-Hee Lim ,  Cedric L. Hugelshofer ,  Jinlong Jiang ,  Victor W. Mak ,  Emma Helen Southgate

IPC分类号： C07D409/14 ,  C07D409/12

CPC分类号： C07D409/14 ,  C07D409/12

摘要： Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

公开(公告)号：US20230174521A1

公开(公告)日：2023-06-08

申请号：US17924780

申请日：2021-05-13

申请人： Merck Sharp & Dohme LLC

发明人： Yeon-Hee Lim ,  Jianming Bao ,  James Patrick Roane

IPC分类号： C07D409/12 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D471/04

摘要： Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

公开(公告)号：US20240059700A1

公开(公告)日：2024-02-22

申请号：US18465497

申请日：2023-09-12

申请人： Merck Sharp & Dohme LLC

发明人： Yeon-Hee Lim ,  Jianming Bao ,  Faben A. Cruz ,  Fa-Xiang Ding ,  Cedric Lorenz Hugelshofer ,  Victor W. Mak ,  James Patrick Roane ,  Jillian R. Sanzone ,  Samantha E. Shockley ,  Rose Yen

IPC分类号： C07D487/04 ,  C07D409/14 ,  C07D471/04 ,  C07D231/56 ,  C07D409/12

CPC分类号： C07D487/04 ,  C07D409/14 ,  C07D471/04 ,  C07D231/56 ,  C07D409/12

摘要： Invented are compounds of formula I




and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

公开(公告)号：US20240025917A1

公开(公告)日：2024-01-25

申请号：US18252261

申请日：2021-11-18

申请人： Merck Sharp & Dohme LLC

发明人： Jianming Bao ,  Natalija Cernaka ,  Alan C. Cheng ,  Ying-Duo Gao ,  Salman Jabri ,  Jovan Alexander Lopez ,  Rohan Merchant ,  Anthony Ken Ogawa ,  Skylar K. Osler ,  Christopher J. Sinz ,  Phillip Patrick Sharp ,  Haiqun Tang ,  Maoqun Tian ,  Dong Xiao ,  Song Yang

IPC分类号： C07D498/10

CPC分类号： C07D498/10

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：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：US11976061B2

公开(公告)日：2024-05-07

申请号：US17494906

申请日：2021-10-06

申请人： Merck Sharp & Dohme LLC

发明人： Yeon-Hee Lim ,  Eric R. Ashley ,  Jianming Bao ,  Chen Cheng ,  James P. Roane ,  Emma Helen Southgate

IPC分类号： C07D409/14 ,  C07D235/26 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07D471/04

CPC分类号： C07D409/14 ,  C07D235/26 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07D471/04

摘要： Invented are compounds of Formula I




and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

公开(公告)号：US20240327391A1

公开(公告)日：2024-10-03

申请号：US18672808

申请日：2024-05-23

申请人： Merck Sharp & Dohme LLC

发明人： Yeon-Hee Lim ,  Jianming Bao ,  James P. Roane

IPC分类号： C07D409/14

CPC分类号： C07D409/14

摘要： Invented are compounds of formula I




and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.