公开(公告)号：US20240208994A1

公开(公告)日：2024-06-27

申请号：US18556231

申请日：2022-04-18

申请人： Merck Sharp & Dohme LLC

发明人： Alan C. Cheng ,  Ying-Duo Gao ,  Song Yang ,  Mihir Mandal ,  Jiafang He ,  Jovan Alexander Lopez ,  Maoqun Tian

IPC分类号： C07D498/10 ,  A61K31/5386 ,  A61K45/06

CPC分类号： C07D498/10 ,  A61K31/5386 ,  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 degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US20240116945A1

公开(公告)日：2024-04-11

申请号：US18240392

申请日：2023-08-31

申请人： Merck Sharp & Dohme LLC

发明人： Vlad Bacauanu ,  Manoj B. Charati ,  Rebecca Elizabeth Johnson ,  Simon B. Lang ,  Ryan Quiroz ,  W. Michael Seganish ,  Song Yang ,  Nancy S. Zepeda

IPC分类号： C07D491/22 ,  A61P35/00

CPC分类号： C07D491/22 ,  A61P35/00

摘要： The present disclosure is directed to alcohol and amine containing exatecan derivatives, and pharmaceutically acceptable salts or solvates thereof, comprising a structure of formula I:




wherein X is defined in the disclosure. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of cancers and/or tumors.

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：US20230272056A1

公开(公告)日：2023-08-31

申请号：US17916664

申请日：2021-04-08

申请人： Merck Sharp & Dohme LLC

发明人： Chung-Ming Hsieh ,  Michelle Castor ,  Ming-Tang Chen ,  Alan C. Cheng ,  Scott A. Hollingsworth ,  Veronica M. Juan ,  Madhura Shidhore ,  Song Yang ,  Renee C.T. Moore

IPC分类号： C07K16/22

CPC分类号： C07K16/22 ,  C07K2317/565 ,  C07K2317/55 ,  C07K2317/92 ,  C07K2317/24

摘要： Provided herein are anti-LAP antibodies (e.g., recombinant humanized, chimeric, and human anti-LAP antibodies) or antigen binding fragments thereof which have therapeutically beneficial properties, such as binding specifically to LAP-TGFβ1 on cells but not to LAP-TGFβ1 in extracellular matrix, as well as compositions including the same. Also provided are uses of these antibodies or antigen binding fragments in therapeutic applications, such as in the treatment of cancer, and diagnostic applications.

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：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.