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：US20240207425A1

公开(公告)日：2024-06-27

申请号：US18536350

申请日：2023-12-12

申请人： Merck Sharp & Dohme LLC

发明人： Manoj B. Charati ,  John A. Flygare ,  Rebecca Elizabeth Johnson ,  Simon B. Lang ,  W. Michael Seganish

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12

CPC分类号： A61K47/68031 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12

摘要： The present disclosure is directed to linker-payloads, and pharmaceutically acceptable salts, solvates, or stereoisomer thereof, comprising a structure of formula I:




The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds, intermediates thereof, and compositions in the prevention or treatment of cancers and/or tumors.

公开(公告)号：US20240358847A1

公开(公告)日：2024-10-31

申请号：US18642038

申请日：2024-04-22

申请人： MERCK SHARP & DOHME LLC

发明人： Minilik Angagaw ,  Edward Paul Bowman ,  Ming-Tang Chen ,  Laurence Fayadat-Dilman ,  Malgorzata A. Gil ,  Marlene C. Hinton ,  Zhong Hua ,  Rebecca Elizabeth Johnson ,  Simon B. Lang ,  W. Michael Seganish ,  Andrew B. Waight

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07K16/30

CPC分类号： A61K47/68031 ,  A61K47/6849 ,  A61P35/00 ,  C07K16/30 ,  C07K2317/565

摘要： TROP2 binders and variants thereof are described. In a specific embodiment, the TROP2 binders that are antibodies that preferentially bind high-expressing TROP2 cells over low-expressing TROP2 cells and conjugates thereof comprising the TROP2 binders conjugated to a payload are described.

公开(公告)号：US20240208987A1

公开(公告)日：2024-06-27

申请号：US18491850

申请日：2023-10-23

申请人： Merck Sharp & Dohme LLC

发明人： Vlad Bacauanu ,  Manoj B. Charati ,  Sijie Chen ,  Rebecca Elizabeth Johnson ,  Simon B. Lang ,  Christian L. Morales ,  Ryan Quiroz ,  W. Michael Seganish ,  Nancy Zepeda

IPC分类号： C07D491/22 ,  A61K47/65 ,  A61K47/68

CPC分类号： C07D491/22 ,  A61K47/65 ,  A61K47/68037

摘要： The present disclosure is directed to linker-payloads, and salts (including pharmaceutically acceptable salts), solvates, or stereoisomers thereof, comprising a structure of formula I:




The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds, intermediates thereof, and compositions in the prevention or treatment of cancers and/or tumors.

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.