公开(公告)号：WO2022232088A1

公开(公告)日：2022-11-03

申请号：PCT/US2022/026268

申请日：2022-04-26

申请人： DANA-FARBER CANCER INSTITUTE, INC. ,  GRAY, Nathanael, S. ,  ZHANG, Tinghu ,  FAN, Mengyang ,  CHE, Jianwei ,  LU, Wenchao ,  DHE-PAGANON, Sirano ,  KWIATKOWSKI, Nicholas, Paul

发明人： GRAY, Nathanael, S. ,  ZHANG, Tinghu ,  FAN, Mengyang ,  CHE, Jianwei ,  LU, Wenchao ,  DHE-PAGANON, Sirano ,  KWIATKOWSKI, Nicholas, Paul

IPC分类号： C07D403/12 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  A61P35/00 ,  A61K31/506

摘要： Provided herein are compounds of Formula (I'), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), or Formula (VIII) and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, or prodrugs thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

公开(公告)号：WO2021247634A1

公开(公告)日：2021-12-09

申请号：PCT/US2021/035343

申请日：2021-06-02

申请人： DANA-FARBER CANCER INSTITUTE, INC. ,  GRAY, Nathanael, S. ,  ZHANG, Tinghu ,  KWIATKOWSKI, Nicholas, Paul ,  FAN, Mengyang ,  CHE, Jianwei ,  LU, Wenchao

发明人： GRAY, Nathanael, S. ,  ZHANG, Tinghu ,  KWIATKOWSKI, Nicholas, Paul ,  FAN, Mengyang ,  CHE, Jianwei ,  LU, Wenchao

IPC分类号： A61P35/00 ,  C07D213/64 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D239/34 ,  C07D257/04 ,  C07D271/10 ,  C07D277/28 ,  C07D401/04 ,  C07D403/04 ,  C07D405/12 ,  C07D513/04 ,  A61K31/505 ,  A61K31/41 ,  A61K31/4174 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/50 ,  A61K31/513 ,  A61K31/506 ,  A61K31/426

摘要： Provided herein are compounds of Formula (I''), Formula (I'), Formula (I), Formula (II'), and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are methods, uses, and kits involving the disclosed compounds and pharmaceutical compositions thereof for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers), inflammatory diseases (e.g., fibrosis), autoimmune diseases (e.g., sclerosis)) in a subject. Provided are methods of inhibiting the activity of a transcription factor (e.g., TEAD, such as TEAD1, TEAD2, TEAD3, TEAD4) and/or inhibiting the transcription of a gene (e.g., a gene controlled or regulated by a transcription factor (e.g., TEAD)) in a subject.