公开(公告)号：US20240124406A1

公开(公告)日：2024-04-18

申请号：US18000049

申请日：2021-06-02

Applicant: Dana-Farber Cancer Institute, Inc.

Inventor： Nathanael S. Gray ,  Tinghu Zhang ,  Nicholas Paul Kwiatkowski ,  Mengyang Fan ,  Jianwei Che ,  Wenchao Lu

IPC: C07D257/04 ,  A61P35/00 ,  C07D213/64 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D239/34 ,  C07D271/10 ,  C07D277/28 ,  C07D401/04 ,  C07D403/04 ,  C07D405/12 ,  C07D513/04

CPC classification number: C07D257/04 ,  A61P35/00 ,  C07D213/64 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D239/34 ,  C07D271/10 ,  C07D277/28 ,  C07D401/04 ,  C07D403/04 ,  C07D405/12 ,  C07D513/04

Abstract: 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.

公开(公告)号：US20240360104A1

公开(公告)日：2024-10-31

申请号：US18553988

申请日：2022-04-26

Applicant: Dana-Farber Cancer Institute, Inc.

Inventor： Nathanael S. Gray ,  Tinghu Zhang ,  Mengyang Fan ,  Jianwei Che ,  Wenchao Lu ,  Sirano Dhe-Paganon ,  Nicholas Paul Kwiatkowski

IPC: C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

CPC classification number: C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

Abstract: 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.