Publication number: 20240360104
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.
Type:
Application
Filed:
April 26, 2022
Publication date:
October 31, 2024
Inventors:
Nathanael S. Gray, Tinghu Zhang, Mengyang Fan, Jianwei Che, Wenchao Lu, Sirano Dhe-Paganon, Nicholas Paul Kwiatkowski
Publication number: 20240124406
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.
Type:
Application
Filed:
June 2, 2021
Publication date:
April 18, 2024
Inventors:
Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski, Mengyang Fan, Jianwei Che, Wenchao Lu
Publication number: 20230192607
Abstract: Provided herein are compounds of (I-A), (I-B), or (II), and pharmaceutically acceptable salts, solvates, hydrates, poly-morphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are methods, uses, and kits involving the inventive 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.
Type:
Application
Filed:
December 23, 2020
Publication date:
June 22, 2023
Applicant:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, Tinghu Zhang, Jianwei Che, Nicholas Paul Kwiatkowski, Mengyang Fan, Wenchao LU