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1. (WO2015117083) DIAZEPANE DERIVATIVES AND USES THEREOF

Pub. No.:    WO/2015/117083    International Application No.:    PCT/US2015/014109
Publication Date: Fri Aug 07 01:59:59 CEST 2015 International Filing Date: Tue Feb 03 00:59:59 CET 2015
IPC: C07D 487/04
A61K 45/06
Applicants: DANA-FARBER CANCER INSTITUTE, INC.
Inventors: BRADNER, James, E.
GRAY, Nathanael
QI, Jun
MCKEOWN, Michael, R.
BUCKLEY, Dennis
Title: DIAZEPANE DERIVATIVES AND USES THEREOF
Abstract:
The present invention provides compounds of any one of Formulae (I), (II-C) (e.g., Formula (II)), and (III), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I), (II-C), and (III) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain- containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.