The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of 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, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
Anti-Fibrotic Pyridinones
申请人:INTERMUNE, INC.
公开号:US20180064692A1
公开(公告)日:2018-03-08
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
USE OF COMPOSITIONS MODULATING CHROMATIN STRUCTURE FOR GRAFT VERSUS HOST DISEASE (GVHD)
申请人:Dana-Farber Cancer Institute, Inc.
公开号:US20190000860A1
公开(公告)日:2019-01-03
In some aspects, the instant disclosure relates to methods of treating chronic graft versus host disease (cGVHD). In some embodiments, the method comprises administering to a subject in need thereof a EZH2 inhibitor, a Bcl6 inhibitor and/or BRD4 inhibitor. The present disclosure is based, at least in part, on the discovery that enhancer of zeste homolog 2 (EZH2) inhibitors, B-cell lymphoma 6 protein (Bcl6) inhibitors and/or bromodomain-containing protein 4 (BRD4) inhibitors can be used to treat chronic graft versus host disease (cGVHD).