Technology Bundle ID
TAB-3575

A Novel Chemical Series for Inhibiting Bromodomain-containing Protein 4 (BRD4) for Treating Cancer

Applications
Linked ID
E-004-2016-0
Lead Inventors
Jeffrey Strovel (ConverGene, LLC)
Co-Inventors
Ajit Jadhav (NCATS)
Daniel Urban (NCATS)
David Maloney (NCATS)
Makoto Yoshioka (ConverGene, LLC)
Shyh Yang (NCATS)
ICs
This technology includes the design, synthesis, and use of a novel chemical series for multiple treatments, including for treating cancer. A series of substituted bicyclic heteroaryl small molecules were found to be a potent inhibitor of bromodomain-containing protein 4 (BRD4) for multiple uses, including cancer. A BRD4 inhibitor is in a class of drugs known as BET inhibitors that are used broadly as anti-inflammatories and as anti-cancer agents. The chemical series exhibited less hepatocyte toxicity compared to existing treatments. For example, the series also identified N-methyl 2-pyridone 1s as a great replacement for dimethylisoxazole, an existing BET inhibitor.
Commercial Applications
BRD4 has been identified as an important target, particularly for cancer. The chemical series has the potential to be used for a variety of indications including but not limited to cancer, diabetes, inflammation, and acute heart failure, and has a large market potential.
Competitive Advantages
The compounds identified in this chemical series have a novel composition and better drug-like properties.

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