PATENT HIGHLIGHT pubs.acs.org/acsmedchemlett
Dihydropteridinone Inhibitors of BRD4 Gerard Rosse* Structure Guided Chemistry, Dart Neuroscience LLC, 7473 Lusk Boulevard, San Diego, California 92121, United States Adjunct Associate Professor, Department of Pharmacology and Physiology, College of Medicine, Drexel University, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States Title:
Dihydropteridinone Inhibitors of BRD4
Patent/Patent Application Number: Priority Application:
WO 2015/117055 A1 US 2014-61934624
Inventors:
Bradner, J. E.; Gray, N.; Qi, J.; McKeown, M. R.; Buckley, D.
Assignee Company:
Dana-Farber Cancer Institute, Inc., USA
Disease Area:
Cancer, diabetes, neurodegenerative diseases
Summary:
The present application claims dihydropteridinone analogs as inhibitors of bromodomain-containing proteins and more
Publication date: Priority date:
Biological Target:
August 6, 2015 January 31, 2014
Bromodomain-containing proteins
specifically BRD4. The compounds of the invention may be useful in male contraception and in the treatment of a wide range of disorders, such as cancer, cardiovascular diseases, and metabolic diseases. Important Compound Classes:
Key Structures:
Biological Assay:
The compounds were evaluated in an acetyl histone displacement assay using Alphascreen. Isothermal titration calorimetry
Pharmacological Data:
Biochemical assays
(ITC) was used to determine Kd values, and cellular activity was measured in BRD4 dependent cell lines (798 and HL60).
’ AUTHOR INFORMATION Corresponding Author
*E-mail:
[email protected]. Notes
Special Issue: Epigenetics
The authors declare no competing financial interest.
r XXXX American Chemical Society
Received:
A
October 1, 2015
dx.doi.org/10.1021/acsmedchemlett.5b00381 | ACS Med. Chem. Lett. XXXX, XXX, 000–000
