Abstract: The present invention is directed to carboxylic acid-containing pharmaceutical compounds where the carboxylic acid moieties have been substituted with cycloalkyl-dione derivatives, as well as tautomers and pharmaceutically acceptable salt forms thereof. These bioisosteric replacements improve the compound's ability to effectively cross the blood brain barrier and result in improved pharmacokinetic, toxicological, and/or safety profiles.
Type:
Grant
Filed:
June 6, 2012
Date of Patent:
September 10, 2013
Assignee:
The Trustees Of The University Of Pennsylvania
Inventors:
Onur Atasoylu, Carlo Ballatore, Kurt R. Brunden, Longchuan Huang, Donna M. Huryn, Michael James, Virginia M. Y. Lee, Francesco Piscitelli, Amos B. Smith, III, James Soper, John Q. Trojanowski