Cycloalkyl-dione derivatives and methods of their use

US8530520B2 · kind B2 · utility

Assignee

• The Trustees of the University of Pennsylvania · US

Inventors

• Onur Atasoylu · Wilmington, US
• Carlo Ballatore · San Diego, US
• Kurt R. Brunden · Media, US
• Longchuan Huang · Philadelphia, US
• Donna M. Huryn · Allentown, US
• Michael James · Raleigh, US
• Virginia M.Y. Lee · Philadelphia, US
• Francesco Piscitelli · Crotone, IT
• Amos B. Smith, III · Yeadon, US
• James Soper · Cambridge, US
• John Q. Trojanowski · Philadelphia, US

Key dates

• Filing date: Jun 6, 2012
• Grant date: Sep 10, 2013
• Expiry date: Jun 6, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.