G. Rosse
Jan 10, 2013
Citations
0
Influential Citations
2
Citations
Journal
ACS medicinal chemistry letters
Abstract
Received: November 15, 2012 Published: November 30, 2012 Title: Metabolites of the Pyrimidine Amine Preladenant as Adenosine A2a Receptor Antagonists Patent/Patent Application Number: WO 2012135084 A1 Publication date: October 4, 2012 Priority Application: US 2011-470213P Priority date: March 31, 2011 Inventors: Ting, P.; Ma, S.; Blumenkrantz, N.; Chowdbury, S.; Neustadt, B. R. Assignee Company: Merck Sharp & Dohme Corp., USA Disease Area: Central Nervous System Disorders Biological Target: Adenosine A2a Receptor Summary: The application claims a single compound,M9, an adenosine A2a receptor antagonist, which is a metabolite of 2-(furan-2-yl)7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine (Preladenant). Preladenant is currently in phase III clinical trials for the treatment of Parkinson’s disease. In addition, the invention describes a method of determining if a subject has been administered Preladenant and of identifying its metabolites after administration to rat, dog, and human. Key Structures: