| 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: |  |
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| Recent Review Articles: | Xu F.; Wu H.; Katritch V.; Han ; Jacobson K. A.; Gao Z. G.; Cherezov V.; Stevens R. C.. Structure of an Agonist-Bound Human A2A Adenosine Receptor. Science, 2011, 15 April, 322–327. | ||
| Biological Assays (Description): | Human adenosine A2a receptor competition biding assay. | ||
| Pharmacological Data: | Adenosine A2a receptor binding assay
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| Synthesis: | Synthesis of Preladenant metabolites and [14C] labeled Preladenant are described. | ||
| Claims: | Claims 2–4, 9–11: Use of compound of the invention in combination with another compound useful in treating Parkinson’s disease or selected from L-DOPA, dopaminergic agonists, MAO-B inhibitors, COMT inhibitors, typcal/atypical antipsychotic agent. | ||
| Claims 5–8: Use of the compound or the combination for the treatment of a variety of central nervous system diseases, stroke, depression, cognitive disease, Parkinson’s disease, Extra-Pyramidal Syndrome (EPS). | |||
| Claim 14: Method of determining if a subject has been administered Preladenant. | |||
The author declares no competing financial interest.