Arylindenopyrimidines and their use as adenosine A2a receptor antagonists

Abstract

This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses as an antagonist of Adenosine A2a receptors. Disorders treated ans / or prevented include Parkinson's Disease.

Description

Cross references to related patent applications This patent application claims priority to US Provisional Patent Application Serial No. 60 / 982,247, filed October 24, 2007. The entire disclosures of the aforementioned related US patent applications are hereby incorporated by reference herein for all purposes. technical field The present invention relates to novel aryl indenopyrimidines and their therapeutic and prophylactic uses. Disorders that may be treated and / or prevented include neurodegenerative disorders and movement disorders that are ameliorated by antagonizing the adenosine A2a receptor. Background technique Adenosine A2a Receptor Adenosine is a purine nucleotide produced by all metabolically active cells in the body. Adenosine exerts its effects through four cell surface receptor subtypes (A1, A2a, A2b, and A3), which belong to the G protein-coupled receptor superfamily (Stiles, G.L. Journal of Biological Chemistry, 1992, 267, 6451) . A1 and AS couple to an ...

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Furthermore, it has been found that A2a knockout mice in which A2a function is genetically blocked are less susceptible to motor impairment and neurochemical changes when they are exposed to the neurotoxin MPTP (Chen, J.F.; Xu, K.; I Petzer, J.P. ; Steal, R.; Xu, Y.H.; Beilstein, M.; Sonsalla, P.K.; Castagnoli, K.; Castagnoli, N., Jr.; Schwarsschild, M.A. Journal of Neuroscience, 2001, 121, RC1 43)

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