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US 2009/0023723 A1Published application
Purinone derivatives for treating neurodegenerative diseases
AssigneePharmacopeia Drug Discovery, Inc.
InventorsAndrew G. Cole, Ian Henderson, Marc-Raleigh Brescia, Axel Metzger, Lan-Ying Qin, Gulzar Ahmed, Brian F. McGuinness, Yuefei Shao, Jingqi Duo
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Abstract
The invention relates to purinone derivatives useful in treating disorders that are mediated by adenosine receptor function, including neurodegenerative diseases and inflammation. The compounds are of the general formula: An example is:
Claims22
A compound of formula:
- wherein
- R1 is selected from lower alkyl lower alkyloxyalkyl, arylalkyl, aryl, substituted aryl and substituted arylalkyl;
- X is selected from NR2a and O;
- R2 is selected from H, C1-C20 hydrocarbon, C1-C20acyl, heterocyclyl other than 2-pyridinyl and 1-imidazolyl, heterocyclylalkyl, substituted alkyl, substituted aryl, substituted heterocyclyl, substituted arylalkyl and substituted heterocyclylalkyl;
- R2Ais selected from H and C1-C10 hydrocarbon;
- or R2 and R2Atogether form a 5-7 membered heterocycle or substituted 5-7 membered heterocycle;
- and
- R3 is selected from H, lower alkyl arylalkyl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl and substituted arylalkyl;
- with the provisos that
- (i) at least one of R1, R2 and R3 must provide an aryl or heteroaryl moeity;
- (ii) when R3 is H, R1 must be other than lower alkyl;
- (iii) when X is NR2A, R2Ais H, and R1 is phenyl or tolyl, then R2 must be other than phenyl and tolyl;
- and
- (iv) R2 is not p-chlorophenethyl.
11 more elements
Dependencies are inferred from the claim text.