P2X purinergic receptor ligands: recently patented compounds.
BACKGROUND
P2X channels are ionotropic purinergic receptors that are currently under scrutiny as attractive targets for novel therapeutics in areas including chronic inflammation, pain and depression. Their wide expression in the CNS, recent advances in the biochemical and pharmacological properties as well as increasing numbers of patents published in this research domain demand a review in this field.


METHODS
The patent literature covering novel drug-like antagonists for each P2X receptor subtype (P2X1R to P2X7R) up to December 2009 is described in this review article together with their recent highlights in pharmacology.


RESULTS
Readers will gain an up-to-date overview of patents covering drug-like antagonists for seven P2X receptor subtypes within the last 4 years.


CONCLUSIONS
P2X7R antagonists and other P2X inhibitors will probably be on the market for combating rheumatoid arthritis and other diseases. Some P2X7R antagonists are already in Phase I and II clinical trials.
Gunosewoyo
Hendra
H
University of Sydney, School of Chemistry, NSW 2006, Australia.
Kassiou
Michael
M
D000818:Animals; D001172:Arthritis, Rheumatoid / Q000188:drug therapy* / Q000503:physiopathology; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D008024:Ligands; D010330:Patents as Topic; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2 / Q000378:metabolism; D058469:Receptors, Purinergic P2X; D058486:Receptors, Purinergic P2X7
D008024:Ligands; C546468:P2RX7 protein, human; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058469:Receptors, Purinergic P2X; D058486:Receptors, Purinergic P2X7