From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis - PubMed (original) (raw)

. 2007 Nov 1;17(21):6013-8.

doi: 10.1016/j.bmcl.2007.07.057. Epub 2007 Aug 19.

Andrew Bailey, Patrick Barton, Timothy N Birkinshaw, Roger V Bonnert, Roger C Brown, David Chapman, John Dixon, Simon D Guile, Robert G Humphries, Simon F Hunt, Francis Ince, Anthony H Ingall, Ian P Kirk, Paul D Leeson, Paul Leff, Richard J Lewis, Barrie P Martin, Dermot F McGinnity, Michael P Mortimore, Stuart W Paine, Garry Pairaudeau, Anil Patel, Aaron J Rigby, Robert J Riley, Barry J Teobald, Wendy Tomlinson, Peter J H Webborn, Paul A Willis

Affiliations

• PMID: 17827008
• DOI: 10.1016/j.bmcl.2007.07.057

From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis

Brian Springthorpe et al. Bioorg Med Chem Lett. 2007.

Abstract

Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y(12) receptor antagonists and exploitation of their SAR is described. Modifications of the acidic side chain and the purine core and investigation of hydrophobic substituents led to a series of neutral molecules. The leading compound, 17 (AZD6140), is currently in a large phase III clinical trial for the treatment of acute coronary syndromes and prevention of thromboembolic clinical sequelae.

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