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The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs |
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| Authors: | Watson Nigel S Adams Carl Belton David Brown David Burns-Kurtis Cynthia L Chaudry Laiq Chan Chuen Convery Máire A Davies David E Exall Anne M Harling John D Irvine Stephanie Irving Wendy R Kleanthous Savvas McLay Iain M Pateman Anthony J Patikis Angela N Roethke Theresa J Senger Stefan Stelman Gary J Toomey John R West Robert I Whittaker Caroline Zhou Ping Young Robert J |
| Affiliation: | a GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom b GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, United States |
| Abstract: | The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the former series were addressed in the later, delivering a robust candidate for progression towards clinical studies. |
| Keywords: | Factor Xa Oral inhibitors Property based design Structure based design P450 inhibition |
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