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Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency |
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| Authors: | Czekaj Mark Klein Scott I Guertin Kevin R Gardner Charles J Zulli Allison L Pauls Henry W Spada Alfred P Cheney Daniel L Brown Karen D Colussi Dennis J Chu Valeria Leadley Robert J Dunwiddie Christopher T |
| Affiliation: | Drug Innovation and Approval, Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. mark.czekaj@aventis.com |
| Abstract: | A systematic modification of the C(3) side-chain of the beta-aminoester class of factor Xa inhibitors and a survey of P(4) variations is described. These changes have resulted in the identification of sub-nanomolar inhibitors with improved selectivity versus related proteases. Coagulation parameters (i.e., APTT doubling concentrations) are also improved. |
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