The study reports the discovery of PD 0348292, a novel, orally bioavailable factor Xa inhibitor that progressed to phase II clinical trials for thrombotic disorders.
Supports further development of oral FXa inhibitors; leaves open clinical efficacy in thrombotic disorders pending human trials.
Herein, we report the discovery of novel, proline-based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional incorporation of 1-(4-amino-3-fluoro-phenyl)-1H-pyridin-2-one 22, as a P4 pharmacophore, we discovered compound 7 (PD 0348292). This compound is a selective, orally bioavailable, efficacious FXa inhibitor that is currently in phase II clinical trials for the treatment and prevention of thrombotic disorders.
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Kohrt et al. (2007) studied this question.
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