Abstract
The synthesis, SAR, pharmacokinetic profile, and modeling studies of both monocyclic and fused pyrazoles containing substituted N-arylpiperidinyl P4 moieties that are potent and selective factor Xa inhibitors will be discussed. Fused pyrazole analog 16a, with a 2′-methylsulfonylphenyl piperidine P4 group, was shown to be the best compound in this series (FXa K i = 0.35 nM) based on potency, selectivity, and pharmacokinetic profile.
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