Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues |
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Authors: | Qiao Jennifer X Cheng Xuhong Smallheer Joanne M Galemmo Robert A Drummond Spencer Pinto Donald J P Cheney Daniel L He Kan Wong Pancras C Luettgen Joseph M Knabb Robert M Wexler Ruth R Lam Patrick Y S |
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Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. jennifer.qiao@bms.com |
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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 Ki = 0.35 nM) based on potency, selectivity, and pharmacokinetic profile. |
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