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Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW. Guertin KR, et al. Among authors: leadley rj. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4. doi: 10.1016/s0960-894x(02)00213-5. Bioorg Med Chem Lett. 2002. PMID: 12039587
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
Choi-Sledeski YM, Kearney R, Poli G, Pauls H, Gardner C, Gong Y, Becker M, Davis R, Spada A, Liang G, Chu V, Brown K, Collussi D, Leadley R Jr, Rebello S, Moxey P, Morgan S, Bentley R, Kasiewski C, Maignan S, Guilloteau JP, Mikol V. Choi-Sledeski YM, et al. J Med Chem. 2003 Feb 27;46(5):681-4. doi: 10.1021/jm020384z. J Med Chem. 2003. PMID: 12593648
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V. Ewing WR, et al. Among authors: leadley rj. J Med Chem. 1999 Sep 9;42(18):3557-71. doi: 10.1021/jm990040h. J Med Chem. 1999. PMID: 10479288
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.
Choi-Sledeski YM, McGarry DG, Green DM, Mason HJ, Becker MR, Davis RS, Ewing WR, Dankulich WP, Manetta VE, Morris RL, Spada AP, Cheney DL, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Leadley RJ, Maignan S, Guilloteau JP, Dunwiddie CT, Pauls HW. Choi-Sledeski YM, et al. Among authors: leadley rj. J Med Chem. 1999 Sep 9;42(18):3572-87. doi: 10.1021/jm990041+. J Med Chem. 1999. PMID: 10479289
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.
Becker MR, Ewing WR, Davis RS, Pauls HW, Ly C, Li A, Mason HJ, Choi-Sledeski YM, Spada AP, Chu V, Brown KD, Colussi DJ, Leadley RJ, Bentley R, Bostwick J, Kasiewski C, Morgan S. Becker MR, et al. Among authors: leadley rj. Bioorg Med Chem Lett. 1999 Sep 20;9(18):2753-8. doi: 10.1016/s0960-894x(99)00466-7. Bioorg Med Chem Lett. 1999. PMID: 10509929
In vitro characterization of a novel factor Xa inhibitor, RPR 130737.
Chu V, Brown K, Colussi D, Choi YM, Green D, Pauls HW, Spada AP, Perrone MH, Leadley RJ Jr, Dunwiddie CT. Chu V, et al. Among authors: leadley rj jr. Thromb Res. 2000 Jul 1;99(1):71-82. doi: 10.1016/s0049-3848(00)00227-9. Thromb Res. 2000. PMID: 11012377
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