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Page 1
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR. Lam PY, et al. Among authors: luettgen jm. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: luettgen jm. J Med Chem. 2001 Feb 15;44(4):566-78. doi: 10.1021/jm000409z. J Med Chem. 2001. PMID: 11170646
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.
Quan ML, Ellis CD, He MY, Liauw AY, Woerner FJ, Alexander RS, Knabb RM, Lam PY, Luettgen JM, Wong PC, Wright MR, Wexler RR. Quan ML, et al. Among authors: luettgen jm. Bioorg Med Chem Lett. 2003 Feb 10;13(3):369-73. doi: 10.1016/s0960-894x(02)00951-4. Bioorg Med Chem Lett. 2003. PMID: 12565931
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.
Quan ML, Ellis CD, He MY, Liauw AY, Lam PY, Rossi KA, Knabb RM, Luettgen JM, Wright MR, Wong PC, Wexler RR. Quan ML, et al. Among authors: luettgen jm. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1023-8. doi: 10.1016/s0960-894x(03)00080-5. Bioorg Med Chem Lett. 2003. PMID: 12643903
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pruitt JR, Pinto DJ, Galemmo RA Jr, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR. Pruitt JR, et al. Among authors: luettgen jm. J Med Chem. 2003 Dec 4;46(25):5298-315. doi: 10.1021/jm030212h. J Med Chem. 2003. PMID: 14640539
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Smallheer JM, Alexander RS, Wang J, Wang S, Nakajima S, Rossi KA, Smallwood A, Barbera F, Burdick D, Luettgen JM, Knabb RM, Wexler RR, Jadhav PK. Smallheer JM, et al. Among authors: luettgen jm. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7. doi: 10.1016/j.bmcl.2004.08.034. Bioorg Med Chem Lett. 2004. PMID: 15454208
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