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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: rossi ka. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
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: rossi ka. 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: rossi ka. 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
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Qiao JX, Cheng X, Modi DP, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR. Qiao JX, et al. Among authors: rossi ka. Bioorg Med Chem Lett. 2005 Jan 3;15(1):29-35. doi: 10.1016/j.bmcl.2004.10.045. Bioorg Med Chem Lett. 2005. PMID: 15582405
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA Jr, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: rossi ka. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. doi: 10.1016/j.bmcl.2006.02.069. Epub 2006 May 30. Bioorg Med Chem Lett. 2006. PMID: 16730984
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
Li YL, Fevig JM, Cacciola J, Buriak J Jr, Rossi KA, Jona J, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY. Li YL, et al. Among authors: rossi ka. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. doi: 10.1016/j.bmcl.2006.07.002. Epub 2006 Jul 25. Bioorg Med Chem Lett. 2006. PMID: 16870435
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Pinto DJ, Galemmo RA Jr, Quan ML, Orwat MJ, Clark C, Li R, Wells B, Woerner F, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: rossi ka. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5584-9. doi: 10.1016/j.bmcl.2006.08.027. Epub 2006 Sep 11. Bioorg Med Chem Lett. 2006. PMID: 16963264
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: rossi ka. J Med Chem. 2007 Nov 1;50(22):5339-56. doi: 10.1021/jm070245n. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914785
58 results