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Page 1
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE Jr, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML. Corte JR, et al. Among authors: pinto dj. Bioorg Med Chem. 2016 May 15;24(10):2257-72. doi: 10.1016/j.bmc.2016.03.062. Epub 2016 Apr 1. Bioorg Med Chem. 2016. PMID: 27073051
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: pinto dj. 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: pinto dj. J Med Chem. 2003 Dec 4;46(25):5298-315. doi: 10.1021/jm030212h. J Med Chem. 2003. PMID: 14640539
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR. Quan ML, et al. Among authors: pinto dj. J Med Chem. 2005 Mar 24;48(6):1729-44. doi: 10.1021/jm0497949. J Med Chem. 2005. PMID: 15771420
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. 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
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. 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
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Qiao JX, Cheng X, Smallheer JM, Galemmo RA, Drummond S, Pinto DJ, Cheney DL, He K, Wong PC, Luettgen JM, Knabb RM, Wexler RR, Lam PY. Qiao JX, et al. Among authors: pinto dj. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1432-7. doi: 10.1016/j.bmcl.2006.11.071. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17174550
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. J Med Chem. 2007 Nov 1;50(22):5339-56. doi: 10.1021/jm070245n. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914785
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Corte JR, Fang T, Pinto DJ, Han W, Hu Z, Jiang XJ, Li YL, Gauuan JF, Hadden M, Orton D, Rendina AR, Luettgen JM, Wong PC, He K, Morin PE, Chang CH, Cheney DL, Knabb RM, Wexler RR, Lam PY. Corte JR, et al. Among authors: pinto dj. Bioorg Med Chem Lett. 2008 May 1;18(9):2845-9. doi: 10.1016/j.bmcl.2008.03.092. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18424044
80 results