Factor Xa inhibitors: next-generation antithrombotic agents.
Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR.
J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/jm100146h PUBLIKATIONSREGISTRET
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Publikationer i urvalet
11 träffarPhenyltriazolinones as potent factor Xa inhibitors.
Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.01.011Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Qiao JX, King SR, He K, Wong PC, Rendina AR, Luettgen JM, Xin B, Knabb RM, Wexler RR, Lam PY.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.11.049Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Qiao JX, Cheney DL, Alexander RS, Smallwood AM, King SR, He K, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.05.0957-fluoroindazoles as potent and selective inhibitors of factor Xa.
Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR.
J Med Chem · journal article · DOI 10.1021/jm701217rStructure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Varnes JG, Wacker DA, Pinto DJ, Orwat MJ, Theroff JP, Wells B, Galemo RA, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2007.11.040Discovery 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.
J Med Chem · journal article · DOI 10.1021/jm070245nDesign, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Varnes JG, Wacker DA, Jacobson IC, Quan ML, Ellis CD, Rossi KA, He MY, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR.
Bioorg Med Chem Lett · comparative study; journal article · DOI 10.1016/j.bmcl.2007.09.091Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Pinto DJ, Galemmo RA, 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.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.08.0271-[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, 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.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.02.069Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Quan ML, Han Q, Fevig JM, Lam PY, Bai S, Knabb RM, Luettgen JM, Wong PC, Wexler RR.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.01.010