Detalhe da pesquisa
1.
From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa inhibitor eliquis.
J Thromb Thrombolysis
; 52(2): 403-407, 2021 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-34351559
2.
First-in-human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS-962212, a direct, reversible, small molecule factor XIa inhibitor in non-Japanese and Japanese healthy subjects.
Br J Clin Pharmacol
; 84(5): 876-887, 2018 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-29346838
3.
Apixaban Versus Warfarin for Mechanical Heart Valve Thromboprophylaxis in a Swine Aortic Heterotopic Valve Model.
Arterioscler Thromb Vasc Biol
; 37(5): 942-948, 2017 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-28232327
4.
Apixaban versus enoxaparin for thromboprophylaxis in medically ill patients.
N Engl J Med
; 365(23): 2167-77, 2011 Dec 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-22077144
5.
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Bioorg Med Chem Lett
; 24(15): 3341-5, 2014 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-24951330
6.
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.
Bioorg Med Chem Lett
; 23(8): 2432-5, 2013 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23478148
7.
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.
Bioorg Med Chem Lett
; 23(6): 1604-7, 2013 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23416003
8.
Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.
J Enzyme Inhib Med Chem
; 26(4): 514-26, 2011 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-21171894
9.
Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor.
Eur J Drug Metab Pharmacokinet
; 36(3): 129-39, 2011 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-21461793
10.
Phenyltriazolinones as potent factor Xa inhibitors.
Bioorg Med Chem Lett
; 20(4): 1373-7, 2010 Feb 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20100660
11.
Sulfation of o-demethyl apixaban: enzyme identification and species comparison.
Drug Metab Dispos
; 37(4): 802-8, 2009 Apr.
Artigo
em Inglês
| MEDLINE | ID: mdl-19131519
12.
Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans.
Drug Metab Dispos
; 37(8): 1738-48, 2009 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-19420130
13.
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Bioorg Med Chem Lett
; 19(2): 462-8, 2009 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19046881
14.
Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs.
Drug Metab Dispos
; 36(2): 303-15, 2008 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-17984286
15.
Achieving 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.
Bioorg Med Chem Lett
; 18(14): 4118-23, 2008 Jul 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18550370
16.
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bioorg Med Chem Lett
; 18(2): 749-54, 2008 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18054227
17.
Sulfonamidolactam inhibitors of coagulation factor Xa.
Bioorg Med Chem Lett
; 18(7): 2428-33, 2008 Apr 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18329876
18.
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Bioorg Med Chem Lett
; 18(9): 2845-9, 2008 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18424044
19.
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.
J Med Chem
; 50(22): 5339-56, 2007 Nov 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17914785
20.
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bioorg Med Chem Lett
; 17(23): 6481-8, 2007 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17933529