Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 88

1.

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.

Perera V, Luettgen JM, Wang Z, Frost CE, Yones C, Russo C, Lee J, Zhao Y, LaCreta FP, Ma X, Knabb RM, Seiffert D, DeSouza M, Mugnier P, Cirincione B, Ueno T, Frost RJA.

Br J Clin Pharmacol. 2018 May;84(5):876-887. doi: 10.1111/bcp.13520. Epub 2018 Mar 5.

2.

Apixaban Versus Warfarin for Mechanical Heart Valve Thromboprophylaxis in a Swine Aortic Heterotopic Valve Model.

Lester PA, Coleman DM, Diaz JA, Jackson TO, Hawley AE, Mathues AR, Grant BT, Knabb RM, Ramacciotti E, Frost CE, Song Y, Wakefield TW, Myers DD Jr.

Arterioscler Thromb Vasc Biol. 2017 May;37(5):942-948. doi: 10.1161/ATVBAHA.116.308649. Epub 2017 Feb 23.

PMID:
28232327
3.

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.

Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3341-5. doi: 10.1016/j.bmcl.2014.05.101. Epub 2014 Jun 7.

PMID:
24951330
4.

Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.

Zhang X, Jiang W, Jacutin-Porte S, Glunz PW, Zou Y, Cheng X, Nirschl AH, Wurtz NR, Luettgen JM, Rendina AR, Luo G, Harper TM, Wei A, Anumula R, Cheney DL, Knabb RM, Wong PC, Wexler RR, Priestley ES.

ACS Med Chem Lett. 2013 Dec 26;5(2):188-92. doi: 10.1021/ml400453z. eCollection 2014 Feb 13.

5.

Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.

Priestley ES, De Lucca I, Zhou J, Zhou J, Saiah E, Stanton R, Robinson L, Luettgen JM, Wei A, Wen X, Knabb RM, Wong PC, Wexler RR.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2432-5. doi: 10.1016/j.bmcl.2013.02.013. Epub 2013 Feb 14.

PMID:
23478148
6.

Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.

Zhang X, Glunz PW, Jiang W, Schmitt A, Newman M, Barbera FA, Bozarth JM, Rendina AR, Wei A, Wen X, Rossi KA, Luettgen JM, Wong PC, Knabb RM, Wexler RR, Scott Priestley E.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1604-7. doi: 10.1016/j.bmcl.2013.01.094. Epub 2013 Jan 30.

PMID:
23416003
7.

The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review.

Pinto DJ, Qiao JX, Knabb RM.

Expert Opin Ther Pat. 2012 Jun;22(6):645-61. doi: 10.1517/13543776.2012.680438. Epub 2012 Jun 3. Review.

PMID:
22655676
8.

A novel prothrombin time assay for assessing the anticoagulant activity of oral factor Xa inhibitors.

Barrett YC, Wang Z, Knabb RM.

Clin Appl Thromb Hemost. 2013 Sep;19(5):522-8. doi: 10.1177/1076029612441859. Epub 2012 Apr 2.

PMID:
22473028
9.

Apixaban versus enoxaparin for thromboprophylaxis in medically ill patients.

Goldhaber SZ, Leizorovicz A, Kakkar AK, Haas SK, Merli G, Knabb RM, Weitz JI; ADOPT Trial Investigators.

N Engl J Med. 2011 Dec 8;365(23):2167-77. doi: 10.1056/NEJMoa1110899. Epub 2011 Nov 13.

10.

Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor.

He K, Luettgen JM, Zhang D, He B, Grace JE Jr, Xin B, Pinto DJ, Wong PC, Knabb RM, Lam PY, Wexler RR, Grossman SJ.

Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):129-39. doi: 10.1007/s13318-011-0037-x. Epub 2011 Apr 2.

PMID:
21461793
11.

Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.

Luettgen JM, Knabb RM, He K, Pinto DJ, Rendina AR.

J Enzyme Inhib Med Chem. 2011 Aug;26(4):514-26. doi: 10.3109/14756366.2010.535793. Epub 2010 Dec 20.

PMID:
21171894
12.

BMS-593214, an active site-directed factor VIIa inhibitor: enzyme kinetics, antithrombotic and antihaemostatic studies.

Wong PC, Luettgen JM, Rendina AR, Kettner CA, Xin B, Knabb RM, Wexler R, Priestley ES.

Thromb Haemost. 2010 Aug;104(2):261-9. doi: 10.1160/TH10-01-0025. Epub 2010 Jun 29.

PMID:
20589312
13.

Factor Xa inhibitors: next-generation antithrombotic agents.

Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR.

J Med Chem. 2010 Sep 9;53(17):6243-74. doi: 10.1021/jm100146h. Review. No abstract available.

PMID:
20503967
14.

Phenyltriazolinones 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. 2010 Feb 15;20(4):1373-7. doi: 10.1016/j.bmcl.2010.01.011. Epub 2010 Jan 11.

PMID:
20100660
15.

Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans.

Zhang D, He K, Raghavan N, Wang L, Mitroka J, Maxwell BD, Knabb RM, Frost C, Schuster A, Hao F, Gu Z, Humphreys WG, Grossman SJ.

Drug Metab Dispos. 2009 Aug;37(8):1738-48. doi: 10.1124/dmd.108.025981. Epub 2009 May 6.

PMID:
19420130
16.

Sulfation of o-demethyl apixaban: enzyme identification and species comparison.

Wang L, Raghavan N, He K, Luettgen JM, Humphreys WG, Knabb RM, Pinto DJ, Zhang D.

Drug Metab Dispos. 2009 Apr;37(4):802-8. doi: 10.1124/dmd.108.025593. Epub 2009 Jan 8.

PMID:
19131519
17.

Highly 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. 2009 Jan 15;19(2):462-8. doi: 10.1016/j.bmcl.2008.11.049. Epub 2008 Nov 18.

PMID:
19046881
18.

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.

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. 2008 Jul 15;18(14):4118-23. doi: 10.1016/j.bmcl.2008.05.095. Epub 2008 May 29.

PMID:
18550370
19.

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.

Bioorg Med Chem Lett. 2008 May 1;18(9):2845-9. doi: 10.1016/j.bmcl.2008.03.092. Epub 2008 Apr 8.

PMID:
18424044
20.

Sulfonamidolactam inhibitors of coagulation factor Xa.

Smallheer JM, Wang S, Laws ML, Nakajima S, Hu Z, Han W, Jacobson I, Luettgen JM, Rossi KA, Rendina AR, Knabb RM, Wexler RR, Lam PY, Quan ML.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2428-33. doi: 10.1016/j.bmcl.2008.02.054. Epub 2008 Feb 26.

PMID:
18329876
21.

Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies.

Wong PC, Crain EJ, Xin B, Wexler RR, Lam PY, Pinto DJ, Luettgen JM, Knabb RM.

J Thromb Haemost. 2008 May;6(5):820-9. doi: 10.1111/j.1538-7836.2008.02939.x. Epub 2008 Feb 25.

22.

Structure-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. 2008 Jan 15;18(2):749-54. Epub 2007 Nov 17.

PMID:
18054227
23.

Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs.

Zhang D, Raghavan N, Chen SY, Zhang H, Quan M, Lecureux L, Patrone LM, Lam PY, Bonacorsi SJ, Knabb RM, Skiles GL, He K.

Drug Metab Dispos. 2008 Feb;36(2):303-15. Epub 2007 Nov 5.

PMID:
17984286
24.

Design, 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. 2007 Dec 1;17(23):6481-8. Epub 2007 Oct 1.

PMID:
17933529
25.

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.

J Med Chem. 2007 Nov 1;50(22):5339-56. Epub 2007 Oct 3.

PMID:
17914785
26.

N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.

He K, Qian M, Wong H, Bai SA, He B, Brogdon B, Grace JE, Xin B, Wu J, Ren SX, Zeng H, Deng Y, Graden DM, Olah TV, Unger SE, Luettgen JM, Knabb RM, Pinto DJ, Lam PY, Duan J, Wexler RR, Decicco CP, Christ DD, Grossman SJ.

J Pharm Sci. 2008 Jul;97(7):2568-80.

PMID:
17914718
27.

Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.

Qiao JX, Wang TC, Wang GZ, Cheney DL, He K, Rendina AR, Xin B, Luettgen JM, Knabb RM, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5041-8. Epub 2007 Jul 13.

PMID:
17643988
28.

SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.

Qiao JX, Chang CH, Cheney DL, Morin PE, Wang GZ, King SR, Wang TC, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4419-27. Epub 2007 Jun 10.

PMID:
17588746
29.

Razaxaban, a direct factor Xa inhibitor, in combination with aspirin and/or clopidogrel improves low-dose antithrombotic activity without enhancing bleeding liability in rabbits.

Wong PC, Crain EJ, Watson CA, Wexler RR, Lam PY, Quan ML, Knabb RM.

J Thromb Thrombolysis. 2007 Aug;24(1):43-51. Epub 2007 Feb 24.

PMID:
17323133
30.

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.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1432-7. Epub 2006 Dec 1.

PMID:
17174550
31.

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.

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5584-9. Epub 2006 Sep 11.

PMID:
16963264
32.

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.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. Epub 2006 Jul 25.

PMID:
16870435
33.

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.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. Epub 2006 May 30.

PMID:
16730984
34.

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.

Fevig JM, Cacciola J, Buriak J Jr, Rossi KA, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3755-60. Epub 2006 May 8.

PMID:
16682200
35.

Aminobenzisoxazoles 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. 2006 Apr 1;16(7):1795-8. Epub 2006 Jan 24.

PMID:
16434195
36.

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.

J Med Chem. 2005 Mar 24;48(6):1729-44.

PMID:
15771420
37.

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.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):29-35.

PMID:
15582405
38.

5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.

Batt DG, Qiao JX, Modi DP, Houghton GC, Pierson DA, Rossi KA, Luettgen JM, Knabb RM, Jadhav PK, Wexler RR.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5269-73.

PMID:
15454209
39.

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.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7.

PMID:
15454208
40.

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.

J Med Chem. 2003 Dec 4;46(25):5298-315.

PMID:
14640539
41.

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.

J Med Chem. 2003 Oct 9;46(21):4405-18.

PMID:
14521405
42.

Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.

Lam PY, Adams JJ, Clark CG, Calhoun WJ, Luettgen JM, Knabb RM, Wexler RR.

Bioorg Med Chem Lett. 2003 May 19;13(10):1795-9.

PMID:
12729667
43.

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.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1023-8.

PMID:
12643903
44.

Inhibition of factor Xa reduces ischemic brain damage after thromboembolic stroke in rats.

Wang X, Xu L, Wang H, Grzanna R, Zhan Y, Knabb RM, Luettgen JM, Bozarth TA, Galemmo RA, Wong PC, Bernard R, Vargas H, Chopp M, Friedman SM, Feuerstein GZ.

Stroke. 2003 Feb;34(2):468-74.

PMID:
12574562
45.

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.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):369-73.

PMID:
12565931
46.

Nonpeptide factor Xa inhibitors III: effects of DPC423, an orally-active pyrazole antithrombotic agent, on arterial thrombosis in rabbits.

Wong PC, Crain EJ, Watson CA, Zaspel AM, Wright MR, Lam PY, Pinto DJ, Wexler RR, Knabb RM.

J Pharmacol Exp Ther. 2002 Dec;303(3):993-1000.

PMID:
12438519
47.

Nonpeptide factor Xa inhibitors: DPC423, a highly potent and orally bioavailable pyrazole antithrombotic agent.

Wong PC, Pinto DJ, Knabb RM.

Cardiovasc Drug Rev. 2002 Summer;20(2):137-52. Review.

PMID:
12177691
48.

Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.

Fevig JM, Pinto DJ, Han Q, Quan ML, Pruitt JR, Jacobson IC, Galemmo RA Jr, Wang S, Orwat MJ, Bostrom LL, Knabb RM, Wong PC, Lam PYS, Wexler RR.

Bioorg Med Chem Lett. 2001 Mar 12;11(5):641-5.

PMID:
11266160
49.

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.

J Med Chem. 2001 Feb 15;44(4):566-78.

PMID:
11170646
50.

Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.

Han Q, Dominguez C, Stouten PF, Park JM, Duffy DE, Galemmo RA Jr, Rossi KA, Alexander RS, Smallwood AM, Wong PC, Wright MM, Luettgen JM, Knabb RM, Wexler RR.

J Med Chem. 2000 Nov 16;43(23):4398-415.

PMID:
11087565

Supplemental Content

Loading ...
Support Center