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Items: 22

1.

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.

Corte JR, Pinto DJP, Fang T, Osuna H, Yang W, Wang Y, Lai A, Clark CG, Sun JH, Rampulla R, Mathur A, Kaspady M, Neithnadka PR, Li YC, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Harper TW, Huang C, Zheng JJ, Bozarth JM, Wu Y, Wong PC, Crain EJ, Seiffert DA, Luettgen JM, Lam PYS, Wexler RR, Ewing WR.

J Med Chem. 2020 Jan 23;63(2):784-803. doi: 10.1021/acs.jmedchem.9b01768. Epub 2020 Jan 2.

PMID:
31833761
2.

Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).

Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR.

J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17.

PMID:
29077405
3.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

Smith LM 2nd, Orwat MJ, Hu Z, Han W, Wang C, Rossi KA, Gilligan PJ, Pabbisetty KB, Osuna H, Corte JR, Rendina AR, Luettgen JM, Wong PC, Narayanan R, Harper TW, Bozarth JM, Crain EJ, Wei A, Ramamurthy V, Morin PE, Xin B, Zheng J, Seiffert DA, Quan ML, Lam PYS, Wexler RR, Pinto DJP.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):472-478. doi: 10.1016/j.bmcl.2015.11.089. Epub 2015 Nov 26.

PMID:
26704266
4.

The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys.

Wong PC, Watson C, Crain EJ.

J Thromb Thrombolysis. 2016 Apr;41(3):514-21. doi: 10.1007/s11239-015-1302-7.

PMID:
26660522
5.

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa.

Wong PC, Quan ML, Watson CA, Crain EJ, Harpel MR, Rendina AR, Luettgen JM, Wexler RR, Schumacher WA, Seiffert DA.

J Thromb Thrombolysis. 2015 Nov;40(4):416-23. doi: 10.1007/s11239-015-1258-7.

PMID:
26249722
6.

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.

Hu Z, Wong PC, Gilligan PJ, Han W, Pabbisetty KB, Bozarth JM, Crain EJ, Harper T, Luettgen JM, Myers JE Jr, Ramamurthy V, Rossi KA, Sheriff S, Watson CA, Wei A, Zheng JJ, Seiffert DA, Wexler RR, Quan ML.

ACS Med Chem Lett. 2015 Apr 8;6(5):590-5. doi: 10.1021/acsmedchemlett.5b00066. eCollection 2015 May 14.

7.

Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.

Wang TC, Qiao JX, Clark CG, Jua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Everlof G, Schumacher WA, Wong PC, Seiffert DA, Stewart AB, Bostwick JS, Crain EJ, Watson CA, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3239-43. doi: 10.1016/j.bmcl.2013.03.125. Epub 2013 Apr 6.

PMID:
23602442
8.

A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits.

Wong PC, Crain EJ, Watson CA, Schumacher WA.

J Thromb Thrombolysis. 2011 Aug;32(2):129-37. doi: 10.1007/s11239-011-0599-0.

PMID:
21614454
9.

Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits.

Zhang D, He K, Raghavan N, Wang L, Crain EJ, He B, Xin B, Luettgen JM, Wong PC.

J Thromb Thrombolysis. 2010 Jan;29(1):70-80. doi: 10.1007/s11239-009-0401-8.

PMID:
19851712
10.

Favorable therapeutic index of the direct factor Xa inhibitors, apixaban and rivaroxaban, compared with the thrombin inhibitor dabigatran in rabbits.

Wong PC, Crain EJ, Watson CA, Xin B.

J Thromb Haemost. 2009 Aug;7(8):1313-20. doi: 10.1111/j.1538-7836.2009.03503.x. Epub 2009 Jun 3.

11.

Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro.

Jiang X, Crain EJ, Luettgen JM, Schumacher WA, Wong PC.

Thromb Haemost. 2009 Apr;101(4):780-2. No abstract available.

PMID:
19350128
12.

Clopidogrel versus prasugrel in rabbits. Effects on thrombosis, haemostasis, platelet function and response variability.

Wong PC, Crain EJ, Watson CA, Hua J, Schumacher WA, Rehfuss R.

Thromb Haemost. 2009 Jan;101(1):108-15.

PMID:
19132196
13.

Arterial antithrombotic and bleeding time effects of apixaban, a direct factor Xa inhibitor, in combination with antiplatelet therapy in rabbits.

Wong PC, Watson CA, Crain EJ.

J Thromb Haemost. 2008 Oct;6(10):1736-41. doi: 10.1111/j.1538-7836.2008.03092.x. Epub 2008 Jul 19.

14.

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.

15.

Platelet aggregometry and receptor binding to predict the magnitude of antithrombotic and bleeding time effects of clopidogrel in rabbits.

Wong PC, Crain EJ, Watson CA, Jiang X, Hua J, Bostwick JS, Ogletree ML, Schumacher WA, Rehfuss R.

J Cardiovasc Pharmacol. 2007 May;49(5):316-24.

PMID:
17513951
16.

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
17.

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
18.

Nonpeptide factor Xa inhibitors II. Antithrombotic evaluation in a rabbit model of electrically induced carotid artery thrombosis.

Wong PC, Crain EJ, Knabb RM, Meade RP, Quan ML, Watson CA, Wexler RR, Wright MR, Slee AM.

J Pharmacol Exp Ther. 2000 Oct;295(1):212-8.

PMID:
10991981
19.

Attitudes toward death-related choices.

Crain EJ, Lester D.

Psychol Rep. 2000 Jun;86(3 Pt 2):1200.

PMID:
10932579
20.

Nonpeptide factor Xa inhibitors: I. Studies with SF303 and SK549, a new class of potent antithrombotics.

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

J Pharmacol Exp Ther. 2000 Jan;292(1):351-7.

PMID:
10604970
21.

Antithrombotic actions of selective inhibitors of blood coagulation factor Xa in rat models of thrombosis.

Wong PC, Crain EJ Jr, Nguan O, Watson CA, Racanelli A.

Thromb Res. 1996 Jul 15;83(2):117-26.

PMID:
8837310
22.

Pharmacology of XR510, a potent orally active nonpeptide angiotensin II AT1 receptor antagonist with high affinity for the AT2 receptor subtype.

Wong PC, Quan ML, Saye JM, Bernard R, Crain EJ Jr, McCall DE, Watson CA, Zaspel AM, Smith RD, Wexler RR, et al.

J Cardiovasc Pharmacol. 1995 Sep;26(3):354-62.

PMID:
8583775

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