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Items: 22

1.

Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.

Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J, Callejo M, Miller MM, Lawrence RM, Banville J, Guy J, Maxwell BD, Priestley ES, Marinier A, Wexler RR, Bouvier M, Gordon DA, Schumacher WA, Yang J.

Sci Transl Med. 2017 Jan 4;9(371). pii: eaaf5294. doi: 10.1126/scitranslmed.aaf5294.

PMID:
28053157
2.

4-Benzothiazole-7-hydroxyindolinyl diaryl ureas are potent P2Y1 antagonists with favorable pharmacokinetics: low clearance and small volume of distribution.

Qiao JX, Wang TC, Hiebert S, Hu CH, Schumacher WA, Spronk SA, Clark CG, Han Y, Hua J, Price LA, Shen H, Chacko SA, Everlof G, Bostwick JS, Steinbacher TE, Li YX, Huang CS, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

ChemMedChem. 2014 Oct;9(10):2327-43. doi: 10.1002/cmdc.201402141. Epub 2014 Jul 2.

PMID:
24989964
3.

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

Jeon YT, Yang W, Qiao JX, Li L, Ruel R, Thibeault C, Hiebert S, Wang TC, Wang Y, Liu Y, Clark CG, Wong HS, Zhu J, Wu DR, Sun D, Chen BC, Mathur A, Chacko SA, Malley M, Chen XQ, Shen H, Huang CS, Schumacher WA, Bostwick JS, Stewart AB, Price LA, Hua J, Li D, Levesque PC, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1294-8. doi: 10.1016/j.bmcl.2014.01.066. Epub 2014 Jan 31.

PMID:
24513044
4.

Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.

Qiao JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY.

J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12.

PMID:
24164581
5.

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
6.

Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.

Chao H, Turdi H, Herpin TF, Roberge JY, Liu Y, Schnur DM, Poss MA, Rehfuss R, Hua J, Wu Q, Price LA, Abell LM, Schumacher WA, Bostwick JS, Steinbacher TE, Stewart AB, Ogletree ML, Huang CS, Chang M, Cacace AM, Arcuri MJ, Celani D, Wexler RR, Lawrence RM.

J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u. Epub 2013 Feb 18.

PMID:
23368907
7.

Bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (PI3K)-β inhibitor in mice.

Bird JE, Smith PL, Bostwick JS, Shipkova P, Schumacher WA.

Thromb Res. 2011 Jun;127(6):560-4. doi: 10.1016/j.thromres.2011.02.007. Epub 2011 Mar 10.

PMID:
21396684
8.

Effect of the direct factor Xa inhibitor apixaban in rat models of thrombosis and hemostasis.

Schumacher WA, Bostwick JS, Stewart AB, Steinbacher TE, Xin B, Wong PC.

J Cardiovasc Pharmacol. 2010 Jun;55(6):609-16. doi: 10.1097/FJC.0b013e3181daded3.

PMID:
20224421
9.

Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats.

Schumacher WA, Seiler SE, Steinbacher TE, Stewart AB, Bostwick JS, Hartl KS, Liu EC, Ogletree ML.

Eur J Pharmacol. 2007 Sep 10;570(1-3):167-74. Epub 2007 Jun 5.

PMID:
17597608
10.

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
11.

Biomarker optimization to track the antithrombotic and hemostatic effects of clopidogrel in rats.

Schumacher WA, Bostwick JS, Ogletree ML, Stewart AB, Steinbacher TE, Hua J, Price LA, Wong PC, Rehfuss RP.

J Pharmacol Exp Ther. 2007 Jul;322(1):369-77. Epub 2007 Apr 9.

PMID:
17420297
12.

Is exogenous tissue plasminogen activator necessary for antithrombotic efficacy of an inhibitor of thrombin activatable fibrinolysis inhibitor (TAFI) in rats?

Bird E, Tamura J, Bostwick JS, Steinbacher TE, Stewart A, Liu Y, Baumann J, Feyen J, Tamasi J, Schumacher WA.

Thromb Res. 2007;120(4):549-58. Epub 2007 Jan 16.

PMID:
17229457
13.

Superiority of enoxaparin over heparin in combination with a GPIIb/IIIa receptor antagonist during coronary thrombolysis in dogs.

Rebello SS, Kasiewski CJ, Bentley RG, Morgan SR, Chu V, Bostwick JS, Klein SI, Perrone MH, Leadley RJ.

Thromb Res. 2001 May 1;102(3):261-71.

PMID:
11369420
14.

Clopidogrel but not ticlopidine produces an antiplatelet effect in the Yucatan minipig.

Bostwick JS, Costanzo S, Byan L, Luo Y, Natarajan C, Bilder G.

Thromb Haemost. 2000 Nov;84(5):928. No abstract available.

PMID:
11127885
15.

Pharmacodynamic activity and antithrombotic efficacy of RPR120844, a novel inhibitor of coagulation factor Xa.

Leadley RJ Jr, Morgan SR, Bentley R, Bostwick JS, Kasiewski CJ, Heran C, Chu V, Brown K, Moxey P, Ewing WR, Pauls H, Spada AP, Perrone MH, Dunwiddie CT.

J Cardiovasc Pharmacol. 1999 Dec;34(6):791-9.

PMID:
10598121
16.

RPR120844, a novel, specific inhibitor of coagulation factor Xa inhibits venous thrombosis in the rabbit.

Bostwick JS, Bentley R, Morgan S, Brown K, Chu V, Ewing WR, Spada AP, Pauls H, Perrone MH, Dunwiddie CT, Leadley RJ Jr.

Thromb Haemost. 1999 Jan;81(1):157-60.

PMID:
10348709
17.

Design of a new class of orally active fibrinogen receptor antagonists.

Klein SI, Molino BF, Czekaj M, Gardner CJ, Chu V, Brown K, Sabatino RD, Bostwick JS, Kasiewski C, Bentley R, Windisch V, Perrone M, Dunwiddie CT, Leadley RJ.

J Med Chem. 1998 Jul 2;41(14):2492-502.

PMID:
9651154
18.

Inhibition of repetitive thrombus formation in the stenosed canine coronary artery by enoxaparin, but not by unfractionated heparin.

Leadley RJ Jr, Kasiewski CJ, Bostwick JS, Bentley R, Dunwiddie CT, Perrone MH.

Arterioscler Thromb Vasc Biol. 1998 Jun;18(6):908-14.

PMID:
9633930
19.

Comparison of enoxaparin, hirulog, and heparin as adjunctive antithrombotic therapy during thrombolysis with rtPA in the stenosed canine coronary artery.

Leadley RJ Jr, Kasiewski CJ, Bostwick JS, Bentley R, McVey MJ, White FJ, Perrone MH, Dunwiddie CT.

Thromb Haemost. 1997 Oct;78(4):1278-85.

PMID:
9364998
20.

Anti-thrombotic activity of RG13965, a novel platelet fibrinogen receptor antagonist.

Bostwick JS, Kasiewski CJ, Chu V, Klein SI, Sabatino RD, Perrone MH, Dunwiddie CT, Cook JJ, Leadley RJ Jr.

Thromb Res. 1996 Jun 15;82(6):495-507.

PMID:
8794522
21.

RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog.

Fitzpatrick LR, Lambert RM, Pendley CE, Martin GE, Bostwick JS, Gessner GW, Airey JE, Youssefyeh RD, Pendleton RG, Decktor DL.

J Pharmacol Exp Ther. 1990 Aug;254(2):450-5.

PMID:
2166791
22.

Antiinflammatory effects of various drugs on acetic acid induced colitis in the rat.

Fitzpatrick LR, Bostwick JS, Renzetti M, Pendleton RG, Decktor DL.

Agents Actions. 1990 Jun;30(3-4):393-402.

PMID:
1974733

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