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Items: 1 to 50 of 84

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.

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
3.

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
4.

New advances in treating thrombotic diseases.

Schumacher WA, Wang X, Wong PC.

Drug Discov Today. 2014 Sep;19(9):1433-4. doi: 10.1016/j.drudis.2014.06.015. Epub 2014 Jun 21. No abstract available.

PMID:
24959954
5.

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
6.

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
7.

Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.

Bolton SA, Sutton JC, Anumula R, Bisacchi GS, Jacobson B, Slusarchyk WA, Treuner UD, Wu SC, Zhao G, Pi Z, Sheriff S, Smirk RA, Bisaha S, Cheney DL, Wei A, Schumacher WA, Hartl KS, Liu E, Zahler R, Seiler SM.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5239-43. doi: 10.1016/j.bmcl.2013.06.028. Epub 2013 Jun 20.

PMID:
23927973
8.

Does plexin-B1, a semaphorin 4D receptor, play a role in thrombosis?

Bird E, Smith PL, Seiffert D, Psaltis GC, Huang J, Schumacher WA.

Thromb Res. 2013 Jun;131(6):564-5. doi: 10.1016/j.thromres.2013.03.018. Epub 2013 Apr 30. No abstract available.

PMID:
23642655
9.

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
10.

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
11.

A platelet target for venous thrombosis? P2Y1 deletion or antagonism protects mice from vena cava thrombosis.

Bird JE, Wang X, Smith PL, Barbera F, Huang C, Schumacher WA.

J Thromb Thrombolysis. 2012 Aug;34(2):199-207. doi: 10.1007/s11239-012-0745-3.

PMID:
22588534
12.

Effects of plasma kallikrein deficiency on haemostasis and thrombosis in mice: murine ortholog of the Fletcher trait.

Bird JE, Smith PL, Wang X, Schumacher WA, Barbera F, Revelli JP, Seiffert D.

Thromb Haemost. 2012 Jun;107(6):1141-50. doi: 10.1160/TH-11-10-0682. Epub 2012 Mar 8.

PMID:
22398951
13.

Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.

Shi Y, O'Connor SP, Sitkoff D, Zhang J, Shi M, Bisaha SN, Wang Y, Li C, Ruan Z, Lawrence RM, Klei HE, Kish K, Liu EC, Seiler SM, Schweizer L, Steinbacher TE, Schumacher WA, Robl JA, Macor JE, Atwal KS, Stein PD.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7516-21. doi: 10.1016/j.bmcl.2011.06.098. Epub 2011 Jun 28.

PMID:
22041058
14.

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
15.

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
16.

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
17.

Inhibition of factor XIa as a new approach to anticoagulation.

Schumacher WA, Luettgen JM, Quan ML, Seiffert DA.

Arterioscler Thromb Vasc Biol. 2010 Mar;30(3):388-92. doi: 10.1161/ATVBAHA.109.197178. Epub 2010 Feb 5. Review.

PMID:
20139363
18.

Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.

Shi Y, Li C, O'Connor SP, Zhang J, Shi M, Bisaha SN, Wang Y, Sitkoff D, Pudzianowski AT, Huang C, Klei HE, Kish K, Yanchunas J Jr, Liu EC, Hartl KS, Seiler SM, Steinbacher TE, Schumacher WA, Atwal KS, Stein PD.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. doi: 10.1016/j.bmcl.2009.10.084. Epub 2009 Oct 23.

PMID:
19896847
19.

Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.

Shi Y, Zhang J, Shi M, O'Connor SP, Bisaha SN, Li C, Sitkoff D, Pudzianowski AT, Chong S, Klei HE, Kish K, Yanchunas J Jr, Liu EC, Hartl KS, Seiler SM, Steinbacher TE, Schumacher WA, Atwal KS, Stein PD.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4034-41. doi: 10.1016/j.bmcl.2009.06.014. Epub 2009 Jun 13.

PMID:
19541481
20.

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
21.

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
22.

Design, structure-activity relationships, X-ray crystal structure, and energetic contributions of a critical P1 pharmacophore: 3-chloroindole-7-yl-based factor Xa inhibitors.

Shi Y, Sitkoff D, Zhang J, Klei HE, Kish K, Liu EC, Hartl KS, Seiler SM, Chang M, Huang C, Youssef S, Steinbacher TE, Schumacher WA, Grazier N, Pudzianowski A, Apedo A, Discenza L, Yanchunas J, Stein PD, Atwal KS.

J Med Chem. 2008 Dec 11;51(23):7541-51. doi: 10.1021/jm800855x.

PMID:
18998662
23.

Prediction of the therapeutic index of marketed anti-coagulants and anti-platelet agents by guinea pig models of thrombosis and hemostasis.

Bird JE, Giancarli MR, Allegretto N, Barbera F, Wong P, Schumacher WA, Ogletree ML, Seiffert D.

Thromb Res. 2008;123(1):146-58. doi: 10.1016/j.thromres.2008.03.010. Epub 2008 May 14.

PMID:
18479740
24.

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
25.

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
26.

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
27.

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
28.

Deficiency in thrombin-activatable fibrinolysis inhibitor (TAFI) protected mice from ferric chloride-induced vena cava thrombosis.

Wang X, Smith PL, Hsu MY, Tamasi JA, Bird E, Schumacher WA.

J Thromb Thrombolysis. 2007 Feb;23(1):41-9.

PMID:
17111204
29.

Effects of factor XI deficiency on ferric chloride-induced vena cava thrombosis in mice.

Wang X, Smith PL, Hsu MY, Gailani D, Schumacher WA, Ogletree ML, Seiffert DA.

J Thromb Haemost. 2006 Sep;4(9):1982-8.

30.

Quantification of platelet composition in experimental venous thrombosis by real-time polymerase chain reaction.

Wang X, Hsu MY, Steinbacher TE, Monticello TM, Schumacher WA.

Thromb Res. 2007;119(5):593-600. Epub 2006 Jun 22.

PMID:
16797058
31.

Murine model of ferric chloride-induced vena cava thrombosis: evidence for effect of potato carboxypeptidase inhibitor.

Wang X, Smith PL, Hsu MY, Ogletree ML, Schumacher WA.

J Thromb Haemost. 2006 Feb;4(2):403-10.

32.

Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.

Shi Y, Zhang J, Stein PD, Shi M, O'Connor SP, Bisaha SN, Li C, Atwal KS, Bisacchi GS, Sitkoff D, Pudzianowski AT, Liu EC, Hartl KS, Seiler SM, Youssef S, Steinbacher TE, Schumacher WA, Rendina AR, Bozarth JM, Peterson TL, Zhang G, Zahler R.

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5453-8. Epub 2005 Oct 5. Erratum in: Bioorg Med Chem Lett. 2006 Mar 1;16(5):1449.

PMID:
16213711
33.

Effects of factor IX or factor XI deficiency on ferric chloride-induced carotid artery occlusion in mice.

Wang X, Cheng Q, Xu L, Feuerstein GZ, Hsu MY, Smith PL, Seiffert DA, Schumacher WA, Ogletree ML, Gailani D.

J Thromb Haemost. 2005 Apr;3(4):695-702. Epub 2005 Feb 23.

34.

Inhibition of tumor necrosis factor-alpha-converting enzyme by a selective antagonist protects brain from focal ischemic injury in rats.

Wang X, Feuerstein GZ, Xu L, Wang H, Schumacher WA, Ogletree ML, Taub R, Duan JJ, Decicco CP, Liu RQ.

Mol Pharmacol. 2004 Apr;65(4):890-6.

PMID:
15044618
35.

Synthesis of potent and highly selective inhibitors of human tryptase.

Slusarchyk WA, Bolton SA, Hartl KS, Huang MH, Jacobs G, Meng W, Ogletree ML, Pi Z, Schumacher WA, Seiler SM, Sutton JC, Treuner U, Zahler R, Zhao G, Bisacchi GS.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3235-8.

PMID:
12372541
36.

Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

Sutton JC, Bolton SA, Hartl KS, Huang MH, Jacobs G, Meng W, Ogletree ML, Pi Z, Schumacher WA, Seiler SM, Slusarchyk WA, Treuner U, Zahler R, Zhao G, Bisacchi GS.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.

PMID:
12372540
37.

Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.

Iwanowicz EJ, Kimball SD, Lin J, Lau W, Han WC, Wang TC, Roberts DG, Schumacher WA, Ogletree ML, Seiler SM.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3183-6.

PMID:
12372529
38.

[Poly-beta-hydroxybutyric acid (PHB) films and plates in defect covering of the osseus skull in a rabbit model].

Kramp B, Bernd HE, Schumacher WA, Blynow M, Schmidt W, Kunze C, Behrend D, Schmitz KP.

Laryngorhinootologie. 2002 May;81(5):351-6. German.

PMID:
12001025
39.

Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.

Das J, Kimball SD, Hall SE, Han WC, Iwanowicz E, Lin J, Moquin RV, Reid JA, Sack JS, Malley MF, Chang CY, Chong S, Wang-Iverson DB, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):45-9.

PMID:
11738570
40.

Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.

Das J, Kimball SD, Reid JA, Wang TC, Lau WF, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):41-4.

PMID:
11738569
41.

[Variations in the course of the internal carotid artery: possible risks in so-called standard operations in the area of the pharynx].

Schumacher WA, Schafig A, Kehrl W, Pau HW.

Laryngorhinootologie. 1998 Sep;77(9):517-20. German.

PMID:
9795930
42.
43.

A ferret model of electrical-induction of arterial thrombosis that is sensitive to aspirin.

Schumacher WA, Steinbacher TE, Megill JR, Durham SK.

J Pharmacol Toxicol Methods. 1996 Feb;35(1):3-10.

PMID:
8645878
44.

Sensitivity of experimental venous and arterial thrombosis and bleeding to ancrod-induced defibrinogenation.

Schumacher WA, Heran CL, Steinbacher TE.

Thromb Res. 1996 Jan 15;81(2):187-94.

PMID:
8822133
45.

Dose-related cardioprotection by ifetroban in relation to inhibition of thrombosis and ex vivo platelet function.

Gomoll AW, Schumacher WA, Ogletree ML.

Pharmacology. 1995 Feb;50(2):92-110.

PMID:
7716179
46.

Thromboxane receptor antagonist BMS-180291, but not aspirin, reduces the severity of pacing-induced ischemia in dogs.

Grover GJ, Schumacher WA, Ogletree ML.

J Cardiovasc Pharmacol. 1994 Sep;24(3):493-9.

PMID:
7528306
47.

Effect of a novel thrombin active-site inhibitor on arterial and venous thrombosis.

Schumacher WA, Balasubramanian N, St Laurent DR, Seiler SM.

Eur J Pharmacol. 1994 Jul 1;259(2):165-71.

PMID:
7957610
48.

2-[3-[2-(4,5-diphenyl-2-oxazolyl) ethyl] phenoxy] acetic acid (BMY 42393): 2). Oral activity and efficacy in animal models of arterial thrombosis.

Seiler SM, Buchanan JO, Schumacher WA, Zavoico GB, Gamberdella M, Fleming JS, Meanwell NA.

Thromb Res. 1994 Apr 15;74(2):125-33.

PMID:
8029813
49.

Comparison of thrombin active site and exosite inhibitors and heparin in experimental models of arterial and venous thrombosis and bleeding.

Schumacher WA, Steinbacher TE, Heran CL, Seiler SM, Michel IM, Ogletree ML.

J Pharmacol Exp Ther. 1993 Dec;267(3):1237-42.

PMID:
8263785
50.

Superior activity of a thromboxane receptor antagonist as compared with aspirin in rat models of arterial and venous thrombosis.

Schumacher WA, Heran CL, Steinbacher TE, Youssef S, Ogletree ML.

J Cardiovasc Pharmacol. 1993 Oct;22(4):526-33.

PMID:
7505353

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