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Items: 29

1.

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
2.

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
3.

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
4.

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
5.

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
6.

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
7.

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
8.

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
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.

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
11.

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
12.

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
13.

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
14.
15.

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
16.

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
17.

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
18.

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
19.

Effects of antithrombotic drugs in a rat model of aspirin-insensitive arterial thrombosis.

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

Thromb Haemost. 1993 May 3;69(5):509-14.

PMID:
8322273
20.

Antiplatelet activity of the long-acting thromboxane receptor antagonist BMS 180,291 in monkeys.

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

Prostaglandins. 1992 Nov;44(5):389-97.

PMID:
1301074
21.

Thrombin inhibition compared with other antithrombotic drugs in rats.

Schumacher WA, Heran CH, Steinbacher TE, Megill JR, Bird JE, Giancarli MR, Durham SK.

Thromb Res. 1992 Oct 15;68(2):157-66.

PMID:
1475778
22.

Pharmacological characterization of potent, long-acting thromboxane receptor antagonists, SQ 33,261 and SQ 33,552.

Harris DN, Michel IM, Goldenberg HJ, Hartl KS, Allen GT, Steinbacher TE, Schumacher WA, Han WC, Hall SE, Floyd DM, et al.

J Pharmacol Exp Ther. 1992 Apr;261(1):131-7.

PMID:
1532833
23.

Thromboxane receptor activation during bronchospasm induced by platelet-activating factor.

Schumacher WA, Steinbacher TE.

J Lipid Mediat. 1991 Jul-Aug;4(1):97-110.

PMID:
1832573
24.

Role of thromboxane receptor activation in the bronchospastic response to endothelin.

Schumacher WA, Steinbacher TE, Allen GT, Ogletree ML.

Prostaglandins. 1990 Jul;40(1):71-9.

PMID:
2143841
25.

Role of thromboxane receptors in Forssman shock in guinea pigs.

Schumacher WA, Steinbacher TE, Allen GT, Ogletree ML.

J Appl Physiol (1985). 1989 Jul;67(1):44-51.

PMID:
2527227
26.

Inhibition of prostaglandin biosynthesis by SQ 28,852, a 7-oxabicyclo[2.2.1]heptane analog.

Harris DN, Phillips MB, Michel IM, Goldenberg HJ, Steinbacher TE, Ogletree ML, Hall SE.

Prostaglandins. 1986 Apr;31(4):651-67.

PMID:
3088677
27.

Effects of SQ 27,427, a thromboxane A2 receptor antagonist, in the human platelet and isolated smooth muscle.

Harris DN, Greenberg R, Phillips MB, Michel IM, Goldenberg HJ, Haslanger MF, Steinbacher TE.

Eur J Pharmacol. 1984 Aug 3;103(1-2):9-18.

PMID:
6090180
28.

Thromboxane receptor antagonist properties of SQ 27,427 in the anesthetized guinea pig.

Greenberg R, Steinbacher TE, Harris DN, Haslanger MF.

Eur J Pharmacol. 1984 Aug 3;103(1-2):19-24.

PMID:
6090175
29.

Antihypertensive activity of captopril (SQ 14,225), an orally active inhibitor of angiotensin converting enzyme in conscious two-kidney perinephritic hypertensive dogs.

Vollmer RR, Boccagno JA, Steinbacher TE, Horovitz ZP, Murthy VS.

J Pharmacol Exp Ther. 1981 Feb;216(2):225-31.

PMID:
6257882

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