Zobrazeno 1 - 10
of 73
pro vyhledávání: '"T. Dunwiddie"'
Autor:
Sebastian Maignan, Suzanne R Morgan, Robert J. Leadley, Valeria Chu, Gardner Charles J, Spada Alfred P, Pauls Henry W, Ross G. Bentley, Christopher T Dunwiddie, Klein Scott I, Jean-Pierre Guilloteau, Mark Czekaj, Karen Brown, Daniel L Cheney, Dennis J Colussi, Christopher L Heran, Kevin R. Guertin, Allison L Zulli, Yong Gong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1671-1674
Further optimization of the beta-aminoester class of factor Xa (fXa) inhibitors is described culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with excellent in vivo anticoagulant activity. An X-ray structur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7b464ff575bc5ebe1e2a29926574c40
https://doi.org/10.1016/s0960-894x(02)00213-5
https://doi.org/10.1016/s0960-894x(02)00213-5
Autor:
Mason Helen J, Karen D. Brown, Valeria Chu, Guyan Liang, Daniel M. Green, Alfred P. Spada, Henry W. Pauls, Ross Bentley, Cuong Ly, Roderick S. Davis, Dennis J. Colussi, Daniel L. Cheney, Michael R. Becker, Y.M. Choi-Sledeski, Christopher T. Dunwiddie, Robert J. Leadley, Ewing William R, John H. Barton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2539-2544
The design, synthesis and SAR of sulfonamidopyrrolidinone fXa inhibitors incorporating a new benzamidine isostere, namely aminoisoquinolines, is described. These inhibitors have higher Caco-2 cell permeability than comparable benzamidines and attain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a71de730d502044d956f73b19dd821f
https://doi.org/10.1016/s0960-894x(99)00421-7
https://doi.org/10.1016/s0960-894x(99)00421-7
Autor:
Alfred P. Spada, Robert J. Leadley, Jonathan S. Mason, Dennis J. Colussi, Ewing William R, Mark H. Perrone, Karen D. Brown, Michael R. Becker, Don D. Cha, Daniel M. Green, Ross Bentley, Henry W. Pauls, Christopher T. Dunwiddie, Jean-Pierre Guilloteau, Y.M. Choi-Sledeski, Sebastien Maignan, Mason Helen J, Vincent E. Manetta, Charles Kasiewski, Valeria Chu, Roderick S. Davis, Suzanne Morgan, Daniel L. Cheney, Jeff Bostwick
Publikováno v:
Journal of Medicinal Chemistry. 42:3557-3571
The discovery of a series of non-peptide factor Xa (FXa) inhibitors incorporating 3-(S)-amino-2-pyrrolidinone as a central template is described. After identifying compound 4, improvements in in vitro potency involved modifications of the liphophilic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2009f497bb352b54bc0c7e881834e15b
https://doi.org/10.1021/jm990040h
https://doi.org/10.1021/jm990040h
Autor:
Robert J. Leadley, Charles Kasiewski, Tara Wentz, Glenda E. Bilder, Jeffery Bostwick, Mark H. Perrone, Saul J. Needle, Betsey O’Conner, Christopher T. Dunwiddie, Lisa Byan, Kenneth Page, Helen Galczenski, Linda Merkel, Persons Paul E, Myers Michael R, Alfred P. Spada, Amin Dilip, Cuong Ly
Publikováno v:
Circulation. 99:3292-3299
Background —Platelet-derived growth factor (PDGF), a purported mediator of arterial response to injury, stimulates proliferation, chemotaxis, and matrix production by activation of its membrane receptor tyrosine kinase. Because these activities und
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65d180846942468a5df5011431ca5416
https://doi.org/10.1161/01.cir.99.25.3292
https://doi.org/10.1161/01.cir.99.25.3292
Autor:
Ewing William R, Robert J. Leadley, Alfred P. Spada, Mark H. Perrone, Christopher T. Dunwiddie, S. Morgan, Henry W. Pauls, Valeria Chu, Jeffrey S. Bostwick, Karen D. Brown, Ross Bentley
Publikováno v:
Thrombosis and Haemostasis. 81:157-160
SummaryThe in vivo antithrombotic activity of RPR120844, a novel synthetic coagulation factor Xa (fXa) inhibitor (Ki = 7 nM), was assessed by its ability to inhibit thrombus formation in a damaged segment of the rabbit jugular vein. Intravenous dose-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f1ed83ecb09809b17f08abe7f2ff8cfa
https://doi.org/10.1055/s-0037-1614434
https://doi.org/10.1055/s-0037-1614434
Autor:
Robert J. Leadley, Mark H. Perrone, Charles Kasiewski, Jeffrey S. Bostwick, Christopher T. Dunwiddie, Ross Bentley
Publikováno v:
Arteriosclerosis, Thrombosis, and Vascular Biology. 18:908-914
Abstract —Experiments were designed to compare the antithrombotic efficacy of enoxaparin and unfractionated heparin (UH) in a model of platelet-dependent cyclic flow reductions (CFRs) in the stenosed canine circumflex coronary artery. Low-molecular
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::604ac45e87ddbc22c0e87ab4bc1abb7b
https://doi.org/10.1161/01.atv.18.6.908
https://doi.org/10.1161/01.atv.18.6.908
Autor:
Robert J. Leadley, Matthew J. McVey, Mark H. Perrone, Ross Bentley, Christopher T. Dunwiddie, Jeffrey S. Bostwick, Charles Kasiewski, Francis J White
Publikováno v:
Thrombosis and Haemostasis. 78:1278-1285
SummaryA canine model of electrolytic injury-induced coronary artery thrombosis and rtPA-induced thrombolysis was used to evaluate the relative antithrombotic efficacy of enoxaparin (a low molecular weight heparin), conventional therapy (heparin or h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::31506d56963d97353b1024fcc56e34dd
https://doi.org/10.1055/s-0038-1657728
https://doi.org/10.1055/s-0038-1657728
Autor:
Rose D'Alisa, Bruce F. Molino, Scott I. Klein, Jeffrey M Dener, Robert J. Leadley, Charles Kasiewski, Christopher T. Dunwiddie, Charles J. Gardner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2225-2230
A series of analogs were prepared based on the known thrombin inhibitor PPACK, in which the D-Phe-Pro dipeptide has been replaced by trans-4-O-benzyl hydroxyproline. One of these analogs is a more potent inhibitor of thrombin, and is more selective,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c89f7d9bba49b5b6a674a2c67451aa9b
https://doi.org/10.1016/0960-894x(96)00404-0
https://doi.org/10.1016/0960-894x(96)00404-0
Autor:
Robert J. Leadley, Bruce F. Molino, Scott I. Klein, Jeffrey S Dener, Christopher T. Dunwiddie, Ralph D. Sabatino, Mark Czekaj, Valeria Chu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1403-1408
Structure-activity relationships developed from work with peptide based fibrinogen receptor antagonists have been successfully applied to the development of simple and highly potent nonpeptide agents of the same class.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::da81eb78b2d474e0007dce3ec31aef6f
https://doi.org/10.1016/0960-894x(96)00236-3
https://doi.org/10.1016/0960-894x(96)00236-3
Autor:
W C Roberts, Ian J. Sarembock, S D Gertz, C T Dunwiddie, Eric R. Powers, Lawrence W. Gimple, G P Vlasuk, Howard L. Haber, Michael Ragosta
Publikováno v:
Circulation. 89:1262-1271
BACKGROUND Balloon angioplasty of atherosclerotic arteries results in activation of the coagulation cascade. Several coagulation factors, including factor Xa and thrombin, are mitogenic for vascular smooth muscle cells in vitro and thus may play a ro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39161e8542daa4d55f5095629e4675b9
https://doi.org/10.1161/01.cir.89.3.1262
https://doi.org/10.1161/01.cir.89.3.1262