Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Valeria Chu"'
Autor:
Marie-Laure Ozoux, Anne Paccaly, Ronald Rosenburg, Bradford K. Jensen, Markus Hinder, U A Shukla, Annke Frick, Valeria Chu
Publikováno v:
The Journal of Clinical Pharmacology. 46:45-51
Direct pharmacokinetic/pharmacodynamic relationships for otamixaban were investigated after rising doses in healthy subjects using mixed-effect modeling. Activated partial thromboplastin time, prothrombin time, dilute prothrombin time, and Russell's
Autor:
Yong Mi Choi-Sledeski, Karen Brown, Robert J. Leadley, Gregory B. Poli, Vincent Mikol, Spada Alfred P, Yong Gong, Robert E. Kearney, Phillip Moxey, Charles J Kasiewski, Ross G. Bentley, Sébastien Maignan, Dennis Collussi, Pauls Henry W, Sam S. Rebello, Davis Roderick S, Valeria Chu, Gardner Charles J, Michael Becker, Jean-Pierre Guilloteau, Guyan Liang, Suzanne R Morgan
Publikováno v:
Journal of Medicinal Chemistry. 46:681-684
The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the
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
Autor:
Robert J. Leadley, Charles J Kasiewski, Ross Bentley, Suzanne R Morgan, Sam S. Rebello, Valeria Chu, Mark H Perrone
Publikováno v:
British Journal of Pharmacology. 133:1190-1198
We compared the antithrombotic efficacy of a potent factor Xa inhibitor, FXV673, to heparin and RPR109891, a GPIIb/IIIa antagonist, when used as adjunctive therapy in a canine model of rt-PA-induced coronary thrombolysis. Thrombus formation was induc
Autor:
Karen Brown, W. Ewing, Ross G. Bentley, Mark H. Perrone, Christopher L. Heran, Robert J. Leadley, Jeffrey S. Bostwick, Charles Kasiewski, Suzanne R Morgan, Spada Alfred P, Dunwiddie Christopher T, Valeria Chu, Phillip Moxey, Pauls Henry W
Publikováno v:
Journal of Cardiovascular Pharmacology. 34:791-799
These studies were designed to examine the pharmacodynamic profile and antithrombotic efficacy of RPR120844, a competitive inhibitor of coagulation factor Xa, with a K(i) of 7 nM against human factor Xa. In vitro, RPR120844 doubled activated partial
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
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
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-
Publikováno v:
European Journal of Medicinal Chemistry. 32:833-839
Summary A series of nonpeptide fibrinogen receptor antagonists based upon the tetrapeptide Arg-Gly-Asp-Arg were prepared. These relatively simple derivatives incorporate a high degree of conformational flexibility that was anticipated to allow them t
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.