Zobrazeno 1 - 10
of 34
pro vyhledávání: '"John R. Toomey"'
Autor:
Ian Moench, Christine G. Schnackenberg, Gatto Gregory J, John R. Toomey, Joanne Kuziw, Karpagam Aravindhan, Robert N. Willette
Publikováno v:
Journal of the Endocrine Society
Increased fibroblast growth factor 23 (FGF23) levels are an independent predictor for adverse cardiac events suggesting a role as a link that drives cardiomyopathic changes in cardiorenal syndrome. The search for the underlying mechanism driving this
Autor:
John R. Toomey, John J. Upson
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 9:e199-e203
With a few notable exceptions, heart failure (HF) drug development has faced substantial attrition while translating preclinical discoveries into clinical efficacy. The high attrition has prompted a reconsideration of the target selection process of
Autor:
Stefan Senger, Máire A. Convery, Robert J. Young, Stephanie Irvine, Iain M. McLay, Robert I. West, David J. Belton, Savvas Kleanthous, Carl Adams, John R. Toomey, Anne M. Exall, Anthony J. Pateman, Theresa J. Roethke, Caroline M. Whittaker, Laiq Chaudry, David E. Davies, Angela Patikis, Cynthia L. Burns-Kurtis, Nigel S. Watson, Gary J. Stelman, David W. Brown, John D. Harling, Wendy R. Irving, Chuen Chan, Ping Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1588-1592
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the
Autor:
Savvas Kleanthous, Alan D. Borthwick, David Brown, Cynthia L. Burns-Kurtis, Matthew Campbell, Laiq Chaudry, Chuen Chan, Marie-Olive Clarte, Máire A. Convery, John D. Harling, Eric Hortense, Wendy R. Irving, Stephanie Irvine, Anthony J. Pateman, Angela N. Patikis, Ivan L. Pinto, Derek R. Pollard, Theresa J. Roethka, Stefan Senger, Gita P. Shah, Gary J. Stelman, John R. Toomey, Nigel S. Watson, Robert I. West, Caroline Whittaker, Ping Zhou, Robert J. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:618-622
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa inhibitors, incorporating neutral and basic monoaryl P4 groups, ultimately producing potent inhibitors with effective levels of ant
Autor:
Connie L. Erickson-Miller, Joseph A. Erhardt, Kodandaram Pillarisetti, Manuel Aivado, Melanie A Abboud, John R. Toomey
Publikováno v:
Experimental Hematology. 37:1030-1037
Objective The thrombopoietin receptor (TPOR) is a therapeutic target for treatment of thrombocytopenia because stimulation of this receptor results in enhanced megakaryocyte proliferation, differentiation, and ultimately platelet production. In addit
Autor:
Anthony J. Pateman, John R. Toomey, Paul F. Koster, Augustin Amour, Saul Needle, Laiq Chaudry, Melanie A Abboud, Champa Patel, Angela Patikis, Cynthia L. Burns-Kurtis, Robert J. Young, Richard E. Valocik, David Brown, Ping Zhou, Chuen Chan, Nigel S. Watson
Publikováno v:
Journal of Cardiovascular Pharmacology. 52:66-71
Background: Factor Xa (FXa) has been a target of considerable interest for drug development efforts aimed at suppressing thrombosis. In this report, a new orally active, small molecule, active-site directed FXa inhibitor, GW813893, has been profiled
Autor:
Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:28-33
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activitie
Autor:
Robert J. Young, David W. Brown, Stefan Senger, Chuen Chan, Máire A. Convery, Anthony J. Pateman, Nigel S. Watson, John R. Toomey, Ping Zhou, Henry Anderson Kelly, Shah Gita Punjabhai, Julia A. Hubbard, Angela Patikis, Cynthia L. Burns-Kurtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2927-2930
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhib
Autor:
Christine G. Schnackenberg, Weike Bao, Robert N. Willette, Anna Zacco, Thimmaiah P Chendrimada, John R. Toomey
Publikováno v:
The FASEB Journal. 29
Autor:
Uri Seligsohn, David Gailani, S Bulvik, John R. Toomey, Taketoshi Ogawa, Jacqueline M. Lane, Ariella Zivelin, Meytal Landau
Publikováno v:
Journal of Thrombosis and Haemostasis. 2:1782-1789
During normal hemostasis, the coagulation protease factor (F)XIa activates FIX. Hereditary deficiency of the FXIa precursor, FXI, is usually associated with reduced FXI protein in plasma, and circulating dysfunctional FXI variants are rare. We identi