Literature DB >> 21349711

The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.

Nigel S Watson1, Carl Adams, David Belton, David Brown, Cynthia L Burns-Kurtis, Laiq Chaudry, Chuen Chan, Máire A Convery, David E Davies, Anne M Exall, John D Harling, Stephanie Irvine, Wendy R Irving, Savvas Kleanthous, Iain M McLay, Anthony J Pateman, Angela N Patikis, Theresa J Roethke, Stefan Senger, Gary J Stelman, John R Toomey, Robert I West, Caroline Whittaker, Ping Zhou, Robert J Young.   

Abstract

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 former series were addressed in the later, delivering a robust candidate for progression towards clinical studies.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21349711     DOI: 10.1016/j.bmcl.2011.01.129

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Electronically Rich N-Substituted Tetrahydroisoquinoline 3-Carboxylic Acid Esters: Concise Synthesis and Conformational Studies.

Authors:  Rami A Al-Horani; Umesh R Desai
Journal:  Tetrahedron       Date:  2012-01-10       Impact factor: 2.457

2.  CSAR 2014: A Benchmark Exercise Using Unpublished Data from Pharma.

Authors:  Heather A Carlson; Richard D Smith; Kelly L Damm-Ganamet; Jeanne A Stuckey; Aqeel Ahmed; Maire A Convery; Donald O Somers; Michael Kranz; Patricia A Elkins; Guanglei Cui; Catherine E Peishoff; Millard H Lambert; James B Dunbar
Journal:  J Chem Inf Model       Date:  2016-05-17       Impact factor: 4.956

  2 in total

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