Publications by authors named "Pierre L Beaulieu"

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Aza follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 1: Mitigating the genotoxic liability of an aniline metabolite.
Pierre L Beaulieu, Gordon Bolger, Martin Duplessis, Alexandre Gagnon, Michel Garneau

Bioorg Med Chem Lett· March 2015

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Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.
Pierre L Beaulieu, Gordon Bolger, Dan Deon, Martin Duplessis, Gulrez Fazal

Bioorg Med Chem Lett· March 2015

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A prodrug strategy for the oral delivery of a poorly soluble HCV NS5B thumb pocket 1 polymerase inhibitor using self-emulsifying drug delivery systems (SEDDS).
Pierre L Beaulieu, Josie De Marte, Michel Garneau, Laibin Luo, Timothy Stammers

Bioorg Med Chem Lett· January 2015

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Discovery of BI 207524, an indole diamide NS5B thumb pocket 1 inhibitor with improved potency for the potential treatment of chronic hepatitis C virus infection.
Pierre L Beaulieu, Paul C Anderson, Richard Bethell, Michael Bös, Yves Bousquet

J Med Chem· December 2014

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A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): application of a one-pot borylation-Suzuki coupling reaction.
Yongda Zhang, Bruce Z Lu, Guisheng Li, Sonia Rodriguez, Jonathan Tan, Pierre L Beaulieu

Org Lett· September 2014

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Molecular dynamics simulations and structure-based rational design lead to allosteric HCV NS5B polymerase thumb pocket 2 inhibitor with picomolar cellular replicon potency.
Oliver Hucke, René Coulombe, Pierre Bonneau, Mégan Bertrand-Laperle, Christian Brochu, Pierre L Beaulieu

J Med Chem· March 2014

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Enantiomeric atropisomers inhibit HCV polymerase and/or HIV matrix: characterizing hindered bond rotations and target selectivity.
Steven R LaPlante, Pat Forgione, Colette Boucher, René Coulombe, James Gillard, Pierre L Beaulieu

J Med Chem· March 2014

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Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).
Steven R LaPlante, Michael Bös, Christian Brochu, Catherine Chabot, René Coulombe, Pierre L Beaulieu

J Med Chem· March 2014

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Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.
Timothy A Stammers, René Coulombe, Martin Duplessis, Gulrez Fazal, Alexandre Gagnon, Pierre L Beaulieu

Bioorg Med Chem Lett· December 2013

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Monitoring drug self-aggregation and potential for promiscuity in off-target in vitro pharmacology screens by a practical NMR strategy.
Steven R LaPlante, Norman Aubry, Gordon Bolger, Pierre Bonneau, Rebekah Carson, Pierre L Beaulieu

J Med Chem· September 2013

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Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: discovery of a quinazolinone chemotype.
Pierre L Beaulieu, René Coulombe, Jianmin Duan, Gulrez Fazal, Cédrickx Godbout

Bioorg Med Chem Lett· July 2013

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Compound aggregation in drug discovery: implementing a practical NMR assay for medicinal chemists.
Steven R LaPlante, Rebekah Carson, James Gillard, Norman Aubry, René Coulombe, Pierre L Beaulieu

J Med Chem· June 2013

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Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.
Timothy A Stammers, René Coulombe, Jean Rancourt, Bounkham Thavonekham, Gulrez Fazal, Pierre L Beaulieu

Bioorg Med Chem Lett· May 2013

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Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV).
Pierre L Beaulieu, Michael Bös, Michael G Cordingley, Catherine Chabot, Gulrez Fazal

J Med Chem· September 2012

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From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons.
Pierre L Beaulieu, James Gillard, Eric Jolicoeur, Jianmin Duan, Michel Garneau

Bioorg Med Chem Lett· June 2011

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Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): central amino acid linker and right-hand-side SAR studies.
Pierre L Beaulieu, Catherine Chabot, Jianmin Duan, Michel Garneau, James Gillard

Bioorg Med Chem Lett· June 2011

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Filibuvir, a non-nucleoside NS5B polymerase inhibitor for the potential oral treatment of chronic HCV infection.
Pierre L Beaulieu

IDrugs· December 2010

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Importance of ligand bioactive conformation in the discovery of potent indole-diamide inhibitors of the hepatitis C virus NS5B.
Steven R LaPlante, James R Gillard, Araz Jakalian, Norman Aubry, René Coulombe, Pierre L Beaulieu

J Am Chem Soc· November 2010

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Metal-free coupling of azoles with 2- and 3-haloindoles providing access to novel 2- or 3-(azol-1-yl)indole derivatives.
Martin Poirier, Sébastien Goudreau, Jason Poulin, Jolaine Savoie, Pierre L Beaulieu

Org Lett· May 2010

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Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.
Pierre L Beaulieu, Nathalie Dansereau, Jianmin Duan, Michel Garneau, James Gillard

Bioorg Med Chem Lett· March 2010

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N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.
Pierre L Beaulieu, Eric Jolicoeur, James Gillard, Christian Brochu, René Coulombe

Bioorg Med Chem Lett· February 2010

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Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.
Sylvie Goulet, Marc-André Poupart, James Gillard, Martin Poirier, George Kukolj, Pierre L Beaulieu

Bioorg Med Chem Lett· January 2010

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Recent advances in the development of NS5B polymerase inhibitors for the treatment of hepatitis C virus infection.
Pierre L Beaulieu

Expert Opin Ther Pat· February 2009

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Non-nucleoside inhibitors of the HCV NS5B polymerase: progress in the discovery and development of novel agents for the treatment of HCV infections.
Pierre L Beaulieu

Curr Opin Investig Drugs· August 2007

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Finger loop inhibitors of the HCV NS5B polymerase: discovery and prospects for new HCV therapy.
Pierre L Beaulieu

Curr Opin Drug Discov Devel· September 2006

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