P. Beaulieu

发表

Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).

C. Brochu, S. LaPlante, M. Bös, 2014, Journal of medicinal chemistry.

Importance of ligand bioactive conformation in the discovery of potent indole-diamide inhibitors of the hepatitis C virus NS5B.

Araz Jakalian, Martin Poirier, C. Brochu, 2010, Journal of the American Chemical Society.

Non-nucleoside benzimidazole-based allosteric inhibitors of the hepatitis C virus NS5B polymerase: inhibition of subgenomic hepatitis C virus RNA replicons in Huh-7 cells.

Yves Bousquet, J. Gillard, P. Beaulieu, 2004, Journal of medicinal chemistry.

An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

Steven R. LaPlante, P. Bonneau, D. Lamarre, 2003, Nature.

2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.

L. Tong, S. Pav, D. Lamarre, 2000, Journal of medicinal chemistry.

Compound aggregation in drug discovery: implementing a practical NMR assay for medicinal chemists.

P. Bonneau, S. LaPlante, R. Coulombe, 2013, Journal of medicinal chemistry.

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).

J. Duan, M. Garneau, Timothy A. Stammers, 2015, Bioorganic & medicinal chemistry letters.

Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.

J. Duan, M. Garneau, S. LaPlante, 2010, Bioorganic & medicinal chemistry letters.

Preparation of Aminoalkyl Chlorohydrin Hydrochlorides: Key Building Blocks for Hydroxyethylamine-Based HIV Protease Inhibitors.

P. Beaulieu, D. Wernic, 1996, The Journal of organic chemistry.

Molecular dynamics simulations and structure-based rational design lead to allosteric HCV NS5B polymerase thumb pocket 2 inhibitor with picomolar cellular replicon potency.

O. Hucke, P. Bonneau, C. Brochu, 2014, Journal of medicinal chemistry.

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).

J. Duan, M. Garneau, S. LaPlante, 2012, Journal of medicinal chemistry.

Specific inhibitors of HCV polymerase identified using an NS5B with lower affinity for template/primer substrate.

D. Lamarre, S. LaPlante, P. Beaulieu, 2004, Nucleic acids research.

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.

Martin Poirier, J. Duan, M. Garneau, 2011, Bioorganic & medicinal chemistry letters.

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.

J. Duan, M. Garneau, S. LaPlante, 2015, Bioorganic & medicinal chemistry letters.

Recent advances in the development of NS5B polymerase inhibitors for the treatment of hepatitis C virus infection

P. Beaulieu, 2009, Expert opinion on therapeutic patents.

Bombesin modulates the association of Src with a nuclear 110-kd protein expressed in dividing prostate cells.

P. Beaulieu, S. Chevalier, A. Aprikian, 2000, Journal of andrology.

The synthesis of 2,5-dihydrofurans from α-allenic alcohols

P. Beaulieu, Veronique M. Morisset, D. Garratt, 1980 .

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.

C. Brochu, S. LaPlante, J. Gillard, 2006, Bioorganic & medicinal chemistry letters.

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.

J. Duan, M. Garneau, P. Anderson, 2014, Journal of medicinal chemistry.

Synthesis of (1R,2S)-1-amino-2-vinylcyclopropanecarboxylic acid vinyl-ACCA) derivatives: key intermediates for the preparation of inhibitors of the hepatitis C virus NS3 protease.

J. Gillard, P. Beaulieu, B. Simoneau, 2005, The Journal of organic chemistry.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.

M. Bös, J. Gillard, P. Beaulieu, 2004, Bioorganic & medicinal chemistry letters.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.

S. LaPlante, M. Bös, J. Gillard, 2004, Bioorganic & medicinal chemistry letters.

An NS 3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

P. Bonneau, D. Lamarre, P. Anderson, 2003 .

Preparation of (2S,4R)-4-Hydroxypipecolic Acid and Derivatives.

P. Beaulieu, Y. Bousquet, I. Guse, 1996 .

Synthesis of ketones by cyclization of cyano and acetylenic radicals: use of .delta.-hydroxy nitriles and .delta.- or .epsilon.-hydroxy acetylenes

P. Beaulieu, D. Clive, 1984 .

An NS 3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

P. Bonneau, D. Lamarre, P. Anderson, 2003 .

Preparation of 3-substituted-2-pyridin-2-ylindoles: regioselectivity of Larock’s indole annulation with 2-alkynylpyridines

E. Hickey, J. Gillard, P. Beaulieu, 2008 .

A Practical Oxone®-Mediated, High-Throughput, Solution-Phase Synthesis of Benzimidazoles from 1,2-Phenylenediamines and Aldehydes and its Application to Preparative Scale Synthesis

P. Beaulieu, B. Haché, Elisabeth von Moos, 2003 .

Binding mode determination of benzimidazole inhibitors of the hepatitis C virus RNA polymerase by a structure and dynamics strategy.

S. LaPlante, J. Gillard, A. Jakalian, 2004, Angewandte Chemie.

Preparation of (2S,4R)-4-Hydroxypipecolic Acid and Derivatives

J. Gillard, P. Beaulieu, Y. Bousquet, 1996 .

PRACTICAL, STEREOSELECTIVE SYNTHESIS OF PALINAVIR, A POTENT HIV PROTEASE INHIBITOR

C. Yoakim, P. Anderson, J. Gillard, 1997 .

Large scale preparation of (2S,3S)-N-Boc-3-amino-1,2-epoxy-4-phenylbutane: A key building block for HIV-protease inhibitors

P. Beaulieu, D. Wernic, Y. Guindon, 1995 .

Preparation of Aminoalkyl Chlorohydrin Hydrochlorides: Key Building Blocks for Hydroxyethylamine-Based HIV Protease Inhibitors.

P. Beaulieu, D. Wernic, 1996, The Journal of organic chemistry.

N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.

J. Duan, M. Garneau, C. Brochu, 2010, Bioorganic & medicinal chemistry letters.

Electrophilic additions to allenes—II : The reaction of benzeneselenenyl chloride with some 1,3-disubstituted allenes

P. Beaulieu, D. Garratt, M. D. Ryan, 1980 .

Practical Synthesis of BILA 2157 BS, a Potent and Orally Active Renin Inhibitor: Use of an Enzyme-Catalyzed Hydrolysis for the Preparation of Homochiral Succinic Acid Derivatives.

J. Gillard, P. Beaulieu, M. Bailey, 1999, The Journal of organic chemistry.

HIV and AIDS Therapeutics

J. Proudfoot, P. Beaulieu, 2000 .

Synthesis of chiral vinylglycines

P. Beaulieu, J. Duceppe, Carolyn Johnson, 1991 .

Enantiospecific synthesis of D-α, ω-diaminoalkanoic acids

P. Beaulieu, P. Schiller, 1988 .

Diastereospecific synthesis of D- and L-allo-threonines and trichlorinated derivatives suitable for the preparation of tritium labelled material.

P. Beaulieu, 1991 .

Synthesis of carbocycles from ω-substituted α,β-unsaturated esters via radical-induced cyclizations

P. Beaulieu, S. Hanessian, D. Dhanoa, 1987 .

Non‐Nucleoside Inhibitors of the Hepatitis C Virus NS5B Polymerase: Discovery and Preliminary SAR of Benzimidazole Derivatives.

P. Beaulieu, Pierre L. Beaulieu, 2004 .

A novel synthetic route to the hexahydrobenzofuran subunit of the avermectins and milbemycins

P. Beaulieu, S. Hanessian, D. Dubé, 1986 .

Synthesis of BILN 2061, an HCV NS3 protease inhibitor with proven antiviral effect in humans.

Martin Poirier, C. Brochu, M. Poirier, 2004, Organic letters.

Dehalogenation of .alpha.-chloro and .alpha.-bromo ketones. Use of sodium O,O-diethyl phosphorotelluroate

P. Beaulieu, D. Clive, 1982 .

Conjugate addition of methyl groups of αβ-unsaturated aldehydes: use of Me5Cu3Li2

P. Beaulieu, D. Clive, V. Farina, 1981 .

Formation of carbon–carbon bonds by ring closure of β-phenylselenocrotonates

P. Beaulieu, D. Clive, 1983 .

Preparation of 4-alkylprolines by intramolecular radical cyclization of chiral serine derivatives

P. Beaulieu, F. Soucy, D. Wernic, 1991 .

Me5Cu3Li2: a reagent for conjugate methylation of .alpha.,.beta.-unsaturated aldehydes

P. Beaulieu, D. Clive, V. Farina, 1982 .

Additions of Group 6A and 7A electrophilic reagents to dimethyl endo,endo-bicyclo[2.2.2]oct-5-ene-2,3-dicarboxylate: Competitive formation of .gamma.- and .delta.-lactones

P. Beaulieu, D. Garratt, M. D. Ryan, 1980 .

Oxone®‐Mediated Synthesis of Benzimidazoles from 1,2‐Phenylenediamines and Aldehydes: Preparation of 2‐(4‐Cyano‐Phenyl)‐1‐[2‐(3,4‐Dimethoxyphenyl)‐Ethyl]‐1H‐Benzimidazole‐5‐Carboxylic Acid Ethyl Ester

J. Gillard, P. Beaulieu, 2014 .

Synthesis of Chiral Vinylglycines.

P. Beaulieu, J. Duceppe, Carolyn Johnson, 1991 .

Safety, pharmacokinetics and antiviral effect of BILB 1941, a novel hepatitis C virus RNA polymerase inhibitor, after 5 days oral treatment

X. Forns, P. Beaulieu, G. Kukolj, 2009, Antiviral therapy.

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

P. Beaulieu, Pierre L Beaulieu, 2007, Current opinion in investigational drugs.

Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.

M. Garneau, S. LaPlante, R. Coulombe, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: discovery of a quinazolinone chemotype.

Araz Jakalian, Martin Poirier, Cédrickx Godbout, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.

Louise Thauvette, Araz Jakalian, M. Bös, 2013, Bioorganic & medicinal chemistry letters.

Binding Site Characterization and Resistance to a Class of Non-nucleoside Inhibitors of the Hepatitis C Virus NS5B Polymerase*

Louise Thauvette, Graham A. McGibbon, P. Beaulieu, 2005, Journal of Biological Chemistry.

Practical, Stereoselective Synthesis of Palinavir, a Potent HIV Protease Inhibitor.

C. Yoakim, P. Anderson, J. Gillard, 2010 .

Progress in natural product chemistry by the chiron and related approaches - synthesis of avermectin B1a

P. Beaulieu, S. Hanessian, D. Dubé, 1987 .

Development of a Pilot-Plant Process for a Nevirapine Analogue HIV NNRT Inhibitor

P. Beaulieu, Ji-Young Kim, D. Norwood, 2008 .

CHAPTER 8:Design and Development of NS5B Polymerase Non‐nucleoside Inhibitors for the Treatment of Hepatitis C Virus Infection

P. Beaulieu, Pierre L. Beaulieu, 2013 .

The reaction of some propargyl alcohols with benzeneselenenyl chloride

P. Beaulieu, Veronique M. Morisset, D. Garratt, 1981 .

Allosteric N-acetamide-indole-6-carboxylic acid thumb pocket 1 inhibitors of hepatitis C virus NS5B polymerase - Acylsulfonamides and acylsulfamides as carboxylic acid replacements

P. Kuhn, J. Duan, M. Garneau, 2013 .

Chapter 111 – Molecular Aspects of Drug Actions: From Receptors to Effectors

P. Beaulieu, C. Litalien, 2006 .

A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): application of a one-pot borylation-Suzuki coupling reaction.

P. Beaulieu, Y. Tsantrizos, C. Senanayake, 2014, Organic letters.

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

P. Beaulieu, 2006, Current opinion in drug discovery & development.

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.

J. Duan, M. Garneau, J. Gillard, 2011, Bioorganic & medicinal chemistry letters.

A potent peptidomimetic inhibitor of HSV ribonucleotide reductase with antiviral activity in vivo

M. Garneau, P. Beaulieu, J. Chafouleas, 1994, Nature.

Purification, characterization, and localization of subunit interaction area of recombinant mouse ribonucleotide reductase R1 subunit.

G. Mann, P. Beaulieu, A. Gräslund, 1994, The Journal of biological chemistry.

Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase with improved in vivo antiviral activity.

M. Garneau, C. Yoakim, N. Moss, 1996, Journal of medicinal chemistry.

Cannabimimetic eicosanoids in cancer and inflammation: an update.

T. Bisogno, P. Beaulieu, A. Rice, 2002, Advances in experimental medicine and biology.

Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase: a new class of antiviral agents.

N. Moss, P. Beaulieu, J. Gauthier, 1995, Journal of medicinal chemistry.

Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.

J. Gillard, M. Poirier, P. Beaulieu, 2010, Bioorganic & medicinal chemistry letters.

Enantiomeric atropisomers inhibit HCV polymerase and/or HIV matrix: characterizing hindered bond rotations and target selectivity.

O. Hucke, S. LaPlante, R. Coulombe, 2014, Journal of medicinal chemistry.

Structure-based design of novel HCV NS 5 B thumb pocket 2 allosteric inhibitors with submicromolar gt 1 replicon potency : Discovery of a

J. Duan, O. Hucke, R. Coulombe, 2013 .

Metal-free coupling of azoles with 2- and 3-haloindoles providing access to novel 2- or 3-(azol-1-yl)indole derivatives.

M. Poirier, P. Beaulieu, J. Savoie, 2010, Organic letters.

Metal‐Free Coupling of Azoles with 2‐ and 3‐Haloindoles Providing Access to Novel 2‐ or 3‐(Azol‐1‐yl)indole Derivatives.

M. Poirier, P. Beaulieu, J. Savoie, 2010 .

Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.

L. Tong, S. Pav, D. Lamarre, 1997, Journal of medicinal chemistry.

Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.

J. Proudfoot, L. Tong, E. Hickey, 1999, Journal of medicinal chemistry.

Monitoring drug self-aggregation and potential for promiscuity in off-target in vitro pharmacology screens by a practical NMR strategy.

P. Bonneau, S. LaPlante, R. Coulombe, 2013, Journal of medicinal chemistry.

Inhibition of herpes simplex virus type 1 ribonucleotide reductase by substituted tetrapeptide derivatives.

J. DiMaio, N. Moss, P. Beaulieu, 1993, Journal of medicinal chemistry.

Chapter 117 – Molecular Mechanisms of Drug Actions: From Receptors to Effectors

P. Beaulieu, C. Litalien, 2011 .