The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K

JY Gauthier, N Chauret, W Cromlish… - Bioorganic & medicinal …, 2008 - Elsevier
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to
address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and …

Effect of common organic solvents on in vitrocytochrome P450-mediated metabolic activities in human liver microsomes

N Chauret, A Gauthier, DA Nicoll-Griffith - Drug Metabolism and Disposition, 1998 - ASPET
In this study, we report the effect of methanol, dimethyl sulfoxide (DMSO), and acetonitrile
on the cytochrome P450 (P450)-mediated metabolism of several substrates in human liver …

In vitro comparison of cytochrome P450-mediated metabolic activities in human, dog, cat, and horse

N Chauret, A Gauthier, J Martin… - Drug Metabolism and …, 1997 - ASPET
As domestic animals such as cat, horse, and dog increasingly become the clinical targets
for drug discovery programs, the need to understand how these animals metabolize …

Discovery of a Potent and Selective Prostaglandin D2 Receptor Antagonist, [(3R)-4-(4-Chloro- benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b] …

…, N Tsou, Y Aubin, KP Bateman, N Chauret… - Journal of medicinal …, 2007 - ACS Publications
The discovery of the potent and selective prostaglandin D 2 (PGD 2 ) receptor (DP)
antagonist [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3…

A generally applicable method for assessing the electrophilicity and reactivity of diverse nitrile-containing compounds

RM Oballa, JF Truchon, CI Bayly, N Chauret… - Bioorganic & medicinal …, 2007 - Elsevier
Nitrile-based inhibitors of cathepsin K have been known for some time and mechanism-of-action
studies have demonstrated that cysteinyl proteases interact with nitriles in a reversible …

BLU-5937: a selective P2X3 antagonist with potent anti-tussive effect and no taste alteration

D Garceau, N Chauret - Pulmonary pharmacology & therapeutics, 2019 - Elsevier
… Author links open overlay panel Denis Garceau , Nathalie Chauret … Denis Garceau
and Nathalie Chauret are employees of BELLUS Health and hold shares in the company. …

Discovery of a potent and selective agonist of the prostaglandin EP4 receptor

X Billot, A Chateauneuf, N Chauret, D Denis… - Bioorganic & medicinal …, 2003 - Elsevier
Analogues of PGE 2 wherein the hydroxycyclopentanone ring has been replaced by a
lactam have been prepared and evaluated as ligands for the EP 4 receptor. An optimized …

Description of a 96-well plate assay to measure cytochrome P4503A inhibition in human liver microsomes using a selective fluorescent probe

N Chauret, N Tremblay, RL Lackman, JY Gauthier… - Analytical …, 1999 - Elsevier
The standard method to evaluate CYP3A inhibition is to study the conversion of the specific
CYP3A probe testosterone to its 6β-hydroxy metabolite in human liver microsomes, in the …

Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: prevention of reactive intermediate formation and covalent binding

N Chauret, D Guay, C Li, S Day, J Silva… - Bioorganic & medicinal …, 2002 - Elsevier
A detailed study directed towards metabolic stability optimization of the alkoxy substituents
on the catechol moiety of CDP-840 is reported. Replacement of the methoxy and …

Evaluation of VCH-759 monotherapy in hepatitis C infection

…, FH Anderson, SS Lee, J Bédard, N Chauret… - Journal of …, 2009 - Elsevier
BACKGROUND/AIMS: VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent
polymerase with sub-micromolar IC 50 values versus genotype 1a/1b replicons. METHODS: The …