Search Results - "CHAURET, Nathalie"

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K by Gauthier, Jacques Yves, Chauret, Nathalie, Cromlish, Wanda, Desmarais, Sylvie, Duong, Le T., Falgueyret, Jean-Pierre, Kimmel, Donald B., Lamontagne, Sonia, Léger, Serge, LeRiche, Tammy, Li, Chun Sing, Massé, Frédéric, McKay, Daniel J., Nicoll-Griffith, Deborah A., Oballa, Renata M., Palmer, James T., Percival, M. David, Riendeau, Denis, Robichaud, Joel, Rodan, Gideon A., Rodan, Sevgi B., Seto, Carmai, Thérien, Michel, Truong, Vouy-Linh, Venuti, Michael C., Wesolowski, Gregg, Young, Robert N., Zamboni, Robert, Black, W. Cameron

“…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…”
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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]indol-3-yl]-acetic Acid (MK-0524) by Sturino, Claudio F, O'Neill, Gary, Lachance, Nicolas, Boyd, Michael, Berthelette, Carl, Labelle, Marc, Li, Lianhai, Roy, Bruno, Scheigetz, John, Tsou, Nancy, Aubin, Yves, Bateman, Kevin P, Chauret, Nathalie, Day, Stephen H, Lévesque, Jean-François, Seto, Carmai, Silva, Jose H, Trimble, Laird A, Carriere, Marie-Claude, Denis, Danielle, Greig, Gillian, Kargman, Stacia, Lamontagne, Sonia, Mathieu, Marie-Claude, Sawyer, Nicole, Slipetz, Deborah, Abraham, William M, Jones, Tom, McAuliffe, Malia, Piechuta, Hana, Nicoll-Griffith, Deborah A, Wang, Zhaoyin, Zamboni, Robert, Young, Robert N, Metters, Kathleen M

“…The discovery of the potent and selective prostaglandin D2 (PGD2) receptor (DP) antagonist…”
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A generally applicable method for assessing the electrophilicity and reactivity of diverse nitrile-containing compounds by Oballa, Renata M., Truchon, Jean-François, Bayly, Christopher I., Chauret, Nathalie, Day, Stephen, Crane, Sheldon, Berthelette, Carl

“…A simple theoretical calculation (reactivity of nitriles with methanethiol) was used to predict the electrophilicity of diverse nitrile warheads. These…”
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BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration by Garceau, Denis, Chauret, Nathalie

“…BLU-5937 is a small molecule that was shown to be a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist. P2X3 receptors are ATP…”
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In Vitro Comparison of Cytochrome P450-Mediated Metabolic Activities in Human, Dog, Cat, and Horse by Chauret, N, Gauthier, A, Martin, J, Nicoll-Griffith, D A

“…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…”
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Discovery of a potent and selective agonist of the prostaglandin EP4 receptor by BILLOT, Xavier, CHATEAUNEUF, Anne, CHAURET, Nathalie, DENIS, Danielle, GREIG, Gillian, MATHIEU, Marie-Claude, METTERS, Kathleen M, SLIPETZ, Deborah M, YOUNG, Robert N

“…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…”
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Substituted coumarins as potent 5-lipoxygenase inhibitors by Grimm, Erich L., Brideau, Christine, Chauret, Nathalie, Chan, Chi-Chung, Delorme, Daniel, Ducharme, Yves, Ethier, Diane, Falgueyret, Jean-Pierre, Friesen, Richard W., Guay, Jocelyne, Hamel, Pierre, Riendeau, Denis, Soucy-Breau, Chantal, Tagari, Philip, Girard, Yves

“…A novel series of substituted coumarin derivatives has been synthesized. SAR studies in this series led to the identification of inhibitor 1. Leukotriene…”
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Hypoxia‐induced down‐regulation of CYP1A1/1A2 and up‐regulation of CYP3A6 involves serum mediators by Fradette, Caroline, Bleau, Anne‐Marie, Pichette, Vincent, Chauret, Nathalie, Du Souich, Patrick

“…Acute moderate hypoxia modifies the catalytic activity and expression of certain isoenzymes of hepatic cytochrome P450 (P450). The aim of this study was to…”
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Selective isolation of in vitro phase II conjugates using a lipophilic anionic exchange solid phase extraction method by Gagné, Sébastien, Laterreur, Julie, Mahrouche, Louiza, Sørensen, Dan, Gauthier, Jacques Yves, Truong, Vouy Linh, Chauret, Nathalie, Lévesque, Jean-François

“…Identification, characterization and structure elucidation of human metabolites of drug candidates is crucial for the pharmaceutical industry to assess their…”
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Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: prevention of reactive intermediate formation and covalent binding by Chauret, Nathalie, Guay, Daniel, Li, Chun, Day, Stephen, Silva, José, Blouin, Marc, Ducharme, Yves, Yergey, James A., Nicoll-Griffith, Deborah A.

“…A detailed study directed towards metabolic stability optimization of the alkoxy substituents on the catechol moiety of CDP-840 is reported. Replacement of the…”
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Interspecies in vitro metabolism of the phosphodiesterase-4 (PDE4) inhibitor L-454,560 by Bateman, Kevin P., Trimble, Laird, Chauret, Nathalie, Silva, Jose, Day, Stephen, Macdonald, Dwight, Dube, Daniel, Gallant, Michel, Mastracchio, Anthony, Perrier, Helene, Girard, Yves, Nicoll-Griffith, Deborah

“…L‐454,560 is a potent phospodiesterase 4 (PDE4) inhibitor which was identified as a development candidate for the treatment of asthma and chronic obstructive…”
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Description of a 96-Well Plate Assay to Measure Cytochrome P4503A Inhibition in Human Liver Microsomes Using a Selective Fluorescent Probe by Chauret, Nathalie, Tremblay, Nathalie, Lackman, Rebecca L., Gauthier, Jacques-Yves, Silva, José M., Marois, Jean, Yergey, James A., Nicoll-Griffith, Deborah A.

“…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…”
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DESIGN OF THE LANDMARK CALM-1 AND CALM-2 PHASE 3 CLINICAL TRIALS OF CAMLIPIXANT IN REFRACTORY CHRONIC COUGH by SMITH, JACKY, SMITH, STEVEN G, IYER, VIVEK, SATIA, IMRAN, CHAURET, NATHALIE, HARVEY, LAURENT, YANG, RONGHUA, GARIN, MARGARET, BONUCCELLI, CATHERINE

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Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists by BELLEY, Michel, GALLANT, Michel, TREMBLAY, Nathalie, LAMONTAGNE, Sonia, CARRIERE, Marie-Claude, DENIS, Danielle, GREIG, Gillian M, SLIPETZ, Deborah, METTERS, Kathleen M, GORDON, Robert, CHI CHUNG CHAN, ZAMBONI, Robert J, ROY, Bruno, HOUDE, Karine, LACHANCE, Nicolas, LABELLE, Marc, TRIMBLE, Laird A, CHAURET, Nathalie, CHUN LI, SAWYER, Nicole

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The Use of 3-[2-(N,N-Diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin (AMMC) as a Specific CYP2D6 Probe in Human Liver Microsomes by CHAURET, Nathalie, DOBBS, Barry, LACKMAN, Rebecca L, BATEMAN, Kevin, NICOLL-GRIFFITH, Deborah A, STRESSER, David M, ACKERMANN, Joseph M, TURNER, Stephanie D, MILLER, Vaughn P, CRESPI, Charles L

“…Recently, a novel nonfluorescent probe 3-[2-( N , N -diethyl- N -methylammonium)-ethyl]-7-methoxy-4-methylcoumarin (AMMC), which produces a fluorescent…”
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Erratum to “Evaluation of human hepatocyte incubation as a new tool for metabolism study of androstenedione and norandrostenedione in a doping control perspective”: [J. Chromatogr. B. 780 (2002) 145–153] by Lévesque, Jean-François, Gaudreault, Mireille, Houle, Robert, Chauret, Nathalie

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USE OF A BENZYLOXY-SUBSTITUTED LACTONE CYCLOOXYGENASE-2 INHIBITOR AS A SELECTIVE FLUORESCENT PROBE FOR CYP3A ACTIVITY IN PRIMARY CULTURED RAT AND HUMAN HEPATOCYTES by Nicoll-Griffith, Deborah A., Chauret, Nathalie, Houle, Robert, Day, Stephen H., D'Antoni, Michelle, Silva, José M.

“…The benzyloxy-substituted lactone cyclooxygenase-2 inhibitor DFB [3-[(3,4-difluorobenzyl)oxy]-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2(5 H )-one] is…”
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Investigation of the in Vitro Metabolism Profile of a Phosphodiesterase-IV Inhibitor, CDP-840: Leading to Structural Optimization by Li, C, Chauret, N, Trimble, L A, Nicoll-Griffith, D A, Silva, J M, MacDonald, D, Perrier, H, Yergey, J A, Parton, T, Alexander, R P, Warrellow, G J

“…CDP-840 is a selective and potent phosphodiesterase type IV inhibitor, whose in vitro metabolism profile was first investigated using liver microsomes from…”
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Dioxabicyclooctanyl Naphthalenenitriles as Nonredox 5-Lipoxygenase Inhibitors:  Structure−Activity Relationship Study Directed toward the Improvement of Metabolic Stability by Delorme, Daniel, Ducharme, Yves, Brideau, Christine, Chan, Chi-Chung, Chauret, Nathalie, Desmarais, Sylvie, Dubé, Daniel, Falgueyret, Jean-Pierre, Fortin, Réjean, Guay, Jocelyne, Hamel, Pierre, Jones, Tom R, Lépine, Carole, Li, Chun, McAuliffe, Malia, McFarlane, Cyril S, Nicoll-Griffith, Deborah A, Riendeau, Denis, Yergey, James A, Girard, Yves

“…Naphthalenic lignan lactone 3a (L-702,539), a potent and selective 5-lipoxygenase (5-LO) inhibitor, is extensively metabolized at two different sites:  the…”
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In Vitro Metabolism of the COX-2 Inhibitor DFU, Including a Novel Glutathione Adduct Rearomatization by Yergey, J A, Trimble, L A, Silva, J, Chauret, N, Li, C, Therien, M, Grimm, E, Nicoll-Griffith, D A

“…The metabolic profile of DFU [5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methylsulphonyl)phenyl-2(5 H )-furanone], a potent and selective COX-2 inhibitor, was…”
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