Search Results - "MELLON, Christophe"

S1331 Colonic Bioactivation and Potent TNFa Inhibition of PALI-2108 in Human ex-vivo Studies: A Promising PDE4 Inhibitor Prodrug for the Oral Treatment of Ulcerative Colitis by Bernard, Joie, Rieder, Florian, Mellon, Christophe, Jones, Mitchell

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Reversible Cysteine Protease Inhibitors Show Promise for a Chagas Disease Cure by NDAO, Momar, BEAULIEU, Christian, BLACK, W. Cameron, ISABEL, Elise, VASQUEZ-CAMARGO, Fabio, NATH-CHOWDHURY, Milli, MASSE, Frédéric, MELLON, Christophe, METHOT, Nathalie, NICOLL-GRIFFITH, Deborah A

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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LOCAL BIOACTIVATION AND EFFICACY OF PALI-2108: A PROMISING PDE4 INHIBITOR PRODRUG FOR ULCERATIVE COLITIS TREATMENT by Bernard, Joie, Mellon, Christophe, Ranger, Maxime, Côté, Bernard, Jones, Mitchell

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TLN-05220, TLN-05223, new Echinosporamicin-type antibiotics, and proposed revision of the structure of bravomicins by Banskota, Arjun H, Aouidate, Mustapha, Sørensen, Dan, Ibrahim, Ashraf, Piraee, Mahmood, Zazopoulos, Emmanuel, Alarco, Anne-Marie, Gourdeau, Henriette, Mellon, Christophe, Farnet, Chris M, Falardeau, Pierre, McAlpine, James B

“…The deposited strain of the hazimicin producer, Micromonospora echinospora ssp . challisensis NRRL 12255 has considerable biosynthetic capabilities as revealed…”
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LOCAL BIOACTIVATION AND EFFICACY OF PALI-2108: A PROMISING PDE4 INHIBITOR PRODRUG FOR ULCERATIVE COLITIS TREATMENT by Bernard, Joie, Mellon, Christophe, Ranger, Maxime, Côté, Bernard, Jones, Mitchell

“…Phosphodiesterase-4 (PDE4) is a key enzyme in cAMP hydrolysis and is involved in various inflammatory and fibrotic diseases, such as ulcerative colitis (UC)…”
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Tu1740 LOCAL BIOACTIVATION AND EFFICACY OF PALI-2108: A PROMISING PDE4 INHIBITOR PRODRUG FOR ULCERATIVE COLITIS TREATMENT by Bernard, Joie, Rieder, Florian, Mellon, Christophe, Cote, Bernard, Jones, Mitchell L.

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Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease by Beaulieu, Christian, Isabel, Elise, Fortier, Angélique, Massé, Frédéric, Mellon, Christophe, Méthot, Nathalie, Ndao, Momar, Nicoll-Griffith, Deborah, Lee, Doris, Park, Hyeram, Black, W. Cameron

“…Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino…”
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Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: Cellular distribution in human leukocyte populations and evidence of diurnal modulation by Veilleux, Alain, Black, W. Cameron, Gauthier, Jacques Yves, Mellon, Christophe, Percival, M. David, Tawa, Paul, Falgueyret, Jean-Pierre

“…Using the cell-permeable, radioiodinated, irreversible inhibitor BIL-DMK, we probed active cysteine cathepsins in blood. Incubation of the probe in human whole…”
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Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases by Gallant, Michel, Beaulieu, Christian, Berthelette, Carl, Colucci, John, Crackower, Michael A., Dalton, Chad, Denis, Danielle, Ducharme, Yves, Friesen, Richard W., Guay, Daniel, Gervais, François G., Hamel, Martine, Houle, Robert, Krawczyk, Connie M., Kosjek, Birgit, Lau, Stephen, Leblanc, Yves, Lee, Ernest E., Levesque, Jean-François, Mellon, Christophe, Molinaro, Carmela, Mullet, Wayne, O’Neill, Gary P., O’Shea, Paul, Sawyer, Nicole, Sillaots, Susan, Simard, Daniel, Slipetz, Deborah, Stocco, Rino, Sørensen, Dan, Truong, Vouy Linh, Wong, Elizabeth, Wu, Jin, Zaghdane, Helmi, Wang, Zhaoyin

“…In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two…”
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The Discovery of 4-{1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic Acid (MK-2894), A Potent and Selective Prostaglandin E 2 Subtype 4 Receptor Antagonist by Blouin, Marc, Han, Yongxin, Burch, Jason, Farand, Julie, Mellon, Christophe, Gaudreault, Mireille, Wrona, Mark, Lévesque, Jean-François, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Vigneault, Erika, Therien, Alex, Clark, Patsy, Rowland, Steve, Xu, Daigen, O’Neill, Gary, Ducharme, Yves, Friesen, Rick

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The Discovery of 4-{1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic Acid (MK-2894), A Potent and Selective Prostaglandin E2 Subtype 4 Receptor Antagonist by Blouin, Marc, Han, Yongxin, Burch, Jason, Farand, Julie, Mellon, Christophe, Gaudreault, Mireille, Wrona, Mark, Lévesque, Jean-François, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Vigneault, Erika, Therien, Alex, Clark, Patsy, Rowland, Steve, Xu, Daigen, O’Neill, Gary, Ducharme, Yves, Friesen, Rick

“…The discovery of highly potent and selective second generation EP4 antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic…”
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3,4-Diarylpiperidines as potent renin inhibitors by Lacombe, Patrick, Arbour, Mélissa, Aspiotis, Renée, Cauchon, Elizabeth, Chen, Austin, Dubé, Daniel, Falgueyret, Jean-Pierre, Fournier, Pierre-André, Gallant, Michel, Grimm, Erich, Han, Yongxin, Juteau, Hélène, Liu, Suzanna, Mellon, Christophe, Ramtohul, Yeeman, Simard, Daniel, St-Jacques, René, Tsui, Gavin Chit

“…The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38…”
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Difluoroethylamines as an amide isostere in inhibitors of cathepsin K by Isabel, Elise, Mellon, Christophe, Boyd, Michael J., Chauret, Nathalie, Deschênes, Denis, Desmarais, Sylvie, Falgueyret, Jean-Pierre, Gauthier, Jacques Yves, Khougaz, Karine, Lau, Cheuk K., Léger, Serge, Levorse, Dorothy A., Li, Chun Sing, Massé, Frédéric, David Percival, M., Roy, Bruno, Scheigetz, John, Thérien, Michel, Truong, Vouy Linh, Wesolowski, Gregg, Young, Robert N., Zamboni, Robert, Cameron Black, W.

“…The trifluoroethylamine group found in cathepsin K inhibitors like odanacatib can be replaced by a difluoroethylamine group. This change increased the basicity…”
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Identification of a Nonbasic, Nitrile-Containing Cathepsin K Inhibitor (MK-1256) that is Efficacious in a Monkey Model of Osteoporosis by Robichaud, Jöel, Black, W. Cameron, Thérien, Michel, Paquet, Julie, Oballa, Renata M, Bayly, Christopher I, McKay, Daniel J, Wang, Qingping, Isabel, Elise, Léger, Serge, Mellon, Christophe, Kimmel, Donald B, Wesolowski, Gregg, Percival, M. David, Massé, Fréderic, Desmarais, Sylvie, Falgueyret, Jean-Pierre, Crane, Sheldon N

“…Herein, we report on the identification of nonbasic, potent, and highly selective, nitrile-containing cathepsin K (Cat K) inhibitors that are built on our…”
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The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor by Isabel, Elise, Bateman, Kevin P., Chauret, Nathalie, Cromlish, Wanda, Desmarais, Sylvie, Duong, Le T., Falgueyret, Jean-Pierre, Gauthier, Jacques Yves, Lamontagne, Sonia, Lau, Cheuk K., Léger, Serge, LeRiche, Tammy, Lévesque, Jean-François, Li, Chun Sing, Massé, Frédéric, McKay, Daniel J., Mellon, Christophe, Nicoll-Griffith, Deborah A., Oballa, Renata M., Percival, M. David, Riendeau, Denis, Robichaud, Joël, Rodan, Gideon A., Rodan, Sevgi B., Seto, Carmai, Thérien, Michel, Truong, Vouy Linh, Wesolowski, Gregg, Young, Robert N., Zamboni, Robert, Black, W. Cameron

“…MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat…”
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An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells by Falgueyret, Jean-Pierre, Black, W. Cameron, Cromlish, Wanda, Desmarais, Sylvie, Lamontagne, Sonia, Mellon, Christophe, Riendeau, Denis, Rodan, Sevgi, Tawa, Paul, Wesolowski, Gregg, Bass, Kathryn E., Venkatraman, Shankar, Percival, M. David

“…We describe a novel diazomethylketone-containing irreversible inhibitor (BIL-DMK) which is specific for a subset of pharmaceutically important cysteine…”
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Discovery of Mix-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases by GALLANT, Michel, BEAULIEU, Christian, GERVAIS, François G, HAMEL, Martine, HOULE, Robert, KRAWCZYK, Connie M, KOSJEK, Birgit, LAU, Stephen, LEBLANC, Yves, LEE, Ernest E, LEVESQUE, Jean-François, MELLON, Christophe, BERTHELETTE, Carl, MOLINARO, Carmela, MULLET, Wayne, O'NEILL, Gary P, O'SHEA, Paul, SAWYER, Nicole, SILLAOTS, Susan, SIMARD, Daniel, SLIPETZ, Deborah, STOCCO, Rino, SØRENSEN, Dan, COLUCCI, John, VOUY LINH TRUONG, WONG, Elizabeth, JIN WU, ZAGHDANE, Helmi, ZHAOYIN WANG, CRACKOWER, Michael A, DALTON, Chad, DENIS, Danielle, DUCHARME, Yves, FRIESEN, Richard W, GUAY, Daniel

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Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors by Robichaud, Joël, Bayly, Christopher, Oballa, Renata, Prasit, Peppi, Mellon, Christophe, Falgueyret, Jean-Pierre, David Percival, M, Wesolowski, Gregg, Rodan, Sevgi B

“…Modelling studies suggested that the introduction of a NH linker between the P3 aryl and P2 leucinamide moieties of our previously reported inhibitor 2 would…”
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Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones by Isabel, Elise, Aspiotis, Renee, Black, W. Cameron, Colucci, John, Fortin, Réjean, Giroux, André, Grimm, Erich L., Han, Yongxin, Mellon, Christophe, Nicholson, Donald W., Rasper, Dita M., Renaud, Johanne, Roy, Sophie, Tam, John, Tawa, Paul, Vaillancourt, John P., Xanthoudakis, Steven, Zamboni, Robert J.

“…Caspase-3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact on the treatment of several degenerative…”
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Enantioselective synthesis of α,α-disubstituted-α-amino acids by a sequential nucleophilic addition to nitriles by Charette, AndréB, Mellon, Christophe

“…The sequential addition of two different nucleophiles to a tartaric acid-derived nitrile produced carbinamines. The adducts from chelation-controlled addition…”
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