Search Results - "BERTHELETTE, Carl"

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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High-Sensitivity NanoLC−MS/MS Analysis of Urinary Desmosine and Isodesmosine by Boutin, Michel, Berthelette, Carl, Gervais, François G, Scholand, Mary-Beth, Hoidal, John, Leppert, Mark F, Bateman, Kevin P, Thibault, Pierre

“…Chronic obstructive pulmonary disease (COPD) is characterized by the degradation of elastin, the major insoluble protein of lung tissues. The degradation of…”
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Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: Discovery of MK-5286 by Li, Lianhai, Berthelette, Carl, Chateauneuf, Anne, Ouellet, Marc, Sturino, Claudio F., Wang, Zhaoyin

“…The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1…”
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Efficient Synthesis of Substituted Vinyl Ethers Using the Julia Olefination by Surprenant, Simon, Chan, Wing Yan, Berthelette, Carl

“…Julia olefination between α-alkoxy sulfones 2a−c and a wide variety of ketones or aldehydes afforded substituted vinyl ethers in 46−90% yields. Sulfones 2a−c…”
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A mild, efficient method for the synthesis of aromatic and aliphatic sulfonamides by Chan, Wing Yan, Berthelette, Carl

“…A two-step method was developed for the synthesis of aromatic and aliphatic sulfonamides from the corresponding sulfinates using…”
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Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold by BEAULIEU, Christian, GUAY, Daniel, DENIS, Danielle, GREIG, Gillian, MATHIEU, Marie-Claude, O'NEILL, Gary, ZHAOYIN WANG, LEBLANC, Yves, ROY, Patrick, DUFRESNE, Claude, ZAMBONI, Robert, BERTHELETTE, Carl, DAY, Stephen, TSOU, Nancy

“…A new series of indole-based antagonists of the PGD(2) receptor subtype 1 (DP1 receptor) was identified and the progress of the structure-activity relationship…”
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An expedient approach to E, Z-dienes using the Julia olefination by Charette, André B, Berthelette, Carl, St-Martin, David

“…New reaction conditions were developed for the synthesis of E, Z-dienes from α,β-unsaturated aldehydes and heteroarylsulfones using the Julia reaction. In most…”
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Practical [14C]-synthesis of molecules containing an acetic acid moiety: application to [14C]-labeled DP1 antagonists by Berthelette, Carl, Wang, Zhaoyin

“…Efficient carbon‐14 labeling of four potent and selective DP1 antagonists is reported. The synthetic sequence began with α‐hydroxylation, reduction of an…”
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Discovery of 4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl)amino]cyclopropyl}benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain by Colucci, John, Boyd, Michael, Berthelette, Carl, Chiasson, Jean-Francois, Wang, Zhaoyin, Ducharme, Yves, Friesen, Rick, Wrona, Mark, Levesque, Jean-Francois, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Therien, Alex G., Clarke, Patsy, Rowland, Steve, Xu, Daigen, Han, Yongxin

“…The discovery of a highly potent and selective EP4 antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and…”
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Identification of an indole series of prostaglandin D2 receptor antagonists by STURINO, Claudio F, LACHANCE, Nicolas, CAUCHON, Elizabeth, CARRIERE, Marie-Claude, DENIS, Danielle, GREIG, Gillian, KARGMAN, Stacia, LAMONTAGNE, Sonia, MATHIEU, Marie-Claude, SAWYER, Nicole, SLIPETZ, Deborah, O'NEILL, Gary, BOYD, Michael, ZHAOYIN WANG, ZAMBONI, Robert, METTERS, Kathleen M, YOUNG, Robert N, BERTHELETTE, Carl, LABELLE, Marc, LIANHAI LI, ROY, Bruno, SCHEIGETZ, John, TSOU, Nancy, BRIDEAU, Christine

“…A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP…”
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Asymmetric synthesis of diarylmethylamines: preparation of selective opioid delta receptor ligands by Delorme, Daniel, Berthelette, Carl, Lavoie, Rico, Roberts, Edward

“…Two different methods were used for the construction of optically active diarylmethylamines. Diastereoselective alkylation on an aldimine/oxazolidine 2a/ 2b…”
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Base-catalyzed deuterium and tritium labeling of aryl methyl sulfones by Scheigetz, John, Berthelette, Carl, Li, Chun, Zamboni, Robert J.

“…A method is presented for conveniently tritiating the aryl methyl sulfones of compounds identified as potent and selective inhibitors of human Cox‐2 and as DP…”
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The Synthesis of Phenylhydrazines from bis(2,2,2-Trichloroethyl) Azodicarboxylates and Electron-Rich Arenes by Dufresne, Claude, Leblanc, Yves, Berthelette, Carl, McCooeye, Chris

“…Phenylhydrazines are readily prepared in a two step sequences using electron rich arenes molecules and bis(2,2,2 trichloroethyl) azodicarboxylate (BTCEAD)…”
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Discovery of a Potent and Selective Prostaglandin D 2 Receptor Antagonist, [(3 R )-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.

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Stereoselective Synthesis of Z Alkenyl Halides via Julia Olefination by Lebrun, Marie-Eve, Le Marquand, Paul, Berthelette, Carl

“…Julia olefination between α-halomethyl sulfones and a variety of aldehydes afforded alkenyl halides in good to excellent yields with high E/Z…”
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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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Azaindoles as potent CRTH2 receptor antagonists by Simard, Daniel, Leblanc, Yves, Berthelette, Carl, Zaghdane, M. Helmi, Molinaro, Carmela, Wang, Zhaoyin, Gallant, Michel, Lau, Stephen, Thao, Trinh, Hamel, Martine, Stocco, Rino, Sawyer, Nicole, Sillaots, Susan, Gervais, Francois, Houle, Robert, Lévesque, Jean-François

“…A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal…”
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New indole amide derivatives as potent CRTH2 receptor antagonists by Zaghdane, Helmi, Boyd, Michael, Colucci, John, Simard, Daniel, Berthelette, Carl, Leblanc, Yves, Wang, Zhaoyin, Houle, Robert, Lévesque, Jean François, Molinaro, Carmela, Hamel, Martine, Stocco, Rino, Sawyer, Nicole, Sillaots, Susan, Gervais, François, Gallant, Michel

“…A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar…”
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Identification of prostaglandin D 2 receptor antagonists based on a tetrahydropyridoindole scaffold by Beaulieu, Christian, Guay, Daniel, Wang, Zhaoyin, Leblanc, Yves, Roy, Patrick, Dufresne, Claude, Zamboni, Robert, Berthelette, Carl, Day, Stephen, Tsou, Nancy, Denis, Danielle, Greig, Gillian, Mathieu, Marie-Claude, O’Neill, Gary

“…A new series of indole-based antagonists of the PGD 2 receptor subtype 1 (DP1 receptor) was identified and the progress of the structure–activity relationship…”
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