Search Results - "FRIESEN, Richard W"

Microsomal Prostaglandin E2 Synthase-1 (mPGES-1): A Novel Anti-Inflammatory Therapeutic Target by Friesen, Richard W, Mancini, Joseph A

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MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation by Xu, Daigen, Rowland, Steven E, Clark, Patsy, Giroux, André, Côté, Bernard, Guiral, Sébastien, Salem, Myriam, Ducharme, Yves, Friesen, Richard W, Méthot, Nathalie, Mancini, Joseph, Audoly, Laurent, Riendeau, Denis

“…Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E(2) (PGE(2)) synthase in the cyclooxygenase pathway. Inhibitors of mPGES-1 may…”
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Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886 by RIENDEAU, Denis, ASPIOTIS, Renee, RUBIN, Joel, FRIESEN, Richard W, ETHIER, Diane, GAREAU, Yves, GRIMM, Erich L, GUAY, Jocelyne, GUIRAL, Sébastien, JUTEAU, Hélène, MANCINI, Joseph A, METHOT, Nathalie

“…A series of potent and selective inhibitors of the inducible microsomal PGE2 synthase (mPGES-1) has been developed based on the indole FLAP inhibitor MK-886…”
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Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors by Giroux, André, Boulet, Louise, Brideau, Christine, Chau, Anh, Claveau, David, Côté, Bernard, Ethier, Diane, Frenette, Richard, Gagnon, Marc, Guay, Jocelyne, Guiral, Sébastien, Mancini, Joseph, Martins, Evelyn, Massé, Frédéric, Méthot, Nathalie, Riendeau, Denis, Rubin, Joel, Xu, Daigen, Yu, Hongping, Ducharme, Yves, Friesen, Richard W.

“…Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective, and orally active mPGES-1 inhibitors. Phenanthrene imidazoles 26 and 44 have…”
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The Discovery of Setileuton, a Potent and Selective 5-Lipoxygenase Inhibitor by Ducharme, Yves, Blouin, Marc, Brideau, Christine, Châteauneuf, Anne, Gareau, Yves, Grimm, Erich L, Juteau, Hélène, Laliberté, Sébastien, MacKay, Bruce, Massé, Frédéric, Ouellet, Marc, Salem, Myriam, Styhler, Angela, Friesen, Richard W

“…The discovery of novel and selective inhibitors of human 5-lipoxygenase (5-LO) is described. These compounds are potent, orally bioavailable, and active at…”
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Dynamic activation of cystic fibrosis transmembrane conductance regulator by type 3 and type 4D phosphodiesterase inhibitors by Liu, Susana, Veilleux, Alain, Zhang, Lei, Young, Andrew, Kwok, Evonne, Laliberté, France, Chung, Christine, Tota, Michael R, Dubé, Daniel, Friesen, Richard W, Huang, Zheng

“…The diseases of cystic fibrosis, chronic obstructive pulmonary disease (COPD), and chronic bronchitis are characterized by mucus-congested and inflamed…”
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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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Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors by Côté, Bernard, Boulet, Louise, Brideau, Christine, Claveau, David, Ethier, Diane, Frenette, Richard, Gagnon, Marc, Giroux, André, Guay, Jocelyne, Guiral, Sébastien, Mancini, Joseph, Martins, Evelyn, Massé, Frédéric, Méthot, Nathalie, Riendeau, Denis, Rubin, Joel, Xu, Daigen, Yu, Hongping, Ducharme, Yves, Friesen, Richard W.

“…Phenanthrene imidazole 3 has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor. Phenanthrene imidazole 3 (MF63) has been…”
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On the controlled oxidative coupling of glycals: a new strategy for the rapid assembly of oligosaccharides by Friesen, Richard W, Danishefsky, Samuel J

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Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment by Gallant, Michel, Aspiotis, Renee, Day, Stephen, Dias, Rebecca, Dubé, Daniel, Dubé, Laurence, Friesen, Richard W., Girard, Mario, Guay, Daniel, Hamel, Pierre, Huang, Zheng, Lacombe, Patrick, Laliberté, Sebastien, Lévesque, Jean-François, Liu, Susana, Macdonald, Dwight, Mancini, Joseph, Nicholson, Donald W., Styhler, Angela, Townson, Karen, Waters, Kerry, Young, Robert N., Girard, Yves

“…The structure–activity relationship of a novel series of 8-biarylnaphthyridinones acting as type 4 phosphodiesterase (PDE4) inhibitors for the treatment of…”
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Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1 by WU, Tom Y. H, JUTEAU, Hélène, BRIDEAU, Christine, DUCHARME, Yves, FRIESEN, Richard W, GUIRAL, Sébastien, DUFRESNE, Lynn, POIRIER, Hugo, SALEM, Myriam, RIENDEAU, Denis, MANCINI, Joseph

“…Microsomal prostaglandin E(2) synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening…”
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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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Trisubstituted ureas as potent and selective mPGES-1 inhibitors by Chiasson, Jean-François, Boulet, Louise, Brideau, Christine, Chau, Anh, Claveau, David, Côté, Bernard, Ethier, Diane, Giroux, André, Guay, Jocelyne, Guiral, Sébastien, Mancini, Joseph, Massé, Frédéric, Méthot, Nathalie, Riendeau, Denis, Roy, Patrick, Rubin, Joel, Xu, Daigen, Yu, Hongping, Ducharme, Yves, Friesen, Richard W.

“…A novel series of trisubstituted ureas has been identified as potent and selective mPGES-1 inhibitors. These compounds are selective over other prostanoid…”
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Optimization and structure–activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor by Guay, Daniel, Boulet, Louise, Friesen, Richard W., Girard, Mario, Hamel, Pierre, Huang, Zheng, Laliberté, France, Laliberté, Sébastien, Mancini, Joseph A., Muise, Eric, Pon, Doug, Styhler, Angela

“…Discovery of the potent and orally active PDE4 inhibitors 18 and 20 (PDE4A IC 50 = 6 and 7 nM; HWB IC 50 = 0.12 and 0.18 μM) is reported. A SAR study of a…”
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Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP₄ receptor by Burch, Jason D, Farand, Julie, Colucci, John, Sturino, Claudio, Ducharme, Yves, Friesen, Richard W, Lévesque, Jean-François, Gagné, Sébastien, Wrona, Mark, Therien, Alex G, Mathieu, Marie-Claude, Denis, Danielle, Vigneault, Erika, Xu, Daigen, Clark, Patsy, Rowland, Steve, Han, Yongxin

“…Two new series of EP₄ antagonists based on naphthalene/quinoline scaffolds have been identified as part of our on-going efforts to develop treatments for…”
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The C3a receptor antagonist SB 290157 has agonist activity by Mathieu, Marie-Claude, Sawyer, Nicole, Greig, Gillian M., Hamel, Martine, Kargman, Stacia, Ducharme, Yves, Lau, Cheuk K., Friesen, Richard W., O’Neill, Gary P., Gervais, Francois G., Therien, Alex G.

“…The anaphylatoxin C3a is an important immune regulator with a number of distinct functions in both innate and adaptive immunity. Many of these roles have been…”
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The preparation of C-arylglycals. The palladium-catalyzed coupling of 3,4,6-tri-O-(tert-butyldimethylsilyl)-1-(tributylstannyl)-D-glucal and aryl bromides by Friesen, Richard W, Sturino, Claudio F

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Observation of .alpha.-silyl carbanions in the metalation of 3,4,6-tri-O-(tert-butyldimethylsilyl)-D-glucal by Friesen, Richard W, Sturino, Claudio F, Daljeet, Anand K, Kolaczewska, Aleksandra

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Catalytic Inactivation of Protein Tyrosine Phosphatase CD45 and Protein Tyrosine Phosphatase 1B by Polyaromatic Quinones by Wang, Qingping, Dubé, Daniel, Friesen, Richard W, LeRiche, Tammy G, Bateman, Kevin P, Trimble, Laird, Sanghara, Joe, Pollex, Rebecca, Ramachandran, Chidambaram, Gresser, Michael J, Huang, Zheng

“…Polyaromatic quinones, such as the environmental pollutants 9,10-phenanthrenediones, elicit a wide range of responses including growth inhibition, immune…”
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Stereoselective oxidative spiroketalization of a C-arylglucal derived from palladium-catalyzed coupling. Synthesis of the C-arylglucoside spiroketal nucleus of the papulacandins by Friesen, Richard W, Sturino, Claudio F

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