Patrick Roy
Merck & Co.
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Publication
Featured researches published by Patrick Roy.
Bioorganic & Medicinal Chemistry Letters | 1996
W.C. Black; Chris Bayly; Michel Belley; Chi-Chung Chan; S. Charleson; Danielle Denis; Jacques-Yves Gauthier; Robert Gordon; Daniel Guay; Stacia Kargman; Cheuk K. Lau; Yves Leblanc; Joseph A. Mancini; Marc Ouellet; David Percival; Patrick Roy; Kathryn Skorey; Philip Tagari; Philip J. Vickers; Elizabeth Wong; Lijing Xu; Petpiboon Prasit
Abstract A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the acetic acid side chain. These compounds show anti-inflammatory activity in rats with no evidence of GI toxicity, even at high doses.
Bioorganic & Medicinal Chemistry Letters | 1997
Michel Therien; Christine Brideau; Chi-Chung Chan; Wanda Cromlish; Jacques Yves Gauthier; Robert Gordon; Gillian Greig; Stacia Kargman; Cheuk K. Lau; Yves Leblanc; Chun-Sing Li; Gary P. O'Neill; Denis Riendeau; Patrick Roy; Zhaoyin Wang; Lijing Xu; Petpiboon Prasit
Abstract A series of 5,6-diarylimidazo[2.1-b]thiazole compounds were prepared and their inhibitory potencies against COX-2 and Cox-1 enzymes were measured. This led to the identification of L-766,112 as a potent, orally active and selective inhibitor of the COX-2 enzyme.
Bioorganic & Medicinal Chemistry Letters | 1997
Patrick Roy; Yves Leblanc; Richard G. Ball; Christine Brideau; Chi-Chung Chan; Nathalie Chauret; Wanda Cromlish; Diane Ethier; Jacques-Yves Gauthier; Robert Gordon; Gillian Greig; Jocelyne Guay; Stacia Kargman; Cheuk K. Lau; Gary P. O'Neill; José M. Silva; Michel Therien; C. van Staden; Elizabeth Wong; Lijing Xu; Petpiboon Prasit
A series of 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles was prepared for evaluation of potency and selectivity against human COX-1 and COX-2 enzymes. This lead to the discovery of L-768,277, a potent and selective COX-2 inhibitor that also demonstrated good in vivo activity.
Bioorganic & Medicinal Chemistry Letters | 1999
Yves Leblanc; Patrick Roy; Susan Boyce; Christine Brideau; Chi-Chung Chan; S. Charleson; Robert Gordon; Erich L. Grimm; Jocelyne Guay; Serge Leger; Chun-Sing Li; Denis Riendeau; Denise M. Visco; Zhaoyin Wang; J.K. Webb; Lijing Xu; Petpiboon Prasit
Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanon e), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied.
Bioorganic & Medicinal Chemistry Letters | 2000
Deborah A. Nicoll-Griffith; James A. Yergey; Laird A. Trimble; José M. Silva; Chun Li; Nathalie Chauret; Jacques Yves Gauthier; Erich L. Grimm; Serge Leger; Patrick Roy; Michel Therien; Zhaoyin Wang; Peppi Prasit; Robert Zamboni; Robert N. Young; Christine Brideau; Chi-Chung Chan; Joseph A. Mancini; Denis Riendeau
Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assay, none of the known human metabolites of rofecoxib inhibits COX-1 nor contributes significantly to the inhibition of COX-2.
Bioorganic & Medicinal Chemistry Letters | 1996
Yves Leblanc; W.C. Black; Chi-Chung Chan; S. Charleson; Daniel Delorme; Danielle Denis; Jacques-Yves Gauthier; Erich L. Grimm; Robert Gordon; Daniel Guay; Pierre Hamel; Stacia Kargman; Cheuk K. Lau; Joseph A. Mancini; Marc Ouellet; David Percival; Patrick Roy; Kathryn Skorey; Philip Tagari; Philip J. Vickers; Elizabeth Wong; Lijing Xu; Petpiboon Prasit
Abstract Both enantiomers of L-761,000 were prepared and evaluated for their cyclooxygenase activities.
Bioorganic & Medicinal Chemistry Letters | 2008
Christian Beaulieu; Daniel Guay; Zhaoyin Wang; Yves Leblanc; Patrick Roy; Claude Dufresne; Robert Zamboni; Carl Berthelette; Stephen Day; Nancy N. Tsou; Danielle Denis; Gillian Greig; Marie-Claude Mathieu; Gary O’Neill
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 study to the identification of potent and selective antagonists is presented. Selective DP1 antagonists with high potency and selectivity were prepared. Of particular interest is the DP1 antagonist 26 with a K(i) value of 1 nM for the DP1 receptor and an IC(50) value of 4.6 nM in a DP1 functional assay for the inhibition of the PGD(2) induced cAMP production in platelet rich plasma (PRP).
Bioorganic & Medicinal Chemistry Letters | 1992
Marc Labelle; Petpiboon Prasit; Michel Belley; Marc Blouin; E. Champion; L. Charette; J.G. DeLuca; Claude Dufresne; Richard Frenette; Jacques-Yves Gauthier; Erich L. Grimm; S.J. Grossman; Daniel Guay; E.G. Herold; Thomas R. Jones; Cheuk K. Lau; Yves Leblanc; Serge Leger; A. Lord; M. McAuliffe; C. McFarlane; Paul Masson; Kathleen M. Metters; Nathalie Ouimet; D.H. Patrick; Helene Perrier; C.B. Pickett; H. Piechuta; Patrick Roy; H. Williams
Abstract A new, potent, orally active leukotriene D 4 receptor antagonist has been discovered. The structure -activity relationship leading to L-695,499 is described.
Bioorganic & Medicinal Chemistry Letters | 2011
Jean-François Chiasson; Louise Boulet; Christine Brideau; Anh Chau; David Claveau; Bernard Cote; Diane Ethier; André Giroux; Jocelyne Guay; Sébastien Guiral; Joseph A. Mancini; Frédéric Massé; Nathalie Méthot; Denis Riendeau; Patrick Roy; Joel Rubin; Daigen Xu; Hongping Yu; Yves Ducharme; Richard W. Friesen
A novel series of trisubstituted ureas has been identified as potent and selective mPGES-1 inhibitors. These compounds are selective over other prostanoid enzymes such as PGF synthase and TX synthase. This series of inhibitors was developed by lead optimization of a hit from an internal HTS campaign. Lead compound 42 is potent in A549 cell assay (IC(50) of 0.34 μM) and in human whole blood assay (IC(50) of 2.1 μM). An efficient and versatile one-pot strategy for the formation of ureas, involving a reductive amination, was developed to generate these inhibitors.
Bioorganic & Medicinal Chemistry Letters | 2002
Yves Leblanc; Patrick Roy; Zhaoyin Wang; Chun Sing Li; Nathalie Chauret; Deborah A. Nicoll-Griffith; José M. Silva; Yves Aubin; James A. Yergey; Chi-Chung Chan; Denis Riendeau; Christine Brideau; Robert Gordon; Lijing Xu; J.K. Webb; Denise M. Visco; Petpiboon Prasit
The COX-2 inhibitor DFP [5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone] was found to have a long half-life in humans. Analogues have been characterized in order to optimize pharmacokinetics. This has lead to the discovery of 5(S)-(5-ethyl-5-methyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone analogue 11 a potent and selective COX-2 inhibitor which is metabolized to a greater extent than DFP upon incubation with rat and human hepatocytes, suggesting a shorter half-life in humans.