J
Jean-Pierre Falgueyret
Researcher at Merck & Co.
Publications - 75
Citations - 4112
Jean-Pierre Falgueyret is an academic researcher from Merck & Co.. The author has contributed to research in topics: Cathepsin K & Arachidonic acid. The author has an hindex of 32, co-authored 74 publications receiving 3923 citations. Previous affiliations of Jean-Pierre Falgueyret include United States Military Academy.
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Journal Article
Etoricoxib (MK-0663): Preclinical Profile and Comparison with Other Agents That Selectively Inhibit Cyclooxygenase-2
Denis Riendeau,M.D. Percival,Christine Brideau,Stella Charleson,Daniel Dube,Diane Ethier,Jean-Pierre Falgueyret,Richard Friesen,R. Gordon,Gillian Greig,Jocelyne Guay,Joseph A. Mancini,Marc Ouellet,E. Wong,Lijing Xu,Susan Boyce,Denise M. Visco,Yves Girard,Petpiboon Prasit,Robert Zamboni,Ian W. Rodger,Michael J. Gresser,Anthony W. Ford-Hutchinson,Robert N. Young,Chi-Chung Chan +24 more
TL;DR: Etoricoxib represents a novel agent that selectively inhibits COX-2 with 106-fold selectivity in human whole blood assays in vitro and with the lowest potency of inhibition ofCOX-1 compared with other reported selective agents.
Journal ArticleDOI
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Jacques Yves Gauthier,Nathalie Chauret,Wanda Cromlish,Sylvie Desmarais,Le T. Duong,Jean-Pierre Falgueyret,Donald B. Kimmel,Sonia Lamontagne,Serge Leger,Tammy LeRiche,Chun Sing Li,Frédéric Massé,Daniel J. McKay,Deborah A. Nicoll-Griffith,Renata Oballa,James T. Palmer,M. David Percival,Denis Riendeau,Joel Robichaud,Gideon A. Rodan,Sevgi B. Rodan,Carmai Seto,Michel Therien,Vouy-Linh Truong,Michael C. Venuti,Gregg Wesolowski,Robert N. Young,Robert Zamboni,W. Cameron Black +28 more
TL;DR: 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 and was more selective in whole cell assays than the published Cat K inhibitors balicatib and relac atib.
Journal ArticleDOI
Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor.
Denis Riendeau,M.D. Percival,Susan Boyce,Christine Brideau,Stella Charleson,Wanda Cromlish,Diane Ethier,Jillian F. Evans,Jean-Pierre Falgueyret,Anthony W. Ford-Hutchinson,R. Gordon,Gillian Greig,Michael J. Gresser,Jocelyne Guay,Stacia Kargman,Serge Leger,Joseph A. Mancini,Gary P. O'Neill,Marc Ouellet,Ian W. Rodger,Michael J. Therien,Zhaoyin Wang,J.K. Webb,E. Wong,Lijing Xu,Robert N. Young,Robert Zamboni,Petpiboon Prasit,Chi-Chung Chan +28 more
TL;DR: The time‐dependent inhibition by DFU was decreased by co‐incubation with arachidonic acid under non‐turnover conditions, consistent with reversible competitive inhibition at the COX active site.
Journal ArticleDOI
Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.
Daniel Dube,Marc Blouin,Christine Brideau,Chi-Chung Chan,Sylvie Desmarais,Diane Ethier,Jean-Pierre Falgueyret,Richard Friesen,Mario Girard,Yves Girard,Jocelyne Guay,Denis Riendeau,Philip Tagari,Robert N. Young +13 more
TL;DR: A series of novel substituted 2-cyanoquinolines have been synthesized and the structure activity relationships were evaluated with respect to their ability to inhibit the formation of leukotrienes via the 5-lipoxygenase enzyme.
Journal Article
Overexpression of human prostaglandin G/H synthase-1 and -2 by recombinant vaccinia virus: inhibition by nonsteroidal anti-inflammatory drugs and biosynthesis of 15-hydroxyeicosatetraenoic acid.
Gary P. O'Neill,J A Mancini,Stacia Kargman,J. Yergey,Matthew Y. W. Kwan,Jean-Pierre Falgueyret,Mark Abramovitz,Brian P. Kennedy,Marc Ouellet,Cromlish Wa +9 more
TL;DR: Human prostaglandin G/H synthase (hPGHS)-1 and hPGHS-2, key enzymes in the formation of prostanoids from arachidonic acid, were expressed at high levels in COS-7 cells using a T7 RNA polymerase/vaccinia virus expression system.