S
Stephen Robert Fletcher
Researcher at Merck & Co.
Publications - 66
Citations - 1936
Stephen Robert Fletcher is an academic researcher from Merck & Co.. The author has contributed to research in topics: GABAA receptor & Receptor. The author has an hindex of 23, co-authored 66 publications receiving 1812 citations. Previous affiliations of Stephen Robert Fletcher include Merck Sharp & Dohme Federal Credit Union & Galápagos NV.
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Journal ArticleDOI
Preclinical Characterization of GLPG0634, a Selective Inhibitor of JAK1, for the Treatment of Inflammatory Diseases
Luc Juliaan Corina Van Rompaey,R Galien,Ellen van der Aar,Philippe Clément-Lacroix,Luc Nelles,Bart Smets,L. Lepescheux,Thierry Christophe,Katja Conrath,Nick Vandeghinste,Béatrice Vayssière,Steve De Vos,Stephen Robert Fletcher,Reginald Brys,Gerben van ’t Klooster,Jean Feyen,Christel Jeanne Marie Menet +16 more
TL;DR: Oral dosing of GLPG0634 in a therapeutic set-up in a collagen-induced arthritis model in rodents resulted in a significant dose-dependent reduction of the disease progression, and this compound is a promising novel therapeutic with potential for oral treatment of rheumatoid arthritis and possibly other immune-inflammatory diseases.
Journal ArticleDOI
[ 3 H]L-655,708, a Novel Ligand Selective for the Benzodiazepine Site of GABA A Receptors which Contain the α5 Subunit
K Quirk,Peter Blurton,Stephen Robert Fletcher,Paul D. Leeson,F. Tang,D. Mellilo,C I Ragan,Ruth M. McKernan +7 more
TL;DR: It is concluded that [3H]L-655,708 is the first radioligand to date which is selective for any BZ2 subtype of the GABAA receptor and should provide a valuable tool for elucidating the structure and function of the alpha 5-containing GabAA receptor subtype.
Journal ArticleDOI
Total Synthesis and Determination of the Absolute Configuration of Epibatidine
Stephen Robert Fletcher,Raymond Baker,Mark Stuart Chambers,Richard H. Herbert,Sarah Christine Hobbs,Steven R. Thomas,Hugh M. Verrier,Alan P. Watt,Richard G. Ball +8 more
TL;DR: In this paper, the synthesis of (+)- and (-)-epibatidine (exo-2-(2-chloropyridin-5-yl)-7-azabicyclo[2.2.1]heptane) via reaction of 5-lithio-2-loropyridine with (+)-and (-)-N-BOC-7-AZA-1-one is described.
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Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634
Christel Jeanne Marie Menet,Stephen Robert Fletcher,Guy Van Lommen,Raphael Geney,Javier Blanc,Koen Kurt Smits,Nolwenn Jouannigot,Pierre Deprez,Ellen van der Aar,Philippe Clément-Lacroix,L. Lepescheux,R Galien,Béatrice Vayssière,Luc Nelles,Thierry Christophe,Reginald Brys,Muriel Uhring,Fabrice Ciesielski,Luc Juliaan Corina Van Rompaey +18 more
TL;DR: Optimize within this chemical series led to identification of GLPG0634 (65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development for RA and phase 2A development for Crohn's disease (CD).
Journal ArticleDOI
Mechanism of inositol monophosphatase, the putative target of lithium therapy
Scott J. Pollack,John R. Atack,M.R. Knowles,George McAllister,C I Ragan,R. Baker,Stephen Robert Fletcher,Leslie L. Iversen,Howard B. Broughton +8 more
TL;DR: Model, kinetic, and mutagenesis studies on the enzyme reveal the requirement for two metal ions in the catalytic mechanism, and a two-metal mechanism is reported, consistent with the reduced catalytic activity observed with substrate analogues lacking the 6-OH.