P
Pascal Savy
Researcher at Hoffmann-La Roche
Publications - 15
Citations - 274
Pascal Savy is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Triple helix & Oligonucleotide. The author has an hindex of 9, co-authored 15 publications receiving 254 citations. Previous affiliations of Pascal Savy include Centre national de la recherche scientifique & Institut de Chimie des Substances Naturelles.
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Journal ArticleDOI
Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.
Brian Safina,Stewart J. Baker,Matt Baumgardner,Paul M. Blaney,Bryan K. Chan,Yung-Hsiang Chen,Matthew W. Cartwright,Georgette Castanedo,Christine Chabot,Arnaud J. Cheguillaume,Paul Goldsmith,David Michael Goldstein,Bindu Goyal,Timothy Hancox,Raj K. Handa,Pravin Iyer,Jasmit Kaur,Rama K. Kondru,Jane R. Kenny,Krintel Sussie Lerche,Jun Li,John Lesnick,Matthew C. Lucas,Cristina Lewis,Sophie Mukadam,Jeremy Murray,Alan Nadin,Jim Nonomiya,Fernando Padilla,Wylie Solang Palmer,Jodie Pang,Neil Anthony Pegg,Steve Price,Karin Reif,Laurent Salphati,Pascal Savy,Eileen Mary Seward,Stephen J. Shuttleworth,Sukhjit Sohal,Zachary Kevin Sweeney,Suzanne Tay,Parcharee Tivitmahaisoon,Bohdan Waszkowycz,Binqing Wei,Qin Yue,Chenghong Zhang,Daniel P. Sutherlin +46 more
TL;DR: The discovery of novel, potent, and selective PI3Kδ inhibitors are reported and a structural hypothesis for isoform (α, β, γ) selectivity gained from interactions in the affinity pocket is described.
Journal ArticleDOI
Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta
Jeremy Murray,Zachary Kevin Sweeney,Bryan K. Chan,Mercedesz Balazs,Erin K. Bradley,Georgette Castanedo,Christine Chabot,David Chantry,Michael Flagella,David Michael Goldstein,Rama K. Kondru,John Lesnick,Jun Li,Matthew C. Lucas,Jim Nonomiya,Jodie Pang,Stephen Price,Laurent Salphati,Brian Safina,Pascal Savy,Eileen Mary Seward,Mark Ultsch,Daniel P. Sutherlin +22 more
TL;DR: A series of potent and selective benzimidazole-based inhibitors of PI3Kδ are identified using a structure-based design approach and the pharmacokinetic properties and the ability of compound 5 to inhibit the function of B-cells in vivo are described.
Journal ArticleDOI
Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions
Robert Heald,Philip Stephen Jackson,Pascal Savy,Mark Jones,Emanuela Gancia,Brenda Burton,Richard Newman,Jason Boggs,Emily Chan,Jocelyn Chan,Edna F. Choo,Mark Merchant,Patrick J. Rudewicz,Mark Ultsch,Christian Wiesmann,Qin Yue,Marcia Belvin,Steve Price +17 more
TL;DR: Using structure-based design, two novel series of highly potent biaryl amine mitogen-activated protein kinase kinase (MEK) inhibitors have been discovered and the most potent compound, 1 (G-894), is orally active in in vivo pharmacodynamic and tumor xenograft models.
Journal ArticleDOI
Bicyclic anti-VZV nucleosides: Thieno analogues retain full antiviral activity.
Andrea Brancale,Christopher McGuigan,Berthe Algain,Pascal Savy,Rachid Benhida,Jean‐Louis Fourrey,Graciela Andrei,Robert Snoeck,Erik De Clercq,Jan Balzarini +9 more
TL;DR: Thieno analogues of the potent and selective furo-pyrimidine anti-VZV nucleoside family are reported and retain full antiviral potency in comparison to the furo parent.
Journal ArticleDOI
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Sue Cramp,Hazel Joan Dyke,Christopher Higgs,David E. Clark,Gill Matthew Iain Andrew,Pascal Savy,Neil Jennings,Steve Price,Peter Lockey,Dennis Norman,Soraya S. Porres,Francis Xavier Wilson,Alison Jones,Nigel Ramsden,Raffaella Mangano,Dan Leggate,Marie Andersson,Richard Hale +17 more
TL;DR: The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H(4) receptor inverse agonists is described, which yielded 18I which possessed increased potency and enhanced microsomal stability.