S. Desrayaud

发表

AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: identification, SAR and pharmacological characterization.

F. Gasparini, I. Vranesic, G. Bilbe, 2014, Bioorganic & medicinal chemistry.

Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.

Jean-Michel Rondeau, Laura Jacobson, M. Staufenbiel, 2012, Journal of medicinal chemistry.

Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.

Clive McCarthy, Jean-Michel Rondeau, Marina Tintelnot-Blomley, 2011, Bioorganic & medicinal chemistry letters.

Design and Development of a Cyclic Decapeptide Scaffold with Suitable Properties for Bioavailability and Oral Exposure

Hans-Jörg Roth, Marianne Fouché, Markus Blatter, 2016, ChemMedChem.

Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile.

M. Fendt, I. Vranesic, S. Desrayaud, 2011, ACS medicinal chemistry letters.

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

S. Urwyler, W. Froestl, K. Lingenhoehl, 2012, Bioorganic & medicinal chemistry letters.

6-[2-(Adamantylidene)-hydroxybenzoxazole]-O-sulfamate, a steroid sulfatase inhibitor for the treatment of androgen- and estrogen-dependent diseases

E. Schreiner, P. Nussbaumer, A. Winiski, 2004, The Journal of Steroid Biochemistry and Molecular Biology.

The priorities/needs of the pharmaceutical industry in drug delivery to the brain

S. Desrayaud, M. Lemaire, 2005 .

MPEP, an mGlu5 receptor antagonist, reduces the development of l-DOPA-induced motor complications in de novo parkinsonian monkeys: Biochemical correlates

L. Grégoire, F. Gasparini, B. Gomez-Mancilla, 2013, Neuropharmacology.

Predicting In Vivo Compound Brain Penetration Using Multi-task Graph Neural Networks

Richard A. Lewis, S. Desrayaud, Raquel Rodríguez-Pérez, 2022, J. Chem. Inf. Model..

Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.

C. Schnell, P. Furet, F. Blasco, 2022, Journal of medicinal chemistry.

MS565: A SPECT Tracer for Evaluating the Brain Penetration of BAF312 (Siponimod)

E. Briard, Y. Auberson, S. Desrayaud, 2015, ChemMedChem.

Brain Penetration of SDZ PSC 833 in Rats

S. Desrayaud, M. Lemaire, 1996 .

Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.

M. Fendt, I. Vranesic, T. Troxler, 2010, Bioorganic & medicinal chemistry letters.

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

C. Schnell, P. Furet, F. Blasco, 2015, Bioorganic & medicinal chemistry letters.

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.

M. Staufenbiel, J. Rondeau, S. Desrayaud, 2013, Bioorganic & medicinal chemistry letters.

Micropreparative isolation and NMR structure elucidation of metabolites of the drug candidate 1-isopropyl-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy) quinazolin-2(1H)-one from rat bile and urine.

S. Desrayaud, J. Blanz, M. Ritzau, 2015, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

A. Picard, S. Urwyler, K. Lingenhoehl, 2017, ChemMedChem.

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Jean-Michel Rondeau, Marina Tintelnot-Blomley, M. Staufenbiel, 2009, Bioorganic & medicinal chemistry letters.

Pharmacokinetic Studies around the Mono‐ and Difunctionalization of a Bioavailable Cyclic Decapeptide Scaffold

H. Roth, M. Blatter, S. Desrayaud, 2016, ChemMedChem.

Design of A Metabolically Stable Tritium-Tracer of the PI3Kδ-Inhibitor CDZ173 (Leniolisib) as a Tool to Study Liver Metabolites

P. Bross, K. Litherland, S. Desrayaud, 2018, Helvetica Chimica Acta.

Brain region-specific enhancement of remyelination and prevention of demyelination by the CSF1R kinase inhibitor BLZ945

E. Giorgetti, N. Accart, N. Beckmann, 2018, Acta neuropathologica communications.

Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine.

S. Desrayaud, M. Lemaire, J. Scherrmann, 1997, Life sciences.

Effect of the Mdr1a P-glycoprotein gene disruption on the tissue distribution of SDZ PSC 833, a multidrug resistance-reversing agent, in mice.

D. Breimer, S. Desrayaud, M. Lemaire, 1998, The Journal of pharmacology and experimental therapeutics.

Hyperdopaminergia and altered locomotor activity in GABAB1‐deficient mice

D. Hoyer, P. Pévet, M. Gassmann, 2006, Journal of neurochemistry.

Cannabinoid Receptor 2 Signaling in Peripheral Immune Cells Modulates Disease Onset and Severity in Mouse Models of Huntington's Disease

S. Tabrizi, K. Bouchard, P. Muchowski, 2012, The Journal of Neuroscience.

Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.

T. Troxler, K. Zimmermann, D. Shimshek, 2013, Bioorganic & medicinal chemistry letters.

Modulation of Oral Bioavailability and Metabolism for Closely Related Cyclic Hexapeptides

T. Vorherr, M. Schaefer, S. Desrayaud, 2017, International Journal of Peptide Research and Therapeutics.

GABAB Receptor Antagonist-Mediated Antidepressant-Like Behavior Is Serotonin-Dependent

D. Slattery, J. Cryan, S. Desrayaud, 2005, Journal of Pharmacology and Experimental Therapeutics.

The positive allosteric modulator GS39783 enhances GABAB receptor‐mediated inhibition of cyclic AMP formation in rat striatum in vivo

S. Urwyler, S. Imobersteg, S. Desrayaud, 2006, Journal of neurochemistry.

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

M. Staufenbiel, P. Paganetti, J. Rondeau, 2010, Bioorganic & medicinal chemistry letters.

Brain region-specific enhancement of remyelination and prevention of demyelination by the CSF1R kinase inhibitor BLZ945

Wilfried Frieauff, E. Giorgetti, N. Accart, 2018, Acta Neuropathologica Communications.

A practical approach to the optimization of positron emission tomography (PET) imaging agents for the central nervous system.

E. Briard, Y. Auberson, S. Desrayaud, 2022, Journal of labelled compounds & radiopharmaceuticals.

Dose-dependent delivery of colchicine to the rat hippocampus by microdialysis

S. Desrayaud, J. Scherrmann, G. Boschi, 1996, Neuroscience Letters.

Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.

P. Ertl, I. Vranesic, G. Laue, 2012, Bioorganic & medicinal chemistry letters.