Serge Burner
Hoffmann-La Roche
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Publication
Featured researches published by Serge Burner.
Journal of Medicinal Chemistry | 2010
Emmanuel Pinard; Alexander Alanine; Daniela Alberati; Markus Bender; Edilio Borroni; Patrick Bourdeaux; Virginie Brom; Serge Burner; Holger Fischer; Dominik Hainzl; Remy Halm; Nicole Hauser; Synese Jolidon; Judith Lengyel; Hans-Peter Marty; Thierry Meyer; Jean-Luc Moreau; Roland Mory; Robert Narquizian; Mathias Nettekoven; Roger David Norcross; Bernd Puellmann; Philipp Schmid; Sebastien Schmitt; Henri Stalder; Roger Wermuth; Joseph G. Wettstein; Daniel Zimmerli
The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve hERG channel selectivity and brain penetration. This effort culminated in the discovery of compound 10a (RG1678), the first potent and selective GlyT1 inhibitor to have a beneficial effect in schizophrenic patients in a phase II clinical trial.
Bioorganic & Medicinal Chemistry Letters | 2010
Emmanuel Pinard; Daniela Alberati; Markus Bender; Edilio Borroni; Virginie Brom; Serge Burner; Holger Fischer; Dominik Hainzl; Remy Halm; Nicole Hauser; Synese Jolidon; Judith Lengyel; Hans-Peter Marty; Thierry Meyer; Jean-Luc Moreau; Roland Mory; Robert Narquizian; Roger David Norcross; Philipp Schmid; Roger Wermuth; Daniel Zimmerli
Benzoylisoindolines were discovered as a novel structural class of GlyT1 inhibitors. SAR studies and subsequent lead optimization efforts focused primarily on addressing hERG liability and on improving in vivo efficacy resulted in the identification of potent GlyT1 inhibitors displaying excellent selectivity and in vivo PD and PK profiles.
ACS Medicinal Chemistry Letters | 2014
Emmanuel Pinard; Daniela Alberati; Ruben Alvarez-Sanchez; Virginie Brom; Serge Burner; Holger Fischer; Nicole Hauser; Sabine Kolczewski; Judith Lengyel; Roland Mory; Christian Saladin; Tanja Schulz-Gasch; Henri Stalder
3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration.
Archive | 2000
Alexander Alanine; Serge Burner; Bernd Buettelmann; Neidhart Marie-Paule Heitz; Georg Jaeschke; Emmanuel Pinard; Rene Wyler
Archive | 2000
Alexander Alanine; Bernd Buettelmann; Serge Burner; Neidhart Marie-Paule Heitz; Georg Jaeschke; Emmanuel Pinard; Rene Wyler
Journal of Labelled Compounds and Radiopharmaceuticals | 2011
Emmanuel Pinard; Serge Burner; Philipp Cueni; Thomas Hartung; Roger David Norcross; Philipp Schmid; Pius Waldmeier; Guy Zielinski; Hayden T. Ravert; Daniel P. Holt; Robert F. Dannals
Tetrahedron Letters | 2008
Emmanuel Pinard; Serge Burner; Philippe Cueni; Francois Montavon; Daniel Zimmerli
Archive | 2000
Alexander Alanine; Bernd Buettelmann; Serge Burner; Neidhart Marie-Paule Heitz; Georg Jaeschke; Emmanuel Pinard; Rene Wyler
Archive | 2005
Marie-Paule Heitz Neidhart; Georg Jaeschke; Bernd Büttelmann; Emmanuel Pinard; Rene Wyler; Alexander Alanine; Serge Burner
Archive | 2005
Pinard Emmanuel; Neidhart Marie-Paule Heitz; Alanine Alexander; Buettelmann Bernd; Jaeschke Georg; Wyler Rene; Serge Burner