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Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors |
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| Authors: | Pinard Emmanuel Alberati Daniela Bender Markus Borroni Edilio Brom Virginie Burner Serge Fischer Holger Hainzl Dominik Halm Remy Hauser Nicole Jolidon Synèse Lengyel Judith Marty Hans-Peter Meyer Thierry Moreau Jean-Luc Mory Roland Narquizian Robert Norcross Roger D Schmid Philipp Wermuth Roger Zimmerli Daniel |
| Affiliation: | F. Hoffmann-La Roche Ltd, Pharmaceutical Research Basel, Basel, Switzerland. emmanuel.pinard@roche.com |
| Abstract: | 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. |
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