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Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.
Pinard E, Alanine A, Alberati D, Bender M, Borroni E, Bourdeaux P, Brom V, Burner S, Fischer H, Hainzl D, Halm R, Hauser N, Jolidon S, Lengyel J, Marty HP, Meyer T, Moreau JL, Mory R, Narquizian R, Nettekoven M, Norcross RD, Puellmann B, Schmid P, Schmitt S, Stalder H, Wermuth R, Wettstein JG, Zimmerli D. Pinard E, et al. Among authors: brom v. J Med Chem. 2010 Jun 24;53(12):4603-14. doi: 10.1021/jm100210p. J Med Chem. 2010. PMID: 20491477
Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.
Pinard E, Alberati D, Bender M, Borroni E, Brom V, Burner S, Fischer H, Hainzl D, Halm R, Hauser N, Jolidon S, Lengyel J, Marty HP, Meyer T, Moreau JL, Mory R, Narquizian R, Norcross RD, Schmid P, Wermuth R, Zimmerli D. Pinard E, et al. Among authors: brom v. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6960-5. doi: 10.1016/j.bmcl.2010.09.124. Epub 2010 Oct 7. Bioorg Med Chem Lett. 2010. PMID: 20974532
Discovery of Orally Available and Brain Penetrant AEP Inhibitors.
Krummenacher D, He W, Kuhn B, Schnider C, Beurier A, Brom V, Sivasothy T, Marty C, Tosstorff A, Hewings DS, Mesch S, Pinard E, Brändlin M, Hochstrasser R, Westwood P, Rothe J, Kronenberger A, Morandi F, Gutbier S, Schuler A, Heer D, Gloria LE, Joedicke L, Rudolph MG, Müller L, Grüninger F, Baumann K, Kaniyappan S, Manevski N, Bartels B. Krummenacher D, et al. Among authors: brom v. J Med Chem. 2023 Dec 28;66(24):17026-17043. doi: 10.1021/acs.jmedchem.3c01804. Epub 2023 Dec 13. J Med Chem. 2023. PMID: 38090813