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1. Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.

Author

Stasi, Luigi Piero, Artusi, Roberto, Bovino, Clara, Buzzi, Benedetta, Canciani, Luca, Caselli, Gianfranco, Colace, Fabrizio, Garofalo, Paolo, Giambuzzi, Silvia, Larger, Patrice, Letari, Ornella, Mandelli, Stefano, Perugini, Lorenzo, Pucci, Sabrina, Salvi, Matteo, and Toro, PierLuigi

Subjects
*HEPTANE, *OREXINS, *SUBSTITUTION reactions, *PHARMACOKINETICS, *MATHEMATICAL optimization, *CYTOCHROME P-450, *DRUG development, *ORGANIC synthesis
Abstract

Abstract: Starting from a orexin 1 receptor selective antagonist 4,4-disubstituted piperidine series a novel potent 5-azaspiro[2.4]heptane dual orexin 1 and orexin 2 receptor antagonist class has been discovered. SAR and Pharmacokinetic optimization of this series is herein disclosed. Lead compound 15 exhibits potent activity against orexin 1 and orexin 2 receptors along with low cytochrome P450 inhibition potential, good brain penetration and oral bioavailability in rats. [Copyright &y& Elsevier]

Published
2013
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