Discovery of novel selective Sigma-1 ligands as cognitive enhancers

Anne Valade; Sophie Binet Cross; Claire Brown; Eric Detrait; Doina Ene; Michel Gillard; Michel Guyaux; Yves Lamberty; Martin Maguire; Nivedita Namdev; Laurent Provins; Eric Schwartz; Céline Vermeiren

doi:10.1039/C1MD00010A

Discovery of novel selective Sigma-1 ligands as cognitive enhancers†

Anne Valade,*^a Sophie Binet Cross,^b Claire Brown,^b Eric Detrait,^a Doina Ene,^b Michel Gillard,^a Michel Guyaux,^a Yves Lamberty,^a Martin Maguire,^b Nivedita Namdev,^b Laurent Provins,^a Eric Schwartz^b and Céline Vermeiren^a

Author affiliations

* Corresponding authors

^a UCB Pharma, UCB NewMedicines, Chemin du Foriest, Braine-L'Alleud, Belgium
E-mail: anne.valade@ucb.com

^b Former UCB Research Inc., Cambridge, USA

Abstract

We disclose the identification and SAR of phenylcyclopropylcarboxamide compounds as novel, selective Sigma-1 ligands presenting excellent drug-like properties, high solubility and metabolic stability. A selected representative, compound 14, demonstrated in vivo very good brain exposure and antiamnesic effect in a mouse model of recognition memory.

MedChemComm

Discovery of novel selective Sigma-1 ligands as cognitive enhancers†

Abstract

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Discovery of novel selective Sigma-1 ligands as cognitive enhancers

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