Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
Daniel Oehlrich1, Frederik J R Rombouts, Didier Berthelot
1Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. doehlric@its.jnj.com
Bioorganic & Medicinal Chemistry Letters
|July 30, 2013
Abstract:
The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a γ-secretase modulator is described. This is a potential disease modifying anti-Alzheimer's drug which demonstrated high in vitro and in vivo potency against Aβ42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
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