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Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.
Oehlrich, Daniel; Rombouts, Frederik J R; Berthelot, Didier; Bischoff, François P; De Cleyn, Michel A J; Jaroskova, Libuse; Macdonald, Gregor; Mercken, Marc; Surkyn, Michel; Trabanco, Andrés A; Tresadern, Gary; Van Brandt, Sven; Velter, Adriana I; Wu, Tongfei; Gijsen, Harrie J M.
  • Oehlrich D; Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. doehlric@its.jnj.com
Bioorg Med Chem Lett ; 23(17): 4794-800, 2013 Sep 01.
Article en En | MEDLINE | ID: mdl-23890837
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 Aß42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperidinas / Triazoles / Diseño de Fármacos / Compuestos Bicíclicos Heterocíclicos con Puentes / Secretasas de la Proteína Precursora del Amiloide / Enfermedad de Alzheimer Límite: Animals / Humans Idioma: En Año: 2013 Tipo del documento: Article
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperidinas / Triazoles / Diseño de Fármacos / Compuestos Bicíclicos Heterocíclicos con Puentes / Secretasas de la Proteína Precursora del Amiloide / Enfermedad de Alzheimer Límite: Animals / Humans Idioma: En Año: 2013 Tipo del documento: Article