1242313-36-5Relevant academic research and scientific papers
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
Oehlrich, Daniel,Rombouts, Frederik J.R.,Berthelot, Didier,Bischoff, Francois P.,De Cleyn, Michel A.J.,Jaroskova, Libuse,MacDonald, Gregor,Mercken, Marc,Surkyn, Michel,Trabanco, Andres A.,Tresadern, Gary,Van Brandt, Sven,Velter, Adriana I.,Wu, Tongfei,Gijsen, Harrie J.M.
, p. 4794 - 4800 (2013/09/02)
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.
SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 178, (2011/02/24)
The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
