937026-26-1Relevant articles and documents
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.
HETEROCYCLIC COMPOUND AND USE THEREOF
-
, (2012/03/26)
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
-
, (2011/08/04)
The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 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.