1213771-64-2Relevant academic research and scientific papers
Discovery of novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives as γ-secretase modulators
Takai, Takafumi,Hoashi, Yasutaka,Tomata, Yoshihide,Morimoto, Sachie,Nakamura, Minoru,Watanabe, Tomomichi,Igari, Tomoko,Koike, Tatsuki
, p. 4245 - 4249 (2015/11/03)
Novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives were designed, synthesized, and evaluated as γ-secretase modulators (GSMs). An optimization study of this series resulted in the identification of (R)-11j, which showed a potent Aβ42-lowering effect, high bioavailability and good blood-brain barrier permeability in mice. Oral administration of (R)-11j significantly reduced brain Aβ42 in mice at a dose of 10 mg/kg.
HETEROCYCLIC COMPOUND AND USE THEREOF
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Page/Page column 75, (2012/06/01)
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and use thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
PROCESS FOR PREPARING CERTAIN CINNAMIDE COMPOUNDS
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Page/Page column 57; 58, (2010/04/06)
This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.
