738624-86-7Relevant academic research and scientific papers
Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors
Zhao, Zhiqiang,Pissarnitski, Dmitri A.,Josien, Hubert B.,Bara, Thomas A.,Clader, John W.,Li, Hongmei,McBriar, Mark D.,Rajagopalan, Murali,Xu, Ruo,Terracina, Giuseppe,Hyde, Lynn,Song, Lixin,Zhang, Lili,Parker, Eric M.,Osterman, Rebecca,Buevich, Alexei V.
, p. 36 - 48 (2016/08/25)
The design, synthesis, SAR, and biological profile of a substituted 4-morpholine sulfonamide series of γ-secretase inhibitors (GSIs) were described. In several cases, the resulting series of GSIs reduced CYP liabilities and improved γ-secretase inhibition activity compared to our previous research series. Selected compounds demonstrated significant reduction of amyloid-β (Aβ) after acute oral dosing in a transgenic animal model of Alzheimer's disease (AD).
SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
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Page/Page column 104, (2010/02/15)
This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected f
