946615-65-2Relevant academic research and scientific papers
Discovery of begacestat, a Notch-1-sparing γ-secretase inhibitor for the treatment of Alzheimer's disease
Mayer, Scott C.,Kreft, Anthony F.,Harrison, Boyd,Abou-Gharbia, Magid,Antane, Madelene,Aschmies, Suzan,Atchison, Kevin,Chlenov, Michael,Cole, Derek C.,Comery, Thomas,Diamantidis, George,Ellingboe, John,Fan, Kristi,Galante, Rocco,Gonzales, Cathleen,Ho, Douglas M.,Hoke, Molly E.,Hu, Yun,Huryn, Donna,Jain, Uday,Jin, Mei,Kremer, Kenneth,Kubrak, Dennis,Lin, Melissa,Lu, Peimin,Magolda, Ron,Martone, Robert,Moore, William,Oganesian, Aram,Pangalos, Menelas N.,Porte, Alex,Reinhart, Peter,Resnick, Lynn,Riddell, David R.,Sonnenberg-Reines, June,Stock, Joseph R.,Sun, Shaiu-Ching,Wagner, Erik,Wang, Ting,Woller, Kevin,Xu, Zheng,Zaleska, Margaret M.,Zeldis, Joseph,Zhang, Minsheng,Zhou, Hua,Jacobsen, J. Steven
supporting information; experimental part, p. 7348 - 7351 (2009/12/23)
SAR on HTS hits 1 and 2 led to the potent, Notch-1-sparing GSI 9, which lowered brain Aβ in Tg2576 mice at 100 mg/kg po. Converting the metabolically labile methyl groups in 9 to trifluoromethyl groups afforded the more stable analogue 10, which had impro
TRIFLUOROMETHYL-CONTAINING PHENYLSULFONAMIDE BETA AMYLOID INHIBITORS
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Page/Page column 7-8, (2008/06/13)
A compound of Formula (I), or pharmaceutically acceptable salts and/or hydrates or prodrugs thereof, wherein Formula (I) has the structure:is provided, wherein R1-R7 are defined herein. These compounds are useful in medicaments for treating a disease sele
