58888-87-2Relevant 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
Process for the synthesis of chirally pure beta-amino-alcohols
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, (2008/06/13)
A process is provided for preparing chirally pure S-enantiomers of α-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding th
Research in dipropylacetic series. XII. Aliphatic ramified acids and alcohols with anticonvulsant activity
Taillandier,Benoit Guyod,Boucherle,et al.
, p. 453 - 462 (2007/10/05)
Previous results obtained about 2 propyl pentanoic acid (dipropylacetic or DPA) have been extended to other dialkylalkanoic acids having less than 14 carbon atoms and to some of their precursors (alcohols) or derivatives (amides). The effect of lengthening the chain bonding between the carbon bearing the two alkyl chains and the functional carbon on about 50 molecules is discussed. The anticonvulsant activity's length and strength often increases when lengthening that chain.
