34564-85-7Relevant academic research and scientific papers
Palladium-Catalyzed One-Pot Reaction of Hydrazones, Dihaloarenes, and Organoboron Reagents: Synthesis and Cytotoxic Activity of 1,1-Diarylethylene Derivatives
Roche, Maxime,Salim, Salim Mmadi.,Bignon, Jér?me,Levaique, Hélène,Brion, Jean-Daniel,Alami, Mouad,Hamze, Abdallah
, p. 6715 - 6727 (2015/10/06)
A new three-component assembly reaction between N-tosylhydrazones, dihalogenated arenes, and boronic acids or boronate esters was developed, producing highly substituted 1,1-diarylethylenes in good yields. The two C-C bonds formed through this coupling ha
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and cns penetrable BACE inhibitors for the treatment of alzheimers disease
Huang, Hongbing,La, Daniel S.,Cheng, Alan C.,Whittington, Douglas A.,Patel, Vinod F.,Chen, Kui,Dineen, Thomas A.,Epstein, Oleg,Graceffa, Russell,Hickman, Dean,Kiang,Louie, Steven,Luo, Yi,Wahl, Robert C.,Wen, Paul H.,Wood, Stephen,Fremeau, Robert T.
, p. 9156 - 9169 (2013/01/15)
A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the structurally related aspartyl protease cathepsin D. Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound 11a resulted in a significant reduction of CNS Aβ40 in naive rats.
4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES
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Page/Page column 10, (2009/09/05)
The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
