1208252-29-2Relevant academic research and scientific papers
PURINE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 23, (2010/04/03)
The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.
Purine derivatives as potent γ-secretase modulators
Rivkin, Alexey,Ahearn, Sean P.,Chichetti, Stephanie M.,Hamblett, Christopher L.,Garcia, Yudith,Martinez, Michelle,Hubbs, Jed L.,Reutershan, Michael H.,Daniels, Matthew H.,Siliphaivanh, Phieng,Otte, Karin M.,Li, Chaomin,Rosenau, Andrew,Surdi, Laura M.,Jung, Joon,Hughes, Bethany L.,Crispino, Jamie L.,Nikov, George N.,Middleton, Richard E.,Moxham, Christopher M.,Szewczak, Alexander A.,Shah, Sanjiv,Moy, Lily Y.,Kenific, Candia M.,Tanga, Flobert,Cruz, Jonathan C.,Andrade, Paula,Angagaw, Minilik H.,Shomer, Nirah H.,Miller, Thomas,Munoz, Benito,Shearman, Mark S.
scheme or table, p. 2279 - 2282 (2010/06/15)
The development of a novel series of purines as γ-secretase modulators for potential use in the treatment of Alzheimer's disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based γ-secretase modulators with 300- to 2000-fold in vitro selectivity over inhibition of Notch cleavage and that selectively reduces Αβ42 in an APP-YAC transgenic mouse model.
