1245737-03-4Relevant articles and documents
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.
