887970-18-5Relevant academic research and scientific papers
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors
Moore, Keith P.,Zhu, Hong,Rajapakse, Hemaka A.,McGaughey, Georgia B.,Colussi, Dennis,Price, Eric A.,Sankaranarayanan, Sethu,Simon, Adam J.,Pudvah, Nicole T.,Hochman, Jerome H.,Allison, Timothy,Munshi, Sanjeev K.,Graham, Samuel L.,Vacca, Joseph P.,Nantermet, Philippe G.
, p. 5831 - 5835 (2008/09/19)
This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one
MACROCYCLIC TERTIARY AMINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 82-83, (2010/11/08)
The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
