847157-48-6Relevant academic research and scientific papers
Conformationally biased P3 amide replacements of β-secretase inhibitors
Stachel, Shawn J.,Coburn, Craig A.,Steele, Thomas G.,Crouthamel, Min-Chi,Pietrak, Beth L.,Lai, Ming-Tain,Holloway, M. Katharine,Munshi, Sanjeev K.,Graham, Samuel L.,Vacca, Joseph P.
, p. 641 - 644 (2007/10/03)
We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the β-secretase inhibitor 7m which has an in vitro IC50 = 35 nM
Macrocyclic inhibitors of β-secretase: Functional activity in an animal model
Stachel, Shawn J.,Coburn, Craig A.,Sankaranarayanan, Sethu,Price, Eric A.,Pietrak, Beth L.,Huang, Qian,Lineberger, Janet,Espeseth, Amy S.,Jin, Lixia,Ellis, Joan,Holloway, M. Katharine,Munshi, Sanjeev,Allison, Timothy,Hazuda, Daria,Simon, Adam J.,Graham, Samuel L.,Vacca, Joseph P.
, p. 6147 - 6150 (2007/10/03)
A macrocyclic inhibitor of β-secretase was designed by covalently cross-linking the P1 and P3 side chains of an isophthalamide-based inhibitor. Macrocyclization resulted in significantly improved potency and physical properties when compared to the initia
PYRROLIDIN-3-YL COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 40, (2010/02/15)
The present invention is directed to pyrrolidin-3-yl derivative compounds 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 i
BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 47, (2010/02/11)
The present invention is directed to benzylether and benzylamino derivative compounds 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.
1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 70, (2010/02/14)
The present invention is directed to 1,3,5-phenyl substituted derivative compounds 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.
MACROCYCLIC BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 10; 20, (2008/06/13)
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is a
