695215-96-4Relevant articles and documents
COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 64, (2010/06/19)
The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
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Page/Page column 27, (2008/06/13)
The present invention is directed to phenylamide and pyridylamide derivative compounds of 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.
Discovery of oxadiazoyl tertiary carbinamine inhibitors of β-secretase (BACE-1)
Rajapakse, Hemaka A.,Nantermet, Philippe G.,Selnick, Harold G.,Munshi, Sanjeev,McGaughey, Georgia B.,Lindsley, Stacey R.,Young, Mary Beth,Lai, Ming-Tain,Espeseth, Amy S.,Shi, Xiao-Ping,Colussi, Dennis,Pietrak, Beth,Crouthamel, Ming-Chih,Tugusheva, Katherine,Huang, Qian,Xu, Min,Simon, Adam J.,Kuo, Lawrence,Hazuda, Daria J.,Graham, Samuel,Vacca, Joseph P.
, p. 7270 - 7273 (2007/10/03)
We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme β-secretase (BACE-1). These novel non-transition-state-derived ligands incorporate a single primary amine to interact with the catalytic aspartates of the
PYRROLIDIN-3-YL COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 34, (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
1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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, (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.
Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
Stachel, Shawn J.,Coburn, Craig A.,Steele, Thomas G.,Jones, Kristen G.,Loutzenhiser, Elizabeth F.,Gregro, Alison R.,Rajapakse, Hemaka A.,Lai, Ming-Tain,Crouthamel, Ming-Chih,Xu, Min,Tugusheva, Katherine,Lineberger, Janet E.,Pietrak, Beth L.,Espeseth, Amy S.,Shi, Xiao-Ping,Chen-Dodson, Elizabeth,Holloway, M. Katharine,Munshi, Sanjeev,Simon, Adam J.,Kuo, Lawrence,Vacca, Joseph P.
, p. 6447 - 6450 (2007/10/03)
We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell
PHENYLCARBOXAMIDE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 21-22, (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
Aspartyl protease inhibitors
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Page 81, (2010/02/07)
The present invention provides compounds having the formula: wherein R1, R′, R2, R3, R3′, R4, X1, X2 and X3 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (β-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by β-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.