845973-56-0Relevant academic research and scientific papers
Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization
Cumming, Jared,Babu, Suresh,Huang, Ying,Carrol, Carolyn,Chen, Xia,Favreau, Leonard,Greenlee, William,Guo, Tao,Kennedy, Matthew,Kuvelkar, Reshma,Le, Thuy,Li, Guoqing,McHugh, Nansie,Orth, Peter,Ozgur, Lynne,Parker, Eric,Saionz, Kurt,Stamford, Andrew,Strickland, Corey,Tadesse, Dawit,Voigt, Johannes,Zhang, Lili,Zhang, Qi
scheme or table, p. 2837 - 2842 (2010/08/04)
With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2′ sub-pocket of the enzyme culmin
CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT
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, (2008/06/13)
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
