861857-72-9Relevant academic research and scientific papers
BACE-2 INHIBITORY COMPOUNDS AND RELATED METHODS OF USE
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Paragraph 0208; 0210, (2017/05/02)
Provided herein are novel compounds of Formulae I-III, and methods of using the same to selectively inhibit BACE2.
Design and synthesis of cell potent BACE-1 inhibitors: Structure-activity relationship of P1′ substituents
Sealy, Jennifer M.,Truong, Anh P.,Tso, Luke,Probst, Gary D.,Aquino, Jose,Hom, Roy K.,Jagodzinska, Barbara M.,Dressen, Darren,Wone, David W.G.,Brogley, Louis,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Dappen, Michael S.,Toth, Gergely,Pan, Hu,Ruslim, Lany,Miller, Jim,Bova, Michael P.,Sinha, Sukanto,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6386 - 6391 (2010/06/11)
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Aβ cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1′ residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.
METHODS OF TREATMENT OF AMYLOIDOSIS USING ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 211-212, (2010/02/13)
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
