676135-73-2Relevant academic research and scientific papers
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.
2-AMINO- AND 2-THIO-SUBSTITUTED 1,3-DIAMINOPROPANES
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Page/Page column 213, (2008/06/13)
Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer’s disease and other diseases characterized by deposition of A beta peptide in a mammal.
SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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Page/Page column 253, (2008/06/13)
The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
METHODS OF TREATMENT OF AMYLOIDOSIS USING ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 183, (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.
SUBSTITUTED UREA AND CARBAMATE, PHENACYL-2-HYDROXY-3-DIAMINOALKANE, AND BENZAMIDE-2-HYDROXY-3-DIAMINOALKANE ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 181, (2010/02/14)
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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Page/Page column 104, (2010/02/14)
The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
