845543-86-4Relevant articles and documents
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
Thompson, Lorin A.,Shi, Jianliang,Decicco, Carl P.,Tebben, Andrew J.,Olson, Richard E.,Boy, Kenneth M.,Guernon, Jason M.,Good, Andrew C.,Liauw, Ann,Zheng, Changsheng,Copeland, Robert A.,Combs, Andrew P.,Trainor, George L.,Camac, Daniel M.,Muckelbauer, Jodi K.,Lentz, Kimberley A.,Grace, James E.,Burton, Catherine R.,Toyn, Jeremy H.,Barten, Donna M.,Marcinkeviciene, Jovita,Meredith, Jere E.,Albright, Charles F.,MacOr, John E.
scheme or table, p. 6909 - 6915 (2011/12/22)
The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.
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.