Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction

ACS Medicinal Chemistry Letters

Volumn 3, Issue 11, 2012, Pages 897-902

  Stamford, Andrew W ^a   Scott, Jack D ^a   Li, Sarah W ^a   Babu, Suresh ^b   Tadesse, Dawit ^b   Hunter, Rachael ^b   Wu, Yusheng ^a   Misiaszek, Jeffrey ^a   Cumming, Jared N ^a   Gilbert, Eric J ^a   Huang, Chunli ^a   McKittrick, Brian A ^a   Hong, Liwu ^a   Guo, Tao ^b   Zhu, Zhaoning ^a   Strickland, Corey ^a   Orth, Peter ^a   Voigt, Johannes H ^a   Kennedy, Matthew E ^a   Chen, Xia ^a   Kuvelkar, Reshma ^a   Hodgson, Robert ^a   Hyde, Lynn A ^a   Cox, Kathleen ^a   Favreau, Leonard ^a   Parker, Eric M ^a   Greenlee, William J ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b Ligand Pharmaceuticals Inc   (United States)

Author keywords

A 40; Alzheimer's disease; BACE1; iminopyrimidinone; inhibitor; X ray crystallography

Indexed keywords

AMYLOID BETA PROTEIN; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; IMINOPYRIMIDINONE DERIVATIVE; PYRIMIDINONE DERIVATIVE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BRAIN CORTEX; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG PENETRATION; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; NONHUMAN; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; PROTEIN CEREBROSPINAL FLUID LEVEL; RAT; STRUCTURE ACTIVITY RELATION;

RATTUS;

EID: 84868540195     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml3001165     Document Type: Article

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