An orally available BACE1 inhibitor that affords robust CNS Aβ reduction without cardiovascular liabilities

ACS Medicinal Chemistry Letters

Volumn 6, Issue 2, 2015, Pages 210-215

  Cheng, Yuan ^a   Brown, James ^a   Judd, Ted C ^a   Lopez, Patricia ^a   Qian, Wenyuan ^a   Powers, Timothy S ^a,c   Chen, Jian Jeffrey ^a   Bartberger, Michael D ^a   Chen, Kui ^a   Dunn, Robert T ^a   Epstein, Oleg ^a   Fremeau, Robert T ^a   Harried, Scott ^a,d   Hickman, Dean ^a,b   Hitchcock, Stephen A ^a   Luo, Yi ^a   Minatti, Ana Elena ^a   Patel, Vinod F ^a,c   Vargas, Hugo M ^a   Wahl, Robert C ^a   Weiss, Matthew M ^a   Wen, Paul H ^a   White, Ryan D ^a   Whittington, Douglas A ^a   Zheng, Xiao Mei ^a   Wood, Stephen ^a   more..

^a AMGEN INC   (United States)

^b Takeda San Diego Inc   (United States)

^c Department of Neuroscience Amgen Inc ^*  (United States)

^d SAB: Knopp Biosciences LLC   (United States)

Author keywords

Alzheimer's disease (AD); aminooxazoline; A ; xanthene; site amyloid precursor protein cleaving enzyme 1 (BACE1)

Indexed keywords

AMYLOID BETA PROTEIN[1-40]; BETA SECRETASE INHIBITOR; HYDROGEN; POTASSIUM CHANNEL HERG; XANTHENE DERIVATIVE;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BEAGLE; CARDIOVASCULAR DISEASE; CELL ASSAY; CEREBROSPINAL FLUID; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG SAFETY; DRUG STABILITY; DRUG TOLERABILITY; EC50; ENZYMATIC ASSAY; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; LIVER MICROSOME; MACACA FASCICULARIS; MALE; NONHUMAN; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; PROCESS OPTIMIZATION; RAT; RHESUS MONKEY; STRUCTURE ACTIVITY RELATION; WILD TYPE;

PRIMATES; RATTUS;

EID: 84922866887     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml500458t     Document Type: Article

References (20)

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