Discovery of AZD3839, a Potent and Selective BACE1 Inhibitor Clinical Candidate for the Treatment of Alzheimer Disease

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

(2012) Jared N. Cumming et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy

(2012) Britt-Marie Swahn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-molecule BACE1 inhibitors: a patent literature review (2006 – 2011)

(2012) Gary Probst et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Design and Synthesis of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β-Amyloid Peptides

(2012) Britt-Marie Swahn et al.   JOURNAL OF MEDICINAL CHEMISTRY

The dynamics of Aβ distribution after γ-secretase inhibitor treatment, as determined by experimental and modelling approaches in a wild type rat

(2012) Leon M. Tai et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

A mutation in APP protects against Alzheimer’s disease and age-related cognitive decline

(2012) Thorlakur Jonsson et al.   NATURE

Flexibility of the flap in the active site of BACE1 as revealed by crystal structures and molecular dynamics simulations

(2011) Yechun Xu et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

2011 Alzheimer’s disease facts and figures

(2011)   Alzheimers & Dementia

Robust Central Reduction of Amyloid-  in Humans with an Orally Available, Non-Peptidic  -Secretase Inhibitor

(2011) P. C. May et al.   JOURNAL OF NEUROSCIENCE

Quantitative Membrane Protein Expression at the Blood–Brain Barrier of Adult and Younger Cynomolgus Monkeys

(2011) Katsuaki Ito et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Quantitative Pharmacokinetic/Pharmacodynamic Analyses Suggest That the 129/SVE Mouse Is a Suitable Preclinical Pharmacology Model for Identifying Small-Molecule  -Secretase Inhibitors

(2011) Y. Lu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Alzheimer's disease

(2011) Clive Ballard et al.   LANCET

The Alzheimer's Disease Neuroimaging Initiative: Annual change in biomarkers and clinical outcomes

(2010) Laurel A. Beckett et al.   Alzheimers & Dementia

Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability

(2010) Michael S. Malamas et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Modeling Effect of a γ-Secretase Inhibitor on Amyloid-β Dynamics Reveals Significant Role of an Amyloid Clearance Mechanism

(2010) Raibatak Das et al.   BULLETIN OF MATHEMATICAL BIOLOGY

β-Secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice

(2010) Wan-Pin Chang et al.   FASEB JOURNAL

BACE: Therapeutic target and potential biomarker for Alzheimer's disease

(2010) Geneviève Evin et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Alzheimer's disease: strategies for disease modification

(2010) Martin Citron   NATURE REVIEWS DRUG DISCOVERY

The secretases: enzymes with therapeutic potential in Alzheimer disease

(2010) Bart De Strooper et al.   Nature Reviews Neurology

Alzheimer's Disease

(2010) Henry W. Querfurth et al.   NEW ENGLAND JOURNAL OF MEDICINE

A γ-secretase inhibitor decreases amyloid-β production in the central nervous system

(2009) Randall J. Bateman et al.   ANNALS OF NEUROLOGY

Progress toward the development of a viable BACE-1 inhibitor

(2009) Shawn J. Stachel   DRUG DEVELOPMENT RESEARCH

Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

(2009) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Species Differences in Blood-Brain Barrier Transport of Three Positron Emission Tomography Radioligands with Emphasis on P-Glycoprotein Transport

(2008) S. Syvanen et al.   DRUG METABOLISM AND DISPOSITION

Extensions to the Visual Predictive Check to facilitate model performance evaluation

(2008) Teun M. Post et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

First Demonstration of Cerebrospinal Fluid and Plasma A  Lowering with Oral Administration of a  -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates

(2008) S. Sankaranarayanan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Efficient Inhibition of the Alzheimer's Disease  -Secretase by Membrane Targeting

(2008) L. Rajendran et al.   SCIENCE