AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics

Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design

(2015) Christopher R. Butler et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central A  Pharmacodynamic Responses in Mice, Dogs, and Humans

(2015) P. C. May et al.   JOURNAL OF NEUROSCIENCE

The Structural Evolution of β-Secretase Inhibitors: A Focus on the Development of Small-Molecule Inhibitors

(2014) Stefania Butini et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Molecular Mechanisms of Alzheimer Disease Protection by the A673T Allele of Amyloid Precursor Protein

(2014) Janice A. Maloney et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Revisiting the peripheral sink hypothesis: inhibiting BACE1 activity in the periphery does not alter β-amyloid levels in the CNS

(2014) Biljana Georgievska et al.   JOURNAL OF NEUROCHEMISTRY

CNS Amyloid- , Soluble APP-  and -  Kinetics during BACE Inhibition

(2014) J. A. Dobrowolska et al.   JOURNAL OF NEUROSCIENCE

BACE1 inhibitor drugs in clinical trials for Alzheimer’s disease

(2014) Robert Vassar   Alzheimers Research & Therapy

β-secretase inhibitor; a promising novel therapeutic drug in Alzheimer’s disease

(2014) Kelly Willemijn Menting et al.   Frontiers in Aging Neuroscience

Sustained peripheral depletion of amyloid-β with a novel form of neprilysin does not affect central levels of amyloid-β

(2013) Simon J. Henderson et al.   BRAIN

AZ-4217: A High Potency BACE Inhibitor Displaying Acute Central Efficacy in Different In Vivo Models and Reduced Amyloid Deposition in Tg2576 Mice

(2013) S. Eketjall et al.   JOURNAL OF NEUROSCIENCE

Population PKPD Modeling of BACE1 Inhibitor-Induced Reduction in Aβ Levels In Vivo and Correlation to In Vitro Potency in Primary Cortical Neurons from Mouse and Guinea Pig

(2013) Juliette Janson et al.   PHARMACEUTICAL RESEARCH

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

(2012) Fredrik Jeppsson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

New Aminoimidazoles as β-Secretase (BACE-1) Inhibitors Showing Amyloid-β (Aβ) Lowering in Brain

(2012) Ylva Gravenfors et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure- and Property-Based Design of Aminooxazoline Xanthenes as Selective, Orally Efficacious, and CNS Penetrable BACE Inhibitors for the Treatment of Alzheimer’s Disease

(2012) Hongbing Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Alzheimer's Disease: Presenilin 2-Sparing  -Secretase Inhibition Is a Tolerable A  Peptide-Lowering Strategy

(2012) T. Borgegard et al.   JOURNAL OF NEUROSCIENCE

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

(2012) Thorlakur Jonsson et al.   NATURE

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

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

The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

(2011) Eric Karran et al.   NATURE REVIEWS DRUG DISCOVERY

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

Application of a Dried-DMSO rapid throughput 24-h equilibrium solubility in advancing discovery candidates

(2009) Yun W. Alelyunas et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

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