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Investigational BACE inhibitors for the treatment of Alzheimer's disease

Expert opinion on investigational drugs, 2019-11, Vol.28 (11), p.967-975

2019

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Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead

European journal of medicinal chemistry, 2018-03, Vol.148, p.436-452

2018

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Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function

Biological psychiatry (1969), 2018-10, Vol.84 (7), p.478-487

2018

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Role of monomeric amyloid-β in cognitive performance in Alzheimer's disease: Insights from clinical trials with secretase inhibitors and monoclonal antibodies

Pharmacological research, 2023-01, Vol.187, p.106631-106631, Article 106631

2023

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Synthesis, Optimization, and Large-Scale Preparation of the Low-Dose Central Nervous System-Penetrant BACE1 Inhibitor LY3202626 via a [3 + 2] Nitrone Cycloaddition

Organic process research & development, 2020-02, Vol.24 (2), p.306-314

2020

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New Highly Selective BACE1 Inhibitors and Their Effects on Dendritic Spine Density In Vivo

International journal of molecular sciences, 2023-07, Vol.24 (15), p.12283

2023

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Evaluation of a Series of β‑Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads

ACS medicinal chemistry letters, 2019-08, Vol.10 (8), p.1159-1165

2019

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Further analyses of the safety of verubecestat in the phase 3 EPOCH trial of mild-to-moderate Alzheimer's disease

Alzheimer's research & therapy, 2019-08, Vol.11 (1), p.68-68, Article 68

2019

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Passive immunotherapy with a novel antibody against 3pE-modified Aβ demonstrates potential for enhanced efficacy and favorable safety in combination with BACE inhibitor treatment in plaque-depositing mice

Neurobiology of disease, 2021-07, Vol.154, p.105365-105365, Article 105365

2021

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Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine β-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation

Bioorganic & medicinal chemistry letters, 2018-04, Vol.28 (6), p.1111-1115

2018

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Do BACE inhibitor failures in Alzheimer patients challenge the amyloid hypothesis of the disease?

Expert review of neurotherapeutics, 2019-07, Vol.19 (7), p.599-602

2019

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A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo

ACS medicinal chemistry letters, 2022-01, Vol.13 (1), p.76-83

2022

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3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors

Bioorganic & medicinal chemistry letters, 2020-04, Vol.30 (8), p.126999, Article 126999

2020

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Evaluation of Small-Animal PET Outcome Measures to Detect Disease Modification Induced by BACE Inhibition in a Transgenic Mouse Model of Alzheimer Disease

Journal of Nuclear Medicine, 2017-12, Vol.58 (12), p.1977-1983

2017

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BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Medicinal research reviews, 2020-01, Vol.40 (1), p.339-384

2020

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

Journal of neurochemistry, 2015-02, Vol.132 (4), p.477-486

2015

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Retinal Optical Coherence Tomography Metrics Are Unchanged in Verubecestat Alzheimer’s Disease Clinical Trial but Correlate with Baseline Regional Brain Atrophy

Journal of Alzheimer's disease, 2021-01, Vol.79 (1), p.275-287

2021

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The Alzheimer's Prevention Initiative Generation Program: Evaluating CNP520 Efficacy in the Prevention of Alzheimer's Disease

The Journal of Prevention of Alzheimer's Disease, 2017, Vol.4 (4), p.242-5

2017

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Transgenic amyloid precursor protein mouse models of amyloidosis. Incomplete models for Alzheimer's disease but effective predictors of anti‐amyloid therapies

Alzheimer's & dementia, 2024-02, Vol.20 (2), p.1459-1464

2024

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What Threshold of Amyloid Reduction Is Necessary to Meaningfully Improve Cognitive Function in Transgenic Alzheimer’s Disease Mice?

JAD reports, 2024-02, Vol.8 (1), p.371-385

2024

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CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

The Journal of neuroscience, 2014-06, Vol.34 (24), p.8336-8346

2014

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Fluorinated Molecules and Nanotechnology: Future 'Avengers' against the Alzheimer's Disease?

International journal of molecular sciences, 2020-04, Vol.21 (8), p.2989

2020

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Functions of the Alzheimer’s Disease Protease BACE1 at the Synapse in the Central Nervous System

Journal of molecular neuroscience, 2016-11, Vol.60 (3), p.305-315

2016

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Emerging drugs to reduce abnormal β-amyloid protein in Alzheimer's disease patients

Expert opinion on emerging drugs, 2016-12, Vol.21 (4), p.377-391

2016

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Investigational BACE inhibitors for the treatment of Alzheimer's disease

Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead

Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function

Role of monomeric amyloid-β in cognitive performance in Alzheimer's disease: Insights from clinical trials with secretase inhibitors and monoclonal antibodies

Synthesis, Optimization, and Large-Scale Preparation of the Low-Dose Central Nervous System-Penetrant BACE1 Inhibitor LY3202626 via a [3 + 2] Nitrone Cycloaddition

New Highly Selective BACE1 Inhibitors and Their Effects on Dendritic Spine Density In Vivo

Evaluation of a Series of β‑Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads

Further analyses of the safety of verubecestat in the phase 3 EPOCH trial of mild-to-moderate Alzheimer's disease

Passive immunotherapy with a novel antibody against 3pE-modified Aβ demonstrates potential for enhanced efficacy and favorable safety in combination with BACE inhibitor treatment in plaque-depositing mice

Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine β-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation

Do BACE inhibitor failures in Alzheimer patients challenge the amyloid hypothesis of the disease?

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo

3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors

Evaluation of Small-Animal PET Outcome Measures to Detect Disease Modification Induced by BACE Inhibition in a Transgenic Mouse Model of Alzheimer Disease

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

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

The BACE‐1 inhibitor CNP520 for prevention trials in Alzheimer's disease

Retinal Optical Coherence Tomography Metrics Are Unchanged in Verubecestat Alzheimer’s Disease Clinical Trial but Correlate with Baseline Regional Brain Atrophy

The Alzheimer's Prevention Initiative Generation Program: Evaluating CNP520 Efficacy in the Prevention of Alzheimer's Disease

Transgenic amyloid precursor protein mouse models of amyloidosis. Incomplete models for Alzheimer's disease but effective predictors of anti‐amyloid therapies

What Threshold of Amyloid Reduction Is Necessary to Meaningfully Improve Cognitive Function in Transgenic Alzheimer’s Disease Mice?

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

Fluorinated Molecules and Nanotechnology: Future 'Avengers' against the Alzheimer's Disease?

Functions of the Alzheimer’s Disease Protease BACE1 at the Synapse in the Central Nervous System

Emerging drugs to reduce abnormal β-amyloid protein in Alzheimer's disease patients

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