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Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators

Bioorganic & medicinal chemistry letters, 2016-03, Vol.26 (6), p.1554-1557

2016

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The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers

The Journal of pharmacology and experimental therapeutics, 2016-07, Vol.358 (1), p.138

2016

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Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (22), p.127530, Article 127530

2020

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Discovery of S3-Truncated, C‑6 Heteroaryl Substituted Aminothiazine β‑Site APP Cleaving Enzyme‑1 (BACE1) Inhibitors

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8593-8600

2016

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What lessons can be learned from failed Alzheimer's disease trials?

Expert review of clinical pharmacology, 2015-05, Vol.8 (3), p.267-269

Toyn, Jeremy

2015

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Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (23), p.5729-5731

2016

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Pharmacodynamics of selective inhibition of γ-secretase by avagacestat

The Journal of pharmacology and experimental therapeutics, 2013-03, Vol.344 (3), p.686-695

2013

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Interpreting Alzheimer's disease clinical trials in light of the effects on amyloid-β

Alzheimer's research & therapy, 2014-01, Vol.6 (2), p.14-14

2014

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Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects

The Journal of pharmacology and experimental therapeutics, 2016-07, Vol.358 (1), p.125

2016

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Synergistic inhibition of Aβ production by combinations of γ-secretase modulators

European journal of pharmacology, 2017-10, Vol.812, p.104-112

2017

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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9208-9223

2012

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Design and optimization of tricyclic gamma-secretase modulators

Bioorganic & medicinal chemistry letters, 2016-03, Vol.26 (5), p.1498-1502

2016

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Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor

ACS medicinal chemistry letters, 2010-06, Vol.1 (3), p.120-124

2010

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Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents

ACS medicinal chemistry letters, 2016-03, Vol.7 (3), p.271-276

2016

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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE)

Bioorganic & medicinal chemistry letters, 2015-11, Vol.25 (22), p.5040-5047

2015

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Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481

ACS medicinal chemistry letters, 2019-03, Vol.10 (3), p.312-317

2019

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The Amyloid-β Rise and γ-Secretase Inhibitor Potency Depend on the Level of Substrate Expression

The Journal of biological chemistry, 2008-08, Vol.283 (34), p.22992-23003

2008

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γ-Secretase Modulators : Can We Combine Potency with Safety?

International journal of alzheimer's disease, 2012, Vol.2012 (2012), p.1-10

2012

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Viable mouse gene ablations that robustly alter brain Aβ levels are rare

BMC neuroscience, 2010-11, Vol.11 (1), p.143-143, Article 143

2010

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γ-Secretase-Dependent Proteolysis of Transmembrane Domain of Amyloid Precursor Protein : Successive Tri- and Tetrapeptide Release in Amyloid β-Protein Production

International journal of alzheimer's disease, 2012, Vol.2012 (2012), p.1-7

2012

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P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice

The Journal of pharmacology and experimental therapeutics, 2008-08, Vol.326 (2), p.502-513

2008

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Modulation of Gamma-Secretase for the Treatment of Alzheimer's Disease

International journal of alzheimer's disease, 2012, Vol.2012 (2012), p.1-10

2012

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Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.537-541

2011

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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (22), p.6916-6924

2011

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Bub2p-dependent spindle checkpoint pathway regulates the Dbf2p kinase in budding yeast

The EMBO journal, 1999-05, Vol.18 (9), p.2424-2434

1999

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Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators

The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers

Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite

Discovery of S3-Truncated, C‑6 Heteroaryl Substituted Aminothiazine β‑Site APP Cleaving Enzyme‑1 (BACE1) Inhibitors

What lessons can be learned from failed Alzheimer's disease trials?

Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat

Interpreting Alzheimer's disease clinical trials in light of the effects on amyloid-β

Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects

Synergistic inhibition of Aβ production by combinations of γ-secretase modulators

Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

Design and optimization of tricyclic gamma-secretase modulators

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor

Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE)

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481

The Amyloid-β Rise and γ-Secretase Inhibitor Potency Depend on the Level of Substrate Expression

γ-Secretase Modulators : Can We Combine Potency with Safety?

Viable mouse gene ablations that robustly alter brain Aβ levels are rare

γ-Secretase-Dependent Proteolysis of Transmembrane Domain of Amyloid Precursor Protein : Successive Tri- and Tetrapeptide Release in Amyloid β-Protein Production

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice

Modulation of Gamma-Secretase for the Treatment of Alzheimer's Disease

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

Bub2p-dependent spindle checkpoint pathway regulates the Dbf2p kinase in budding yeast

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