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The Target of Ezetimibe Is Niemann-Pick C1-Like 1 (NPC1L1)

Proceedings of the National Academy of Sciences - PNAS, 2005-06, Vol.102 (23), p.8132-8137

2005

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Strategic and Tactical Approaches to the Synthesis of 5,6-Dihydro-[1,2,4]oxadiazines

Heterocycles, 2016-12, Vol.92 (12), p.2166

2016

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Discovery of Orally Efficacious Tetracyclic Metabotropic Glutamate Receptor 1 (mGluR1) Antagonists for the Treatment of Chronic Pain

Journal of medicinal chemistry, 2007-11, Vol.50 (23), p.5550-5553

2007

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Intracellular Retention of Three Quinuclidine Derivatives in Caco-2 Permeation Experiments: Mechanisms and Impact on Estimating Permeability and Active Efflux Ratio

Drug metabolism letters, 2016-09, Vol.10 (3), p.161-171

2016

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Beta-lactam cholesterol absorption inhibitors

Current medicinal chemistry, 2004-07, Vol.11 (14), p.1873-1887

Burnett, Duane A

2004

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Discovery of quinuclidine modulators of cellular progranulin

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128209-128209, Article 128209

2021

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The identification of intestinal scavenger receptor class B, type I (SR-BI) by expression cloning and its role in cholesterol absorption

Biochimica et biophysica acta, 2002-01, Vol.1580 (1), p.77-93

2002

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Discovery and characterization of novel TRPML1 agonists

Bioorganic & medicinal chemistry letters, 2024-01, Vol.98, p.129595-129595, Article 129595

2024

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Discovery of oxazoline enhancers of cellular progranulin release

Bioorganic & medicinal chemistry letters, 2023-01, Vol.80, p.129048-129048, Article 129048

2023

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Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.14426-14447

2021

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Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer’s Disease

Journal of medicinal chemistry, 2017-03, Vol.60 (6), p.2383-2400

2017

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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8806-8817

2015

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Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP‑4 Inhibitors for the Treatment of Type 2 Diabetes

ACS medicinal chemistry letters, 2016-05, Vol.7 (5), p.498-501

2016

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Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Bioorganic & medicinal chemistry, 2016-11, Vol.24 (21), p.5534-5545

2016

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Identification of Presenilin 1-Selective γ-Secretase Inhibitors with Reconstituted γ-Secretase Complexes

Biochemistry (Easton), 2011-06, Vol.50 (22), p.4973-4980

2011

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SAR of tricyclic sulfones as γ-secretase inhibitors

Science China. Chemistry, 2011-11, Vol.54 (11), p.1688-1701

2011

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Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (23), p.5836-5841

2016

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Characterization of FRM-36143 as a new γ-secretase modulator for the potential treatment of familial Alzheimer's disease

Alzheimer's research & therapy, 2016-08, Vol.8 (1), p.34-34, Article 34

2016

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Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)- hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption

Journal of medicinal chemistry, 1998-03, Vol.41 (6), p.973-980

1998

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Dopamine D1/D5 Receptor Antagonists with Improved Pharmacokinetics: Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of Benzazepine D1/D5 Antagonists

Journal of medicinal chemistry, 2005-02, Vol.48 (3), p.680-693

2005

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Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (4), p.1575-1578

2012

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Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.844-849

2013

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Iminoheterocycles as γ-secretase modulators

Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (18), p.5380-5384

2010

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Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (3), p.311-314

2002

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Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure–activity relationship studies

Bioorganic & medicinal chemistry letters, 2010-06, Vol.20 (12), p.3632-3635

2010

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The Target of Ezetimibe Is Niemann-Pick C1-Like 1 (NPC1L1)

Strategic and Tactical Approaches to the Synthesis of 5,6-Dihydro-[1,2,4]oxadiazines

Discovery of Orally Efficacious Tetracyclic Metabotropic Glutamate Receptor 1 (mGluR1) Antagonists for the Treatment of Chronic Pain

Intracellular Retention of Three Quinuclidine Derivatives in Caco-2 Permeation Experiments: Mechanisms and Impact on Estimating Permeability and Active Efflux Ratio

Beta-lactam cholesterol absorption inhibitors

Discovery of quinuclidine modulators of cellular progranulin

The identification of intestinal scavenger receptor class B, type I (SR-BI) by expression cloning and its role in cholesterol absorption

Discovery and characterization of novel TRPML1 agonists

Discovery of oxazoline enhancers of cellular progranulin release

Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator

Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer’s Disease

Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP‑4 Inhibitors for the Treatment of Type 2 Diabetes

Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Identification of Presenilin 1-Selective γ-Secretase Inhibitors with Reconstituted γ-Secretase Complexes

SAR of tricyclic sulfones as γ-secretase inhibitors

Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

Characterization of FRM-36143 as a new γ-secretase modulator for the potential treatment of familial Alzheimer's disease

Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)- hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption

Dopamine D1/D5 Receptor Antagonists with Improved Pharmacokinetics: Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of Benzazepine D1/D5 Antagonists

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

Iminoheterocycles as γ-secretase modulators

Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure–activity relationship studies

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