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Discovery of a Tetracyclic Quinoxaline Derivative as a Potent and Orally Active Multifunctional Drug Candidate for the Treatment of Neuropsychiatric and Neurological Disorders

Journal of medicinal chemistry, 2014-03, Vol.57 (6), p.2670-2682

2014

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Rearrangement of 3,3-Disubstituted Indolenines and Synthesis of 2,3-Substituted Indoles

Organic letters, 2006-12, Vol.8 (25), p.5769-5771

2006

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Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

Neuropharmacology, 2020-12, Vol.181, p.108333-108333, Article 108333

2020

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Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano‑1H‑pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor

Journal of medicinal chemistry, 2017-09, Vol.60 (18), p.7810-7819

2017

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Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABA A receptor positive allosteric modulator

Neuropharmacology, 2020-12, Vol.181, p.108333

2020

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The major brain cholesterol metabolite 24(S)-hydroxycholesterol is a potent allosteric modulator of N-methyl-D-aspartate receptors

The Journal of neuroscience, 2013-10, Vol.33 (44), p.17290-17300

2013

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Identification of a series of benzoxazoles as potent 5-HT6 ligands

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (4), p.1115-1117

2009

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Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases

Journal of medicinal chemistry, 2019-07, Vol.62 (13), p.5979-6002

2019

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Pharmacological characterization of SAGE‐718, a novel positive allosteric modulator of N‐methyl‐d‐aspartate receptors

British journal of pharmacology, 2024-04, Vol.181 (7), p.1028-1050

2024

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Novel neuroactive steroids as positive allosteric modulators of NMDA receptors: mechanism, site of action, and rescue pharmacology on GRIN variants associated with neurological conditions

Cellular and molecular life sciences : CMLS, 2023-02, Vol.80 (2), p.42-42, Article 42

2023

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SAGE-718: A First-in-Class N‑Methyl‑d‑Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment

Journal of medicinal chemistry, 2022-07, Vol.65 (13), p.9063-9075

2022

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Asymmetric Synthesis of the Squalene Synthase Inhibitor Zaragozic Acid C

Journal of the American Chemical Society, 1994-12, Vol.116 (26), p.12111-12112

1994

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Neuroactive Steroid N‑Methyl‑d‑aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity

Journal of medicinal chemistry, 2019-08, Vol.62 (16), p.7526-7542

2019

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Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human β-Secretase (BACE1) Inhibitors

Journal of medicinal chemistry, 2010-02, Vol.53 (3), p.1146-1158

2010

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5-HT6 medicinal chemistry

International review of neurobiology, 2010, Vol.94, p.1-34

2010

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Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure–Activity Relationships of Heterocyclic Substitution at C‑21

Journal of medicinal chemistry, 2015-04, Vol.58 (8), p.3500-3511

2015

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WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: a novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity

The Journal of pharmacology and experimental therapeutics, 2010-01, Vol.332 (1), p.190

2010

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Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models

Epilepsy research, 2017-08, Vol.134, p.16-25

2017

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The synthetic neuroactive steroid SGE-516 reduces status epilepticus and neuronal cell death in a rat model of soman intoxication

Epilepsy & behavior, 2017-03, Vol.68, p.22-30

2017

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5-HT6 antagonists as potential treatment for cognitive dysfunction

Drug development research, 2009-03, Vol.70 (2), p.145-168

2009

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One-pot synthesis of highly substituted indolines

Tetrahedron, 2010-01, Vol.66 (3), p.573-577

2010

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5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

Journal of medicinal chemistry, 2010-11, Vol.53 (21), p.7639-7646

2010

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Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators

Journal of medicinal chemistry, 2011-07, Vol.54 (14), p.5070-5081

2011

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Approaches to palliative therapies for Alzheimer's disease

Current topics in medicinal chemistry, 2006-03, Vol.6 (6), p.553

Robichaud, Albert J

2006

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Di-substituted pyridinyl aminohydantoins as potent and highly selective human β-secretase (BACE1) inhibitors

Bioorganic & medicinal chemistry, 2010-01, Vol.18 (2), p.630-639

2010

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Discovery of a Tetracyclic Quinoxaline Derivative as a Potent and Orally Active Multifunctional Drug Candidate for the Treatment of Neuropsychiatric and Neurological Disorders

Rearrangement of 3,3-Disubstituted Indolenines and Synthesis of 2,3-Substituted Indoles

Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano‑1H‑pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor

Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABA A receptor positive allosteric modulator

The major brain cholesterol metabolite 24(S)-hydroxycholesterol is a potent allosteric modulator of N-methyl-D-aspartate receptors

Identification of a series of benzoxazoles as potent 5-HT6 ligands

Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases

Pharmacological characterization of SAGE‐718, a novel positive allosteric modulator of N‐methyl‐d‐aspartate receptors

Novel neuroactive steroids as positive allosteric modulators of NMDA receptors: mechanism, site of action, and rescue pharmacology on GRIN variants associated with neurological conditions

SAGE-718: A First-in-Class N‑Methyl‑d‑Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment

Asymmetric Synthesis of the Squalene Synthase Inhibitor Zaragozic Acid C

Neuroactive Steroid N‑Methyl‑d‑aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity

Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human β-Secretase (BACE1) Inhibitors

5-HT6 medicinal chemistry

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure–Activity Relationships of Heterocyclic Substitution at C‑21

WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: a novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity

Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models

The synthetic neuroactive steroid SGE-516 reduces status epilepticus and neuronal cell death in a rat model of soman intoxication

5-HT6 antagonists as potential treatment for cognitive dysfunction

One-pot synthesis of highly substituted indolines

5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators

Approaches to palliative therapies for Alzheimer's disease

Di-substituted pyridinyl aminohydantoins as potent and highly selective human β-secretase (BACE1) inhibitors

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