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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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Breakthroughs in neuroactive steroid drug discovery

Bioorganic & medicinal chemistry letters, 2018-01, Vol.28 (2), p.61-70

2018

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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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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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Highly Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitors

Journal of medicinal chemistry, 2011-11, Vol.54 (21), p.7621-7638

2011

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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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WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A novel 5-hydroxytryptamine 2C receptor-selective agonist with preclinical antipsychotic-like activity

The Journal of pharmacology and experimental therapeutics, 2007-01, Vol.320 (1), p.486

2007

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Discovery of Imidazo[1,5-a]pyrido[3,2-e]pyrazines as a New Class of Phosphodiesterase 10A Inhibitiors

Journal of medicinal chemistry, 2010-06, Vol.53 (11), p.4399-4411

2010

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WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity

The Journal of pharmacology and experimental therapeutics, 2005-05, Vol.313 (2), p.862

2005

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Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist

The Journal of pharmacology and experimental therapeutics, 2011-06, Vol.337 (3), p.673

2011

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Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503

Brain research, 2006-02, Vol.1073-1074, p.240-251

2006

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Acylguanidines as Small-Molecule β-Secretase Inhibitors

Journal of medicinal chemistry, 2006-10, Vol.49 (21), p.6158-6161

2006

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Novel triazines as potent and selective phosphodiesterase 10A inhibitors

Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (18), p.5876-5884

2012

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Acylguanidine inhibitors of β-secretase : Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

Bioorganic & medicinal chemistry letters, 2008-02, Vol.18 (3), p.1063-1066

2008

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Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (3), p.824-827

2010

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Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405)

The Journal of pharmacology and experimental therapeutics, 2008-04, Vol.325 (1), p.134

2008

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Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives

Bioorganic & medicinal chemistry, 2008-07, Vol.16 (14), p.6707-6723

2008

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3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT6 receptor modulators

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1657-1660

2010

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Advances toward New Antidepressants with Dual Serotonin Transporter and 5-HT1A Receptor Affinity within a Class of 3-Aminochroman Derivatives. Part 2

Journal of medicinal chemistry, 2008-11, Vol.51 (21), p.6980-7004

2008

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3,4-Dihydropyrimido(1,2- a)indol-10(2 H)-ones as potent non-peptidic inhibitors of caspase-3

Bioorganic & medicinal chemistry, 2009-11, Vol.17 (22), p.7755-7768

2009

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Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT1A receptor and the serotonin transporter

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (1), p.222-227

2010

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Studies toward the discovery of the next generation of antidepressants. Part 5 : 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1338-1341

2006

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Acylguanidine inhibitors of β-secretase : Optimization of the pyrrole ring substituents extending into the S'1 substrate binding pocket

Bioorganic & medicinal chemistry letters, 2008-01, Vol.18 (2), p.767-771

2008

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Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT1A Receptor Antagonists

Journal of medicinal chemistry, 2009-08, Vol.52 (15), p.4955-4959

2009

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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

Breakthroughs in neuroactive steroid drug discovery

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

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

Highly Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitors

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

WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole]: A novel 5-hydroxytryptamine 2C receptor-selective agonist with preclinical antipsychotic-like activity

Discovery of Imidazo[1,5-a]pyrido[3,2-e]pyrazines as a New Class of Phosphodiesterase 10A Inhibitiors

WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity

Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist

Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503

Acylguanidines as Small-Molecule β-Secretase Inhibitors

Novel triazines as potent and selective phosphodiesterase 10A inhibitors

Acylguanidine inhibitors of β-secretase : Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405)

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives

3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT6 receptor modulators

Advances toward New Antidepressants with Dual Serotonin Transporter and 5-HT1A Receptor Affinity within a Class of 3-Aminochroman Derivatives. Part 2

3,4-Dihydropyrimido(1,2- a)indol-10(2 H)-ones as potent non-peptidic inhibitors of caspase-3

Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT1A receptor and the serotonin transporter

Studies toward the discovery of the next generation of antidepressants. Part 5 : 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity

The Synthesis and Biological Evaluation of Quinolyl-piperazinyl Piperidines as Potent Serotonin 5-HT1A Antagonists

Acylguanidine inhibitors of β-secretase : Optimization of the pyrrole ring substituents extending into the S'1 substrate binding pocket

Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT1A Receptor Antagonists

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