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Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia

Journal of medicinal chemistry, 2016-01, Vol.59 (2), p.504-530

2016

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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia

Neuropharmacology, 2012-02, Vol.62 (2), p.978-987

2012

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Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist

Journal of neurogenetics, 2011-03, Vol.25 (1-2), p.52-61

2011

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Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia

Current topics in medicinal chemistry, 2011-03, Vol.11 (6), p.696-725

2011

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Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (1), p.126-132

2016

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Discovery of [11C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors

Bioorganic & medicinal chemistry letters, 2015-11, Vol.25 (21), p.4893-4898

2015

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Syntheses, Thermal Reactivities, and Computational Studies of Aryl-Fused Quinoxalenediynes: Effect of Extended Benzannelation on Bergman Cyclization Energetics

Journal of organic chemistry, 2012-11, Vol.77 (22), p.10329-10339

2012

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Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding

Bioorganic & medicinal chemistry letters, 2009-06, Vol.19 (11), p.2997-3001

2009

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Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP

Bioorganic & medicinal chemistry letters, 2005-04, Vol.15 (8), p.2041-2045

2005

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Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs

Anti-cancer agents in medicinal chemistry, 2010-11, Vol.10 (9), p.697-712

2010

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Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia

Journal of medicinal chemistry, 2023-01, Vol.66 (2), p.1157-1171

2023

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Stem Cell‐based therapies for COVID‐19‐related acute respiratory distress syndrome

Journal of cellular and molecular medicine, 2022-05, Vol.26 (9), p.2483-2504

2022

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Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP

Bioorganic & medicinal chemistry letters, 2006-06, Vol.16 (12), p.3175-3179

2006

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Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis

Journal of medicinal chemistry, 2015-10, Vol.58 (19), p.7888-7894

2015

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The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey

Neuropharmacology, 2013-01, Vol.64, p.215-223

2013

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Molecular markers and mechanisms of stroke: RNA studies of blood in animals and humans

Journal of Cerebral Blood Flow & Metabolism, 2011-07, Vol.31 (7), p.1513-1531

2011

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Genetic deletion and pharmacological inhibition of phosphodiesterase 10A protects mice from diet-induced obesity and insulin resistance

Diabetes (New York, N.Y.), 2014-01, Vol.63 (1), p.300-311

2014

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The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design

Bioorganic & medicinal chemistry letters, 2017-12, Vol.27 (23), p.5167-5171

2017

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SPINT2 is hypermethylated in both IDH1 mutated and wild-type glioblastomas, and exerts tumor suppression via reduction of c-Met activation

Journal of neuro-oncology, 2019-05, Vol.142 (3), p.423-434

2019

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D-2-Hydroxyglutarate Is Necessary and Sufficient for Isocitrate Dehydrogenase 1 Mutant-Induced MIR148A Promoter Methylation

Molecular cancer research, 2018-06, Vol.16 (6), p.947-960

2018

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Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction

ACS medicinal chemistry letters, 2021-04, Vol.12 (4), p.540-547

2021

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Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia

Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia

Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia

Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia

Discovery of [11C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors

Syntheses, Thermal Reactivities, and Computational Studies of Aryl-Fused Quinoxalenediynes: Effect of Extended Benzannelation on Bergman Cyclization Energetics

Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding

Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP

Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs

Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats

Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia

Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia

Stem Cell‐based therapies for COVID‐19‐related acute respiratory distress syndrome

Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP

Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis

The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey

Molecular markers and mechanisms of stroke: RNA studies of blood in animals and humans

Discovery of [(2R,5R)-5-{[(5-Fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): A Dual Orexin Receptor Antagonist with Potent Sleep-Promoting Properties

Genetic deletion and pharmacological inhibition of phosphodiesterase 10A protects mice from diet-induced obesity and insulin resistance

The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design

SPINT2 is hypermethylated in both IDH1 mutated and wild-type glioblastomas, and exerts tumor suppression via reduction of c-Met activation

D-2-Hydroxyglutarate Is Necessary and Sufficient for Isocitrate Dehydrogenase 1 Mutant-Induced MIR148A Promoter Methylation

Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer

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