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

Christopher D. Cox, Michael J. Breslin, David B. Whitman, +25

Journal of Medicinal Chemistry

Psychotropic MedicationPharmacotherapyPrimary InsomniaMolecular PharmacologyMedicinal Chemistry +15

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

Christopher J. Winrow, Anthony L. Gotter, Christopher D. Cox, +12

Neuropharmacology

Molecular PharmacologyPharmacological CharacterizationMedicinePhysiologyNeuropharmacology +5

Discovery of [(2<i>R</i>,5<i>R</i>)‐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

Paul J. Coleman, John D. Schreier, Christopher D. Cox, +23

ChemMedChem

Sleep DisordersNeurotransmitterPeptide SciencePharmacotherapyExperimental Pharmacology +17

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

Sean M. Smith, Jason M. Uslaner, Christopher D. Cox, +12

Neuropharmacology

Inhibitor Thpp-1Novel Phosphodiesterase 10ABehavioral NeuroscienceMedicinePharmacology +9

CO Cross‐Coupling of Activated Aryl and Heteroaryl Halides with Aliphatic Alcohols

Peter E. Maligres, Jing Li, Shane W. Krska, +2

Angewandte Chemie International Edition

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

David B. Whitman, Christopher D. Cox, Michael J. Breslin, +19

ChemMedChem

Discovery of 5′′‐Chloro‐<i>N</i>‐[(5,6‐dimethoxypyridin‐2‐yl)methyl]‐2,2′:5′,3′′‐terpyridine‐3′‐carboxamide (MK‐1064): A Selective Orexin 2 Receptor Antagonist (2‐SORA) for the Treatment of Insomnia

Anthony J. Roecker, Swati P. Mercer, John D. Schreier, +20

ChemMedChem

Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP

Anthony J. Roecker, Paul J. Coleman, Swati P. Mercer, +17

Bioorganic & Medicinal Chemistry Letters

BiochemistryNatural SciencesMacromolecular MachineMolecular BiologyKinesin Spindle Protein +5

Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors

Izzat T. Raheem, Abbas M. Walji, Daniel J. Klein, +25

Journal of Medicinal Chemistry

Lead CompoundsPharmacotherapyAntiviral DrugChemical BiologyPharmaceutical Chemistry +17

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

Izzat T. Raheem, Michael J. Breslin, Christine Fandozzi, +15

Bioorganic & Medicinal Chemistry Letters

Psychoactive DrugPsychiatryMedicinePsychotropic MedicationPsychopharmacology +7