Orexin receptor antagonists – a patent review (2010 to August 2014)

To Dream, Perchance Of Sleep

(2015)   CHEMICAL & ENGINEERING NEWS

Discovery of MK-3697: A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia

(2014) Anthony J. Roecker et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant

(2014) Scott D. Kuduk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure–activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1

(2014) Thierry Sifferlen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor Antagonist

(2014) Christoph Boss et al.   ChemMedChem

Entry-into-humans study with ACT-462206, a novel dual orexin receptor antagonist, comparing its pharmacodynamics with almorexant

(2014) Matthias Hoch et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Effects of a newly developed potent orexin-2 receptor-selective antagonist, compound 1 m, on sleep/wakefulness states in mice

(2014) Keishi Etori et al.   Frontiers in Neuroscience

Discovery and development of orexin receptor antagonists as therapeutics for insomnia

(2013) C J Winrow et al.   BRITISH JOURNAL OF PHARMACOLOGY

Discovery of 5′′-Chloro-N-[(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

(2013) Anthony J. Roecker et al.   ChemMedChem

Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist

(2013) Michel A. Steiner et al.   ChemMedChem

Synthesis and Evaluation of Novel Radioligands for Positron Emission Tomography Imaging of the Orexin-2 Receptor

(2013) Norihito Oi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia

(2013) Claudia Betschart et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Paul J. Coleman et al.   ChemMedChem

Differential Roles of Orexin Receptor-1 and -2 in the Regulation of Non-REM and REM Sleep

(2011) M. Mieda et al.   JOURNAL OF NEUROSCIENCE

Orexin Receptor Antagonists: A New Concept In CNS Disorders?

(2010) John Gatfield et al.   ChemMedChem

Lateral hypothalamic orexin/hypocretin neurons: A role in reward-seeking and addiction

(2009) Gary Aston-Jones et al.   BRAIN RESEARCH

Biomedical Application of Orexin/Hypocretin Receptor Ligands in Neuroscience

(2009) Christoph Boss et al.   JOURNAL OF MEDICINAL CHEMISTRY

Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat

(2009) C. Dugovic et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Biochemical and Electrophysiological Characterization of Almorexant, a Dual Orexin 1 Receptor (OX1)/Orexin 2 Receptor (OX2) Antagonist: Comparison with Selective OX1 and OX2 Antagonists

(2009) P. Malherbe et al.   MOLECULAR PHARMACOLOGY

A key role for orexin in panic anxiety

(2009) Philip L Johnson et al.   NATURE MEDICINE

Functions of orexins in peripheral tissues

(2008) M. V. Heinonen et al.   Acta Physiologica