Orexin research: patent news from 2016

Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies

(2017) Hiroshi Nagase et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of ghrelin-induced feeding in rats by pretreatment with a novel dual orexin receptor antagonist

(2017) Mariko So et al.   Journal of Physiological Sciences

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology

(2016) Craig A. Stump et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach

(2016) Bibia Heidmann et al.   ChemMedChem

Pharmacophore Model To Discover OX1 and OX2 Orexin Receptor Ligands

(2016) Ainoleena Turku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An alerting structure: human orexin receptor 1

(2016) Daniel Wacker et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An alerting structure: human orexin receptor 1

(2016) Daniel Wacker et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man

(2016) Anthony L. Gotter et al.   Scientific Reports

Recent trends in orexin research—2010 to 2015

(2015) Christoph Boss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2015) Anthony J. Roecker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate

(2015) Michael A. Letavic et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the First Selective, Nonpeptidic Orexin 2 Receptor Agonists

(2015) Alexander Heifetz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tactical Approaches to Interconverting GPCR Agonists and Antagonists

(2015) Peter I. Dosa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist

(2015) Yu Yoshida et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists

(2015) Takashi Nagahara et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The orexin type 1 receptor is overexpressed in advanced prostate cancer with a neuroendocrine differentiation, and mediates apoptosis

(2014) David Alexandre et al.   EUROPEAN JOURNAL OF CANCER

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

(2014) Christoph Boss   EXPERT OPINION ON THERAPEUTIC PATENTS

Orexin neurons suppress narcolepsy via 2 distinct efferent pathways

(2014) Emi Hasegawa et al.   JOURNAL OF CLINICAL INVESTIGATION

Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant

(2014) Jie Yin et al.   NATURE

Motivational activation: a unifying hypothesis of orexin/hypocretin function

(2014) Stephen V Mahler et al.   NATURE NEUROSCIENCE

Hypocretin (orexin) regulation of sleep-to-wake transitions

(2014) Luis de Lecea et al.   Frontiers in Pharmacology

Orexin/hypocretin receptor signalling: a functional perspective

(2013) C S Leonard et al.   BRITISH JOURNAL OF PHARMACOLOGY

Orexin/hypocretin receptor signalling cascades

(2013) J P Kukkonen 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

Differential actions of orexin receptors in brainstem cholinergic and monoaminergic neurons revealed by receptor knockouts: implications for orexinergic signaling in arousal and narcolepsy

(2013) Kristi A. Kohlmeier et al.   Frontiers in Neuroscience

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

Orexin Receptor Antagonism, a New Sleep-Enabling Paradigm: A Proof-of-Concept Clinical Trial

(2012) P Hoever et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Orexin receptor antagonism for treatment of insomnia: A randomized clinical trial of suvorexant

(2012) W. J. Herring et al.   NEUROLOGY

Dual Hypocretin Receptor Antagonism Is More Effective for Sleep Promotion than Antagonism of Either Receptor Alone

(2012) Stephen R. Morairty et al.   PLoS One

The Orexin Antagonist SB-649868 Promotes and Maintains Sleep in Men with Primary Insomnia

(2012) Paolo Bettica et al.   SLEEP

Aberrant Expression of OX1 Receptors for Orexins in Colon Cancers and Liver Metastases: an Openable Gate to Apoptosis

(2011) T. Voisin et al.   CANCER RESEARCH

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

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