PMID

Data

Article Title

Organization

Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.

Wuxi Apptec (Shanghai)

Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.

Merck

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

University of Tsukuba

Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.

Smithkline Beecham Pharmaceuticals

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

Merck Research Laboratories

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

Merck Research Laboratories

Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).

Novartis Institutes For Biomedical Research

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

Kitasato University

Recent trends in orexin research--2010 to 2015.

Actelion Pharmaceuticals

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.

Eisai

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

TBA

Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.

Merck Research Laboratories

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.

Actelion Pharmaceuticals

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Merck Research Laboratories

Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.

Eisai

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

Merck Research Laboratories

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.

Merck Research Laboratories

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

Merck Research Laboratories

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.

Actelion Pharmaceuticals

Truncated Orexin Peptides: Structure-Activity Relationship Studies.

Research Triangle Institute

Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).

Merck Research Laboratories

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.

Novartis Institutes For Biomedical Research

Synthesis and evaluation of novel radioligands for positron emission tomography imaging of the orexin-2 receptor.

Eisai

Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.

Research Triangle Institute

Selective orexin receptor antagonists.

Janssen Pharmaceutica

Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.

Actelion Pharmaceuticals

Radiosynthesis and evaluation of [11C]EMPA as a potential PET tracer for orexin 2 receptors.

Harvard Medical School

Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.

Actelion Pharmaceuticals

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

Glaxosmithkline

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies.

Research Triangle Institute

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.

Scripps Florida

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Merck Research Laboratories

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.

Merck Research Laboratories

Proline bis-amides as potent dual orexin receptor antagonists.

Merck Research Laboratories

Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists.

Takeda Pharmaceutical

Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists.

Takeda Pharmaceutical

2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.

Glaxosmithkline

Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.

Merck Research Laboratories

Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.

Actelion Pharmaceuticals

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Actelion Pharmaceuticals

Biomedical application of orexin/hypocretin receptor ligands in neuroscience.

Actelion Pharmaceuticals

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

Merck Research Laboratories

Methyl-containing pharmaceuticals: Methylation in drug design.

Xenon Pharmaceuticals

Design and synthesis of novel orexin 2 receptor agonists with a 1,3,5?trioxazatriquinane skeleton.

University of Tsukuba

Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring.

University of Tsukuba

Essential structure of orexin 1 receptor antagonist YNT-707: Conversion of the 16-cyclopropylmethyl group to the 16-sulfonamide group in d-nor-nalfurafine derivatives.

University of Tsukuba

Design and synthesis of novel orexin 2 receptor agonists based on naphthalene skeleton.

University of Tsukuba

Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.

University of Tsukuba

Discovery of novel orexin receptor antagonists using a 1,3,5-trioxazatriquinane bearing multiple effective residues (TriMER) library.

University of Tsukuba

Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.

Takeda Pharmaceutical

Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists.

Research Triangle Institute

Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands.

University of Leipzig

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.

Banyu Tsukuba Research Institute

Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.

Janssen Research & Development

Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.

Philipps-University

Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.

Banyu Tsukuba Research Institute

Antagonists of Orexin Receptors as Potential Treatment of Sleep Disorders, Obesity, Eating Disorders, and Other Neurological and Psychiatric Disorders.

Therachem Research Medilab (India)

Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.

Taisho Pharmaceutical

Essential structure of orexin 1 receptor antagonist YNT-707, part V: Structure-activity relationship study of the substituents on the 17-amino group.

University of Tsukuba

Pharmacophore Model To Discover OX1 and OX2 Orexin Receptor Ligands.

University of Helsinki

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Palack£

Essential structure of orexin 1 receptor antagonist YNT-707, part III: Role of the 14-hydroxy and the 3-methoxy groups in antagonistic activity toward the orexin 1 receptor in YNT-707 derivatives lacking the 4,5-epoxy ring.

University of Tsukuba

Essential structure of orexin 1 receptor antagonist YNT-707, Part IV: The role of D-ring in 4,5-epoxymorphinan on the orexin 1 receptor antagonistic activity.

University of Tsukuba

Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.

Sosei Heptares

Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.

Johnson and Johnson Pharmaceutical Research and Development

Azulene-based compounds for targeting orexin receptors.

University of Helsinki

Essential structure of orexin 1 receptor antagonist YNT-707, Part II: Drastic effect of the 14-hydroxy group on the orexin 1 receptor antagonistic activity.

University of Tsukuba

Essential structure of orexin 1 receptor antagonist YNT-707, Part I: Role of the 4,5-epoxy ring for binding with orexin 1 receptor.

University of Tsukuba

Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide.

Taisho Pharmaceutical