136 articles for thisTarget
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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
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
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
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
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