115 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
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
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.
Banyu Tsukuba Research Institute
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
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
Glutathione transferase from Plasmodium falciparum--interaction with malagashanine and selected plant natural products.
University Of Zimbabwe
Conferin, potent antioxidant and anti-inflammatory isoflavone from Caragana conferta Benth.
University Of Karachi
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms.
Universitätsklinikum Frankfurt
Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.
University Of North Carolina
Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.
Merck Research Laboratories
A(3) adenosine receptors in human neutrophils and promyelocytic HL60 cells: a pharmacological and biochemical study.
University Of Ferrara
Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels.
Synaptic Pharmaceutical
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Smithkline Beecham Pharmaceuticals
Pharmacokinetic/pharmacodynamic relationship of benzodiazepines in the direct cortical stimulation model of anticonvulsant effect.
Leiden University
Structural combination of established 5-HT(2A) receptor ligands: new aspects of the binding mode.
University Of Mainz
A new screening assay for allosteric inhibitors of cSrc.
Chemical Genomics Centre Of The Max Planck Society
Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1).
University Of Manchester
Tetraiodobenzimidazoles are potent inhibitors of protein kinase CK2.
University Of Padova
5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.
Anadys Pharmaceuticals
Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins.
Sapienza University Of Rome
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Abbott Laboratories
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Bristol-Myers Squibb
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.
Monash University
Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid.
Universita Degli Studi Di Firenze
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.
Gsk
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Wyeth Research
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.
Gsk
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
National Institutes Of Health
Phylogenomic Analysis of the Microviridin Biosynthetic Pathway Coupled with Targeted Chemo-Enzymatic Synthesis Yields Potent Protease Inhibitors.
University Of Helsinki
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.
Pfizer
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
Merck Research Laboratories