157 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
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 diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.
Merck Research Laboratories
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
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists.
Pharmacopeia
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
Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats.
Idorsia Pharmaceuticals
Design and synthesis of novel orexin 2 receptor agonists with a 1,3,5‑trioxazatriquinane skeleton.
University of Tsukuba
Novel 3-Aminopyrrolidine and Piperidine Macrocyclic Orexin Receptor Agonists for Treating Sleep Disorders.
Smith, Gambrell & Russell
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
Orexin Receptor Agonists as Possible Treatment for Narcolepsy and Idiopathic Hypersomnia.
Therachem Research Medilab
Novel Macrocyclic Urea Orexin Receptor Agonists for Treating Sleep Disorders.
Smith, Gambrell & Russell
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
Novel 5-Alkyl Pyrrolidine Orexin Receptor Agonists for Treating Sleep Disorders.
Smith, Gambrell & Russell
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
Janssen Research & Development
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
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
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity.
University of Florida
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
Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists
Chronos Therapeutics
Amide compounds for treatment of immune and inflammatory disorders
Achillion Pharmaceuticals
1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives and preparation method therefor and use thereof
Southern Medical University
Isothiazolo[5,4-D]pyrimidine compound as IRAK4 inhibitor
Chia Tai Tianqing Pharmaceutical Group
Alpha-hydroxy phenylacetic acid pharmacophore or bioisostere Mcl-1 protein antagonists
Amgen
6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Compounds and compositions useful for treating disorders related to NTRK
Blueprint Medicines
Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders
AchÉ
3-oxa-8-azabicyclo[3.2.1]octane derivatives and their use in the treatment of cancer and hemoglobinopathies
Ctxt
Substituted N-[2-(4-phenoxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide and N-[2-(4-benzyloxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide derivatives P2X7 receptor antagonists
Axxam
3-oxa-8-azabicyclo[3.2.1]octane derivatives and their use in the treatment of cancer and hemoglobinopathies
Ctxt
Discovery of potent inhibitors of PLproCoV2 by screening a library of selenium-containing compounds
University Ofamsterdam
Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof
University of Texas
C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
Merck Sharp & Dohme
Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase.
Institute For Advanced Studies In Basic Sciences (Iasbs)
Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.
South Dakota State University
Acetaldehyde-derived modifications on cytosolic human carbonic anhydrases.
University of Tampere and Tampere University Hospital
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.
Shandong University
Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.
Ataturk University
Digoxin derivatives with enhanced selectivity for the a2 isoform of Na,K-ATPase: effects on intraocular pressure in rabbits.
Weizmann Institute of Science
Affinity Selection-Mass Spectrometry Identifies a Novel Antibacterial RNA Polymerase Inhibitor.
Merck
hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.
University of California Riverside
Site-specific inhibitory mechanism for amyloid ß42 aggregation by catechol-type flavonoids targeting the Lys residues.
Kyoto University
Sulfur-containing heterocyclic derivative having Beta secretase inhibitory activity
Shionogi
4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
Actelion Pharmaceuticals
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities.
Yueyang Vocational Technical College
Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibitors: A hybrid pharmacophore approach.
Indian Institute of Technology (Banaras Hindu University)
Blind prediction of host-guest binding affinities: a new SAMPL3 challenge.
University of California San Diego
Boronic acid bearing liphagane compounds as inhibitors of P13K-α and/or β
Counsel of Scientific & Industrial Research
Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group
Bayer Intellectual Property
Structural basis for low-affinity binding of non-R2 carboxylate-substituted tricyclic quinoline analogs to CK2a: comparative molecular dynamics simulation studies.
Beijing University of Technology
Identification of 1, 4-Dihydrothieno [3', 2':5, 6]thiopyrano[4, 3-c] pyrazole derivatives as human 5-Lipo-oxygenase inhibitors.
Peking University
Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
Johannes Gutenberg—Universitat Mainz
Characterization of nicotinamidases: steady state kinetic parameters, classwide inhibition by nicotinaldehydes, and catalytic mechanism.
Cornell University
Identification and Characterization of Small Molecule Inhibitors of a Plant Homeodomain Finger.
University of Wisconsin
A tertiary alcohol analog of gamma-hydroxybutyric acid as a specific gamma-hydroxybutyric acid receptor ligand.
University of Maryland
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.
Taisho Pharmaceutical
Characterization of a tropane radioligand, [(3)H]2beta-propanoyl-3beta-(4-tolyl) tropane ([(3)H]PTT), for dopamine transport sites in rat brain.
Wake Forest University
(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.
Smithkline Beecham Pharmaceuticals
GR127935: a potent and selective 5-HT1D receptor antagonist.
Glaxo Research and Development
A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.
The Scripps Research Institute
Psychotomimetic opiate receptors labeled and visualized with (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine.
TBA