52 articles for thisTarget
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Article Title
Organization
Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Merck Research Laboratories
Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.
Astrazeneca
Pseudosaccharin amines as potent and selective KV1.5 blockers.
Bristol-Myers Squibb Research and Development
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Astrazeneca
Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.
Bristol-Myers Squibb
Synthesis and evaluation of diphenylphosphinic amides and diphenylphosphine oxides as inhibitors of Kv1.5.
Astrazeneca
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Bristol-Myers Squibb
Pyrano-[2,3b]-pyridines as potassium channel antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.
Cardiome Pharma
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
Abbott Laboratories
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.
Glaxosmithkline
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Merck Research Laboratories
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers.
Bristol-Myers Squibb Pharmaceutical Research and Development
Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists.
Bristol-Myers Squibb
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Wyeth Research
Benzopyran sulfonamides as KV1.5 potassium channel blockers.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Merck Research Laboratories
Evolution of thiazolidine-based blockers of human Kv1.5 for the treatment of atrial arrhythmias.
Procter and Gamble Pharmaceuticals
Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers.
Procter & Gamble Pharmaceuticals
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Merck Research Laboratories
Discovery and synthesis of tetrahydroindolone-derived carbamates as Kv1.5 blockers.
Procter and Gamble Pharmaceuticals
Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers.
Procter & Gamble Pharmaceuticals
Synthesis and evaluation of (2-phenethyl-2H-1,2,3-triazol-4-yl)(phenyl)methanones as Kv1.5 channel blockers for the treatment of atrial fibrillation.
Procter & Gamble Pharmaceuticals
A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
Institute of Medical Research Biotechnology Centre
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of
Ucb
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.
Aventis Pharma Deutschland
Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5.
Aventis Pharma Deutschland
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Sareum
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
University of Washington
Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.
Bristol-Myers Squibb
Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease.
TBA
Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.
Astrazeneca
Alkoxypsoralens, novel nonpeptide blockers of Shaker-type K+ channels: synthesis and photoreactivity.
University of Kiel
Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel.
Astrazeneca
Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors.
China Pharmaceutical University
Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels.
University of Ljubljana
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid)
Sage Therapeutics
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Vanderbilt University Institute of Imaging Science