PMID

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Article Title

Organization

Discovery of a novel Kv7 channel opener as a treatment for epilepsy.

Pfizer

Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.

University of Kansas Specialized Chemistry Center

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

Bristol-Myers Squibb

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Novel KCNQ2/Q3 agonists as potential therapeutics for epilepsy and neuropathic pain.

Icagen

(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.

Vanderbilt University Medical Center

3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.

Astrazeneca

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.

Vanderbilt University Medical Center

N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.

TBA

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis and biological activity of pyrazolo[1,5-a]pyrimidin-7(4H)-ones as novel Kv7/KCNQ potassium channel activators.

Hebei Medical University

Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Abbott Laboratories

Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.

Shanghai Institute of Materia Medica

Beyond Retigabine: Design, Synthesis, and Pharmacological Characterization of a Potent and Chemically Stable Neuronal Kv7 Channel Activator with Anticonvulsant Activity.

University of Salerno

General Pharmacological Activation Mechanism of K

East China Normal University

Discovery, synthesis and biological characterization of a series of

University of Nebraska

Development of an automated screen for Kv7.2 potassium channels and discovery of a new agonist chemotype.

University of Michigan

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

Bristol-Myers Squibb Pharmaceutical Research Institute

The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.

The Bristol-Myers Squibb Pharmaceutical Research Institute

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and Optimization of K

University of Pittsburgh

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.

Marquette University

Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.

University Federico Ii of Naples

Discovery of Novel Retigabine Derivatives as Potent KCNQ4 and KCNQ5 Channel Agonists with Improved Specificity.

Chinese Academy of Sciences

Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators.

Abbvie

Potassium channel modulators as possible treatment for pain: patent highlight.

Therachem Research Medilab (India)

Kv7 (KCNQ) channel modulators and neuropathic pain.

Neurosearch

Novel K

Glaxosmithkline

Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy.

Nanjing University of Technology

Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.

Nanjing University of Technology

Discovery of a Series of Indazole TRPA1 Antagonists.

Pfizer