Research Triangle Institute

Other

Icagen, Inc.

James Barnwell Thomas

Frank Ivy Carroll

Scott P Runyon

S Wayne Mascarella

Hernan A Navarro

Rangan Maitra

Sanju Narayanan

Kenneth S Rehder

Srinivas Olepu

Grant Andrew McNaughton-Smith

George Salvatore Amato

F Ivy Carroll

Chad M Kormos

Juan P Cueva

Lawrence E Brieaddy

Roger G Hale

Pauline Wanjiku Ondachi

Robert Anthony Thomas, Deceased

Tingwei Cai

Robert Anthony Thomas

By Margaretanne Thomas, Legal Representative

Chunyang Jin

Juan Pablo Cueva

S Wayne c/o Res Triangle Institute Mascarella

This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

Apelin receptor (APJ) agonists and uses thereof

Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc. 

Substituted 1,2,3,4-tetrahydroisoquinolines as kappa opioid antagonists

Provided are opioid receptor antagonists represented by the formula (I): where R, Y, R, R, R, Rand Rare as defined herein.

Arylpiperazine opioid receptor antagonists

Provided are compounds represented by the formula: where R, Y, R, R, R, R, R, G, R, E, E, A, B, W, X, Y and Z are as defined herein. 

1-substituted 4-arylpiperazine as kappa opioid receptor antagonists

Provided are opioid receptor antagonists represented by the formula (I) where R, Y, R, R, R, Rand Rare as defined herein.

Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

Fused ring heterocycles as potassium channel modulators

Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Kappa opioid receptor ligands

Growing community of inventors

Efland, NC, United States of America

James Barnwell Thomas