Research Triangle Institute

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Scott P Runyon

James Barnwell Thomas

Sanju Narayanan

Hernan A Navarro

Rangan Maitra

Frank Ivy Carroll

Kenneth S Rehder

S Wayne Mascarella

Srinivas Olepu

John A Kepler

Michael A Rogawski

Matthew Orr

Rafal Kaminski

Carla Hassler

Edgar Cook

Lawrence E Brieaddy

Chad M Kormos

Juan P Cueva

Yanan Zhang

Pauline Wanjiku Ondachi

Rainer Reinscheid

James B Thomas

Craig Shiner

Brian Gilmour

Danni Harris

Chunyang Jin

Yanyan Zhang

Hernan Navarro

Edgar (deceased) Cook

Pauline W Ondachi

Juan Pablo Cueva

John Kepler

Cook Edgar

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

Heterocyclic apelin receptor (APJ) agonists and uses thereof

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

Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

Neuropeptide S receptor (NPSR) agonists

Neuropeptide S receptor agonists are provided. The NPS agonists include peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage. 

Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties

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

Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties

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.

Growing community of inventors

Hillsborough, NC, United States of America

Scott P Runyon