Research Triangle Institute

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

Virginia Commonwealth University

Dignity Health

University of Michigan

Dignity Health Doing Business As St. Joseph's Hospital and Medical Center and Barrow Neurological Institute

Dignity Health Doing Business As St. Joseph's Hospital Medical Center and Barrow Neurological Institute

Hernan A Navarro

Frank Ivy Carroll

Scott P Runyon

James Barnwell Thomas

S Wayne Mascarella

John A Kepler

Michael A Rogawski

Matthew Orr

Rafal Kaminski

M Imad Damaj

Edgar Cook

Bruce Edward Blough

Pauline Wanjiku Ondachi

Ronald J Lukas

Brian Frazier Thomas

Clarence Edgar Cook

Ana Zamfira Muresan

Lawrence E Brieaddy

Carol Delta Sloan

Chad M Kormos

F Ivy Carroll

James H Woods

James B Thomas

Emily M Jutkiewicz

Tingwei Cai

Chunyang Jin

Pauline W Ondachi

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

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

The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.

Hydroxybupropion analogues for treating drug dependence

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

Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2'-fluoro-3&#x2032;-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.

Nicotinic receptor compounds

The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.

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.

Hexahydroindenopyridine compounds are provided which act as spermicides and/or fungicides, spermicidal and/or fungicidal compositions containing the same, and methods for killing motile sperm and/or fungi using the compounds and compositions.

Spermicidal and/or antifungal composition and methods of using the same

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

Compounds which bind to opioid receptors are provided. In a preferred embodiment of the invention, the compounds are opioid receptor antagonists. The present invention also provides methods of treating conditions which are mediated by an opioid receptor.

Octahydroisoquinoline compounds as opioid receptor modulators

Structurally novel opioid receptor agonists are provided, and the use of these agonists in treatment of chronic and/or acute pain.

Opioid receptor agonist compounds and their use in treatment of pain

Growing community of inventors

Research Triangle Park, NC, United States of America

Hernan A Navarro