Research Triangle Institute

University of Arkansas

The United States of America as Represented by the Department of Health

Virginia Commonwealth University

Racon Incorporated

US Government as Represented by the Secretary of the Army

University of Michigan

Dignity Health

The United States of America Represented by the Secretary of Health and

Frank Ivy Carroll

Philip Abraham

Anita H Lewin

James Barnwell Thomas

Michael J Kuhar

John W Boja

S Wayne Mascarella

Hernan A Navarro

Scott P Runyon

Samuel Michael Owens

Bruce Edward Blough

Pauline Wanjiku Ondachi

M Imad Damaj

Lawrence E Brieaddy

Juan P Cueva

Chad M Kormos

Dale E Stelz

Wilson M Whaley

Richard B Rothman

James H Woods

Ronald J Lukas

James B Thomas

Peter K Chiang

Ana Zamfira Muresan

Felipe N Padilla

Emily M Jutkiewicz

Samuel W Mascarella

Tingwei Cai

Hern&aacute;n A Navarro

Desong Zhong

Chunyang Jin

Joh W Boja

Michelle M Richard

Pauline W Ondachi

Juan Pablo Cueva

S Wayne c/o Res Triangle Institute Mascarella

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

The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.

Monoamine reuptake inhibitors

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

The invention provides bupropion analog compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.

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

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

The invention generally relates to hapten compounds comprising either (+) methamphetamine or (+) amphetamine conjugated to a linker. Generally speaking, hapten compounds of the invention may be used to elicit an immune response to one or more of (+) methamphetamine, (+) amphetamine, or (+) MDMA.

Methamphetamine-like hapten compounds, linkers, carriers and compositions and uses thereof

Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.

Nicotinic receptor compounds

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

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.

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

Durham, NC, United States of America

Frank Ivy Carroll