Research Triangle Institute

Bristol-myers Squibb Compnay

University of Arkansas

Virginia Commonwealth University

Dignity Health

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

F Ivy Carroll

S Wayne Mascarella

James Barnwell Thomas

Anita H Lewin

S Michael Owens

Melinda Gunnell

Joanne J Bronson

Muzammil M Mansuri

Stanley V D'Andrea

Hernan A Navarro

Ralph L Henry

Kenneth M Tramposch

Bruce Edward Blough

Ronald J Lukas

M Imad Damaj

Ana Zamfira Muresan

Eric C Peterson

Katharine M Greene

Yingni Chi

Stephen A Steiner

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.

Hydroxybupropion analogues for treating drug dependence

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.

Hapten compounds and compositions and uses thereof

The invention generally relates to monoclonal antibodies that recognize at least one compound from the group consisting of (+) methamphetamine, (+) amphetamine, and (+) 3,4-methylenedioxymethamphetamine ((+) MDMA). Generally speaking, the monoclonal antibodies do not recognize (&#x2212;) methamphetamine, (&#x2212;) amphetamine, or (&#x2212;) MDMA.

Monoclonal antibodies that selectively recognize methamphetamine and methamphetamine like compounds

Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states.

Compounds and methods for promoting smoking cessation

Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, 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

Structurally novel kappa opioid receptor antagonists are provided 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.

A powerful new anti-convulsant and anti-ischemic pharmaceutical, 5-aminocarbonyl-5H-dibenzo�a,d!cycloheptene-5,10-imine is prepared according to a novel synthesis which converts the starting material, commercially available dibenzosubernone to ADCI without the use of chromatographic purification, hazardous reagents or extreme conditions. The starting material is converted to the corresponding imine through ammonia exposure, and directly converted with acetone cyanohydrin in the presence of sodium cyanide to a 5-amino, 5-cyanocycloheptene intermediate. The intermediate is cyclized using bromine, followed by a reduction of the bromine-carbon bond using sodium cyanoborohydride. The target compound is obtained through selective hydrolysis. An overall yield of 46 percent or better is obtained.

Synthesis of 5-aminocarbonyl-5H-dibenzo�a,d!cyclohepten-5,10-imine

Certain novel alicyclic compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.

Alicyclic phospholipase A.sub.2 inhibitors

Compounds of the formula ##STR1## wherein R.sub.1 is CH.dbd.CY--C(CH.sub.3).dbd.CHX wherein X and Y are different and each is of the formula ##STR2## wherein R' and R' independently are H or alkyl of C.sub.1-6 and R.sub.1 includes all possible geometric isomers are demonstrated effective in treating inflammation, both topically and internally. The mechanism appears to be the inhibition of phospholipase A.sub.2 enzymes.

Growing community of inventors

Durham, NC, United States of America

F Ivy Carroll