Research Triangle Institute

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

Ann Decker

Richard B Rothman

Bruce Edward Blough

Kevin M Page

Antonio Landavazo

Richard Rothman

The disclosure provides monoamine neurotransmitter releaser and/or monoamine uptake inhibitor compounds having biogenic amine transporter activity but lacking substantial activity at 5-HTreceptor subtypes. The phenethylamine or vinylogous phenethylamine compounds of the disclosure are useful in treating diseases, conditions and/or disorders mediated by activity of one or more of the monoamine neurotransmitters.

Vinylogous phenethylamines as neurotransmitter releasers

Provided herein are compounds and prodrugs and methods of preparation of compounds and prodrugs that are capable of functioning as releasers and/or uptake inhibitors of one or more monoamine neurotransmitters, including dopamine, serotonin, and norepinephrine. Also provided are pharmaceutical compositions comprising one or more of these compounds or prodrugs, which may further comprise one or more additional therapeutic agents. Also provided are methods of treatment of various conditions that may be responsive to modification of monoamine neurotransmitter levels, such as pre-obesity, obesity, addiction, and depression.

Phenylmorpholines and analogues thereof

Growing community of inventors

Durham, NC, United States of America

Ann Decker