Quinazolines as biogenic amine transport modulators

US10087148B2 · kind B2 · utility

Assignees

• THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, OFFICE OF TECHNOLOGY TRANSFER—NATIONAL INSTITUTES OF HEALTH · US
• Southern Research Institute · US

Inventors

• Subramaniam Ananthan · Birmingham, US
• Richard B. Rothman · Baltimore, US

Key dates

• Filing date: Dec 4, 2015
• Grant date: Oct 2, 2018
• Expiry date: Dec 4, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.