MYC G-quadruplex stabilizing small molecules and their use

US10604499B2 · kind B2 · utility

Assignee

• The United States of America, as represented by the Secretary, Department of Health and Human Services · US

Inventors

• John Schneekloth, JR. · Frederick, US
• John Simmons · Bethesda, US
• Kenneth Felsenstein · Bethesda, US
• Beverly Mock · Bethesda, US
• Lindsey Saunders · Frederick, US
• David Calabrese · Lausanne, CH
• Elena Leon · Bethesda, US

Key dates

• Filing date: Dec 12, 2018
• Grant date: Mar 31, 2020
• Expiry date: Dec 12, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Methods for treating a tumor, such as a benign or malignant tumor, are disclosed herein. The methods include administering a therapeutically effective amount of a small molecule that selectively binds to and stabilizes G-quadruplex DNA in the promoter of the c-MYC gene to the subject. The methods are also of use to decrease the size and/or number of metastases. Compounds for use in the disclosed methods are also provided.