Inactivators of O6-alkylguanine-DNA alkyltransferase

US8188055B2 · kind B2 · utility

Assignees

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

Inventors

• Robert C. Moschel · Frederick, US
• Anthony E. Pegg · Hershey, US
• Sahar Javanmard · Potomac, US
• Natalia Loktionova · Hershey, US
• Gary Pauly · Frederick, US

Key dates

• Filing date: Mar 12, 2008
• Grant date: May 29, 2012
• Expiry date: Oct 26, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07H19/173
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).