Substituted pyrazino[1′,2′:1 ,5]pyrrolo[2,3-b]indole-1,4-diones for cancer treatment

US10220099B2 · kind B2 · utility

Assignees

• Massachusetts Institute of Technology · US
• The Board of Trustees of the University of Illinois · US

Inventors

• Mohammad Movassaghi · Lincoln, US
• Justin Kim · Burbank, US
• Paul J. Hergenrother · Champaign, US
• Karen Morrison · Champaign, US
• Nicolas Cedric Boyer · Somerville, US

Key dates

• Filing date: May 10, 2016
• Grant date: Mar 5, 2019
• Expiry date: May 10, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The synthesis of various pyrazino[1′,2′:1,5]pyrrolo[2,3-b]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-c: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R4-R8, R3′, R6′, and n are as defined herein, are provided. These biologically active derivatives have been further used to prepare cell-specific drug conjugates effective in treating various diseases including cancer.