6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity

US11111253B2 · kind B2 · utility

Assignee

• University of Pittsburgh—Of the Commonwealth System of Higher Education · US

Inventors

• Donna M. Huryn · Allentown, US
• Peter Wipf · Pittsburgh, US
• Jennifer Rubin Grandis · Pittsburgh, US
• Matthew G. LaPorte · Girard, US
• Paul A. Johnston · Hawthorne, US
• Mark E. Schurdak · Warrendale, US
• Raffaele Colombo · Pittsburgh, US

Key dates

• Filing date: Apr 10, 2020
• Grant date: Sep 7, 2021
• Expiry date: Apr 10, 2040

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds that selectivity inhibit the STAT3 pathway and not the STAT1 pathway and exhibit anti-proliferative activity are disclosed. Also disclosed are methods of treatment of cancers that are characterized by overexpression of STAT3, which are safer that other therapies.