Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer

US10836759B2 · kind B2 · utility

Assignees

• The University of North Carolina at Chapel Hill · US
• The United States of America, as represented by the Secretary, Department of Health and Human Services · US

Inventors

• Matthew B. Boxer · Point of Rocks, US
• Xiaodong Wang · Zhejiang, CN
• Kyle Ryan Brimacombe · Bethesda, US
• Mindy Irene Emily Davis · Rockville, US
• Yuhong Fang · Rockville, US
• Matthew Hall · Deakins Range, US
• Ajit Jadhav · Chantilly, US
• Surendra Karavadhi · Gaithersburg, US
• Li Liu · Doylestown, US
• Natalia Martinez · Rockville, US
• Andrew Louis McIver · Durham, US
• Rajan Pragani · Rockville, US
• Jason Rohde · Poolesville, US
• Anton Simeonov · Rockville, US
• Wei Zhao · North Potomac, US
• Min-Jui Richard Shen · Boyds, US

Key dates

• Filing date: Jun 21, 2017
• Grant date: Nov 17, 2020
• Expiry date: Jun 21, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/07
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; R1 and R2 are each independently a halogen, CN, CF3, CHF2, CH2F, a C1-C10alkyl group, a C1-C10alkoxy group, a di(C1-C5alkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.