Activators of the human pyruvate kinase M2 receptor

US8841305B2 · kind B2 · utility

Assignee

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

Inventors

• Craig J. Thomas · Gaithersburg, US
• Douglas S. Auld · Waltham, US
• James Inglese
• Amanda P. Skoumbourdis · Langhorne, US
• Jian-Kang Jiang · Columbia, US
• Matthew B. Boxer · Point of Rocks, US

Key dates

• Filing date: Oct 9, 2009
• Grant date: Sep 23, 2014
• Expiry date: Oct 9, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.