Inhibitors

US9512115B2 · kind B2 · utility

Assignee

• PROBIODRUG AG · DE

Inventors

• Ulrich Heiser · Halle (Saale), DE
• Mirko Buchholz · Halle (Saale), DE
• Robert Sommer · Halle (Saale), DE
• Antje Meyer · Halle (Saale), DE
• Hans-Ulrich Demuth · Halle (Saale), DE

Key dates

• Filing date: Mar 14, 2014
• Grant date: Dec 6, 2016
• Expiry date: Mar 14, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.