Inhibitors

US8486940B2 · kind B2 · utility

Assignee

• PROBIODRUG AG · DE

Inventors

• Ulrich Heiser · Halle (Saale), DE
• Daniel Ramsbeck · Halle (Saale), DE
• Robert Sommer · Halle (Saale), DE
• Antje Meyer · Halle (Saale), DE
• Torsten Hoffmann · Weil am Rhein, DE
• Livia Boehme · Halle (Saale), DE
• Hans-Ulrich Demuth · Halle (Saale), DE

Key dates

• Filing date: Sep 13, 2010
• Grant date: Jul 16, 2013
• Expiry date: Feb 6, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to novel pyrrolidine derivatives of formula (I):wherein R1, R2 and R3 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.