Probiodrug Ag

Antje Hamann

Ulrich Heiser

Hans-Ulrich Demuth

Michael Thormann

Andreas Treml

Michael Almstetter

Robert Sommer

Ulf-Torsten Gaertner

Stephan Schilling

Torsten Hoffmann

Mirko Buchholz

Jens-Ulrich Rahfeld

Holger Cynis

Kathrin Gans

Michael Wermann

Torsten Hoffman

Astrid Kehlen

Daniel Friedrich

Compounds of general formula (I): wherein R, R, R, R, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.

Inhibitors of glutaminyl cyclase

The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barr&#xe9; syndrome, chronic inflammatory demyelinizing polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.

Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions

Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B and Rare as defined throughout the description and the claims.

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Dieskau, Germany

Antje Hamann