Probiodrug Ag

Vivoryon Therapeutics Ag

Michael Wermann

Stephan Schilling

Jens-Ulrich Rahfeld

Hans-Ulrich Demuth

Christoph Parthier

Milton T Stubbs

David Ruiz-Carillo

Birgit Koch

Ulrich Heiser

Torsten Hoffmann

Mirko Buchholz

Michael Thormann

Andreas Treml

Daniel Ramsbeck

Michael Almstetter

Holger Cynis

Robert Sommer

Dagmar Schlenzig

Anett Stephan

Ulf-Torsten Gaertner

Kathrin Gans

Antje Hamann

Stephen Schilling

Daniel Friedrich

Astrid Kehlen

Marvin Hempel

Milton Stubbs

The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin &#x3b2; and/or &#x3b1;, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin &#x3b2; and/or &#x3b1;, and compounds and pharmaceutical compositions for use in such methods.

Inhibitors of meprin &#x3b1; and &#x3b2;

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

Novel crystal structures of human and murine glutaminyl cyclase (QC, EC 2.3.2.5), methods of preparing the crystals, as well as the use of said crystal structures for identifying inhibitors of human and murine glutaminyl cyclase.

Crystal structure of glutaminyl cyclase

A crystal comprising human isoglutaminyl cyclase having a characterized space group of P1211 and unit cell dimensions of +/&#x2212;5% of a=126.51 &#x212b;, b=109.68 &#x212b;, c=159.53 &#x212b;, &#x3b1;=90.0&#xb0;, &#x3b2;=104.9&#xb0; and &#x3b3;=90.0&#xb0;.

Crystal structure of isoglutaminyl cyclase

A novel crystal structures of human and murine glutaminyl cyclase (QC, EC 2.3.2.5), methods of preparing the crystals, as well as the use of said crystal structures for identifying inhibitors of human and murine glutaminyl cyclase.

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Halle/Saale, Germany

Michael Wermann