Probiodrug Ag

Vivoryon Therapeutics N.v.

Osi Pharmaceuticals, Inc.

Ingenium Pharmaceuticals Gmbh

Other

Astrazeneca Ab

Prosidion Limited

Vivorian Therapeutics N.v

Ulrich Heiser

Hans-Ulrich Demuth

Torsten Hoffmann

Mirko Buchholz

Andre Johannes Niestroj

Stephan Schilling

Daniel Ramsbeck

Robert Sommer

André Johannes Niestroj

Antje Meyer

Livia Boehme

Michael Thormann

Andreas Treml

Ulf-Torsten Gaertner

Lutz Zeitlmann

Antje Hamann

Michael Altmstetter

Jens-Ulrich Rahfeld

Michael Almstetter

Dagmar Schlenzig

Torsten Hoffman

Ingeborg Lues

Michael A Pleiss

Holger Cynis

Hans Allgeier

Martin Augustin

Konrad Glund

Kathrin Gans

Stephan Von Hoersten

Michael Wermann

Matthias Hoffmann

Anke Mueller

Bernd Gerhartz

Kerstin Kühn-Wache

Anke Müller

Susanne Aust

Joachim Baer

Ingo Schulz

Wolfgang Brandt

Joachim Bär

Antje Harmann

Andreas Marquardt

Daniel Friedrich

Astrid Kehlen

André J Niestroj

Livia Böhme

Kerstin c/o Probiodrug Ag Kuehn-Wache

Compounds of formula (I):A-B-D-Eor a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: These compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

Inhibitors

The present invention is concerned with a crystalline pharmaceutically acceptable salt of the glutaminyl cyclase inhibitor Varoglutamstat. Varoglutamstat is chemically designated as(S)-1-(1H-benzo[d]imidazol-5-yl)-5-(4-propoxyphenyl) imidazolidin-2-one and is also known under the code PQ912. The invention further relates to a polymorphic form of the hydrochloride salt of(S)-1-(1H-benzo[d]imidazol-5-yl)-5-(4-propoxyphenyl) imidazolidin-2-one, to processes for preparing said hydrochloride salt and its polymorphic form, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing them.

Crystalline pharmaceutically acceptable salt and polymorphic form of the glutaminyl cyclase inhibitor Varoglutamstat

The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are 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.

The invention relates to a compound of formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein A is heteraryl selected from 1H-benzimidazolyl and imidazo[1,2-a]pyridine, and R, R, R, Rand Rare as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) and its isoenzyme glutaminyl-peptide cyclotransferase-like protein (QPCTL). QC and QPCTL catalyze 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. 

Inhibitors of glutaminyl cyclase

Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: 

The invention relates to novel pyrrolidine derivatives of formula (I): wherein R, Rand Rare 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.

Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.

Radiolabelled glutaminyl cyclase (QC) inhibitors and uses of same

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 R, R, R, Rand Rare 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. 

Compounds of formula (I), combinations and uses thereof for disease therapy,  

The invention relates to novel heterocyclic derivatives 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.

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein

Compounds of general Formula (I): wherein R, R, R, R, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.

Inhibitors of protein kinases

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.

Growing community of inventors

Halle/Saale, Germany

Ulrich Heiser