Abstract: Diagnostic assays for the diagnosis of amyloidosis, in particular Alzheimer's disease, and related aspects. In particular, monoclonal antibodies and an antibody assay are provided.
Type:
Grant
Filed:
March 16, 2012
Date of Patent:
August 19, 2014
Assignee:
Probiodrug AG
Inventors:
Martin Kleinschmidt, Stephan Schilling, Jens-Ulrich Rahfeld, Kristin Ebermann, Hans-Ulrich Demuth
Abstract: Provided herein are methods for treating and preventing neurodegenerative disease in a mammal by administering an inhibitor of glutaminyl cyclase (QC). Neurodegenerative diseases treatable or preventable according to methods described herein include mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia.
Type:
Grant
Filed:
July 21, 2009
Date of Patent:
August 19, 2014
Assignee:
Probiodrug AG
Inventors:
Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
Abstract: 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 R1 are as defined throughout the description and the claims.
Abstract: A crystal comprising human isoglutaminyl cyclase having a characterized space group of P1211 and unit cell dimensions of +/?5% of a=126.51 ?, b=109.68 ?, c=159.53 ?, ?=90.0°, ?=104.9° and ?=90.0°.
Type:
Grant
Filed:
October 28, 2011
Date of Patent:
June 3, 2014
Assignee:
Probiodrug AG
Inventors:
Anett Stephan, Stephan Schilling, Jens-Ulrich Rahfeld, Michael Wermann, Christoph Parthier, Hans-Ulrich Demuth, David Ruiz-Carillo, Milton T. Stubbs
Abstract: Novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
Type:
Grant
Filed:
April 11, 2008
Date of Patent:
April 1, 2014
Assignee:
Probiodrug AG
Inventors:
Hans-Ulrich Demuth, Torsten Hoffmann, Andre Johannes Niestroj, Stephan Schilling, Ulrich Heiser
Abstract: Novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs), which are isoenzymes of glutaminyl cyclase (QC, EC 2.3.2.5), and to isolated nucleic acids coding for these isoenzymes, all of which are useful for the discovery of new therapeutic agents, for measuring cyclase activity, and for determining the inhibitory activity of compounds against these glutaminyl cyclase isoenzymes.
Type:
Grant
Filed:
December 13, 2011
Date of Patent:
February 11, 2014
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Holger Cynis, Jens-Ulrich Rahfeld, Hans-Ulrich Dermuth
Abstract: 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.
Type:
Grant
Filed:
April 21, 2011
Date of Patent:
September 24, 2013
Assignee:
Probiodrug AG
Inventors:
Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
Abstract: 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.
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.
Type:
Grant
Filed:
September 13, 2010
Date of Patent:
July 16, 2013
Assignee:
Probiodrug AG
Inventors:
Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
Abstract: The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of diseases that can be treated by modulation of QC-activity, e.g. diseases selected from the group consisting of duodenal cancer with or w/o Heliobacter pylori infections, colorectal cancer, Zolliger-Ellison syndrome, Familial British Dementia and Familial Danish Dementia.
Type:
Grant
Filed:
July 29, 2008
Date of Patent:
June 25, 2013
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Torsten Hoffmann, Andre Johannes Niestroj, Hans-Ulrich Demuth, Ulrich Heiser
Abstract: 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.
Abstract: The present invention relates to 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 R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(he
Type:
Grant
Filed:
November 8, 2007
Date of Patent:
April 16, 2013
Assignee:
Probiodrug AG
Inventors:
Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
Abstract: 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.
Type:
Grant
Filed:
August 19, 2011
Date of Patent:
April 2, 2013
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Jens-Ulrich Rahfeld, Birgit Koch, Michael Wermann, Christoph Parthier, David Ruiz-Carillo, Milton T. Stubbs
Abstract: A double transgenic non-human animal, in particular a transgenic mouse encoding Qpct proteins, which have been implicated in Qpct-related diseases, and Amyloid Precursor Protein (APP). Also provided are cells and cell lines comprising transgenes encoding for Qpct and APP. Also provided are methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.
Type:
Application
Filed:
August 10, 2012
Publication date:
February 28, 2013
Applicant:
PROBIODRUG AG
Inventors:
Sigrid Graubner, Wolfgang Jagla, Stephan Schilling, Holger Cynis, Hans-Ulrich Demuth, Torsten Hoffmann, Michael Wermann, Katrin Schulz, Christoph Baeuscher, Stefanie Kohlmann
Abstract: Provided herein are methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis and pancreatitis.
Type:
Grant
Filed:
February 28, 2008
Date of Patent:
December 25, 2012
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
Abstract: 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.
Type:
Application
Filed:
May 24, 2012
Publication date:
November 29, 2012
Applicant:
PROBIODRUG AG
Inventors:
Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
Abstract: 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.
Abstract: A transgenic non-human animal, in particular a transgenic mouse encoding A? peptide proteins, which have been implicated in A? peptide-related diseases. Cells and cell lines comprising transgenes encoding for A? peptide. Methods and compositions for evaluating agents that affect A? peptide, for use in compositions for the treatment of A? peptide-related diseases.
Type:
Grant
Filed:
September 12, 2008
Date of Patent:
October 9, 2012
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Holger Cynis, Hans-Ulrich Demuth, Wolfgang Jagla, Sigrid Graubner