Patents by Inventor Ulrich Heiser

Ulrich Heiser has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20200377493
    Abstract: 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).
    Type: Application
    Filed: April 3, 2018
    Publication date: December 3, 2020
    Inventors: Ulrich HEISER, Torsten HOFFMANN, Ingeborg LUES, Antje MEYER
  • Publication number: 20200223825
    Abstract: 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 R1, R2, R3, R4 and R5 are 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.
    Type: Application
    Filed: September 20, 2018
    Publication date: July 16, 2020
    Inventors: Ulrich HEISER, Robert SOMMER
  • Patent number: 9656991
    Abstract: 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: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 23, 2017
    Assignee: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj, Robert Sommer
  • Patent number: 9650362
    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 23, 2015
    Date of Patent: May 16, 2017
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Patent number: 9610368
    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: Grant
    Filed: December 15, 2014
    Date of Patent: April 4, 2017
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
  • Patent number: 9512082
    Abstract: 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: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: December 6, 2016
    Assignee: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj
  • Patent number: 9512115
    Abstract: 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 R1, R2, R3, R4 and R5 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: March 14, 2014
    Date of Patent: December 6, 2016
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Mirko Buchholz, Robert Sommer, Antje Meyer, Hans-Ulrich Demuth
  • Publication number: 20160039795
    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: Application
    Filed: September 23, 2015
    Publication date: February 11, 2016
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Publication number: 20160031869
    Abstract: 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 R1, R2, R3, R4 and R5 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: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Ulrich Heiser, Mirko Buchholz, Robert Sommer, Antje Meyer, Hans-Ulrich Demuth
  • Patent number: 9181233
    Abstract: 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.
    Type: Grant
    Filed: March 3, 2011
    Date of Patent: November 10, 2015
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Patent number: 9173885
    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: June 5, 2013
    Date of Patent: November 3, 2015
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Publication number: 20150272947
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, 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.
    Type: Application
    Filed: June 11, 2015
    Publication date: October 1, 2015
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Patent number: 9126987
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: September 8, 2015
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
  • Patent number: 9067888
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, 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.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: June 30, 2015
    Assignee: AstraZeneca AB
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Patent number: 9034907
    Abstract: 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 and R2, R3, R4, R5, R6, X1, X2, X3, X4, Y and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 19, 2015
    Assignee: Probiodrug AG
    Inventors: Mirko Buchholz, Ulrich Heiser
  • Publication number: 20150104389
    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: December 15, 2014
    Publication date: April 16, 2015
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
  • Patent number: 8962860
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, 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.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: February 24, 2015
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Almstetter, Michael Thormann, Andreas Treml, Hans-Ulrich Demuth, Torsten Hoffman
  • Publication number: 20150038516
    Abstract: Compounds of general Formula I: wherein R1, R2, R3, x, A and Ra are as defined herein are inhibitors of cyclin-dependent kinases and are useful for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.
    Type: Application
    Filed: May 5, 2014
    Publication date: February 5, 2015
    Applicant: AstraZeneca AB
    Inventors: Hans Allgeier, Martin Augustin, SR., Anke Muller, Lutz Zeitlmann, Andreas Marquardt, Michael A. Pleiss, Ulrich Heiser, Andre Johannes Niestroj
  • Patent number: 8945510
    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: Grant
    Filed: May 24, 2012
    Date of Patent: February 3, 2015
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
  • Patent number: 8889709
    Abstract: 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-Barré 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.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: November 18, 2014
    Assignee: Probiodrug AG
    Inventors: Hans-Ulrich Demuth, Stephan Schilling, Michael Wermann, Holger Cynis, Astrid Kehlen, Daniel Friedrich, Torsten Hoffmann, Kathrin Gans, Jens-Ulrich Rahfeld, Ulrich Heiser, Michael Almstetter, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Thormann, Andreas Treml