Patents by Inventor Mirko Buchholz

Mirko Buchholz 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).

  • Patent number: 11958871
    Abstract: The present invention relates to novel compounds which are particularly useful as inhibitors of bacterial glutaminyl cyclases (bacQC); pharmaceutical compositions comprising such compounds; compounds and/or pharmaceutical compositions for use in methods for treatment, in particular for use in the treatment of periodontitis and related conditions; as well as to crystals comprising bacterial glutaminyl cyclases, methods for identifying candidate compounds which may associate with the binding pocket of a bacQC and/or are bacQC inhibitors.
    Type: Grant
    Filed: February 22, 2019
    Date of Patent: April 16, 2024
    Assignee: FRAUNHOFER-GESELLSCHAFT ZUR FÖRDERUNG DER ANGEWANDTEN FORSCHUNG E.V.
    Inventors: Christian Jäger, Linda Liebe, Daniel Ramsbeck, Miriam Linnert, Stefanie Geissler, Anke Piechotta, Diane Meitzner, Holger Cynis, Mirko Buchholz
  • Publication number: 20230122243
    Abstract: The present invention relates to novel hydroxamic acid derivatives useful as inhibitors of astacin metalloproteinases, in particular procollagen C-proteinase (PCP) enzymes, meprins, ovastacin and/or nematode astacins; more particularly human or mammalian meprin ?, meprin ?, BMP-1, ovastacin and/or DPY-31 from nematodes; pharmaceutical compositions comprising such compounds; methods for treatment or prophylaxis of diseases or conditions, especially such that are related to said metalloproteinases; and compounds and pharmaceutical compositions for use in such methods.
    Type: Application
    Filed: June 12, 2020
    Publication date: April 20, 2023
    Inventors: Daniel RAMSBECK, Kathrin TAN, Dagmar SCHLENZIG, Mirko BUCHHOLZ, Holger CYNIS, Stephan SCHILLING
  • Publication number: 20220195016
    Abstract: The present invention relates to a peptide with a length of 25 amino acids or less comprising the sequence X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13 (SEQ ID No: 1) as well as to A peptide with a length of 25 amino acids or less comprising the sequence X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14 (SEQ ID No: 2). The present invention further relates to a nanostructure comprising a nucleic acid scaffold and at least two peptide moieties, wherein the sequence of each of the at least two peptide moieties is independently selected from the sequence of the peptide of the invention as well as pharmaceutical compositions, nucleic acids, methods and uses related thereto.
    Type: Application
    Filed: April 17, 2020
    Publication date: June 23, 2022
    Inventors: David Michael Smith, Christin Möser, Thomas Grunwald, Leila Issmail, Christian Jäger, Martin Kleinschmidt, Daniel Ramsbeck, Mirko Buchholz
  • Publication number: 20210401996
    Abstract: The present invention generally relates to controlled release of tetracycline antibiotics. Specifically, it relates to a complex comprising a tetracycline compound (TC) or a pharmaceutically acceptable salt, hydrate or solvate thereof and a divalent metal carboxylate; a pharmaceutical preparation comprising the complex, methods for manufacturing the complex and the pharmaceutical preparation, and a complex or a pharmaceutical preparation for use in a method for treatment of the human or animal body, in particular for therapy and/or prophylaxis of a bacterial infection; and/or wherein antibiotic activity is maintained over a prolonged period of time; and/or for the therapy and/or prophylaxis of an acute, chronic or recurrent periodontal disease.
    Type: Application
    Filed: October 29, 2019
    Publication date: December 30, 2021
    Inventors: Andreas KIESOW, Mirko BUCHHOLZ, Sandra SAREMBE, Karsten MÄDER, Martin KIRCHBERG, Sigrun EICK
  • Patent number: 11186572
    Abstract: The present invention relates to bacterial glutaminyl cyclases and inhibitors thereof for use in the treatment of periodontitis and related conditions, and provides a bacterial glutaminyl cyclase (bacQC); an antibody which recognizes the bacQC, a method for identifying an inhibitor of the bacQC; a compound according to Formula (I); a pharmaceutical composition comprising a bacQC inhibitor compound; a bacQC inhibitor compound and/or a pharmaceutical composition for use in a method for treatment of the human or animal body, for use in a method for therapy or prophylaxis of a bacterial infection, and for use in a method for therapy and/or prophylaxis of an acute, chronic or recurrent periodontal disease.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: November 30, 2021
    Assignee: Fraunhofer-Gesellschaft zur Forderung der Angewandten Forschung E.V.
    Inventors: Jan Potempa, Sigrun Eick, Nadine Taudte, Jens-Ulrich Rahfeld, Mirko Buchholz, Hans-Ulrich Demuth
  • Publication number: 20210198189
    Abstract: The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin ? and/or ?, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin ? and/or ?, and compounds and pharmaceutical compositions for use in such methods.
    Type: Application
    Filed: March 8, 2021
    Publication date: July 1, 2021
    Applicant: Vivoryon Therapeutics AG
    Inventors: Michael Wermann, Mirko Buchholz, Hans-Ulrich Demuth, Daniel Ramsbeck, Dagmar Schlenzig, Stephen Schilling
  • Patent number: 10975019
    Abstract: The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin ? and/or ?, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin ? and/or ?, and compounds and pharmaceutical compositions for use in such methods.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: April 13, 2021
    Assignee: Vivoryon Therapeutics AG
    Inventors: Michael Wermann, Mirko Buchholz, Hans-Ulrich Demuth, Daniel Ramsbeck, Dagmar Schlenzig, Stephen Schilling
  • Publication number: 20200392174
    Abstract: The present invention relates to novel compounds which are particularly useful as inhibitors of bacterial glutaminyl cyclases (bacQC); pharmaceutical compositions comprising such compounds; compounds and/or pharmaceutical compositions for use in methods for treatment, in particular for use in the treatment of periodontitis and related conditions; as well as to crystals comprising bacterial glutaminyl cyclases, methods for identifying candidate compounds which may associate with the binding pocket of a bacQC and/or are bacQC inhibitors.
    Type: Application
    Filed: February 22, 2019
    Publication date: December 17, 2020
    Inventors: Christian JÄGER, Linda LIEBE, Daniel RAMSBECK, Miriam LINNERT, Stefanie GEISSLER, Anke PIECHOTTA, Diane MEITZNER, Holger CYNIS, Mirko BUCHHOLZ
  • Publication number: 20190367511
    Abstract: The present invention relates to bacterial glutaminyl cyclases and inhibitors thereof for use in the treatment of periodontitis and related conditions, and provides a bacterial glutaminyl cyclase (bacQC); an antibody which recognizes the bacQC, a method for identifying an inhibitor of the bacQC; a compound according to Formula (I); a pharmaceutical composition comprising a bacQC inhibitor compound; a bacQC inhibitor compound and/or a pharmaceutical composition for use in a method for treatment of the human or animal body, for use in a method for therapy or prophylaxis of a bacterial infection, and for use in a method for therapy and/or prophylaxis of an acute, chronic or recurrent periodontal disease.
    Type: Application
    Filed: December 1, 2017
    Publication date: December 5, 2019
    Inventors: Jan Potempa, Sigrun Eick, Nadine Taudte, Jens-Ulrich Rahfeld, Mirko Buchholz, Hans-Ulrich Demuth
  • Publication number: 20190127317
    Abstract: The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin ? and/or ?, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin ? and/or ?, and compounds and pharmaceutical compositions for use in such methods.
    Type: Application
    Filed: April 18, 2017
    Publication date: May 2, 2019
    Inventors: Michael Wermann, Mirko Buchholz, Hans-Ulrich Demuth, Daniel Ramsbeck, Dagmar Schlenzig, Stephen Schilling
  • 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: 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: 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: 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: 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
  • Patent number: 8809010
    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
  • Patent number: 8772508
    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.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: July 8, 2014
    Assignee: Probiodrug AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Antje Hamann
  • Patent number: 8420684
    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
  • Patent number: 8278345
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repre
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: October 2, 2012
    Assignee: Probiodrug AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj