Patents by Inventor Werner Simon

Werner Simon 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: 11926631
    Abstract: The invention relates to methods for synthesizing amanitin derivatives having an amino group attached to position 6? of the central tryptophan moiety. The invention furthermore relates to an amanitin derivative having an amino group attached to position 6? of the central tryptophan moiety, conjugates of such amanitin derivative, and pharmaceutical compositions comprising such conjugates.
    Type: Grant
    Filed: May 11, 2022
    Date of Patent: March 12, 2024
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Werner Simon, Susanne Werner-Simon, Christian Lutz, Christoph Müller, Torsten Hechler, Michael Kulke
  • Publication number: 20230233703
    Abstract: The invention relates to a conjugate comprising (a) an amatoxin comprising (i) an amino acid 4 with a 6?-deoxy position; and (ii) an amino acid 8 with an S-deoxy position; (b) a target-binding moiety; and (c) optionally a linker linking said amatoxin and said target-binding moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
    Type: Application
    Filed: February 27, 2023
    Publication date: July 27, 2023
    Inventors: Christian LUTZ, Jan ANDERL, Christoph MUELLER, Werner SIMON, Susanne WERNER-SIMON, Torsten HECHLER, Michael KULKE
  • Patent number: 11702451
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having a hydroxy group attached to the central tryptophan moiety. The invention furthermore relates to novel amanitin derivatives having a hydroxy group attached to position 4?, 5? or 7? of the central tryptophan moiety, novel conjugates of such amanitin derivatives, and pharmaceutical compositions comprising such conjugates.
    Type: Grant
    Filed: January 13, 2021
    Date of Patent: July 18, 2023
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Christian Lutz, Werner Simon, Susanne Werner-Simon, Christoph Müller, Torsten Hechler, Michael Kulke
  • Publication number: 20230173087
    Abstract: The present invention relates to prodrugs comprising a linker comprising five- or six-membered cyclic acetals and an adjacent specific cleavage site, and to precursor compounds for the synthesis of said prodrugs. In one aspect the present invention relates to antibody-targeted amatoxin conjugates comprising said linkers, to methods for their synthesis, and to the use of said antibody-targeted amatoxin conjugates. In a further aspect, the invention relates to pharmaceutical compositions comprising said conjugates, and to the use of said conjugates or compositions for therapeutic purposes, in particular for tumor therapy and oncology.
    Type: Application
    Filed: May 22, 2020
    Publication date: June 8, 2023
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Christoph Mueller, Werner Simon, Susanne Werner-Simon, Francesca Gallo, Torsten Hechler, Michael Kulke, Andreas Pahl
  • Patent number: 11590238
    Abstract: The invention relates to a conjugate comprising (a) an amatoxin comprising (i) an amino acid 4 with a 6?-deoxy position; and (ii) an amino acid 8 with an S-deoxy position; (b) a target-binding moiety; and (c) optionally a linker linking said amatoxin and said target-binding moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: February 28, 2023
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Christian Lutz, Jan Anderl, Christoph Müller, Werner Simon, Susanne Werner-Simon, Torsten Hechler, Michael Kulke
  • Patent number: 11583569
    Abstract: The invention relates to a PSMA-targeting conjugate comprising (a) an amatoxin; (b) a small molecule PSMA-targeting moiety; and (c) optionally a linker linking said amatoxin and said small molecule PSMA-targeting moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
    Type: Grant
    Filed: September 24, 2018
    Date of Patent: February 21, 2023
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Francesca Gallo, Barbara Korsak, Christoph Mueller, Torsten Hechler, Andreas Pahl, Michael Kulke, Werner Simon, Christian Lutz
  • Patent number: 11446388
    Abstract: The invention relates to a conjugate comprising (a) an amatoxin comprising (i) an amino acid 4 with a 6?-deoxy position; and (ii) an amino acid 8 with an S-deoxy position; (b) a BCMA-binding moiety comprising (i) the variable domains of humanized antibody J22.9-ISY, and (ii) a heavy chain constant region comprising a D265C mutation; and (c) a protease-cleavable linker linking said amatoxin and said target-binding moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate, particularly for use in the treatment of multiple myeloma.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: September 20, 2022
    Assignee: HEIDELBERG PHARMA RESEARCH GMBH
    Inventors: Torsten Hechler, Michael Kulke, Christian Lutz, Andreas Pahl, Christoph Müller, Werner Simon, Anikó Pálfi
  • Publication number: 20220274995
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having an amino group attached to position 6? of the central tryptophan moiety. The invention furthermore relates to a novel amanitin derivative having an amino group attached to position 6? of the central tryptophan moiety, novel conjugates of such amanitin derivative, and pharmaceutical compositions comprising such conjugates.
    Type: Application
    Filed: May 11, 2022
    Publication date: September 1, 2022
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Werner Simon, Susanne Werner-Simon, Christian Lutz, Christoph Müller, Torsten Hechler, Michael Kulke
  • Patent number: 11420971
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having an amino group attached to position 6? of the central tryptophan moiety. The invention furthermore relates to a novel amanitin derivative having an amino group attached to position 6? of the central tryptophan moiety, novel conjugates of such amanitin derivative, and pharmaceutical compositions comprising such conjugates.
    Type: Grant
    Filed: August 6, 2018
    Date of Patent: August 23, 2022
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Werner Simon, Susanne Werner-Simon, Christian Lutz, Christoph Müller, Torsten Hechler, Michael Kulke
  • Publication number: 20220133902
    Abstract: The present application relates to a composition comprising (a) at least one immune checkpoint inhibitor and (b) at least one conjugate, wherein said conjugate is comprising (i) a target binding moiety, (ii) at least one amatoxin, and (iii) optionally at least one linker connecting said target binding moiety with said at least one amatoxin. The present application further relates to said composition for use in treating a patient having a cancer, and to a pharmaceutical formulation comprising said composition and additional excipients, as well as to methods of producing and using said composition.
    Type: Application
    Filed: November 4, 2021
    Publication date: May 5, 2022
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Michael Kulke, Torsten Hechler, Andreas Pahl, Christoph Müller, Susanne Werner-Simon
  • Publication number: 20220024870
    Abstract: The present invention relates to novel methods and compounds for synthesizing amanitin derivatives. The invention in particular relates to methods for synthesizing (S)-6-hydroxy-tryptophan derivatives which can be used as building blocks for synthesizing amanitin derivatives or amatoxin drug conjugates. The invention further relates to intermediate compounds of said synthesis pathways for use in amanitin derivative and amatoxin drug conjugate synthesis, and to the use of particular catalysts suited for mediating said synthesis pathways.
    Type: Application
    Filed: December 11, 2019
    Publication date: January 27, 2022
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Werner Simon, Susanne Werner-Simon, Christoph Müller
  • Publication number: 20210138081
    Abstract: The invention relates to a conjugate comprising (a) an amatoxin comprising (i) an amino acid 4 with a 6?-deoxy position; and (ii) an amino acid 8 with an S-deoxy position; (b) a target-binding moiety; and (c) optionally a linker linking said amatoxin and said target-binding moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
    Type: Application
    Filed: March 2, 2017
    Publication date: May 13, 2021
    Inventors: Christian Lutz, Jan Anderl, Christoph Müller, Werner Simon, Susanne Werner-Simon, Torsten Hechler, Michael Kulke
  • Publication number: 20210130412
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having a hydroxy group attached to the central tryptophan moiety. The invention furthermore relates to novel amanitin derivatives having a hydroxy group attached to position 4?, 5? or 7? of the central tryptophan moiety, novel conjugates of such amanitin derivatives, and pharmaceutical compositions comprising such conjugates.
    Type: Application
    Filed: January 13, 2021
    Publication date: May 6, 2021
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Christian Lutz, Werner Simon, Susanne Werner-Simon, Christoph Müller, Torsten Hechler, Michael Kulke
  • Patent number: 10961277
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having a hydroxy group attached to the central tryptophan moiety. The invention furthermore relates to novel amanitin derivatives having a hydroxy group attached to position 4?, 5? or 7? of the central tryptophan moiety, novel conjugates of such amanitin derivatives, and pharmaceutical compositions comprising such conjugates.
    Type: Grant
    Filed: August 6, 2018
    Date of Patent: March 30, 2021
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Christian Lutz, Werner Simon, Susanne Werner-Simon, Christoph Müller, Torsten Hechler, Michael Kulke
  • Publication number: 20210077571
    Abstract: The present invention relates to an amatoxin-linker construct comprising an amatoxin according to formula (I) wherein: R1 and R2 are each —OH, R3 is NH2, or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R4 is H or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R5 is absent or ?O, wherein R3 and R4 cannot be the same, for use in the manufacture of a binding moiety-toxin conjugate for the treatment of a solid tumor, and a respective binding moiety-toxin conjugate for the treatment of a solid tumor.
    Type: Application
    Filed: April 12, 2019
    Publication date: March 18, 2021
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Christoph Müller, Werner Simon, Christian Lutz, Susanne Werner-Simon, Torsten Hechler, Michael Kulke, Andreas Pahl
  • Publication number: 20210061805
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having an amino group attached to position 6? of the central tryptophan moiety. The invention furthermore relates to a novel amanitin derivative having an amino group attached to position 6? of the central tryptophan moiety, novel conjugates of such amanitin derivative, and pharmaceutical compositions comprising such conjugates.
    Type: Application
    Filed: August 6, 2018
    Publication date: March 4, 2021
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Werner Simon, Susanne Werner-Simon, Christian Lutz, Christoph Müller, Torsten Hechler, Michael Kulke
  • Publication number: 20200407440
    Abstract: Amatoxins, as well as antibody-drug conjugates (ADCs) comprising an amatoxin are provided, as well as compositions and methods of using the same. The compositions and methods provided herein can also be used to prepare a patient for hematopoietic stem cell transplant therapy and to improve the engraftment of hematopoietic stem cell transplants by selectively depleting endogenous hematopoietic stem cells prior to the transplant procedure. Methods and compositions for the treatment of various hematopoietic diseases, metabolic disorders, cancers, and autoimmune diseases, as well as prevention of graft-versus-host-disease (GVHD), are provided.
    Type: Application
    Filed: April 24, 2020
    Publication date: December 31, 2020
    Inventors: Charlotte Fenton McDonagh, Rajiv Panwar, Ganapathy N. Sarma, Torsten Hechler, Michael Kulke, Andreas Pahl, Christoph Mueller, Werner Simon, Christian Lutz, Francesca Gallo
  • Publication number: 20200345807
    Abstract: The invention relates to a PSMA-targeting conjugate comprising (a) an amatoxin; (b) a small molecule PSMA-targeting moiety; and (c) optionally a linker linking said amatoxin and said small molecule PSMA-targeting moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
    Type: Application
    Filed: September 24, 2018
    Publication date: November 5, 2020
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Francesca Gallo, Barbara Korsak, Christoph Mueller, Torsten Hechler, Andreas Pahl, Michael Kulke, Werner Simon, Christian Lutz
  • Patent number: 10723766
    Abstract: The invention relates to ?-amaninamide (1; x=0, 1 or 2), ?-amaninamidic acid (2; x=0, 1 or 2), and ?-amaninamidic hydroxamic acid (3; x=0, 1 or 2), novel derivatives of ?-amanitin (4), and methods and novel building blocks for the synthesis thereof.
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: July 28, 2020
    Assignee: Heidelberg Pharma Research GmbH
    Inventors: Susanne Werner-Simon, Christian Lutz, Christoph Müller, Werner Simon
  • Publication number: 20200181200
    Abstract: The invention relates to novel methods for synthesizing amanitin derivatives having a hydroxy group attached to the central tryptophan moiety. The invention furthermore relates to novel amanitin derivatives having a hydroxy group attached to position 4?, 5? or 7? of the central tryptophan moiety, novel conjugates of such amanitin derivatives, and pharmaceutical compositions comprising such conjugates.
    Type: Application
    Filed: August 6, 2018
    Publication date: June 11, 2020
    Applicant: Heidelberg Pharma Research GmbH
    Inventors: Christian Lutz, Werner Simon, Susanne Werner-Simon, Christoph Müller, Torsten Hechler, Michael Kulke