Patents Assigned to Lead Discovery Center GmbH
  • Patent number: 11945822
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 11, 2019
    Date of Patent: April 2, 2024
    Assignees: QURIENT CO., LTD., LEAD DISCOVERY CENTER GMBH
    Inventors: Kiyean Nam, Jaeseung Kim, Yeejin Jeon, Donghoon Yu, Mooyoung Seo, Dongsik Park, Jan Eickhoff, Gunther Zischinsky
  • Patent number: 11858937
    Abstract: The present invention relates to pyrazolo [1,5-a][1,3,5]triazine and pyrazolo [1,5-a]pyrimidine derivatives having Formula I: and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 11, 2019
    Date of Patent: January 2, 2024
    Assignees: QURIENT CO., LTD., LEAD DISCOVERY CENTER GMBH
    Inventors: Kiyean Nam, Jaeseung Kim, Yeejin Jeon, Donghoon Yu, Mooyoung Seo, Dongsik Park, Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Patent number: 11111238
    Abstract: The invention provides novel coumarin derivatives as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: September 7, 2021
    Assignees: Lead Discovery Center GmbH, Max Planck Gesellschaft zur Förderung der Wissenschften e.V., SOTIO a.s.
    Inventors: Raffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Uwe Koch, Bert Klebl, Axel Choidas, Anke Unger, Nils-Göran Larsson, Maria Falkenberg-Gustafsson, Claes M. Gustafsson
  • Patent number: 10934274
    Abstract: The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.
    Type: Grant
    Filed: April 14, 2016
    Date of Patent: March 2, 2021
    Assignees: QURIENT CO., LTD., LEAD DISCOVERY CENTER GMBH
    Inventors: Kiyean Nam, Jaeseung Kim, Seohyun Ahn, Yeejin Jeon, Doohyung Lee, Dongsik Park, Young-In Yang, SaeYeon Lee, Jeongjun Kim, Jiye Ahn, Hana Kim, Chun-won Jung, Carsten Schultz-Fademrecht
  • Patent number: 10883137
    Abstract: The present invention relates to methods for detection of nucleotide polymerase activity and methods of detecting compounds that modulate nucleotide polymerase activity, by detecting product formation of the nucleotide polymerase to be tested based on determination of close proximity of two labeled nucleotide probes able to bind the product of the nucleotide polymerase. It is preferred that proximity dependent energy transfer, such as forster resonance energy transfer, between said labeled nucleotide probes is determined. The invention further provides kits comprising components for carrying out the inventive methods for detection of nucleotide polymerase activity.
    Type: Grant
    Filed: May 30, 2016
    Date of Patent: January 5, 2021
    Assignees: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V., LEAD DISCOVERY CENTER GMBH
    Inventors: Tim Bergbrede, Nils-Göran Larsson, Claes Gustafsson, Maria Falkenberg-Gustafsson
  • Patent number: 10703735
    Abstract: The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
    Type: Grant
    Filed: July 23, 2019
    Date of Patent: July 7, 2020
    Assignees: Lead Discovery Center GmbH, Max Planck Gesellschaft zur Förderung der Wissenschaften e. V.
    Inventors: Raffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Uwe Koch, Bert Klebl, Axel Choidas, Anke Unger, Nils-Göran Larsson, Maria Falkenberg-Gustafsson, Claes M. Gustafsson
  • Patent number: 9567345
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: February 14, 2017
    Assignee: Lead Discovery Center GmbH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Patent number: 9453051
    Abstract: The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: September 27, 2016
    Assignees: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.V., Lead Discovery Center GmbH
    Inventors: Gunter Fischer, Miroslav Malesevic, Frank Erdmann, Jan Kuhling, Michael Bukrinsky, Stephanie Constant, Gerd Ruhter, Peter Nussbaumer, Klaus Dinkel
  • Patent number: 9242937
    Abstract: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: January 26, 2016
    Assignees: Bayer Intellectual Property GmbH, LEAD DISCOVERY CENTER GMBH
    Inventors: Gerd Rühter, Peter Nussbaumer, Axel Choidas, Carsten Schulz-Fademrecht, Bert Klebl, Jan Eickhoff
  • Patent number: 9096608
    Abstract: Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: August 4, 2015
    Assignee: Lead Discovery Center GmbH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
  • Publication number: 20150111873
    Abstract: Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 23, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
  • Patent number: 8999982
    Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: April 7, 2015
    Assignees: Lead Discovery Center GmbH, Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.
    Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
  • Publication number: 20150018329
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 15, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Publication number: 20140303167
    Abstract: The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
    Type: Application
    Filed: August 22, 2012
    Publication date: October 9, 2014
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
  • Publication number: 20140296304
    Abstract: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2012
    Publication date: October 2, 2014
    Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Gerd Rühter, Peter Nussbaumer, Axel Choidas, Carsten Schulz-Fademrecht, Bert Klebl, Jan Eickhoff
  • Publication number: 20140287454
    Abstract: The present invention relates to a method of selecting (a) cell(s), (a) tissue(s) or (a) cell culture(s) with susceptibility to a selective CDK9 inhibitor. Also a method for determining the responsiveness of a mammalian tumor cell or cancer cell to treatment with a selective CDK9 inhibitor is described herein. In particular, the present invention provides for an in vitro method for the identification of a responder for or a patient sensitive to a selective CDK9 inhibitor, whereby the patient is suspected to suffer from NUT midline carcinoma (NMC). The present invention also relates to a method of monitoring or predicting the efficacy of a treatment of NUT midline carcinoma (NMC), wherein treatment with a selective CDK9 inhibitor is in particular envisaged. Also the use of a (transgenic) non-human animal or a (transgenic) cell having at least one rearrangement in the NUT gene for screening and/or validation of a medicament for the treatment NUT midline carcinoma (NMC) is described.
    Type: Application
    Filed: August 22, 2012
    Publication date: September 25, 2014
    Applicants: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V., LEAD DISCOVERY CENTER GmbH
    Inventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
  • Publication number: 20140179662
    Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2012
    Publication date: June 26, 2014
    Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
  • Publication number: 20140018365
    Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 16, 2014
    Applicants: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCCHAFTEN E.V., LEAD DISCOVERY CENTER GMBH
    Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
  • Publication number: 20130079345
    Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 20, 2011
    Publication date: March 28, 2013
    Applicants: BAYER INTELLECTUAL PROPERTY GMBH, LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Peter Nussbaumer, Gerd Ruhter, Carsten Schultz-Fademrecht, Ulrich Lucking, Axel Choidas, Bert Klebl
  • Patent number: 8084457
    Abstract: The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: December 27, 2011
    Assignees: Lead Discovery Center GmbH, Bayer Pharma AG
    Inventors: Axel Choidas, Alexander Backes, Matt Cotten, Ola Engkvist, Beatrice Felber, Achim Freisleben, Klaus Godl, Zoltán Greff, Peter Habenberger, Doris Hafenbradl, Christian Hartung, Thomas Herget, Edmund Hoppe, Bert Klebl, Andrea Missio, Gerhard Müller, Wilfried Schwab, Birgit Zech, Jose Bravo, John Harris, Joelle Le, Jackie Macritchie, Vladimir Savic, Brad Sherborne, Don Simpson