Patents by Inventor Stefan Nikolaus GRADL

Stefan Nikolaus GRADL 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).

  • 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH
    Publication number: 20230365524
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 20, 2023
    Publication date: November 16, 2023
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., President and Fellows of Harvard College, The General Hospital Corporation
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MÜLLER, Sherif El SHEIKH, Han Jie ZHOU, Changjia ZHAO, David B. SYKES, Steven James FERRARA, Kery LIU, Michael KRÖBER, Claudia MERZ, Michael NIEHUES, Martina SCHÄFER, Katja ZIMMERMANN, Carl Friedrich NISING
  • 4,5-annulated 1,2,4-triazolones
    Patent number: 11787797
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 28, 2021
    Date of Patent: October 17, 2023
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus Gradl, Duy Nguyen, Knut Eis, Judith Günther, Timo Stellfeld, Andreas Janzer, Sven Christian, Thomas Mueller, Sherif El Sheikh, Han Jie Zhou, Changjia Zhao, David B. Sykes, Steven James Ferrara, Kery Liu, Simon Anthony Herbert, Claudia Merz, Michael Niehues, Carl Friedrich Nising, Martina Schäfer, Katja Zimmermann, Jörg Knäblein, Kai Thede, Thomas Faupel
  • Dihydrooxadiazinones
    Patent number: 11773070
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: July 14, 2022
    Date of Patent: October 3, 2023
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin
  • 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH
    Patent number: 11713304
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 20, 2021
    Date of Patent: August 1, 2023
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus Gradl, Duy Nguyen, Knut Eis, Judith Günther, Timo Stellfeld, Andreas Janzer, Sven Christian, Thomas Müller, Sherif El Sheikh, David B. Sykes, Steven James Ferrara, Michael Kröber, Claudia Merz, Michael Niehues, Martina Schäfer, Katja Zimmermann, Carl Friedrich Nising
  • DIHYDROOXADIAZINONES
    Publication number: 20230017200
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: July 11, 2022
    Publication date: January 19, 2023
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel ELLERMANN, Stefan Nikolaus GRADL, Charlotte Christine KOPITZ, Martin LANGE, Adrian TERSTEEGEN, Philip LIENAU, Christa HEGELE-HARTUNG, Detlev SÜLZLE, Timothy A. LEWIS, Heidi GREULICH, Xiaoyun WU, Matthew MEYERSON, Alex BURGIN
  • DIHYDROOXADIAZINONES
    Publication number: 20220396554
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: July 14, 2022
    Publication date: December 15, 2022
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel ELLERMANN, Stefan Nikolaus GRADL, Charlotte Christine KOPITZ, Martin LANGE, Adrian TERSTEEGEN, Philip LIENAU, Christa HEGELE-HARTUNG, Detlev SÜLZLE, Timothy A. LEWIS, Heidi GREULICH, Xiaoyun WU, Matthew MEYERSON, Alex BURGIN
  • Dihydrooxadiazinones
    Patent number: 11427553
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 2, 2018
    Date of Patent: August 30, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin
  • Method for the preparation of a 2,4,5-trisubstituted 1,2,4-triazolone
    Patent number: 11365179
    Abstract: The present invention provides methods for the preparation of Compound (I): Compound (I), the use of intermediates for the preparation of said compound and its crystalline form A.
    Type: Grant
    Filed: April 3, 2019
    Date of Patent: June 21, 2022
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Jorma Hassfeld, Stefan Nikolaus Gradl, Philipp Rubenbauer, Henricus Nicolaas Sebastiaan Van Der Haas, Reinerus Gerardus Gieling
  • 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH
    Publication number: 20220135536
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 20, 2021
    Publication date: May 5, 2022
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MÜLLER, Sherif El SHEIKH, David B. SYKES, Steven James FERRARA, Michael KRÖBER, Claudia MERZ, Michael NIEHUES, Martina SCHÄFER, Katja ZIMMERMANN, Carl Friedrich NISING
  • 1,2,4-TRIAZIN-3(2H)-ONE COMPOUNDS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
    Publication number: 20210353630
    Abstract: The present invention includes name compounds of general formula (I): (I) in which R1, R2, R3 and R4 are as defined herein, methods for their preparation, pharmaceutical compositions and combinations comprising said compounds, and their use for the treatment of hyperproliferative diseases.
    Type: Application
    Filed: July 30, 2021
    Publication date: November 18, 2021
    Applicants: BAYER AKTIENGESELLSCHAFT, THE BROAD INSTITUTE, INC.
    Inventors: Stefan Nikolaus GRADL, Manuel ELLERMANN, Philip LIENAU, Charlotte Christine KOPITZ, Martin LANGE, Adrian TERSTEEGEN, Detlev SÜLZLE, Timothy A. LEWIS, Heidi GREULICH, Xiaoyun WU
  • 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamides
    Patent number: 11161825
    Abstract: The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: November 2, 2021
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Jörg Weiske, Carlo Stresemann, Stefan Nikolaus Gradl, Ulrike Röhn, Clara Christ, Holger Steuber, Manfred Husemann, Norbert Schmees, Kai Thede, Stephan Siegel, Antonius Ter Laak
  • 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH
    Patent number: 11130745
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: August 18, 2020
    Date of Patent: September 28, 2021
    Assignees: BAYER AKTIENGELLSCHAFT, BAYER PHARMA AKTIEGELLSCHAFT, THE BROAD INSTITUTE INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus Gradl, Duy Nguyen, Knut Eis, Judith Günther, Timo Stellfeld, Andreas Janzer, Sven Christian, Thomas Müller, Sherif El Sheikh, David B. Sykes, Steven James Ferrara, Michael Kröber, Claudia Merz, Michael Niehues, Martina Schäfer, Katja Zimmermann, Carl Friedrich Nising
  • 4,5-ANNULATED 1,2,4-TRIAZOLONES
    Publication number: 20210188846
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: January 28, 2021
    Publication date: June 24, 2021
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MUELLER, Sherif El SHEIKH, Han Jie ZHOU, Changjia ZHAO, David B. SYKES, Steven James FERRARA, Kery LIU, Simon Anthony HERBERT, Claudia MERZ, Michael NIEHUES, Carl Friedrich NISING, Martina SCHÄFER, Katja ZIMMERMANN, Jörg KNÄBLEIN, Kai THEDE, Thomas FAUPEL
  • 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH
    Publication number: 20210188805
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 18, 2020
    Publication date: June 24, 2021
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MÜLLER, Sherif El SHEIKH, Han Jie ZHOU, Changjia ZHAO, David B. SYKES, Steven James FERRARA, Kery LIU, Michael KRÖBER, Claudia MERZ, Michael NIEHUES, Martina SCHÄFER, Katja ZIMMERMANN, Carl Friedrich NISING
  • 4,5-annulated 1,2,4-triazolones
    Patent number: 10968216
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: April 6, 2021
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus Gradl, Duy Nguyen, Knut Eis, Judith Günther, Timo Stellfeld, Andreas Janzer, Sven Christian, Thomas Mueller, Sherif El Sheikh, Han Jie Zhou, Changjia Zhao, David B. Sykes, Steven James Ferrara, Kery Liu, Simon Anthony Herbert, Claudia Merz, Michael Niehues, Carl Friedrich Nising, Martina Schäfer, Katja Zimmermann, Jörg Knäblein, Kai Thede, Thomas Faupel
  • METHOD FOR THE PREPARATION OF A 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONE
    Publication number: 20210032212
    Abstract: The present invention provides methods for the preparation of Compound (I): Compound (I), the use of intermediates for the preparation of said compound and its crystalline form A.
    Type: Application
    Filed: April 3, 2019
    Publication date: February 4, 2021
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Jorma Hassfeld, Stefan Nikolaus Gradl, Philipp Rubenbauer, Henricus Nicolaas Sebastiaan VAN DER HAAS, Reinerus Gerardus GIELING
  • 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH
    Publication number: 20200377472
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 18, 2020
    Publication date: December 3, 2020
    Applicants: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus GRADL, Duy NGUYEN, Knut EIS, Judith GÜNTHER, Timo STELLFELD, Andreas JANZER, Sven CHRISTIAN, Thomas MÜLLER, Sherif El SHEIKH, Han Jie ZHOU, Changjia ZHAO, David B. SYKES, Steven James FERRARA, Kery LIU, Michael KRÖBER, Claudia MERZ, Michael NIEHUES, Martina SCHÄFER, Katja ZIMMERMANN, Carl Friedrich NISING
  • DIHYDROOXADIAZINONES
    Publication number: 20200369633
    Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 2, 2018
    Publication date: November 26, 2020
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin
  • 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH
    Patent number: 10815215
    Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: October 27, 2020
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGELLSCHAFT, THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, THE GENERAL HOSPITAL CORPORATION
    Inventors: Stefan Nikolaus Gradl, Duy Nguyen, Knut Eis, Judith Günther, Timo Stellfeld, Andreas Janzer, Sven Christian, Thomas Müller, Sherif El Sheikh, Han Jie Zhou, Changjia Zhao, David B. Sykes, Steven James Ferrara, Kery Liu, Michael Kröber, Claudia Merz, Michael Niehues, Martina Schäfer, Katja Zimmermann, Carl Friedrich Nising
  • 6-PHENYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES AS PDE3A AND PDE3B INHIBITORS FOR TREATING CANCER
    Publication number: 20200247783
    Abstract: The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I):
    Type: Application
    Filed: August 2, 2018
    Publication date: August 6, 2020
    Applicants: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Detlev Sülzle, Timothy Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson