Patents by Inventor Stefan KAULFUSS

Stefan KAULFUSS 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).

  • Covalent PPARG inverse-agonists
    Publication number: 20240150277
    Abstract: The present invention includes compounds of formula (I) and methods for its preparation and treatment of disorders with activated peroxisome preoliferator-activated receptor gamma (PPARG), particularly cancer.
    Type: Application
    Filed: August 31, 2023
    Publication date: May 9, 2024
    Applicants: Bayer Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Stephan SIEGEL, Knut EIS, Timo STELLFELD, Léa Aurelie BOUCHÉ, Elisabeth POOK, Joseph Peter BLUCK, Philip LIENAU, Constantia PANTELIDOU, Isabel Sophie JERCHEL-FURAU, Ulf BRÜEGGEMEIER, Sven CHRISTIAN, Detlev SÜLZLE, Anders Roland FRIBERG, Simon HOLTON, Christian LECHNER, Stefan KAULFUSS, Hanna MEYER, Douglas ORSI, Steven James FERRARA, Jonathan GOLDSTEIN, Matthew MEYERSON, Christopher LEMKE
  • Covalent PPARG inverse-agonists
    Publication number: 20240109850
    Abstract: The present invention includes compounds of formula (I) and methods for its preparation and treatment of disorders with activated peroxisome preoliferator-activated receptor gamma (PPARG), particularly cancer.
    Type: Application
    Filed: August 31, 2023
    Publication date: April 4, 2024
    Applicants: Bayer Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Knut EIS, Elisabeth POOK, Ulf BRÜGGEMEIER, Adelaide Clara F. A. DE LEMOS, Sven CHRISTIAN, Isabel Sophie JERCHEL-FURAU, Ulrike RAUH, Nico BRÄUER, Timo STELLFELD, Anders Roland FRIBERG, Christian LECHNER, Stefan KAULFUSS, Hanna MEYER, Charlotte Christine KOPITZ, Steven James FERRARA, Jonathan GOLDSTEIN, Matthew MEYERSON, Christopher LEMKE, Timothy A. LEWIS
  • Substituted macrocyclic indole derivatives
    Patent number: 11891404
    Abstract: The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: September 8, 2022
    Date of Patent: February 6, 2024
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Sven Wittrock, David McKinney, Michael H. Serrano-Wu, Chris Lemke, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick Ryan McCarren, Rebecca Ann Harvey
  • SUBSTITUTED 3,6-DIHYDRO-2H-1,3,4-OXADIAZIN-2-ONES FOR THE TREATMENT OF SARCOMA
    Publication number: 20230405015
    Abstract: The present invention provides a method of treatment of sarcoma comprising administering to a patient in need thereof a compound of general formula (I), in which R1, R2, R3, and R4, are as defined herein, alone or in pharmaceutical compositions or combinations comprising said compounds as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: August 31, 2023
    Publication date: December 21, 2023
    Applicants: Bayer Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Martin LANGE, Stefan KAULFUSS, Charlotte Christine KOPITZ, Heidi GREULICH, Xiaoyun WU, Matthew MEYERSON
  • SUBSTITUTED HETEROCYCLIC COMPOUNDS AND THERAPEUTIC USES THEREOF
    Publication number: 20230391769
    Abstract: Compounds of formula (I), process for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 27, 2021
    Publication date: December 7, 2023
    Inventors: Volker Schulze, Anne Mengel, Adelaide Clara Faria Alvares De Lemos, Sven Christian, Ulf Bömer, Roman Hillig, Christian Lechner, Jérémie Xavier Mortier, Stefan Kaulfuss, Steven Corsello, Katarzyna Handing, Amael Madec, Laura Furst, Mrinal Shekhar, Markus Berger, Rajesha Rupaimoole, Philip Lienau, Douglas Orsi, David McKinney, Krzysztof Brezezinka
  • SUBSTITUTED PYRROLO-PYRIDINONE DERIVATIVES AND THERAPEUTIC USES THEREOF
    Publication number: 20230365554
    Abstract: Compounds of formula (I), process for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 27, 2021
    Publication date: November 16, 2023
    Inventors: Volker Schulze, Anne Mengel, Adelaide Clara Faria Alvares De Lemos, Ulrike Rauh, Ulf Bömer, Roman Hillig, Christian Lechner, Jeremie Xavier G. Mortier, Detlev Sülzle, Stefan Kaulfuss, Steven Corsello, Katarzyna Handing, Alisha Caliman, Amael Madec
  • SUBSTITUTED 1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20230339939
    Abstract: Compounds of formula (I), process for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 27, 2021
    Publication date: October 26, 2023
    Inventors: Volker Schulze, Anne Mengel, Adelaide Clara Faria Alvares De Lemos, Sven Christian, Ulf Bömer, v Hillig, Christian Lechner, Jérémie Xavier Mortier, Stefan Kaulfuss, Steven Corsello, Katarzyna Handing, Amael Madec, Laura Furst, Mrinal Shekhar, Markus Berger, Rajesha Rupaimoole, Philip Lienau, Douglas Orsi, David McKinney, Krzysztof Brezezinka
  • ARYL SUBSTITUTED PYRROLO-PYRIDINONES AND THERAPEUTIC USES THEREOF
    Publication number: 20230322767
    Abstract: Compounds of formula (I), process for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 27, 2021
    Publication date: October 12, 2023
    Inventors: Volker Schulze, Anne Mengel, Adelaide Clara Faria Alvares De Lemos, Ulrike Rauh, Ulf Bömer, Roman Hillig, Christian Lechner, Jérémie Xavier Mortier, Stefan Kaulfuss, Steven Corsello, Katarzyna Handing, Amael Madec, Laura Furst, Mrinal Shekhar, David McKinney
  • SUBSTITUTED MACROCYCLIC INDOLE DERIVATIVES
    Publication number: 20230112244
    Abstract: The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: September 8, 2022
    Publication date: April 13, 2023
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Sven Wittrock, David McKinney, Michael H. Serrano-Wu, Chris Lemke, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick Ryan McCarren, Rebecca Ann Harvey
  • 3-AMINO-2-[2-(ACYLAMINO)PYRIDIN-4-YL]-1,5,6,7-TETRAHYDRO-4H-PYRROLO[3,2-C]PYRIDIN-4-ONE AS CSNK1 INHIBITORS
    Publication number: 20230046077
    Abstract: The present invention relates to compounds of formula (I) processes for their production and their use as pharmaceuticals. The compounds are inhibitors of Casein kinase 1 alpha and/or delta (CSNK1? and/or ?) useful for the treatment of proliferative disorders.
    Type: Application
    Filed: February 6, 2020
    Publication date: February 16, 2023
    Inventors: Volker Schulze, Anne Mengel, Jens Schroeder, Adelaide Clara Faria Alvares De Lemos, Wilhelm Bone, Ulf Bomer, Detlev Sulzle, Clara Christ, Roman Hillig, Christian Lechner, Steven Corsello, Kasia Handing, Alisha Caliman, Ulrike Rauh, Stefan Kaulfuss, Jérémie Mortier
  • PYRIMIDINEDIONE DERIVATIVES
    Publication number: 20220411381
    Abstract: The present invention covers pyrimidinedione derivatives of general formula (I): (I), in which R1, R2, R4, 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: Application
    Filed: September 25, 2020
    Publication date: December 29, 2022
    Applicant: Bayer Aktiengesellschaft
    Inventors: Lea Aurelie BOUCHE, Stefan KAULFUSS, Katja ZIMMERMANN, Hartmut REHWINKEL, Roland NEUHAUS, Roman HILLIG, Duy NGUYEN, Judith GÜNTHER, Adelaide Clara FARIA ALVARES DE LEMOS
  • Macrocyclic chlorine substituted indole derivatives
    Patent number: 11478451
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Date of Patent: October 25, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Chris Lemke, Michael H. Serrano-Wu, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Laura Furst, Guo Wei, Patrick R. McCarren, Rebecca Ann Harvey, Daniel Payne, Thomas Pesnot, Craig Wilson
  • Macrocyclic chlorine substituted indole derivatives
    Patent number: 11447504
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Date of Patent: September 20, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Katrin Nowak-Reppel, Jérémie Xavier Mortier, Patrick R. McCarren, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Laura Furst, Guo Wei, Rebecca Ann Harvey, Daniel Payne, Thomas Pesnot, Craig Wilson
  • Substituted macrocyclic indole derivatives
    Patent number: 11440923
    Abstract: The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Date of Patent: September 13, 2022
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel, Sven Wittrock, David McKinney, Michael H. Serrano-Wu, Chris Lemke, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Laura Furst, Guo Wei, Patrick R. McCarren, Rebecca Ann Harvey
  • MACROCYCLIC FLUORINE SUBSTITUTED INDOLE DERIVATIVES
    Publication number: 20220281891
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: March 10, 2022
    Publication date: September 8, 2022
    Inventors: Steven J. Ferrara, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning
  • Macrocyclic indole derivatives
    Patent number: 11401278
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Date of Patent: August 2, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Laura Furst, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Guo Wei, Patrick R. McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel
  • Macrocyclic fluorine substituted indole derivatives
    Patent number: 11286263
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Date of Patent: March 29, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Steven James Ferrara, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning
  • MACROCYCLIC INDOLE DERIVATIVES
    Publication number: 20210292341
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Publication date: September 23, 2021
    Inventors: Laura Furst, Michael H. Serrano-Wu, Christopher Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Guo Wei, Patrick Ryan McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel
  • MACROCYCLIC CHLORINE SUBSTITUTED INDOLE DERIVATIVES
    Publication number: 20210277022
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Publication date: September 9, 2021
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel, Jeremie Xavier Mortier, Patrick Ryan McCarren, Michael H. Serrano-Wu, Christopher Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Rebecca Ann Flarvey, Daniel Payne, Thomas Pesnot, Craig Wilson
  • SUBSTITUTED MACROCYCLIC INDOLE DERIVATIVES
    Publication number: 20210269456
    Abstract: The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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: November 15, 2018
    Publication date: September 2, 2021
    Inventors: Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel, Sven Wittrock, David McKinney, Michael H. Serrano-Wu, Christopher Lemke, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick Ryan McCarren, Rebecca Ann Harvey