Patents by Inventor Kiel Lazarski

Kiel Lazarski 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).

  • 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
  • Spirocyclic degronimers for target protein degradation
    Patent number: 11185592
    Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: May 22, 2020
    Date of Patent: November 30, 2021
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
  • 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
  • ARYL ANNULATED MACROCYCLIC INDOLE DERIVATIVES
    Publication number: 20210253598
    Abstract: The present invention relates to aryl annulated 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: August 19, 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, Steven James Ferrara, Michael H. Serrano-Wu, Christopher Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan MacCarren, Rebecca Ann Harvey, Craig Wilson
  • Macrocyclic indole derivatives
    Patent number: 10981932
    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 2019 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: May 17, 2017
    Date of Patent: April 20, 2021
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc.
    Inventors: Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Clara Christ, Kai Thede, Joachim Kuhnke, Manfred Moewes, Knut Eis, Amaury Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Philip Lienau, Ulrike Sack, Arne Scholz, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick R. McCarren
  • SPIROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
    Publication number: 20210106688
    Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Application
    Filed: May 22, 2020
    Publication date: April 15, 2021
    Applicant: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
  • COMPOUNDS
    Publication number: 20210079005
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: November 25, 2020
    Publication date: March 18, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Annick Goergler, Georg Jaeschke, Buelent Kocer, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Ulrike Obst Sander, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • MACROCYCLIC FLUORINE SUBSTITUTED INDOLE DERIVATIVES
    Publication number: 20210079018
    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: March 18, 2021
    Inventors: Steven J. Ferrara, Michael H. Serrano-Wu, Christopher Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan MacCarren, 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
  • 2-BENZOPYRAZINYL-N-HETEROARYL-2-PHENYL-ACETAMIDE COMPOUNDS
    Publication number: 20210070739
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: November 24, 2020
    Publication date: March 11, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • 2-benzopyrazinyl-n-heteroaryl-2-phenyl-acetamide compounds
    Patent number: 10882848
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Grant
    Filed: June 21, 2019
    Date of Patent: January 5, 2021
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • C3-carbon linked glutarimide degronimers for target protein degradation
    Patent number: 10849982
    Abstract: This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: December 1, 2020
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Kiel Lazarski, Gesine Kerstin Veits, Harit U. Vora
  • BIFUNCTIONAL MOLECULES THAT DEGRADE EGFR
    Publication number: 20200361930
    Abstract: The present invention provides compounds that cause specifically the degradation of EGFR via the targeted ubiquitination of EGFR protein and subsequent proteasomal degradation. The present compounds are useful for the treatment of various cancers.
    Type: Application
    Filed: August 4, 2020
    Publication date: November 19, 2020
    Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • BIFUNCTIONAL INHIBITORS WITH EGFR HAVING A E3 UBIQUITIN LIGASE MOIETY
    Publication number: 20200308171
    Abstract: Present invention provides bifunctional compounds that comprise an E3 Ubiquitin Ligase moiety that is linked to a moiety that inhibit EGFR, where the target protein can be proximate to the ubiquitin ligase to effect degradation of said protein. Present compounds are useful for the treatment of various cancers.
    Type: Application
    Filed: June 16, 2020
    Publication date: October 1, 2020
    Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.
    Inventors: Georg Jaeschke, Bernd Kuhn, Antonio Ricci, Daniel Rueher, Sandra Steiner, Yvonne Alice Nagel, Martin Duplessis, Kiel Lazarski, Yanke Liang
  • Spirocyclic degronimers for target protein degradation
    Patent number: 10660968
    Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: May 26, 2020
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
  • MACROCYCLIC INDOLE DERIVATIVES
    Publication number: 20200087322
    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: May 17, 2017
    Publication date: March 19, 2020
    Inventors: Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Clara Christ, Kai Thede, Joachim Kuhnke, Manfred Moewes, Knut Eis, Amaury Fernandez-Montalvan, Nicolas Werbeck, Ursula Moenning, Philip Lienau, Ulrike Sack, Arne Scholz, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick R. McCarren
  • 2-BENZOPYRAZINYL-N-HETEROARYL-2-PHENYL-ACETAMIDE COMPOUNDS
    Publication number: 20190308955
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: June 21, 2019
    Publication date: October 10, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • SPIROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
    Publication number: 20190076540
    Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Application
    Filed: November 9, 2018
    Publication date: March 14, 2019
    Applicant: C4 Theraprutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael