Abstract: New treatments for Ikaros and/or Aiolos mediated disorders are provided that comprise administering an effective amount of a cereblon binder that degrades Ikaros or Aiolos by the ubiquitin proteasome pathway.
Type:
Application
Filed:
February 7, 2023
Publication date:
June 22, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
David Proia, James A. Henderson, Minsheng He, Andrew Charles Good, Andrew J. Phillips
Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
Type:
Application
Filed:
August 1, 2022
Publication date:
June 22, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Adrian Britschgi, Fabian Dey, Annick Goergler, Eric Andre Kusznir, Moreno Attilio Wichert
Abstract: The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
Type:
Grant
Filed:
June 17, 2022
Date of Patent:
June 13, 2023
Assignee:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Martin Duplessis, Jae Young Ahn, Alexander W. Hird, Ryan E. Michael, Kiel Lazarski, Yanke Liang, Georg Jaeschke, Antonio Ricci, Annick Goergler, Daniel Rueher
Abstract: Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.
Type:
Application
Filed:
December 19, 2022
Publication date:
May 11, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Martin Duplessis, Mark E. Fitzgerald, Victoria Garza, Andrew Charles Good, Katrina L. Jackson, Yanke Liang, Moses Moustakim, Morgan Welzel O'Shea, Gesine Kerstin Veits, Jeremy L. Yap, Robert T. Yu, Cosimo Dolente, David Stephen Hewings, Daniel Hunziker, Bernd Kuhn, Piergiorgio Francesco Tommaso Pettazzoni, Fabienne Ricklin, Claus Riemer, Juergen Wichmann
Abstract: The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
Type:
Application
Filed:
June 17, 2022
Publication date:
April 13, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Martin Duplessis, Jae Young Ahn, Alexander W. Hird, Ryan E. Michael, Kiel Lazarski, Yanke Liang, Georg Jaeschke, Antonio Ricci, Annick Goergler, Daniel Rueher
Abstract: The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
Type:
Grant
Filed:
November 24, 2020
Date of Patent:
April 11, 2023
Assignee:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Roger Norcross, Philipp Schmid
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 11, 2021
Publication date:
March 30, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
Abstract: Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
Type:
Application
Filed:
April 18, 2022
Publication date:
March 16, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
James A. Henderson, Minsheng He, Andrew Charles Good, Andrew John Phillips
Abstract: BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.
Type:
Application
Filed:
September 1, 2022
Publication date:
March 2, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Rhamy Zeid, Ning Yin, Katrina L. Jackson, Gesine Kerstin Veits, Moses Moustakim, Jeremy L. Yap
Abstract: The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
February 21, 2023
Assignee:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Bernd Kuhn, Roger Norcross, Stephan Roever, Philipp Schmid
Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
Type:
Application
Filed:
February 1, 2021
Publication date:
January 19, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
Abstract: The present invention provides heterocyclic compounds that bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation in a human or other host. The present invention also provides compounds that can be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
Type:
Application
Filed:
September 2, 2021
Publication date:
January 19, 2023
Applicant:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Roger Norcross, Fabian Dey, Annick Goergler, Eric Kusznir
Abstract: This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.
Type:
Application
Filed:
June 18, 2021
Publication date:
November 24, 2022
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Katrina L. Jackson, Minsheng He, Yanke Liang, Mark E. Fitzgerald, Victoria Garza
Abstract: This invention provides amine-linked C3-glutarimide Degronimers and Degrons for therapeutic applications as described further herein, and methods of use and compositions thereof as well as methods for their preparation.
Type:
Application
Filed:
December 14, 2020
Publication date:
October 6, 2022
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Chi-li Chen, Martin Duplessis, Minsheng He, Kiel Lazarski
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:
Application
Filed:
November 30, 2020
Publication date:
October 6, 2022
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Kiel Lazarski, Gesine Kerstin Veits, Harit U. Vora
Abstract: This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that 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. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
October 4, 2022
Assignee:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Martin Duplessis, Chi-Li Chen
Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
Type:
Application
Filed:
January 14, 2022
Publication date:
September 15, 2022
Applicant:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
Abstract: Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
Type:
Grant
Filed:
October 11, 2021
Date of Patent:
August 9, 2022
Assignee:
C4 Therapeutics, Inc.
Inventors:
James A. Henderson, Minsheng He, Andrew Charles Good, Andrew John Phillips