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:
Application
Filed:
November 24, 2020
Publication date:
March 11, 2021
Applicant:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Roger Norcross, Philipp Schmid
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:
Application
Filed:
October 16, 2020
Publication date:
February 4, 2021
Applicant:
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:
Grant
Filed:
May 11, 2020
Date of Patent:
February 2, 2021
Assignee:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
Abstract: The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
Type:
Application
Filed:
September 24, 2020
Publication date:
January 14, 2021
Applicant:
C4 Therapeutics, Inc.
Inventors:
James A. Henderson, Gesine Kerstin Veits, Minsheng He, Christopher G. Nasveschuk, Andrew J. Phillips, Andrew Charles Good
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
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
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
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:
March 4, 2020
Publication date:
July 2, 2020
Applicant:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Adrian Britschgi, Fabian Dey, Annick Goergler, Eric Andre Kusznir, Moreno Attilio Wichert
Abstract: The present invention provides selected glutarimides 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:
March 4, 2020
Publication date:
July 2, 2020
Applicant:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Annick Goergler, Philipp Schmid, Fabian Dey, Eric Andre Kusznir
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:
March 4, 2020
Publication date:
July 2, 2020
Applicant:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
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
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:
Grant
Filed:
November 9, 2018
Date of Patent:
May 12, 2020
Assignee:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
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:
Application
Filed:
December 19, 2019
Publication date:
May 7, 2020
Applicant:
C4 Therapeutics, Inc.
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Martin Duplessis, Chi-Li Chen