48 patents
Utility
Spirocyclic Compounds
18 Jan 24
The present invention provides compounds and intermediates.
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Roger Norcross, Philipp Schmid
Filed: 6 Mar 23
Utility
Spirocyclic Compounds
28 Dec 23
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.
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Bernd Kuhn, Roger Norcross, Stephan Roever, Philipp Schmid
Filed: 24 Jan 23
Utility
Tricyclic Heterobifunctional Compounds for Degradation of Targeted Proteins
23 Nov 23
Heterobifunctional compounds for targeted protein degradation that include a tricyclic cereblon binder linked to an appropriate protein targeting ligand to degrade a targeted disease-mediating protein of interest are provided.
Christopher G. Nasveschuk, Corey Don Anderson, James A. Henderson, Victoria Garza, Yanke Liang, Moses Moustakim, Katrina L. Jackson, Martin Duplessis
Filed: 14 Apr 23
Utility
Degraders and Degrons for Targeted Protein Degradation
9 Nov 23
Pharmaceutical Degraders and Degrons for use in therapeutic applications are described herein.
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Minsheng He, Kiel Lazarski
Filed: 12 Dec 22
Utility
Glutarimides for medical treatment
31 Oct 23
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.
Roger Norcross, Annick Goergler, Philipp Schmid, Fabian Dey, Eric Andre Kusznir
Filed: 4 Mar 20
Utility
Tricyclic Ligands for Degradation of IKZF2 or IKZF4
26 Oct 23
Tricyclic compounds that degrade IKZF2 and/or IKZF4 are provided for medical therapy, including abnormal cellular proliferation, including cancer, inflammatory disorders, neurodegenerative disorders or autoimmune disorders.
Christopher G. Nasveschuk, James A. Henderson, Moses Moustakim, Andrew Charies Good, David Prola
Filed: 14 Apr 23
Utility
Dihydrobenzimidazolones for medical treatment
17 Oct 23
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.
Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
Filed: 14 Jan 22
Utility
Cereblon binders for the degradation of ikaros
12 Sep 23
James A. Henderson, Gesine Kerstin Veits, Minsheng He, Christopher G. Nasveschuk, Andrew J. Phillips, Andrew Charles Good
Filed: 24 Sep 20
Utility
N/O-Linked Degrons and Degronimers for Protein Degradation
7 Sep 23
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.
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Martin Duplessis, Chi-Li Chen
Filed: 3 Oct 22
Utility
Compounds for Targeted Degradation of Ret
27 Jul 23
Novel compounds which act as protein degradation inducing moieties for proto-oncogene tyrosine-protein kinase receptor (RET), which may be either wild type RET or a mutant form of RET.
James A. Henderson, Christopher G. Naveschuk, Kiel Lazarski, Victoria Garza, Moses Moustakim, Jae Young Ahn, Gesine Kerstin Veits, Morgan Welzel O'Shea, Ryan E. Michael, Jeremy L. Yap, Yanke Liang, Andrew Charles Good, Mark E. Fitzgerald, Robert T. Yu
Filed: 3 Feb 23
Utility
Compounds for targeted degradation of BRD9
4 Jul 23
Christopher G. Nasveschuk, Rhamy Zeid, Ning Yin, Katrina L. Jackson, Gesine Kerstin Veits, Moses Moustakim, Jeremy L. Yap
Filed: 2 Dec 21
Utility
Braf Degraders
11 May 23
Present invention provides compounds that cause specifically the degradation of BRAF.
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
Filed: 19 Dec 22
Utility
Isoindolinone and Indazole Compounds for the Degradation of Egfr
13 Apr 23
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.
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
Filed: 17 Jun 22
Utility
Spirocyclic compounds
11 Apr 23
The present invention provides compounds and intermediates.
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Roger Norcross, Philipp Schmid
Filed: 24 Nov 20
Utility
Spirocyclic Degronimers for Target Protein Degradation
30 Mar 23
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.
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
Filed: 11 Nov 21
Utility
Tricyclic Degraders of Ikaros and Aiolos
16 Mar 23
Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
James A. Henderson, Minsheng He, Andrew Charles Good, Andrew John Phillips
Filed: 18 Apr 22
Utility
Compounds for Targeted Degradation of BRD9
2 Mar 23
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.
Christopher G. Nasveschuk, Rhamy Zeid, Ning Yin, Katrina L. Jackson, Gesine Kerstin Veits, Moses Moustakim, Jeremy L. Yap
Filed: 1 Sep 22
Utility
Spirocyclic compounds
21 Feb 23
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.
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Bernd Kuhn, Roger Norcross, Stephan Roever, Philipp Schmid
Filed: 16 Oct 20
Utility
Bifunctional Compounds for the Treatment of Cancer
26 Jan 23
Martin DUPLESSIS, Delphine GAUFRETEAU, Roman HUTTER, Eleonora JOVCHEVA, Bernd KUHN, Kiel LAZARSKI, Yanke LIANG, Thomas LUEBBERS, Laetitia Janine MARTIN, Rainer E. MARTIN, Barbara Johanna MUELLER, Roger NORCROSS, Philipp SCHMID, Jean-Yves WACH
Filed: 28 Oct 20
Utility
Heterocyclic Degronimers for Target Protein Degradation
19 Jan 23
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.
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
Filed: 1 Feb 21