公开(公告)号：US20190076539A1

公开(公告)日：2019-03-14

申请号：US16186333

申请日：2018-11-09

Applicant: C4 Therapeutics, Inc.

Inventor： Andrew J. Phillips ,  Chris G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Chi-li Chen ,  Martin Duplessis ,  Minsheng He ,  Kiel Lazarski

IPC: A61K47/54 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/45 ,  A61K31/4709 ,  A61K31/513

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.

公开(公告)号：US12157735B2

公开(公告)日：2024-12-03

申请号：US17965569

申请日：2022-10-13

Applicant: C4 Therapeutics, Inc.

Inventor： Christopher G. Nasveschuk ,  Rhamy Zeid ,  Ning Yin ,  Katrina L. Jackson ,  Gesine Kerstin Veits ,  Moses Moustakim ,  Jeremy L. Yap

IPC: C07D471/04 ,  A61P35/00 ,  C07D401/14

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.

公开(公告)号：US20240287076A1

公开(公告)日：2024-08-29

申请号：US18289438

申请日：2022-05-05

Applicant: BIOGEN MA INC. ,  C4 THERAPEUTICS, INC.

Inventor： Kevin M. Guckian ,  Eric Stefan ,  Corey Don Anderson ,  Jae Young Ahn ,  Morgan Welzel O'Shea ,  Jeremy L. Yap ,  Xinpeng Cheng ,  Brian T. Hopkins ,  Isaac Marx ,  Marta Nevalainen

IPC: C07D487/04 ,  A61K31/53

CPC classification number: C07D487/04 ,  A61K31/53

Abstract: This disclosure relates to compounds of Formula (A): BTK-L-DSM (A) or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches BTK to DSM, and BTK is a Btk binding moiety represented by Formula (I) or Formula (II) that is covalently attached to linker L: in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of Btk proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of Btk proteins. The present disclosure also provides methods of treating disorders responsive to modulation of Btk activity and/or degradation of Btk with at least one compound described herein.

公开(公告)号：US12048748B2

公开(公告)日：2024-07-30

申请号：US17524558

申请日：2021-11-11

Applicant: C4 Therapeutics, Inc.

Inventor： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Kiel Lazarski ,  Ryan E. Michael

IPC: A61K31/435 ,  A61K31/438 ,  A61K47/54 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

CPC classification number: A61K47/545 ,  A61K31/435 ,  A61K31/438 ,  A61K47/554 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

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.

公开(公告)号：US20240199581A1

公开(公告)日：2024-06-20

申请号：US18534395

申请日：2023-12-08

Applicant: C4 Therapeutics, Inc.

Inventor： Christopher G. Nasveshuk ,  Katrina L. Jackson ,  Yanke Liang ,  Robert T. Yu ,  Martin Duplessis ,  Mark E. Fitzgerald ,  Victoria Garza ,  Andrew Charles Good ,  Morgan Welzel O'Shea ,  Gesine Kerstin Veits ,  Cosimo Dolente ,  David Stephen Hewings ,  Daniel Hunziker ,  Daniela Krummenacher ,  Piergiorgio Franceso Tommaso Pettazzoni ,  Juergen Wichmann

IPC: C07D401/14 ,  A61P35/00 ,  C07D405/14 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

CPC classification number: C07D401/14 ,  A61P35/00 ,  C07D405/14 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention provides compounds or their pharmaceutically acceptable salts and their pharmaceutical compositions that can be administered to a host such as a human in need thereof for the treatment of a disorder, such as cancer, mediated by mutant BRAF. The compounds efficiently degrade Class I, II and III mutant BRAF proteins.

公开(公告)号：US20240076300A1

公开(公告)日：2024-03-07

申请号：US18144800

申请日：2023-05-08

Applicant: C4 Therapeutics, Inc.

Inventor： 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

IPC: C07D519/00 ,  A61K9/00 ,  A61K9/02 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K9/009 ,  A61K9/02 ,  A61K9/08 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  C07D487/04

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.

公开(公告)号：US20230372496A1

公开(公告)日：2023-11-23

申请号：US18134971

申请日：2023-04-14

Applicant: C4 Therapeutics, Inc.

Inventor： Christopher G. Nasveschuk ,  Corey Don Anderson ,  James A. Henderson ,  Victoria Garza ,  Yanke Liang ,  Moses Moustakim ,  Katrina L. Jackson ,  Martin Duplessis

IPC: A61K47/55 ,  A61K47/54

CPC classification number: A61K47/55 ,  A61K47/545

Abstract: 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.

公开(公告)号：US20230190760A1

公开(公告)日：2023-06-22

申请号：US18106893

申请日：2023-02-07

Applicant: C4 Therapeutics, Inc.

Inventor： David Proia ,  James A. Henderson ,  Minsheng He ,  Andrew Charles Good ,  Andrew J. Phillips

IPC: A61K31/5377 ,  A61P35/00

CPC classification number: A61K31/5377 ,  A61P35/00

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.

公开(公告)号：US20230145336A1

公开(公告)日：2023-05-11

申请号：US18084380

申请日：2022-12-19

Applicant: C4 Therapeutics, Inc.

Inventor： 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

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.

公开(公告)号：US20230095223A1

公开(公告)日：2023-03-30

申请号：US17524558

申请日：2021-11-11

Applicant: C4 Therapeutics, Inc.

Inventor： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Kiel Lazarski ,  Ryan E. Michael

IPC: A61K47/54 ,  C07D498/20 ,  C07D471/10 ,  C07D519/00 ,  A61K31/435 ,  A61K31/438

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.