公开(公告)号：US11673902B2

公开(公告)日：2023-06-13

申请号：US17843769

申请日：2022-06-17

申请人： C4 Therapeutics, Inc.

发明人： 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分类号： C07D519/00 ,  A61K47/32 ,  A61K9/20 ,  A61K9/48 ,  A61K9/02 ,  A61K9/08 ,  A61K47/10 ,  A61K47/12 ,  A61K9/00 ,  A61K47/26 ,  A61K47/38 ,  C07D487/04

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

摘要： 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：US20230110648A1

公开(公告)日：2023-04-13

申请号：US17843769

申请日：2022-06-17

申请人： C4 Therapeutics, Inc.

发明人： 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分类号： C07D519/00 ,  C07D487/04 ,  A61K9/20 ,  A61K9/48 ,  A61K9/02 ,  A61K9/08 ,  A61K47/10 ,  A61K47/12 ,  A61K9/00 ,  A61K47/26 ,  A61K47/38 ,  A61K47/32

摘要： 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：US20230233692A1

公开(公告)日：2023-07-27

申请号：US18105735

申请日：2023-02-03

申请人： C4 Therapeutics, Inc.

发明人： 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

IPC分类号： A61K47/55

CPC分类号： A61K47/55

摘要： 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.

公开(公告)号：US20240287076A1

公开(公告)日：2024-08-29

申请号：US18289438

申请日：2022-05-05

申请人： BIOGEN MA INC. ,  C4 THERAPEUTICS, INC.

发明人： 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分类号： C07D487/04 ,  A61K31/53

CPC分类号： C07D487/04 ,  A61K31/53

摘要： 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：US20240076300A1

公开(公告)日：2024-03-07

申请号：US18144800

申请日：2023-05-08

申请人： C4 Therapeutics, Inc.

发明人： 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分类号： 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分类号： 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

摘要： 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：US20240158418A1

公开(公告)日：2024-05-16

申请号：US18516589

申请日：2023-11-21

申请人： C4 Therapeutics, Inc.

发明人： 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分类号： C07D519/00 ,  A61P35/04

CPC分类号： C07D519/00 ,  A61P35/04

摘要： The invention provides for the treatment of mutant epidermal growth factor receptor (EGFR) mediated cancer that has metastasized to the brain or other area of the central nervous system with a compound that degrades a mutant form of EGFR via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The invention also provides advantageous drug combinations for the treatment of such cancer that include a compound herein that degrades a mutant form of EGFR in combination with a second anti-cancer agent.