公开(公告)号：US20230295145A1

公开(公告)日：2023-09-21

申请号：US18323240

申请日：2023-05-24

Applicant: Genentech, Inc.

Inventor： Jakob Fuhrmann ,  Nicholas John Skelton ,  Peter Scott Dragovich

IPC: C07D413/14 ,  C07D417/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D401/14 ,  C07D487/04 ,  A61P35/00

CPC classification number: C07D413/14 ,  C07D417/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D401/14 ,  C07D487/04 ,  A61P35/00

Abstract: The present disclosure relates to compounds and pharmaceutical compositions thereof, and methods of using the compounds and compositions in therapy, such as methods of treating cancer.

公开(公告)号：US20250064945A1

公开(公告)日：2025-02-27

申请号：US18709947

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Huifen Chen ,  Peter Scott Dragovich ,  Leanna Renee Staben ,  Jing Wang

IPC: A61K47/55 ,  A61K31/519 ,  A61K47/54 ,  C07D487/04 ,  C07D519/00

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20250059198A1

公开(公告)日：2025-02-20

申请号：US18710130

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Fabio Broccatelli ,  Huifen Chen ,  Peter Scott Dragovich ,  Jing Wang

IPC: C07D487/08 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.