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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.
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公开(公告)号：US12187709B2
公开(公告)日：2025-01-07
申请号：US18052851
申请日：2022-11-04
Applicant: Genentech, Inc.
Inventor： Malcolm Huestis , Michael John Lambrecht , Jun Liang , Man Un Ung , Xiaojing Wang , Jason Robert Zbieg , Bing-Yan Zhu , Lisa Marie Barton , Fabio Broccatelli , Georgette Marie Castanedo , Araz Jakalian , Robin Larouche-Gauthier , Arun Yadav
IPC: C07D403/12 , A61P35/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D493/08
Abstract: A compound, of formula (I): suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.
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公开(公告)号：US20240300927A1
公开(公告)日：2024-09-12
申请号：US18275655
申请日：2022-02-03
Applicant: Genentech, Inc.
Inventor： Jun Liang , Araz Jakalian , Michael John Lambrecht , Robin Larouche-Gauthier , Malcolm Huestis , Man Un Ung , Xiaojing Wang , Arun Yadav , Jason Robert Zbieg , Fabio Broccatelli
IPC: C07D405/14 , A61K31/4439
CPC classification number: C07D405/14 , A61K31/4439
Abstract: Various amide compounds that bind Cbl-B, including those that are selective for C-Cbl, and methods of making and using the same. Representative amide compounds include molecules falling within the following formulae:
