公开(公告)号：US20230002367A1

公开(公告)日：2023-01-05

申请号：US17771127

申请日：2020-10-26

Applicant: Hoffmann-La Roche Inc. ,  C4 THERAPEUTICS, INC.

Inventor： Delphine GAUFRETEAU ,  Roman HUTTER ,  Eleonora JOVCHEVA ,  Bernd KUHN ,  Thomas LUEBBERS ,  Rainer E. MARTIN ,  Laetitia Janine MARTIN ,  Barbara Johanna MUELLER ,  Roger NORCROSS ,  Fabienne RICKLIN ,  Philipp SCHMID ,  Jean-Yves WACH ,  Juergen WICHMANN ,  Martin DUPLESSIS ,  Kiel LAZARSKI ,  Yanke LIANG

IPC: C07D417/14 ,  C07D471/08 ,  C07D471/10 ,  C07D498/10 ,  C07D487/08

Abstract: The invention provides a bifunctional compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein said Targeting Ligand, Linker and Degron are as described herein.

公开(公告)号：US20230024096A1

公开(公告)日：2023-01-26

申请号：US17771204

申请日：2020-10-28

Applicant: Hoffmann-La Roche Inc. ,  C4 THERAPEUTICS, INC.

Inventor： 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

IPC: A61K47/55 ,  A61K47/54 ,  A61K45/06

Abstract: The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).

公开(公告)号：US20240368150A1

公开(公告)日：2024-11-07

申请号：US18546087

申请日：2022-02-10

Applicant: Hoffmann-La Roche Inc.

Inventor： Adrian BRITSCHGI ,  Roman HUTTER ,  Holger KUEHNE ,  Bernd KUHN ,  Thomas LUEBBERS ,  Laetitia Janine MARTIN ,  Barbara Johanna MUELLER ,  Juergen WICHMANN ,  Marco BRANDSTAETTER

IPC: C07D417/04 ,  A61K31/554 ,  A61K31/69 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/08 ,  C07D491/107 ,  C07D519/00 ,  C07F5/02

Abstract: The present invention provides new bicyclic tetrahydroazepine derivatives having the general formula (I), wherein X, Y, R1, R2, R3, R4, R5, R6, R6a are as defined herein, compositions including the compounds, processes of manufacturing the compounds and methods of using them in the treatment of cancer.

公开(公告)号：US20200339522A1

公开(公告)日：2020-10-29

申请号：US16811656

申请日：2020-03-06

Applicant: Hoffmann-La Roche Inc.

Inventor： Jerome HERT ,  Daniel HUNZIKER ,  Holger KUEHNE ,  Thomas LUEBBERS ,  Rainer E. MARTIN ,  Patrizio MATTEI ,  Werner NEIDHART ,  Hans RICHTER ,  Markus RUDOLPH ,  Emmanuel PINARD

IPC: C07D249/08 ,  C07D487/04 ,  C07D249/12 ,  C07D409/12 ,  C07D413/12 ,  C07D231/12 ,  C07F7/08 ,  C07D401/12 ,  C07D407/12 ,  C07D407/04 ,  C07D471/04 ,  C07D237/14 ,  C07D403/12 ,  C07D417/12 ,  C07D231/56 ,  A61P27/02 ,  C07B41/04 ,  C07D231/20 ,  C07D249/04

Abstract: The invention provides novel compounds having the general formula (I) wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.