公开(公告)号：US20230002367A1

公开(公告)日：2023-01-05

申请号：US17771127

申请日：2020-10-26

申请人： Hoffmann-La Roche Inc. ,  C4 THERAPEUTICS, INC.

发明人： 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分类号： C07D417/14 ,  C07D471/08 ,  C07D471/10 ,  C07D498/10 ,  C07D487/08

摘要： 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：US20180222866A1

公开(公告)日：2018-08-09

申请号：US15945429

申请日：2018-04-04

申请人： Hoffmann-La Roche Inc.

发明人： Maude GIROUD ,  Wolfgang HAAP ,  Bernd KUHN ,  Rainer E. MARTIN

IPC分类号： C07D231/14 ,  A61P33/02 ,  C07D263/34 ,  C07D249/06 ,  C07D261/18 ,  C07D271/06 ,  C07D271/10 ,  C07D401/04 ,  C07D213/56 ,  C07D405/04 ,  C07D403/04 ,  C07D401/12

CPC分类号： C07D231/14 ,  A61P33/02 ,  C07D213/56 ,  C07D249/06 ,  C07D261/10 ,  C07D261/18 ,  C07D263/34 ,  C07D271/06 ,  C07D271/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04

摘要： The invention relates to a compound of formula (I) wherein R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

公开(公告)号：US20230203056A1

公开(公告)日：2023-06-29

申请号：US18172506

申请日：2023-02-22

申请人： Hoffmann-La Roche Inc.

发明人： Joerg BENZ ,  Uwe GRETHER ,  Benoit HORNSPERGER ,  Carsten KROLL ,  Bernd KUHN ,  Rainer E. MARTIN ,  Fionn O'HARA ,  Hans RICHTER ,  Martin RITTER ,  Philipp SCHMID

IPC分类号： C07D491/147 ,  C07D487/04

CPC分类号： C07D491/147 ,  C07D487/04

摘要： The invention provides new heterocyclic compounds having the general formula (I)




wherein X, Y, Z, A, L, B, and R1 to R3 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20220098176A1

公开(公告)日：2022-03-31

申请号：US17465536

申请日：2021-09-02

申请人： Hoffmann-La Roche Inc.

发明人： Joerg BENZ ,  Uwe GRETHER ,  Benoit HORNSPERGER ,  Carsten KROLL ,  Bernd KUHN ,  Rainer E. MARTIN ,  Fionn O'HARA ,  Bernd PUELLMANN ,  Hans RICHTER ,  Martin RITTER

IPC分类号： C07D403/06 ,  C07D487/04 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14 ,  A61K9/20 ,  A61K9/48

摘要： The invention provides new heterocyclic compounds having the general formula (I) wherein B, C, L, X, Y, RL and R3 to R5 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20240199587A1

公开(公告)日：2024-06-20

申请号：US18490967

申请日：2023-10-20

申请人： Hoffmann-La Roche Inc.

发明人： Machoud AMOUSSA ,  Joerg BENZ ,  Niels Kevin BRIAN ,  Kallie FRISTON ,  Maude GIROUD ,  Uwe GRETHER ,  Katrin GROEBKE ZBINDEN ,  Benoit HORNSPERGER ,  Carsten KROLL ,  Bernd KUHN ,  Camiel John LEAKE ,  Rainer E. MARTIN ,  David Friedrich Erhard NIPPA ,  Fionn Susannah O’HARA ,  Bernd PUELLMANN ,  Hans RICHTER ,  Martin RITTER ,  Didier ROMBACH ,  Philipp Claudio SCHMID ,  Shounan ZHANG

IPC分类号： C07D403/14 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

CPC分类号： C07D403/14 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

摘要： The invention provides new heterocyclic compounds having the general formula (I)




wherein A, B, X, and R1 to R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20200317624A1

公开(公告)日：2020-10-08

申请号：US16793178

申请日：2020-02-18

申请人： Hoffmann-La Roche Inc.

发明人： Jerome HERT ,  Daniel HUNZIKER ,  Christoph KURATLI ,  Rainer E. MARTIN ,  Patrizio MATTEI ,  Alexander Lee SATZ

IPC分类号： C07D239/90 ,  C07D401/04 ,  C07D471/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R12, R13, R14, A1, A2, A3, n and m 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

申请人： Hoffmann-La Roche Inc. ,  C4 THERAPEUTICS, INC.

发明人： 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分类号： A61K47/55 ,  A61K47/54 ,  A61K45/06

摘要： 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：US20200339522A1

公开(公告)日：2020-10-29

申请号：US16811656

申请日：2020-03-06

申请人： Hoffmann-La Roche Inc.

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

IPC分类号： 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

摘要： 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.

公开(公告)号：US20230310641A1

公开(公告)日：2023-10-05

申请号：US18145453

申请日：2022-12-22

申请人： Hoffmann-La Roche Inc.

发明人： Kerstin HOFER ,  Rainer E. MARTIN ,  Mohamed Yosry Hassan MOHAMED ,  Tobias OELSCHLAEGEL ,  Felix Franz SCHUMACHER ,  Tatjana SELA

IPC分类号： A61K47/68 ,  C07K16/32 ,  A61K47/54 ,  C07K16/28

CPC分类号： A61K47/6871 ,  A61K47/6811 ,  C07K16/32 ,  A61K47/6851 ,  A61K47/6807 ,  A61K47/549 ,  C07K16/2896 ,  C07K16/2881 ,  A61K2039/505

摘要： The present invention relates to a modified antibody comprising a heavy chain and a light chain, wherein the heavy chain or/and the light chain comprises one or more first recognition site(s) for the transglutaminase from Kutzneria albida (KalbTG) or a functionally active variant thereof. The one or more first recognition site(s) are introduced at one or more selected position(s) within the antibody's heavy chain and/or light chain. The invention further relates to one or more nucleic acids encoding the modified antibody according to the invention as well as a covalent conjugate comprising (i) the modified antibody according to the invention and (ii) one or more non-antibody moieties (payload(s)) covalently conjugated to the one or more first recognition site(s) either directly or via a first linker. In certain embodiments, the non-antibody moiety comprises a therapeutic entity and optionally a second linker. The present invention further relates to a method of covalently conjugating a modified antibody according to the invention to non-antibody moieties. In case the non-antibody moiety comprises a therapeutic entity, the present invention further relates to the conjugate of the modified antibody according to the invention and the therapeutic entity as pharmaceutical composition, for use as a medicament as well as for use in treating a disease.

公开(公告)号：US20220106328A1

公开(公告)日：2022-04-07

申请号：US17552816

申请日：2021-12-16

申请人： Hoffmann-La Roche Inc.

发明人： Joerg BENZ ,  Luca GOBBI ,  Uwe GRETHER ,  Benoit HORNSPERGER ,  Carsten KROLL ,  Bernd KUHN ,  Rainer E. MARTIN ,  Fionn O`HARA ,  Bernd PUELLMANN ,  Hans RICHTER ,  Martin RITTER

IPC分类号： C07D498/04 ,  A61K9/20 ,  A61K9/48

摘要： The invention provides new heterocyclic compounds having the general formulae (Ia) and (Ib) wherein A, B, and L are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.