公开(公告)号：US20230081720A1

公开(公告)日：2023-03-16

申请号：US17613020

申请日：2020-05-19

申请人： NOVARTIS AG ,  LES LABORATOIRES SERVIER

发明人： Matthew T. Burger ,  Maia Chanrion ,  Frédéric Colland ,  Marton Csekei ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Jean-Michel Henlin ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  Eric McNeill ,  Mark G. Palermo ,  Francesca Rocchetti ,  Jérôme Starck ,  Bing Yu ,  Qiang Zhang ,  Ágnes Proszenyák ,  Szabolcs Sipos ,  Zhuoliang Chen ,  Katsumasa Nakajima ,  Joseph Anthony D'Alessio ,  John William Blankenship

IPC分类号： A61K47/68

摘要： Anti-CD74 antibody-drug conjugates are disclosed. The anti-CD74 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD74 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20230092679A1

公开(公告)日：2023-03-23

申请号：US17613006

申请日：2020-05-19

申请人： NOVARTIS AG ,  LES LABORATOIRES SERVIER

发明人： Matthew T. Burger ,  Maia Chanrion ,  Frédéric Colland ,  Marton Csekei ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Jean-Michel Henlin ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  Eric McNeill ,  Mark G. Palermo ,  Francesca Rocchetti ,  Jérôme Starck ,  Bing Yu ,  Qiang Zhang ,  Ágnes Proszenyák ,  Szabolcs Sipos ,  Zhuoliang Chen ,  Katsumasa Nakajima ,  Joseph Anthony D'Alessio

IPC分类号： A61K47/68 ,  A61K47/65 ,  A61K31/505 ,  A61P35/00

摘要： Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20240269304A1

公开(公告)日：2024-08-15

申请号：US18038435

申请日：2021-11-23

申请人： Novartis AG ,  Les Laboratoires Servier

发明人： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Eric McNeill ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Bing Yu ,  Qiang Zhang ,  Frédéric Colland ,  James Edward Paul Davidson ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  James Brooke Murray ,  Tibor Novak ,  Jérôme Benoit Starck

IPC分类号： A61K47/68 ,  A61P35/00

CPC分类号： A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61P35/00

摘要： Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure farther relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20240182464A1

公开(公告)日：2024-06-06

申请号：US18275379

申请日：2022-02-01

申请人： Les Laboratoirens Serviece ,  Novartis AG

发明人： András Herner ,  Piroska Markacz ,  Gang Liu ,  Katsumasa Nakajima ,  Tibor Novak ,  Georges-Alain Franzetti ,  Jérôme-Benoît Starck ,  Frédéric Colland ,  Patrice Desos ,  Attila Paczal ,  Bianka Szokol ,  Mátyás Pál Timari ,  Vilibald Kun ,  Matthew T. Burger ,  Joseph Anthony D'Alessio ,  Katherine Elizabeth Seiss ,  Rany Mathew Thomas ,  Liang Zhao

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D417/14

CPC分类号： C07D471/04 ,  A61P35/00 ,  C07D417/14

摘要： The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.