公开(公告)号：WO2022152705A1

公开(公告)日：2022-07-21

申请号：PCT/EP2022/050460

申请日：2022-01-11

Applicant: LES LABORATOIRES SERVIER ,  VERNALIS (R&D) LIMITED

Inventor： STOKES, Stephen ,  BEDFORD, Simon ,  CHEN, I-Jen ,  DAVIDSON, James Edward Paul ,  DAVIES, Nicholas ,  GRAHAM, Christopher John ,  MCKENNA, Sean Martin ,  MEISSNER, Johannes W.G. ,  MURRAY, James ,  PARSONS, Rachel Jane ,  RAY, Stuart ,  SANDERS, Emma ,  WALMSLEY, Claire Louise ,  BROUGH, Paul Andrew ,  KOTSCHY, András ,  PROSZENYÁK, Ágnes ,  SINAI, Ádám ,  BÁLINT, Balázs ,  CSÉKEI, Márton ,  ZWILLINGER, Márton ,  GARAMVÖLGYI, Rita ,  SIPOS, Szabolcs ,  KUN, Vilibald ,  SZABÓ, Zoltán ,  CHANRION, Maïa ,  ROCCHETTI, Francesca ,  COLLAND, Frédéric ,  MARAGNO, Ana Leticia ,  BRESSON, Laura

IPC: C07D205/04 ,  C07C71/00 ,  C07D213/72 ,  C07D215/233 ,  C07D221/20 ,  C07D401/12 ,  C07D405/12 ,  C07D491/056 ,  C07D495/04 ,  A61K31/404 ,  A61P35/00 ,  C07C49/697 ,  C07C233/52 ,  C07C229/50 ,  C07C323/61

Abstract: Compounds of Formula (I) wherein R1, R3, R11, R12, X, Y1, Y2, Y3, Y4 and formula (II) are as defined in the description. Medicaments.

公开(公告)号：WO2020236825A2

公开(公告)日：2020-11-26

申请号：PCT/US2020/033615

申请日：2020-05-19

Applicant: NOVARTIS AG ,  LES LABORATOIRES SERVIER

Inventor： BURGER, Matthew, T. ,  CHANRION, Maia ,  COLLAND, Frederic ,  CSEKEI, Marton ,  DELACOUR, Lea ,  DESOS, Patrice ,  GENESTE, Olivier ,  HENLIN, Jean-Michel ,  KOSTOVA, Vesela ,  KOTSCHY, Andras ,  MARAGNO, Ana, Leticia ,  MCNEILL, Eric ,  PALERMO, Mark, G. ,  ROCCHETTI, Francesca ,  STARCK, Jerome ,  YU, Bing ,  ZHANG, Qiang ,  PROSZENYAK, Agnes ,  SIPOS, Szabolcs ,  D'ALESSIO, Joseph, Anthony ,  NAKAJIMA, Katsumasa ,  CHEN, Zhuoliang

IPC: A61K47/68 ,  A61K47/6803 ,  A61K47/6867 ,  A61K47/6889

Abstract: 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：WO2020236817A2

公开(公告)日：2020-11-26

申请号：PCT/US2020/033602

申请日：2020-05-19

Applicant: NOVARTIS AG ,  LES LABORATOIRES SERVIER

Inventor： BURGER, Matthew, T. ,  CHANRION, Maia ,  COLLAND, Frederic ,  CSEKEI, Marton ,  DELACOUR, Lea ,  DESOS, Patrice ,  GENESTE, Olivier ,  HENLIN, Jean-Michel ,  KOSTOVA, Vesela ,  KOTSCHY, Andras ,  MARAGNO, Ana, Leticia ,  MCNEILL, Eric ,  PALERMO, Mark, G. ,  ROCCHETTI, Francesca ,  STARCK, Jerome ,  YU, Bing ,  ZHANG, Qiang ,  PROSZENYAK, Agnes ,  SIPOS, Szabolcs ,  D'ALESSIO, Joseph, Anthony ,  CHEN, Zhuoliang ,  BLANKENSHIP, John, William ,  NAKAJIMA, Katsumasa

IPC: A61K47/68 ,  A61K47/6803 ,  A61K47/6867 ,  A61K47/6889

Abstract: 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.