公开(公告)号：US20230081720A1

公开(公告)日：2023-03-16

申请号：US17613020

申请日：2020-05-19

Applicant: NOVARTIS AG ,  LES LABORATOIRES SERVIER

Inventor： 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: A61K47/68

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.

公开(公告)号：US10975080B2

公开(公告)日：2021-04-13

申请号：US15736959

申请日：2016-06-15

Applicant: NOVARTIS AG

Inventor： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4523 ,  A61P35/00

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10968235B2

公开(公告)日：2021-04-06

申请号：US16418978

申请日：2019-05-21

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D471/10 ,  C07D491/107 ,  C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D495/10

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10934285B2

公开(公告)日：2021-03-02

申请号：US16309076

申请日：2017-06-12

Applicant: Novartis AG

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Matthew J. Lamarche ,  Dyuti Majumdar ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Fan Yang ,  Bing Yu

IPC: C07D487/14 ,  C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D455/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20190185475A1

公开(公告)日：2019-06-20

申请号：US15736959

申请日：2016-06-15

Applicant: NOVARTIS AG

Inventor： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC: C07D487/04 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10112931B2

公开(公告)日：2018-10-30

申请号：US15499824

申请日：2017-04-27

Applicant: NOVARTIS AG

Inventor： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Clifford Sutton ,  Yaping Wang ,  Qian Zhao

IPC: C07D413/14 ,  C07D413/04 ,  C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

公开(公告)号：US20180065949A1

公开(公告)日：2018-03-08

申请号：US15726189

申请日：2017-10-05

Applicant: NOVARTIS AG

Inventor： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC: C07D401/04 ,  C07D401/14 ,  C07D249/14 ,  C07D241/26

CPC classification number: C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US09688672B2

公开(公告)日：2017-06-27

申请号：US15209731

申请日：2016-07-13

Applicant: NOVARTIS AG

Inventor： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Clifford Sutton ,  Yaping Wang ,  Qian Zhao

IPC: C07D413/14 ,  A61K31/506 ,  C07D413/04 ,  C07D417/14 ,  A61K31/5377

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.