公开(公告)号：US20220073537A1

公开(公告)日：2022-03-10

申请号：US17532367

申请日：2021-11-22

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: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  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：US10336774B2

公开(公告)日：2019-07-02

申请号：US15899821

申请日：2018-02-20

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: C07D401/04 ,  C07D401/14 ,  C07D471/10 ,  C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D403/04 ,  C07D491/107 ,  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：US10301278B2

公开(公告)日：2019-05-28

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 ,  C07D241/26 ,  C07D249/14

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：US12209098B2

公开(公告)日：2025-01-28

申请号：US17182744

申请日：2021-02-23

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: A61K31/497 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D498/10

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：US20240042051A1

公开(公告)日：2024-02-08

申请号：US18038437

申请日：2021-11-23

Applicant: Francesca Rocchetti ,  Novartis AG

Inventor： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Claudia Judith Klinter ,  Eric McNeill ,  Cornelia Anne Mundt ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Tamas Schweighoffer ,  Bing Yu ,  Katharina Winkelbach ,  Qiang Zhang ,  Laura Bresson ,  Frédéric Colland ,  Ana Leticia Maragno ,  Francesca Rocchetti

IPC: A61K47/68 ,  A61P35/00

CPC classification number: A61K47/6867 ,  A61K47/6889 ,  A61P35/00 ,  A61K47/6803

Abstract: Anti-CD48 antibody-drug conjugates are disclosed. The anti-CD48 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD48 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：US20220348553A1

公开(公告)日：2022-11-03

申请号：US17808895

申请日：2022-06-24

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC: C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and 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：US20200181168A1

公开(公告)日：2020-06-11

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: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  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：US20180201623A1

公开(公告)日：2018-07-19

申请号：US15899821

申请日：2018-02-20

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

CPC classification number: C07D498/10 ,  C07B2200/07 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  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：US20150152093A1

公开(公告)日：2015-06-04

申请号：US14408418

申请日：2014-03-12

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 Sutton ,  Yaping Wang ,  Qian Zhao

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

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.

Abstract translation: 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US11905283B2

公开(公告)日：2024-02-20

申请号：US17130374

申请日：2020-12-22

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

CPC classification number: 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.