公开(公告)号：US20210300919A1

公开(公告)日：2021-09-30

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 ,  C07D513/04 ,  C07D495/04 ,  C07D487/04 ,  C07D401/14 ,  C07D519/00 ,  C07D455/02 ,  C07D403/14 ,  A61P35/00

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：US20200002330A1

公开(公告)日：2020-01-02

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

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：US20180051015A1

公开(公告)日：2018-02-22

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 ,  C07D417/14 ,  C07D413/04 ,  A61K31/506 ,  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.

公开(公告)号：US20240199609A1

公开(公告)日：2024-06-20

申请号：US18523565

申请日：2023-11-29

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.

公开(公告)号：US20230091510A1

公开(公告)日：2023-03-23

申请号：US17612280

申请日：2020-05-19

Applicant: Novartis AG

Inventor： Zhuoliang CHEN ,  Katsumasa NAKAJIMA ,  Matthew T. BURGER ,  Joseph Anthony D'ALESSIO ,  Eric MCNEILL ,  Mark G, PALMERO ,  Bing YU ,  Qiang ZHANG

IPC: A61K47/68 ,  A61K47/54 ,  A61K47/60 ,  A61K47/61 ,  A61P35/00 ,  C07K16/28 ,  C07K5/062

Abstract: Provided herein are linkers, linker-drug groups and anti-body-drug conjugates comprising hydrophilic groups.