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：US10220036B2

公开(公告)日：2019-03-05

申请号：US15538348

申请日：2015-12-21

Applicant: Novartis AG

Inventor： Ho Man Chan ,  Xiang-Ju Justin Gu ,  Ying Huang ,  Ling Li ,  Yuan Mi ,  Wei Qi ,  Martin Sendzik ,  Yongfeng Sun ,  Long Wang ,  Zhengtian Yu ,  Hailong Zhang ,  Ji Yue (Jeff) Zhang ,  Man Zhang ,  Qiong Zhang ,  Kehao Zhao

IPC: A61K31/539 ,  A61K31/343 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D487/04 ,  A61K31/519 ,  A61K45/06

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.

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.