公开(公告)号：US20210371429A1

公开(公告)日：2021-12-02

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: 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：US10287266B2

公开(公告)日：2019-05-14

申请号：US15736925

申请日：2016-06-15

Applicant: NOVARTIS AG

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Andriana Jouk ,  Rajesh Karki ,  Matthew J. LaMarche ,  Gang Liu ,  Mark G. Palermo ,  Lawrence Blas Perez ,  Patrick James Sarver ,  Michael David Shultz ,  Martin Sendzik ,  Bakary-Barry Toure ,  Bing Yu

IPC: C07D401/14 ,  C07D401/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, 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：US11931363B2

公开(公告)日：2024-03-19

申请号：US17505271

申请日：2021-10-19

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: C07D307/78 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D307/79 ,  C07D307/83 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D487/04

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：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：US20130172354A1

公开(公告)日：2013-07-04

申请号：US13773052

申请日：2013-02-21

Applicant: Novartis AG

Inventor： Paul A. Barsanti ,  Cheng Hu ,  Jeff Jin ,  Robert Keyes ,  Robert Kucejko ,  Xiaodong Lin ,  Yue Pan ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

IPC: C07D401/04 ,  C07D409/14 ,  C07D413/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: A61K31/497 ,  C07D213/74 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。

公开(公告)号：US11952386B2

公开(公告)日：2024-04-09

申请号：US17182756

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

CPC classification number: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07B2200/07

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：US20220396585A1

公开(公告)日：2022-12-15

申请号：US17182756

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: 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：US10689378B2

公开(公告)日：2020-06-23

申请号：US16311621

申请日：2017-06-06

Applicant: Novartis AG

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

IPC: C07D471/04 ,  A61P35/00

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R6, R7 and R8 are as defined herein.