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：US20200369643A1

公开(公告)日：2020-11-26

申请号：US16987322

申请日：2020-08-06

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：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：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：US12129246B1

公开(公告)日：2024-10-29

申请号：US18589841

申请日：2024-02-28

Applicant: Novartis AG

Inventor： Daniela Angst ,  Philippe Bolduc ,  Matthew William Carson ,  Atwood Kim Cheung ,  Véronique Darsigny ,  Xiang Gao ,  Viktor Hornak ,  Keith Jendza ,  Rajesh Karki ,  Ajay Kumar Lal ,  Gang Liu ,  Justin Yik Ching Mao ,  Jeffrey M. McKenna ,  Erik Meredith ,  Muneto Mogi ,  Vivek Rauniyar ,  Liansheng Su ,  Ritesh Tichkule ,  Shuangxi Wang ,  Chun Zhang ,  Liang Zhao ,  Rui Zheng

IPC: C07D403/14 ,  A61K31/517 ,  A61K31/55 ,  A61K45/06 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14

CPC classification number: C07D403/14 ,  A61K31/517 ,  A61K31/55 ,  A61K45/06 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14

Abstract: The disclosure relates to a compound of Formula (I):




or a pharmaceutically acceptable salt thereof wherein A, Ra to Rd, and R4 to R7, are as described herein, as well as compositions and methods of using such compounds.

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：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.