公开(公告)号：US11952386B2

公开(公告)日：2024-04-09

申请号：US17182756

申请日：2021-02-23

申请人： NOVARTIS AG

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

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

摘要： 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

申请人： NOVARTIS AG

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

摘要： 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：US20210371429A1

公开(公告)日：2021-12-02

申请号：US17182744

申请日：2021-02-23

申请人： NOVARTIS AG

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

摘要： 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：US20210309663A1

公开(公告)日：2021-10-07

申请号：US17191139

申请日：2021-03-03

申请人： NOVARTIS AG

发明人： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC分类号： C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4523 ,  A61P35/00

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 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：US20240270738A1

公开(公告)日：2024-08-15

申请号：US18602126

申请日：2024-03-12

申请人： NOVARTIS AG

发明人： Christopher ADAIR ,  Katsumasa Nakajima ,  Rukundo Ntaganda ,  Julien Papillon ,  Troy Douglas Smith

IPC分类号： C07D417/12 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K45/06

摘要： A method of preparing compound of Formula (1), or a pharmaceutically acceptable salt thereof,




wherein R1 through R6 are as defined herein.

公开(公告)号：US20220089597A1

公开(公告)日：2022-03-24

申请号：US17191082

申请日：2021-03-03

申请人： NOVARTIS AG

发明人： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC分类号： C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4523 ,  A61P35/00

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 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

申请人： NOVARTIS AG

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

摘要： 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

申请人： NOVARTIS AG

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

摘要： 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：US20200181168A1

公开(公告)日：2020-06-11

申请号：US16418978

申请日：2019-05-21

申请人： NOVARTIS AG

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

摘要： 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

申请人： NOVARTIS AG

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

CPC分类号： C07D498/10 ,  C07B2200/07 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

摘要： 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.