公开(公告)号：US09815813B2

公开(公告)日：2017-11-14

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： A61K31/4427 ,  C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D249/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： 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：US20180362496A1

公开(公告)日：2018-12-20

申请号：US16117674

申请日：2018-08-30

申请人： 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

发明人： 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分类号： C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D471/04 ,  C07D409/14 ,  C07D239/48 ,  C07D487/04 ,  C07D403/04 ,  C07D249/14

摘要： 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：US10774065B2

公开(公告)日：2020-09-15

申请号：US16117674

申请日：2018-08-30

申请人： 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

发明人： 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分类号： C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

摘要： 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：US20180186770A1

公开(公告)日：2018-07-05

申请号：US15736925

申请日：2016-06-15

申请人： 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

发明人： 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分类号： C07D401/14 ,  C07D491/107 ,  C07D498/10 ,  C07D471/10 ,  C07D401/04

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2, R4a, R5b, 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：US20180064709A1

公开(公告)日：2018-03-08

申请号：US15561209

申请日：2016-03-23

申请人： Nicole Buschmann ,  Robin Alec Fairhurst ,  Jorge Garcia Fortanet ,  Pascal Furet ,  Diana Graus Porta ,  Nafeeza Hafeez ,  Bo Han ,  Thomas Knoepfel ,  Matthew J. LaMarche ,  Catherine Leblanc

发明人： Nicole Buschmann ,  Robin Alec Fairhurst ,  Jorge Garcia Fortanet ,  Pascal Furet ,  Diana Graus Porta ,  Nafeeza Hafeez ,  Bo Han ,  Thomas Knoepfel ,  Matthew J. LaMarche ,  Catherine Leblanc

IPC分类号： A61K31/496 ,  A61K31/497

CPC分类号： A61K31/496 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K2300/00

摘要： A pharmaceutical combination comprising N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, or a pharmaceutically acceptable salt thereof, and at least one active ingredient, as defined herein, or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, for simultaneous or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

公开(公告)号：US20170204080A1

公开(公告)日：2017-07-20

申请号：US15110498

申请日：2015-01-16

申请人： 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

发明人： 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分类号： C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

摘要： 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：US20170015680A1

公开(公告)日：2017-01-19

申请号：US15110511

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

IPC分类号： C07D498/10 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D401/04 ,  C07D401/14

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.

摘要翻译： 其中p，q，Y1，Y2，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b，R7和R8定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。

公开(公告)号：US20170001975A1

公开(公告)日：2017-01-05

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang CHEN ,  Michael DORE ,  Jorge Garcia FORTANET ,  Rajesh KARKI ,  Mitsunori KATO ,  Matthew J. LAMARCHE ,  Lawrence Blas PEREZ ,  Sarah WILLIAMS ,  Martin SENDZIK

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： 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.

摘要翻译： 本发明涉及式I化合物：其中Y1，Y2，Y3，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。

公开(公告)号：US10308660B2

公开(公告)日：2019-06-04

申请号：US15736989

申请日：2016-06-15

申请人： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Matthew J. LaMarche ,  Martin Sendzik ,  Victoriano Tamez, Jr. ,  Bing Yu

发明人： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Matthew J. LaMarche ,  Martin Sendzik ,  Victoriano Tamez, Jr. ,  Bing Yu

IPC分类号： C07D401/04 ,  C07D491/107 ,  C07D401/14 ,  A61P35/00

摘要： The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, 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：US10093646B2

公开(公告)日：2018-10-09

申请号：US15110498

申请日：2015-01-16

申请人： 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

发明人： 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分类号： C07D401/04 ,  C07D409/14 ,  C07D471/04 ,  C07D403/04 ,  C07D401/14 ,  C07D487/04

摘要： 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.