公开(公告)号：EP3310779B1

公开(公告)日：2019-05-08

申请号：EP16731341.0

申请日：2016-06-15

申请人： Novartis AG

发明人： BAGDANOFF, Jeffrey T. ,  CHEN, Zhuoliang ,  DORE, Michael ,  FORTANET, Jorge Garcia ,  KATO, Misunori ,  LAMARCHE, Matthew J. ,  SARVER, Patrick James ,  SHULTZ, Michael ,  SMITH, Troy Douglas ,  WILLIAMS, Sarah

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P35/00 ,  A61P9/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/28

公开(公告)号：EP3468972A1

公开(公告)日：2019-04-17

申请号：EP17733041.2

申请日：2017-06-12

申请人： NOVARTIS AG

发明人： CHEN, Zhuoliang ,  FORTANET, Jorge Garcia ,  KARKI, Rajesh ,  LAMARCHE, Matthew J. ,  MAJUMDAR, Dyuti ,  PEREZ, Lawrence Blas ,  SENDZIK, Martin ,  SMITH, Troy Douglas ,  YANG, Fan ,  YU, Bing

IPC分类号： C07D471/04 ,  A61K31/4545 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  A61P9/00 ,  A61P35/00

公开(公告)号：EP3094629B1

公开(公告)日：2018-08-22

申请号：EP15703106.3

申请日：2015-01-16

申请人： Novartis AG

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

IPC分类号： C07D249/14 ,  C07D241/26 ,  A61K31/495 ,  A61P35/04

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：EP3310771A1

公开(公告)日：2018-04-25

申请号：EP16731665.2

申请日：2016-06-15

申请人： Novartis AG

发明人： CHEN, Zhuoliang ,  FORTANET, Jorge Garcia ,  LAMARCHE, Matthew J. ,  SENDZIK, Martin ,  TAMEZ, JR., Victoriano ,  YU, Bing

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D491/107 ,  A61K31/537 ,  A61K31/513 ,  A61K31/4545 ,  A61P35/00 ,  A61P9/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/28

摘要： The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.

公开(公告)号：EP3273959A1

公开(公告)日：2018-01-31

申请号：EP16712083.1

申请日：2016-03-23

申请人： NOVARTIS AG

发明人： BUSCHMANN, Nicole ,  FAIRHURST, Robin Alec ,  FURET, Pascal ,  KNOEPFEL, Thomas ,  LEBLANC, Catherine ,  MAH, Robert ,  LIAO, Lv ,  XIONG, Jing ,  HAN, Bo ,  WANG, Can ,  GRAUS PORTA, Diana ,  ZHAO, Xianglin ,  WARTMANN, Markus ,  FORTANET, Jorge Garcia ,  HAFEEZ, Nafeeza ,  LAMARCHE, Matthew J. ,  PORTER, Dale

IPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/513 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00

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：EP3094628A1

公开(公告)日：2016-11-23

申请号：EP15703321.8

申请日：2015-01-16

申请人： Novartis AG

发明人： CHEN, Christine Hiu-tung ,  CHEN, Zhuoliang ,  DORE, Michael ,  FORTANET, Jorge Garcia ,  KARKI, Rajesh ,  KATO, Mitsunori ,  LAMARCHE, Matthew J. ,  PEREZ, Lawrence Blas ,  SMITH, Troy Douglas ,  WILLIAMS, Sarah ,  GIRALDES, John William ,  TOURE, Bakary-barry ,  SENDZIK, Martin

IPC分类号： C07D241/18 ,  C07D241/20 ,  A61K31/495 ,  A61P35/04

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： 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，R 2A，2B，3A，3B，4A，4B，5A，R 5B，R 7和R 8在发明概述中所定义; 能够抑制SHP2的活性。 本发明进一步提供了一种用于本发明的化合物的制备方法，药物制剂，其包括测试的化合物并使用化合物的方法和在与SHP2的异常活性相关的疾病或病症的管理审查的组合物。

公开(公告)号：EP3310774A1

公开(公告)日：2018-04-25

申请号：EP16731666.0

申请日：2016-06-15

申请人： Novartis AG

发明人： TOURE, Bakary-Barry ,  CHEN, Zhuoliang ,  FORTANET, Jorge Garcia ,  JOUK, Andriana ,  KARKI, Rajesh ,  LAMARCHE, Matthew J. ,  LIU, Gang ,  PALERMO, Mark G. ,  PEREZ, Lawrence Blas ,  SARVER, Patrick James ,  SHULTZ, Michael David ,  YU, Bing

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10 ,  A61K31/506 ,  A61K31/537 ,  A61P35/00 ,  A61P9/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/28

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

摘要： 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：EP3094627A1

公开(公告)日：2016-11-23

申请号：EP15703105.5

申请日：2015-01-16

申请人： Novartis AG

发明人： CHEN, Christine Hiu-tung ,  CHEN, Zhuoliang ,  FORTANET, Jorge Garcia ,  GRUNENFELDER, Denise ,  KARKI, Rajesh ,  KATO, Mitsunori ,  LAMARCHE, Matthew J. ,  PEREZ, Lawrence Blas ,  STAMS, Travis Matthew ,  WILLIAMS, Sarah

IPC分类号： C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  A61K31/505 ,  A61K31/4965

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, p,Y1 Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R4a and R5b are defined in the claims; 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）的化合物：其中M，P，Y1 Y2，Y3，R1，R 2A，2B，3A，3B，4A，R 4B，R 4a和R 5b分别在权利要求中所定义; 能够抑制SHP2的活性。 本发明进一步提供了一种用于本发明的化合物的制备方法，药物制剂，其包括测试的化合物并使用化合物的方法和在与SHP2的异常活性相关的疾病或病症的管理审查的组合物。

公开(公告)号：EP3094627B1

公开(公告)日：2018-08-22

申请号：EP15703105.5

申请日：2015-01-16

申请人： Novartis AG

发明人： CHEN, Christine Hiu-tung ,  CHEN, Zhuoliang ,  FORTANET, Jorge Garcia ,  GRUNENFELDER, Denise ,  KARKI, Rajesh ,  KATO, Mitsunori ,  LAMARCHE, Matthew J. ,  PEREZ, Lawrence Blas ,  STAMS, Travis Matthew ,  WILLIAMS, Sarah

IPC分类号： C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  A61K31/505 ,  A61K31/4965

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, p,Y1 Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R4a and R5b are defined in the claims; 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：EP3310779A1

公开(公告)日：2018-04-25

申请号：EP16731341.0

申请日：2016-06-15

申请人： Novartis AG

发明人： BAGDANOFF, Jeffrey T. ,  CHEN, Zhuoliang ,  DORE, Michael ,  FORTANET, Jorge Garcia ,  KATO, Misunori ,  LAMARCHE, Matthew J. ,  SARVER, Patrick James ,  SHULTZ, Michael ,  SMITH, Troy Douglas ,  WILLIAMS, Sarah

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P35/00 ,  A61P9/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/28

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.