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：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：EP3094628B1

公开(公告)日：2018-08-08

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.

公开(公告)号：EP3094629A1

公开(公告)日：2016-11-23

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.

摘要翻译： 本发明涉及式I的化合物：其中Y1，Y2，Y3，R1，R 2A，2B，3A，3B，4A，4B，5A，R 5B是本发明的概述中所定义; 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：EP2137162B1

公开(公告)日：2018-08-01

申请号：EP08717784.6

申请日：2008-03-13

申请人： Novartis AG

发明人： DAI, Miao ,  HE, Feng ,  JAIN, Rishi Kumar ,  KARKI, Rajesh ,  KELLEHER, Joseph, III ,  LEI, John ,  LLAMAS, Luis ,  MCEWAN, Michael A. ,  MILLER-MOSLIN, Karen ,  PEREZ, Lawrence Blas ,  PEUKERT, Stefan ,  YUSUFF, Naeem

IPC分类号： C07D237/28 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07F9/58 ,  C07D405/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/048 ,  C07D498/14 ,  C07D237/30 ,  A61K31/502 ,  A61K31/4545

CPC分类号： C07D401/12 ,  C07D237/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/048 ,  C07D498/14 ,  C07F9/65583

摘要： The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:

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：EP2137162A1

公开(公告)日：2009-12-30

申请号：EP08717784.6

申请日：2008-03-13

申请人： Novartis AG

发明人： DAI, Miao ,  HE, Feng ,  JAIN, Rishi Kumar ,  KARKI, Rajesh ,  KELLEHER, Joseph, III ,  LEI, John ,  LLAMAS, Luis ,  MCEWAN, Michael A. ,  MILLER-MOSLIN, Karen ,  PEREZ, Lawrence Blas ,  PEUKERT, Stefan ,  YUSUFF, Naeem

IPC分类号： C07D237/28 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07F9/58 ,  C07D405/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/048 ,  C07D498/14 ,  C07D237/30 ,  A61K31/502 ,  A61K31/4545

CPC分类号： C07D401/12 ,  C07D237/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/048 ,  C07D498/14 ,  C07F9/65583

摘要： The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:

摘要翻译： 本公开涉及与涉及Hedgehog途径的病理学的诊断和治疗有关的化合物，包括但不限于肿瘤形成，癌症，瘤形成和非恶性过度增殖性疾病; 具体涉及式I化合物：

公开(公告)号：EP3390404A1

公开(公告)日：2018-10-24

申请号：EP16815543.0

申请日：2016-12-15

申请人： Novartis AG

发明人： AVERSA, Robert John ,  BURGER, Matthew T. ,  DILLON, Michael Patrick ,  DINEEN JR., Thomas A. ,  KARKI, Rajesh ,  RAMURTHY, Savithri ,  RAUNIYAR, Vivek ,  ROBINSON, Richard ,  SARVER, Patrick James

IPC分类号： C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4196

CPC分类号： C07D498/04 ,  A61P35/00 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044

摘要： The present invention provides compounds of Formula (A): (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent, and methods of using the compositions and combinations to treat conditions including cancers.

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.