公开(公告)号：US20170210724A1

公开(公告)日：2017-07-27

申请号：US15481852

申请日：2017-04-07

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Xingyu Lin ,  Jason Burch

IPC: C07D401/10 ,  C07D401/14 ,  C07D491/107 ,  C07D409/14 ,  C07D405/14 ,  C07D495/04 ,  C07D495/06 ,  C07D471/04 ,  C07D487/04 ,  C07D413/10 ,  C07D403/10 ,  C07D405/10 ,  C07D417/14 ,  C07D491/048 ,  C07D413/14

CPC classification number: C07D401/10 ,  A61K31/395 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D495/04 ,  C07D495/06

Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20170145034A1

公开(公告)日：2017-05-25

申请号：US15425698

申请日：2017-02-06

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Jason Burch

IPC: C07D513/04 ,  C07D401/14 ,  C07D491/052 ,  C07D471/04 ,  C07D413/10 ,  C07D491/048 ,  C07D403/14 ,  C07D413/14 ,  C07D495/04 ,  C07D487/04 ,  C07D417/10 ,  C07D403/10 ,  C07D401/10

CPC classification number: C07D513/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20160213652A1

公开(公告)日：2016-07-28

申请号：US15085164

申请日：2016-03-30

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Minghua Sun ,  Xiaojing Wang ,  Wesley Blackaby ,  Alastair James Hodges ,  Andrew Sharpe

IPC: A61K31/427 ,  A61K31/4439 ,  A61K31/4375 ,  A61K45/06

CPC classification number: A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I的环醚吡唑-4-基 - 杂环基甲酰胺化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中R 2是环状醚，X是噻唑基，吡嗪基，吡啶基或嘧啶基，是有用的 用于抑制Pim激酶，以及用于治疗诸如由Pim激酶介导的癌症的疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20160096850A9

公开(公告)日：2016-04-07

申请号：US14466153

申请日：2014-08-22

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Jason Burch

IPC: C07D513/04 ,  C07D471/04 ,  C07D403/10 ,  C07D401/14 ,  C07D413/10 ,  C07D491/052 ,  C07D487/04 ,  C07D401/10

CPC classification number: C07D513/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20140088117A1

公开(公告)日：2014-03-27

申请号：US14036160

申请日：2013-09-25

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Minghua Sun ,  Xiaojing Wang ,  Wesley Blackaby ,  Alastair James Hodges ,  Andrew Sharpe

IPC: C07D417/12 ,  A61K31/427 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/506 ,  C07D405/14 ,  A61K31/497

CPC classification number: A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I的环醚吡唑-4-基 - 杂环基甲酰胺化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中R 2是环状醚，X是噻唑基，吡嗪基，吡啶基或嘧啶基，是有用的 用于抑制Pim激酶，以及用于治疗诸如由Pim激酶介导的癌症的疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。