公开(公告)号：US20160185797A1

公开(公告)日：2016-06-30

申请号：US15060325

申请日：2016-03-03

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

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：US20150158851A1

公开(公告)日：2015-06-11

申请号：US14618827

申请日：2015-02-10

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Frederick Brookfield ,  Richard A. Goldsmith ,  Kevin Hon Luen Lau ,  Colin H. MacKinnon ,  Daniel Fred Ortwine ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D487/10 ,  C07D413/14 ,  C07D491/044 ,  C07D417/14 ,  C07D495/10 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/10 ,  C07D491/044 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  Y02P20/582

Abstract: Provided herein are compounds of formula (AA): stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, Ra, p, R5 and R6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.

Abstract translation: 本文提供了式（AA）的化合物：其立体异构体或其药学上可接受的盐，其中A，Ra，p，R 5和R 6在本文中定义，包括化合物的组合物和制备和使用该化合物治疗疾病的方法。

公开(公告)号：US20140309210A1

公开(公告)日：2014-10-16

申请号：US14178527

申请日：2014-02-12

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Richard A. Goldsmith ,  Daniel Fred Ortwine ,  Richard Pastor ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D491/052 ,  C07D417/14 ,  C07D471/04 ,  C07D409/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052

Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.

Abstract translation: 式I的化合物：立体异构体或其药学上可接受的盐，其中X，X 1，X 2，X 3，R 1，R 2，R 3，R 4，R 5和R 6在本文中描述，包括化合物的组合物和制备和使用化合物的方法 用于治疗疾病。

公开(公告)号：US20150065482A1

公开(公告)日：2015-03-05

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.

Abstract translation: 本发明涉及式（O）的化合物：其中Q，A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到NF-kB信号传导的不期望或过度活化的疾病和病症。

公开(公告)号：US20160200739A1

公开(公告)日：2016-07-14

申请号：US15074100

申请日：2016-03-18

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 ,  C07D413/14 ,  C07D471/04 ,  C07D413/10 ,  C07D401/10 ,  C07D403/10 ,  C07D491/052

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：US09931323B2

公开(公告)日：2018-04-03

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 ,  C07D417/12 ,  C07D405/14 ,  A61K31/497 ,  A61K31/506 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

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.

公开(公告)号：US09605005B2

公开(公告)日：2017-03-28

申请号：US15074100

申请日：2016-03-18

Applicant: Genentech, Inc.

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

IPC: C07D401/00 ,  C07D513/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

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：US09328106B2

公开(公告)日：2016-05-03

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 ,  C07D405/14 ,  A61K45/06 ,  A61K31/427 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/506 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

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：US20150057260A1

公开(公告)日：2015-02-26

申请号：US14466176

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 ,  Xingyu Lin ,  Jason Burch

IPC: C07D495/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D491/107 ,  C07D403/14 ,  C07D401/10

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.

Abstract translation: 本发明涉及式（O）的化合物：其中A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到NF-kB信号传导的不期望或过度活化的疾病和病症。

公开(公告)号：US09963446B2

公开(公告)日：2018-05-08

申请号：US15266243

申请日：2016-09-15

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Huifen Chen ,  Xiaojing Wang

IPC: C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/06 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/4985 ,  A61K45/06 ,  C07D487/04

Abstract: Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein 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.