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：US11603373B2

公开(公告)日：2023-03-14

申请号：US16626219

申请日：2018-06-20

Applicant: Genentech, Inc.

Inventor： Zhonghua Pei ,  Richard Pastor ,  Lewis Gazzard ,  Brendan Parr ,  Wendy Liu ,  Rohan Mendonca ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D221/00 ,  C07D335/00 ,  C07D487/04 ,  C07D471/08 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00

Abstract: Presently provided are inhibitors of cellularly expressed TD02 and IDO1, and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

公开(公告)号：US20200165260A1

公开(公告)日：2020-05-28

申请号：US16777049

申请日：2020-01-30

Applicant: Genentech, Inc.

Inventor： Yun-Xing Cheng ,  Paul Gibbons ,  Terry Kellar ,  Wei Li ,  Rohan Mendonca ,  Po-wai Yuen ,  Mark Edward Zak ,  Lei Zhang

IPC: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.

公开(公告)号：US20180305355A1

公开(公告)日：2018-10-25

申请号：US15820515

申请日：2017-11-22

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-wai Yuen

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

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.