公开(公告)号：US20220204517A1

公开(公告)日：2022-06-30

申请号：US17654131

申请日：2022-03-09

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：US20190322661A1

公开(公告)日：2019-10-24

申请号：US16438135

申请日：2019-06-11

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 ,  C07D403/14 ,  A61K31/519 ,  C07D519/00 ,  A61P11/06

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

公开(公告)号：US20180265515A1

公开(公告)日：2018-09-20

申请号：US15986256

申请日：2018-05-22

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

CPC classification number: 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：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：US20240132507A1

公开(公告)日：2024-04-25

申请号：US18496146

申请日：2023-10-27

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Zhonghua Pei ,  Brendan Parr ,  Wendy Liu ,  Richard Pastor ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Hima Potturi ,  Guoshen Wu ,  Xingyu Lin ,  Yanyan Chu ,  Po-wai Yuen

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Presently provided are inhibitors of 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：US11236046B2

公开(公告)日：2022-02-01

申请号：US16657102

申请日：2019-10-18

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D417/12 ,  C07D451/02 ,  C07D491/048 ,  C07D405/14

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20180118680A1

公开(公告)日：2018-05-03

申请号：US15851322

申请日：2017-12-21

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/14 ,  C07D417/12 ,  C07D403/12 ,  C07D451/02 ,  C07D405/14 ,  C07D401/14 ,  C07D491/048 ,  C07D401/12

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20170226132A1

公开(公告)日：2017-08-10

申请号：US15499662

申请日：2017-04-27

Applicant: Genentech, Inc.

Inventor： Nicholas C. Ray ,  Yun-Xing Cheng ,  Christine Edwards ,  Simon C. Goodacre ,  Wei Li ,  Snahel Patel ,  Matthew W. Cartwright ,  Mohammed Sajad ,  Po-wai Yuen ,  Mark E. Zak

IPC: C07D519/00 ,  C07D471/04

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.

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：US11649241B2

公开(公告)日：2023-05-16

申请号：US17174733

申请日：2021-02-12

Applicant: Genentech, Inc.

Inventor： Mark Zak ,  F. Anthony Romero ,  Po-wai Yuen ,  Emily J. Hanan

IPC: C07D487/04 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

Abstract: Compounds of Formula I and methods of use as Janus kinase inhibitors are described herein.