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：US10435414B2

公开(公告)日：2019-10-08

申请号：US16044862

申请日：2018-07-25

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Keira Garland ,  Emily Hanan ,  Hans Purkey ,  Steven T. Staben ,  Robert Andrew Heald ,  Jamie Knight ,  Calum Macleod ,  Aijun Lu ,  Guosheng Wu ,  Siew Kuen Yeap

IPC: A61K31/4188 ,  A61K31/424 ,  A61K31/498 ,  A61K31/5365 ,  A61K45/06 ,  C07D498/04 ,  C07D498/06 ,  C07D519/00 ,  A61K31/4196 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/5383 ,  A61K31/553 ,  C07D491/044

Abstract: Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

公开(公告)号：US09988400B2

公开(公告)日：2018-06-05

申请号：US15094687

申请日：2016-04-08

Applicant: Genentech, Inc.

Inventor： Yu Jiang ,  Guosheng Wu ,  Po-Wai Yuen ,  Elisia Villemure ,  Jacob Schwarz ,  Cuong Ly ,  Benjamin Sellers ,  Matthew Volgraf

IPC: C07D513/04 ,  C07D513/10 ,  C07D513/14 ,  C07D519/00

CPC classification number: C07D513/14 ,  C07D513/04 ,  C07D513/10 ,  C07D519/00

Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

公开(公告)号：US20160222033A1

公开(公告)日：2016-08-04

申请号：US15094687

申请日：2016-04-08

Applicant: Genentech, Inc.

Inventor： Jiang Yu ,  Guosheng Wu ,  Po-Wai Yuen ,  Elisia Villemure ,  Jacob Schwarz ,  Cuong Ly ,  Benjamin Sellers ,  Volgraf Matthew

IPC: C07D513/14 ,  C07D513/10 ,  C07D519/00 ,  C07D513/04

CPC classification number: C07D513/14 ,  C07D513/04 ,  C07D513/10 ,  C07D519/00

Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract translation: 本发明涉及某些噻唑并嘧啶酮化合物，包含这些化合物的药物组合物，以及使用这些化合物的治疗方法。

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：US11279735B2

公开(公告)日：2022-03-22

申请号：US16816969

申请日：2020-03-12

Applicant: Genentech, Inc.

Inventor： Emily J. Hanan ,  Georgette Castanedo ,  Marie Gabrielle Braun ,  Keira Garland ,  Peter Andrew Smith ,  Richard Pastor ,  Paul Gibbons ,  Yunxing Cheng ,  Guosheng Wu ,  Yuhong Fu ,  Po-Wai Yuen

IPC: C07K11/02 ,  A61K38/00

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US10280165B2

公开(公告)日：2019-05-07

申请号：US15783373

申请日：2017-10-13

Applicant: Genentech, Inc.

Inventor： Matthew Volgraf ,  Yu Jiang ,  Elisia Villemure ,  Benjamin Sellers ,  Guosheng Wu ,  Aijun Lu

IPC: A61K31/519 ,  C07D471/04 ,  A61P25/00

Abstract: The invention relates to pyridopyrimidinone compounds of formula I or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein, as well as pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

公开(公告)号：US20180127414A1

公开(公告)日：2018-05-10

申请号：US15783373

申请日：2017-10-13

Applicant: Genentech, Inc.

Inventor： Matthew Volgraf ,  Yu Jiang ,  Elisia Villemure ,  Benjamin Sellers ,  Guosheng Wu ,  Aijun Lu

IPC: C07D471/04 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61P25/00

Abstract: The invention relates to pyridopyrimidinone compounds of formula I or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein, as well as pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

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：US20230047209A1

公开(公告)日：2023-02-16

申请号：US17366923

申请日：2021-07-02

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Georgette Castanedo ,  Paul Gibbons ,  Joachim Rudolph ,  William Vernier ,  Ramsay Beveridge ,  Yao Wu ,  Guosheng Wu

IPC: C07D471/04 ,  C07D475/00

Abstract: Described herein are pyrido-pyrimidinone and pteridinone compounds or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods treating cancer, alone and in combination with other therapeutic agents.