公开(公告)号：US20240199594A1

公开(公告)日：2024-06-20

申请号：US18365392

申请日：2023-08-04

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle BRAUN ,  Emily HANAN ,  Steven T. Staben ,  Robert Andrew HEALD ,  Calum MACLEOD ,  Richard ELLIOTT

IPC: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

CPC classification number: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

Abstract: Described herein are benzoxazepin oxazolidinone 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：US20210309660A1

公开(公告)日：2021-10-07

申请号：US16858004

申请日：2020-04-24

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Peter Dragovich ,  Lewis J. Gazzard ,  Thomas Pillow ,  Steven T. Staben ,  Binqing Wei ,  Jianfeng Xin

IPC: C07D471/16 ,  C07D493/10 ,  C07D403/04 ,  C07D417/14 ,  C07D413/14 ,  A61P35/00

Abstract: The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

公开(公告)号：US12152040B2

公开(公告)日：2024-11-26

申请号：US17198240

申请日：2021-03-10

Applicant: Genentech, Inc.

Inventor： Robert Anthony Blake ,  Peter Dragovich ,  Lewis J. Gazzard ,  Susan Kaufman ,  Tracy Kleinheinz ,  Thomas Pillow ,  Steven T. Staben ,  Binqing Wei

IPC: C07D495/14 ,  A61P35/00 ,  C07D495/16

Abstract: The present disclosure relates to compounds and salts thereof that are useful for inhibiting target polypeptides and proteins, in particular, bromodomain (e.g., BRD4) proteins. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated diseases or disorders.

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：US20180327420A1

公开(公告)日：2018-11-15

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

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

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：US20170210733A1

公开(公告)日：2017-07-27

申请号：US15481764

申请日：2017-04-07

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Emily Hanan ,  Steven T. Staben ,  Robert Andrew Heald ,  Calum MacLeod ,  Richard Elliott

IPC: C07D413/14 ,  C07D267/08

CPC classification number: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

Abstract: Described herein are benzoxazepin oxazolidinone 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. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.

公开(公告)号：US09643980B2

公开(公告)日：2017-05-09

申请号：US15200307

申请日：2016-07-01

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Emily Hanan ,  Steven T. Staben ,  Robert Andrew Heald ,  Calum MacLeod ,  Richard Elliott

IPC: A61K31/553 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00 ,  A61K45/06

CPC classification number: C07D498/04 ,  A61K31/553 ,  A61K45/06

Abstract: Described herein are benzoxazepin oxazolidinone 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：US11242344B2

公开(公告)日：2022-02-08

申请号：US16858004

申请日：2020-04-24

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Peter Dragovich ,  Lewis J. Gazzard ,  Thomas Pillow ,  Steven T. Staben ,  Binqing Wei ,  Jianfeng Xin

IPC: C07D471/16 ,  C07D493/10 ,  A61P35/00 ,  C07D417/14 ,  C07D413/14 ,  C07D403/04

Abstract: The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

公开(公告)号：US20180127404A1

公开(公告)日：2018-05-10

申请号：US15729507

申请日：2017-10-10

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Emily Hanan ,  Steven T. Staben ,  Robert Andrew Heald ,  Calum MacLeod ,  Richard Elliott

IPC: C07D413/14 ,  C07D267/08

CPC classification number: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

Abstract: Described herein are benzoxazepin oxazolidinone 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. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.

公开(公告)号：US20180065983A1

公开(公告)日：2018-03-08

申请号：US15258175

申请日：2016-09-07

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

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

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.