公开(公告)号：US09650393B2

公开(公告)日：2017-05-16

申请号：US15200301

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: C07D498/04 ,  A61K31/553

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：US11760753B2

公开(公告)日：2023-09-19

申请号：US17075583

申请日：2020-10-20

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 ,  A61P11/00 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  A61K45/06 ,  C07B43/06

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：US10851091B2

公开(公告)日：2020-12-01

申请号：US16140392

申请日：2018-09-24

Applicant: Genentech, Inc.

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

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

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：US10112932B2

公开(公告)日：2018-10-30

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

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：US10065970B2

公开(公告)日：2018-09-04

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.

公开(公告)号：US20180162873A9

公开(公告)日：2018-06-14

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.

公开(公告)号：US20170015678A1

公开(公告)日：2017-01-19

申请号：US15200301

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: C07D498/04 ,  A61K31/553

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.

Abstract translation: 本文描述了具有式（I）结构的磷酸肌醇-3激酶（PI3K）调节活性或功能的苯并氧氮杂恶唑烷酮化合物：或其立体异构体，互变异构体或其药学上可接受的盐，以及本文所述的取代基和结构特征。 还描述了包括式I化合物的药物组合物和药物，以及将PI3K调节剂单独使用并与其它治疗剂联合用于治疗介导或依赖于PI3K调节异常的疾病或病症的方法。

公开(公告)号：US20170002022A1

公开(公告)日：2017-01-05

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: C07D498/04 ,  A61K31/553 ,  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.

Abstract translation: 本文描述了具有具有式I结构的磷酸肌醇-3激酶（PI3K）调节活性或功能的苯并恶嗪酮恶唑烷酮化合物：或其立体异构体，互变异构体或其药学上可接受的盐，以及本文所述的取代基和结构特征。 还描述了包括式I化合物的药物组合物和药物，以及将PI3K调节剂单独使用并与其它治疗剂联合用于治疗介导或依赖于PI3K调节异常的疾病或病症的方法。