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.

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：US09346817B2

公开(公告)日：2016-05-24

申请号：US14013256

申请日：2013-08-29

Applicant: Genentech, Inc.

Inventor： Robert Andrew Heald ,  Neville James McLean

IPC: C07D491/056 ,  A61K31/5377 ,  C07D491/04 ,  C07D498/04 ,  A61K39/395 ,  A61K45/06

CPC classification number: C07D491/056 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  C07D491/04 ,  C07D498/04

Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

Abstract translation: 描述了具有抗癌活性，抗炎活性或免疫调节性质的更具体地具有PI3激酶调节或抑制活性的式I的二氧杂环丁烷酮和恶嗪 - [2,3-d]嘧啶PI3K抑制剂化合物。 描述了使用式I的三环PI3K抑制剂化合物用于体外，原位和体内诊断或治疗哺乳动物细胞，生物体或相关病理条件的方法。

公开(公告)号：US20140065136A1

公开(公告)日：2014-03-06

申请号：US14013256

申请日：2013-08-29

Applicant: Genentech, Inc.

Inventor： Robert Andrew Heald ,  Neville James McLean

IPC: C07D491/056 ,  A61K39/395 ,  A61K45/06 ,  A61K31/5377

CPC classification number: C07D491/056 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  C07D491/04 ,  C07D498/04

Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

Abstract translation: 描述了具有抗癌活性，抗炎活性或免疫调节性质的更具体地具有PI3激酶调节或抑制活性的式I的二氧杂环丁烷酮和恶嗪 - [2,3-d]嘧啶PI3K抑制剂化合物。 描述了使用式I的三环PI3K抑制剂化合物用于体外，原位和体内诊断或治疗哺乳动物细胞，生物体或相关病理条件的方法。

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。