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：US20150368244A1

公开(公告)日：2015-12-24

申请号：US14137972

申请日：2013-12-20

Applicant: Genentech, Inc.

Inventor： Hazel Joan Dyke ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Charles Goodacre ,  Joseph P. Lyssikatos ,  Calum MacLeod ,  Karen Williams ,  Huifen Chen

IPC: C07D471/14 ,  A61K31/496 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D471/14 ,  A61K31/496 ,  A61K31/519 ,  A61K45/06

Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及有用的式（I），（Ia），（Ib），（Ic），（Id），（Ie），（If），（Ig）和（Ih）的1,5-二氮杂咔唑化合物 作为激酶抑制剂，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

公开(公告)号：US20130261104A1

公开(公告)日：2013-10-03

申请号：US13890949

申请日：2013-05-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  C07D513/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/541 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4375 ,  C07D491/107

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

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：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：US20150087630A1

公开(公告)日：2015-03-26

申请号：US14255898

申请日：2014-04-17

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Hazel Joan Dyke ,  Charles Ellwood ,  Emanuela Gancia ,  Lewis Gazzard ,  Simon Goodacre ,  Samuel Kintz ,  Joseph Lyssikatos ,  Calum MacLeod ,  Karen Williams

IPC: C07D471/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/4375 ,  C07D519/00

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D491/107 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.

Abstract translation: 式（I）化合物用于治疗癌症的方法：其中X，Y，X，R 3，R 5和R 6如本文所定义。

公开(公告)号：US20140171408A1

公开(公告)日：2014-06-19

申请号：US14185700

申请日：2014-02-20

Applicant: Genentech, Inc.

Inventor： Toby Jonathan Blench ,  Charles Ellwood ,  Simon Charles Goodacre ,  Yingjie Lai ,  Jun Liang ,  Calum MacLeod ,  Steven R. Magnuson ,  Vickie Hsiao-Wei Tsui ,  Karen Williams ,  Birong Zhang

IPC: A61K31/5377 ,  C07D513/04 ,  A61K31/519 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506

CPC classification number: A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  C07D513/04

Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.

Abstract translation: 提供式I化合物，立体异构体，互变异构体，溶剂合物，前药和药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义，药物组合物包括式I化合物和药学上可接受的 载体，佐剂或载体，在治疗中使用化合物或组合物的方法，以及制备式I化合物的方法。

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：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.