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：US09951064B2

公开(公告)日：2018-04-24

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury ,  Robert Heald ,  Eileen M. Seward

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/517 ,  A61K31/5386 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

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：US20240150364A1

公开(公告)日：2024-05-09

申请号：US18507678

申请日：2023-11-13

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

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：US20200002345A1

公开(公告)日：2020-01-02

申请号：US16561432

申请日：2019-09-05

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

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.