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：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：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：US09890152B2

公开(公告)日：2018-02-13

申请号：US14745159

申请日：2015-06-19

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Emily Hanan ,  Timothy Heffron ,  Hans Purkey ,  Richard Leonard Elliott ,  Robert Heald ,  Jamie Knight ,  Michael Lainchbury ,  Eileen M. Seward

IPC: C07D471/04 ,  C07D498/10 ,  A61K31/506 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/541 ,  A61K31/538 ,  C07D491/107 ,  C07D519/00 ,  A61K31/5355 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  A61K45/06 ,  C07D491/107 ,  C07D498/08 ,  C07D498/10 ,  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：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.