公开(公告)号：US20240199594A1

公开(公告)日：2024-06-20

申请号：US18365392

申请日：2023-08-04

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

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：US20190263793A1

公开(公告)日：2019-08-29

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 ,  A61K31/553 ,  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：US20210246129A1

公开(公告)日：2021-08-12

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 ,  C07D498/04 ,  A61K31/553 ,  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.

公开(公告)号：US20160244456A1

公开(公告)日：2016-08-25

申请号：US15144422

申请日：2016-05-02

Applicant: Genentech, Inc.

Inventor： Jeffrey BLANEY ,  Paul A. GIBBONS ,  Emily HANAN ,  Joseph P. LYSSIKATOS ,  Steven R. MAGNUSON ,  Richard PASTOR ,  Thomas E. RAWSON ,  Aihe ZHOU ,  Bing-Yan ZHU

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia 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 JAK kinase activity in a patient.

Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。