公开(公告)号：US20140323477A1

公开(公告)日：2014-10-30

申请号：US14266617

申请日：2014-04-30

Applicant: Genentech, Inc.

Inventor： James J. CRAWFORD ,  Wendy LEE ,  Joachim RUDOLPH

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders using such compounds.

Abstract translation: 具有式I的化合物或其药学上可接受的盐，其中R 1，R 2，X 1，X 2和Ar如本文所定义，是PAK1的抑制剂。 还公开了使用这些化合物治疗癌症和过度增殖性疾病的组合物和方法。

公开(公告)号：US20240174696A1

公开(公告)日：2024-05-30

申请号：US18526572

申请日：2023-12-01

Applicant: Genentech, Inc.

Inventor： Steven John MCKERRALL ,  Alice Rose WONG ,  James John CRAWFORD ,  Wendy LEE ,  Kwong Wah LAI ,  Guillaume PELLETIER ,  Stéphanie ROY ,  Dana Krystin WINTER ,  Mikiko OKUMURA ,  Ruth Dorel

IPC: C07D519/00 ,  A61P11/00

CPC classification number: C07D519/00 ,  A61P11/00

Abstract: Disclosed are 2,8-diazaspiro[4.5]decane compounds, including (pyrido[3,4-d]pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane compounds, (2,6-naphthyridin-1-yl)-2,8-diazaspiro[4.5]decane compounds, and (1,7-naphthyridin-4-yl)-2,8-diazaspiro[4.5]decane compounds, that are inhibitors of LATS1/2, compositions containing these compounds, and methods for inhibiting LATS1/2 activity.

公开(公告)号：US20200181154A1

公开(公告)日：2020-06-11

申请号：US16789081

申请日：2020-02-12

Applicant: Genentech, Inc.

Inventor： Roland J. BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/14 ,  C07D471/04 ,  A61K31/502 ,  C07D405/14 ,  C07D401/14 ,  A61K31/519 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/496 ,  A61K45/06

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20190194209A1

公开(公告)日：2019-06-27

申请号：US16289287

申请日：2019-02-28

Applicant: Genentech, Inc.

Inventor： Roland J. BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/496 ,  A61K45/06 ,  C07D401/14 ,  C07D471/14 ,  C07D471/04 ,  A61K31/502 ,  C07D405/14 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20180057500A1

公开(公告)日：2018-03-01

申请号：US15690140

申请日：2017-08-29

Applicant: Genentech, Inc.

Inventor： Roland J BILLEDEAU ,  James J. CRAWFORD ,  Saul JAIME-FIGUEROA ,  Wendy LEE ,  Francisco Javier LOPEZ-TAPIA ,  Sung-Sau SO

IPC: C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  C07D401/14 ,  A61K31/502 ,  C07D471/14 ,  A61K31/496

CPC classification number: C07D487/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.