公开(公告)号：US20190263794A1

公开(公告)日：2019-08-29

申请号：US16398795

申请日：2019-04-30

Applicant: Genentech, Inc.

Inventor： Sarah M. Bronner ,  James J. Crawford ,  Andrew Cridland ,  Patrick Cyr ,  Benjamin Fauber ,  Emanuela Gancia ,  Alberto Gobbi ,  Christopher Hurley ,  Jonathan Killen ,  Wendy Lee ,  Olivier Rene ,  Monique Bodil Van Niel ,  Stuart Ward ,  Paul Winship ,  Jason Zbieg

IPC: C07D413/14 ,  C07D403/14 ,  C07D405/14

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, p, q A, B, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US10280144B2

公开(公告)日：2019-05-07

申请号：US15801192

申请日：2017-11-01

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  James J. Crawford ,  Sarah M. Bronner ,  Monique Bodil van Niel ,  Andrew Cridland ,  Emanuela Gancia ,  Christopher Hurley ,  Jonathan Killen ,  Stuart Ward

IPC: C07D237/26 ,  C07D237/28

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US20180072683A1

公开(公告)日：2018-03-15

申请号：US15801192

申请日：2017-11-01

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  James J. Crawford ,  Sarah M. Bronner ,  Monique Bodil van Niel ,  Andrew Cridland ,  Emanuela Gancia ,  Christopher Hurley ,  Jonathan Killen ,  Stuart Ward

IPC: C07D237/26

CPC classification number: C07D237/26 ,  C07D237/28

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R1, R2, R3, R4 and R5are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US08754077B2

公开(公告)日：2014-06-17

申请号：US14154008

申请日：2014-01-13

Applicant: Genentech, Inc.

Inventor： James J. Crawford ,  Daniel F. Ortwine ,  BinQing Wei ,  Wendy B. Young

IPC: A61K31/5377 ,  A61K31/502 ,  A61K31/5383

CPC classification number: A61K31/506 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. 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.

Abstract translation: 提供了其中X 1，X 2和X 3中的一个或两个为N的式I化合物，其包括用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于 治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US11008312B2

公开(公告)日：2021-05-18

申请号：US16398795

申请日：2019-04-30

Applicant: Genentech, Inc.

Inventor： Sarah M. Bronner ,  James J. Crawford ,  Andrew Cridland ,  Patrick Cyr ,  Benjamin Fauber ,  Emanuela Gancia ,  Alberto Gobbi ,  Christopher Hurley ,  Jonathan Killen ,  Wendy Lee ,  Olivier Rene ,  Monique Bodil Van Niel ,  Stuart Ward ,  Paul Winship ,  Jason Zbieg

IPC: C07D413/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D401/14

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, p, q A, B, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US20150031674A1

公开(公告)日：2015-01-29

申请号：US14340792

申请日：2014-07-25

Applicant: GENENTECH, INC.

Inventor： Joachim Rudolph ,  Lewis J. Gazzard ,  James J. Crawford ,  Chudi Ndubaku ,  Joy Drobnick ,  Wendy Lee

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中R1，R2，R3，R4，R5，Ra，Rb，Rc，Rd，Re，n，r，s和t如本文所定义，哪些化合物是PAK1的抑制剂。 还公开了用于治疗癌症和过度增殖性疾病的组合物和方法。