公开(公告)号：US20130217666A1

公开(公告)日：2013-08-22

申请号：US13768873

申请日：2013-02-15

Applicant: Genentech, Inc.

Inventor： Steven Staben ,  Georgette Castanedo ,  Christian A.G.N. Montalbetti ,  Jianwen Feng

IPC: C07D513/04 ,  C07D498/04

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D498/00 ,  C07D498/12 ,  C07D513/04 ,  C07D519/00

Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20130129820A1

公开(公告)日：2013-05-23

申请号：US13738829

申请日：2013-01-10

Applicant: Genentech, Inc.

Inventor： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于调节 脂质激酶（包括PI3K）的活性，以及​​用于治疗脂质激酶介导的疾病如癌症。 公开了使用式Ia-d的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。