公开(公告)号：EP2114950B1

公开(公告)日：2016-03-09

申请号：EP07865255.9

申请日：2007-12-05

申请人： Genentech, Inc. ,  F.Hoffmann-La Roche AG

发明人： CASTANEDO, Georgette ,  DOTSON, Jennafer ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  STABEN, Steven ,  SUTHERLIN, Daniel P. ,  TSUI, Vickie ,  WANG, Shumei ,  ZHU, Bing-Yan ,  BAYLISS, Tracy ,  CHUCKOWREE, Irina ,  FOLKES, Adrian ,  WAN, Nan Chi

IPC分类号： C07D491/048 ,  C07D495/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/048 ,  C07D495/04

公开(公告)号：EP2114949A1

公开(公告)日：2009-11-11

申请号：EP07854962.3

申请日：2007-12-05

申请人： F.HOFFMANN-LA ROCHE AG ,  Genentech, Inc.

发明人： BAYLISS, Tracy ,  CHUCKOWREE, Irina ,  FOLKES, Adrian ,  OXENFORD, Sally ,  WAN, Nan, Chi ,  CASTANEDO, Georgette ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  STABEN, Steven ,  SUTHERLIN, Daniel P. ,  ZHU, Bing-Yan

IPC分类号： C07D491/04 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/519 ,  A61P35/00

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

摘要： 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. [Insert Formula Ic and Id]

摘要翻译： 其中X是S或O，吗啉是吗啉基团，且R 3是单环杂芳基并包括其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐的式Ia-d化合物可用于调节 包括PI3K的脂质激酶的活性，以及​​用于治疗诸如由脂质激酶介导的癌症的疾病。 公开了使用式Ia-d化合物体外，原位和体内诊断，预防或治疗哺乳动物细胞中的此类病症或相关病理学病症的方法。 [插入公式Ic和Id]

公开(公告)号：EP2041139B1

公开(公告)日：2011-11-09

申请号：EP07755937.5

申请日：2007-04-24

申请人： F.Hoffmann-La Roche AG ,  Genentech, Inc.

发明人： FOLKES, Adrian ,  SHUTTLEWORTH, Stephen ,  CHUCKOWREE, Irina ,  OXENFORD, Sally ,  WAN, Nan Chi ,  CASTANEDO, Georgette ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  SUTHERLIN, Daniel, P. ,  ZHU, Bing-Yan ,  GOLDSMITH, Richard

IPC分类号： C07D491/04

CPC分类号： A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：EP2114950A2

公开(公告)日：2009-11-11

申请号：EP07865255.9

申请日：2007-12-05

申请人： Genentech, Inc. ,  F.HOFFMANN-LA ROCHE AG

发明人： CASTANEDO, Georgette ,  DOTSON, Jennafer ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  STABEN, Steven ,  SUTHERLIN, Daniel P. ,  TSUI, Vickie ,  WANG, Shumei ,  ZHU, Bing-Yan ,  BAYLISS, Tracy ,  CHUCKOWREE, Irina ,  FOLKES, Adrian ,  WAN, Nan Chi

IPC分类号： C07D491/048 ,  C07D495/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/048 ,  C07D495/04

摘要： 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. Formula (Ic) and (Id).

公开(公告)号：EP2046799A1

公开(公告)日：2009-04-15

申请号：EP07776052.8

申请日：2007-04-24

申请人： Genentech, Inc. ,  F.HOFFMANN-LA ROCHE AG

发明人： CASTANEDO, Georgette ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MALESKY, Kimberly ,  MATHIEU, Simon ,  OLIVERO, Alan ,  SUTHERLIN, Daniel, P. ,  TSUI, Vickie ,  WANG, Shumei ,  WEISMANN, Christian ,  ZHU, Bing-Yan ,  DOTSON, Jennafer ,  FOLKES, Adrian ,  SHUTTLEWORTH, Stephen ,  OXENFORD, Sally ,  HANCOX, Tim ,  BAYLISS, Tracy

IPC分类号： C07D491/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/04 ,  C07D495/04

摘要： Compounds of Formulas (Ia) and (Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula (Ia) and (Ib) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

摘要翻译： 式Ia和Ib的化合物，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，可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia和Ib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。

公开(公告)号：EP2041139A2

公开(公告)日：2009-04-01

申请号：EP07755937.5

申请日：2007-04-24

申请人： F.HOFFMANN-LA ROCHE AG ,  Genentech, Inc.

发明人： FOLKES, Adrian ,  SHUTTLEWORTH, Stephen ,  CHUCKOWREE, Irina ,  OXENFORD, Sally ,  WAN, Nan Chi ,  CASTANEDO, Georgette ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  SUTHERLIN, Daniel, P. ,  ZHU, Bing-Yan ,  GOLDSMITH, Richard

IPC分类号： C07D491/04

CPC分类号： A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

摘要翻译： 式Ia和Ib化合物及其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐可用于抑制包括PI3K在内的脂质激酶，以及用于治疗诸如由脂质激酶介导的癌症等疾病。 公开了使用式Ia和Ib化合物体外，原位和体内诊断，预防或治疗哺乳动物细胞中的此类病症或相关病理学病症的方法。

公开(公告)号：EP2794605A1

公开(公告)日：2014-10-29

申请号：EP12812254.6

申请日：2012-12-21

申请人： F.Hoffmann-La Roche AG

发明人： ALIAGAS-MARTIN, Ignacio ,  CRAWFORD, James ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  LEE, Wendy

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/4353 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K31/506 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04

摘要： Compounds having the formula I wherein A, R
1a , R
1b , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , R
8 , R
a , R
b , X
1 , X
2 , X
3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

摘要翻译： 其中A，R 1a，R 1b，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R a，R b，X 1，X 2，X 3和 n如本文所定义是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。

公开(公告)号：EP2748159A1

公开(公告)日：2014-07-02

申请号：EP12755816.1

申请日：2012-08-24

申请人： F.Hoffmann-La Roche AG

发明人： ALIAGAS-MARTIN, Ignacio ,  CRAWFORD, James ,  LEE, Wendy ,  MATHIEU, Simon ,  RUDOLPH, Joachim

IPC分类号： C07D403/14 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D403/14 ,  A61K31/506 ,  A61K45/06

摘要： Compounds having the formula I wherein A, Z, R
1a , R
1b , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , R
9 , R
10, R
a , R
b and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

公开(公告)号：EP2265610A1

公开(公告)日：2010-12-29

申请号：EP09718306.5

申请日：2009-02-27

申请人： Array Biopharma, Inc. ,  Genentech, Inc.

发明人： AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  DE MEESE, Jason ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  LUNGHOFER, Paul ,  MORENO, David ,  NEWHOUSE, Brad ,  REN, Li ,  SEO, Jeongbeob ,  TIAN, Hongqi ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  GUNZNER, Janet ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B.

IPC分类号： C07D471/04 ,  C07C311/08 ,  A61K31/437 ,  A61P13/12 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07C311/08

摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro,
in situ, and
in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

公开(公告)号：EP2265610B1

公开(公告)日：2012-12-12

申请号：EP09718306.5

申请日：2009-02-27

申请人： Array Biopharma, Inc. ,  Genentech, Inc.

发明人： AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  DE MEESE, Jason ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  LUNGHOFER, Paul ,  MORENO, David ,  NEWHOUSE, Brad ,  REN, Li ,  SEO, Jeongbeob ,  TIAN, Hongqi ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  GUNZNER, Janet ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B.

IPC分类号： C07D471/04 ,  C07C311/08 ,  A61K31/437 ,  A61P13/12 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07C311/08