公开(公告)号：EP2348860A1

公开(公告)日：2011-08-03

申请号：EP09824234.0

申请日：2009-11-02

申请人： Genentech, Inc.

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

IPC分类号： A01N43/90 ,  A61K31/519

CPC分类号： C07D487/04

摘要： 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. Ia

公开(公告)号：EP2445346A1

公开(公告)日：2012-05-02

申请号：EP10792616.4

申请日：2010-06-23

申请人： Genentech, Inc.

发明人： BERGERON, Philippe ,  COHEN, Frederick ,  ESTRADA, Anthony ,  KOEHLER, Michael F.T. ,  LEE, Wendy ,  LY, Cuong ,  LYSSIKATOS, Joseph P. ,  PEI, Zhonghua ,  ZHAO, Xianrui

IPC分类号： A01N43/54

CPC分类号： C07D491/052 ,  C07D491/048 ,  C07D491/18 ,  C07D519/00

摘要： Disclosed are compounds of Formula (I), including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR). Formula (I).

公开(公告)号：EP3670514A1

公开(公告)日：2020-06-24

申请号：EP19211640.8

申请日：2010-07-02

申请人： Genentech, Inc.

发明人： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC分类号： C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I 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 Janus kinase activity in a patient are disclosed.

公开(公告)号：EP3333169A1

公开(公告)日：2018-06-13

申请号：EP17192475.6

申请日：2010-07-02

申请人： Genentech, Inc.

发明人： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC分类号： C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I 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 Janus kinase activity in a patient are disclosed.

公开(公告)号：EP2448941B1

公开(公告)日：2017-11-08

申请号：EP10794815.0

申请日：2010-07-02

申请人： Genentech, Inc.

发明人： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan ,  HURLEY, Christopher

IPC分类号： C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D487/04

公开(公告)号：EP2348860B1

公开(公告)日：2015-05-27

申请号：EP09824234.0

申请日：2009-11-02

申请人： Genentech, Inc.

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

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： C07D487/04

公开(公告)号：EP3333169B1

公开(公告)日：2020-01-01

申请号：EP17192475.6

申请日：2010-07-02

申请人： Genentech, Inc.

发明人： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC分类号： C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

公开(公告)号：EP2448941A2

公开(公告)日：2012-05-09

申请号：EP10794815.0

申请日：2010-07-02

申请人： Genentech, Inc.

发明人： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC分类号： C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D487/04

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R
1 , R
2 and R
3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I 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 Janus kinase activity in a patient are disclosed.

摘要翻译： 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及对患者中Janus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。

公开(公告)号：EP2288260A1

公开(公告)日：2011-03-02

申请号：EP09767860.1

申请日：2009-06-19

申请人： Genentech, Inc.

发明人： ZHU, Bing-Yan ,  SIU, Michael ,  MAGNUSON, Steven, R. ,  PASTOR, Richard ,  HAIYING, He ,  YISONG, Xiao ,  JIFU, Zheng ,  XING, Xu ,  JUNPING, Zhao ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  HURLEY, Christopher A. ,  LIANG, Jun

IPC分类号： A01N43/64 ,  A61K31/41

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

摘要： A compound of Formula (I), enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R
1 , R
2 , R
3 , R
4 and R
5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula (I) 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 JAK kinase activity in a patient are disclosed. Formula (I).

摘要翻译： 其中R 1，R 2，R 3，R 4和R 5如本文所定义的式（I）化合物，其对映体，非对映异构体，互变异构体或可药用盐可用作JAK激酶抑制剂。 公开了包含式（I）化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻患者对JAK激酶活性的抑制作用的疾病或病症的严重程度或减轻其严重程度的方法。 公式（I）。