公开(公告)号：EP3322711A1

公开(公告)日：2018-05-23

申请号：EP16813437.7

申请日：2016-06-23

Applicant: University Health Network

Inventor： SAMPSON, Peter Brent ,  PATEL, Narendra Kumar B. ,  PAULS, Heinz W. ,  LI, Sze-Wan ,  NG, Grace ,  LAUFER, Radoslaw ,  LIU, Yong ,  LANG, Yunhui

IPC: C07D495/04 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

CPC classification number: C07D495/04 ,  A61K31/4355 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/551 ,  A61K39/395 ,  A61K45/06 ,  A61K2039/505 ,  A61P35/00 ,  C07K16/2818 ,  A61K2300/00

Abstract: Thienopyridinone compounds of Formula (I) and pharmaceutically acceptable salts thereof are described. In these compounds, one of X1; X2, and X3 is S and the other two are each independently CR, wherein R and all other variables are as defined herein. The compounds are shown to inhibit HPK1 kinase activity and to have in vivo antitumor activity. The compounds can be effectively combined with pharmaceutically acceptable carriers and also with other immunomodulatory approaches, such as checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).

公开(公告)号：EP2920181A1

公开(公告)日：2015-09-23

申请号：EP13855919.0

申请日：2013-11-15

Applicant: University Health Network (UHN)

Inventor： LIU, Yong ,  PAULS, Heinz W. ,  LAUFER, Radoslaw ,  LI, Sze-Wan ,  SAMPSON, Peter Brent ,  FEHER, Miklos ,  NG, Grace ,  PATEL, Narendra Kumar B. ,  LANG, Yunhui

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.

Abstract translation: 本教导提供由结构式（1-0）表示的化合物或其药学上可接受的盐。 还描述了药物组合物及其使用方法。

公开(公告)号：EP2417127B1

公开(公告)日：2014-02-26

申请号：EP10761154.3

申请日：2010-04-06

Applicant: University Health Network

Inventor： SAMPSON, Peter Brent ,  Ll, Sze-Wan ,  LIU, Yong ,  PAULS, Heinz W. ,  EDWARDS, Louise G. ,  FORREST, Bryan T. ,  FEHER, Miklos ,  PATEL, Narendra Kumar B. ,  PAN, Guohua

IPC: C07D403/04 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D403/14 ,  C07D471/14 ,  C07D471/04

CPC classification number: A61K31/553 ,  A61K31/416 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10

公开(公告)号：EP2556070A1

公开(公告)日：2013-02-13

申请号：EP11764989.7

申请日：2011-04-06

Applicant: University Health Network

Inventor： CUMMING, Graham ,  PATEL, Narenda Kumar B. ,  FORREST, Bryan, T. ,  LIU, Yong ,  LI, Sze-Wan ,  SAMPSON, Peter Brent ,  EDWARDS, Louise, G. ,  PAULS, Heinz W.

IPC: C07D403/04 ,  C07D231/56 ,  C07D413/14

CPC classification number: C07D403/10 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/56 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14

Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.

Abstract translation: 本发明涉及制备由结构式（A）表示的螺环丙基吲哚满酮化合物的新合成方法：（A）或其药学上可接受的盐。 还包括本文所述的合成中间体。

公开(公告)号：EP2235004A1

公开(公告)日：2010-10-06

申请号：EP08865534.5

申请日：2008-12-19

Applicant: University Health Network

Inventor： PAULS, Heinz, W. ,  FORREST, Bryan, T. ,  LAUFER, Radoslaw ,  FEHER, Miklos ,  SAMPSON, Peter, Brent ,  PAN, Guohua ,  LIU, Yong ,  LI, Sze-Wan

IPC: C07D403/06 ,  A61K31/416 ,  A61K31/4192 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

CPC classification number: C07D403/06 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.