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公开(公告)号:CA2989684A1
公开(公告)日:2016-12-29
申请号:CA2989684
申请日:2016-06-23
Applicant: UNIV 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
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).
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公开(公告)号:HRP20161498T1
公开(公告)日:2016-12-16
申请号:HRP20161498
申请日:2016-11-14
Applicant: UNIV HEALTH NETWORK
Inventor: SAMPSON PETER BRENT , LIU YONG , LI SZE-WAN , FORREST BRYAN T , PAULS HEINZ W , EDWARDS LOUISE G , FEHER MIKLOS , PATEL NARENDRA KUMAR B , LAUFER RADOSLAW , PAN GUOHUA
IPC: C07D413/14 , A61K31/5377 , A61P35/00 , C07D403/04 , C07D403/10 , C07D403/14
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公开(公告)号:CA2680366C
公开(公告)日:2016-06-21
申请号:CA2680366
申请日:2008-03-06
Applicant: UNIV HEALTH NETWORK
Inventor: PAULS HEINZ W , SAMPSON PETER BRENT , FORREST BRYAN T , LAUFER RADOSLAW , LIU YONG , FEHER MIKLOS , YAO YI , PAN GUOHUA
IPC: C07C275/28 , A61K31/195 , A61K31/34 , A61K31/381 , A61K31/41 , A61K31/44 , A61K31/495 , A61P35/00 , C07C233/52 , C07C233/83 , C07C237/42 , C07C275/06 , C07C307/06 , C07C307/10 , C07C311/19 , C07C311/29 , C07D213/71 , C07D213/82 , C07D231/12 , C07D231/14 , C07D277/44 , C07D307/68 , C07D307/82 , C07D333/34 , C07D333/40 , C07D401/04 , C07D409/06 , C07D413/04 , C07D413/06 , C07D417/04
Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号:SG183875A1
公开(公告)日:2012-10-30
申请号:SG2012065090
申请日:2011-04-06
Applicant: UNIV HEALTH NETWORK
Inventor: SAMPSON PETER BRENT , LIU YONG , LI SZE-WAN , FORREST BRYAN T , PAULS HEINZ W , EDWARDS LOUISE G , FEHER MIKLOS , PATEL NARENDRA KUMAR B , LAUFER RADOSLAW , PAN GUOHUA
Abstract: The invention is directed to a compound represented by the following structural formula pharmaceutically acceptable salts thereof: (I). 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.
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公开(公告)号:PL3322711T3
公开(公告)日:2021-10-25
申请号:PL16813437
申请日:2016-06-23
Applicant: UNIV 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 , A61K31/4355 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K31/551 , A61K39/00 , A61K39/395 , A61K45/06 , A61P35/00 , C07K16/28
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公开(公告)号:SI3322711T1
公开(公告)日:2021-08-31
申请号:SI201631189
申请日:2016-06-23
Applicant: UNIV HEALTH NETWORK
Inventor: SAMPSON PETER BRENT , PATEL NARENDRA KUMAR B , PAULS HEINZ W , LI SZE-WAN , NG GRACE , LAUFER RADOSLAW , LIU YONG , LANG YUNHUI
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公开(公告)号:HRP20210895T1
公开(公告)日:2021-08-20
申请号:HRP20210895
申请日:2021-06-07
Applicant: UNIV 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 , A61K31/4355 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K31/551 , A61K39/00 , A61K39/395 , A61K45/06 , A61P35/00 , C07K16/28
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公开(公告)号:CA2889919C
公开(公告)日:2021-08-17
申请号:CA2889919
申请日:2013-11-15
Applicant: UNIV HEALTH NETWORK
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
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.
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公开(公告)号:NZ707432A
公开(公告)日:2020-01-31
申请号:NZ70743213
申请日:2013-11-15
Applicant: UNIV HEALTH NETWORK
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
Abstract: The present teachings provide a compound represented by structural formula (II-A0), or a pharmaceutically acceptable salt thereof. R1 is –NHRb1, where Rb1 is alkyl which may be optionally substituted with one or more groups as defined herein. R2 is optionally substituted heterocycloalkyl, heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted heterocyclyloxy or substituted amino (and wherein the substituents are as defined herein). R4 is chloro or methyl. Rd is cyclopropyl. Specific compounds include N-cyclopropyl-4-(7-(((trans-3-hydroxy-3-methylcyclobutyl)methyl)amino)-5-(pyridin-3-yloxy)pyrazolo[1,5-a]pyrimidin-3-yl)-2-methylbenzamide (CFI-402257) and N-cyclopropyl-4-(7-((cyclopropylmethyl)amino)-5-(((1S,2R)-2-hydroxycyclohexyl)amino)pyrazolo[1,5-a]pyrimidin-3-yl)-2-methylbenzamide. Also described are pharmaceutical compositions and uses thereof, such as for the inhibitors of tyrosine threonine kinase (TTK) and for the treatment of cancers such as pancreatic cancer, prostate cancer, lung cancer, melanoma, breast cancer, colon cancer, or ovarian cancer.
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公开(公告)号:HRP20181041T1
公开(公告)日:2018-09-21
申请号:HRP20181041
申请日:2018-07-05
Applicant: UNIV HEALTH NETWORK
Inventor: LAUFER RADOSLAW , NG GRACE , LI SZE-WAN , PAULS HEINZ W , LIU YONG , PATEL NARENDRA KUMAR B
IPC: C07D487/04 , A61K31/519 , A61P35/00
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