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1.发明申请
公开(公告)号：WO2009015485A1
公开(公告)日：2009-02-05
申请号：PCT/CA2008001415
申请日：2008-08-01
Applicant: UNIV HEALTH NETWORK , PAULS HEINZ W , FORREST BRYAN T , SAMPSON PETER BRENT , LIU YONG , LAUFER RADOSLAW , LANG YUNHUI , FEHER MIKIOS , YAO YI , PAN GUOHUA
Inventor： PAULS HEINZ W , FORREST BRYAN T , SAMPSON PETER BRENT , LIU YONG , LAUFER RADOSLAW , LANG YUNHUI , FEHER MIKIOS , YAO YI , PAN GUOHUA
IPC: C07D211/58 , A61K31/17 , A61K31/397 , A61K31/40 , A61K31/445 , A61P3/10 , A61P35/00 , C07C275/32 , C07D205/04 , C07D207/50 , C07D211/56
CPC classification number: C07D211/58 , C07C275/36 , C07D205/04 , C07D207/09 , C07D211/56 , C07D405/12
Abstract: A CPTl 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.
Abstract translation: CPT1抑制剂化合物由结构式（I）或其药学上可接受的盐表示：或其药学上可接受的盐。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。 治疗患有癌症的受试者的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。
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公开(公告)号：MD3322711T2
公开(公告)日：2021-07-31
申请号：MDE20180529
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
Abstract: Sunt descrişi compuşii tienopiridinonici cu Formula (I) şi sărurile acceptabile farmaceutic ale acestora. În aceşti compuşi, unul dintre X1; X2 şi X3 sunt S şi celelalte două sunt fiecare independent CR, în care R şi toate celelalte variabile sunt definite aici. Se arată că compuşii inhibă activitatea kinazei HPK1 şi au activitate antitumorală in vivo. Compuşii pot fi combinaţi eficient cu purtători acceptabili farmaceutic şi, de asemenea, cu alte abordări imunomodulatoare, cum ar fi inhibarea punctului de control sau inhibitorii oxidării triptofanului. Formula (I).
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公开(公告)号：AU2016282289B2
公开(公告)日：2020-12-24
申请号：AU2016282289
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 X
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公开(公告)号：EP2920181A4
公开(公告)日：2016-07-27
申请号：EP13855919
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
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: 本发明提供由结构式（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。
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5.发明公开
公开(公告)号：EP2766352A4
公开(公告)日：2015-06-03
申请号：EP12840107
申请日：2012-10-12
Applicant: UNIV HEALTH NETWORK UHN
Inventor： PAULS HEINZ W , LAUFER RADOSLAW , LIU YONG , LI SZE-WAN , FORREST BRYAN T , LANG YUNHUI , PATEL NARENDRA KUMAR B , EDWARDS LOUISE G , NG GRACE , SAMPSON PETER BRENT , FEHER MIKLOS , AWREY DONALD E
IPC: C07D409/12 , A61K31/416 , A61P35/00 , C07D231/56 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D451/06 , C07D491/107 , C07D493/10
CPC classification number: C07D231/56 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D451/06 , C07D491/107 , C07D493/10
Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
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Patent Agency Ranking
公开(公告)号：LT3322711T
公开(公告)日：2021-05-10
申请号：LT16813437
申请日：2016-06-23
Applicant: UNIV HEALTH NETWORK
Inventor： LIU YONG , SAMPSON PETER BRENT , PATEL NARENDRA KUMAR B , PAULS HEINZ W , LI SZE-WAN , NG GRACE , LAUFER RADOSLAW , 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：EA035421B1
公开(公告)日：2020-06-11
申请号：EA201890059
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: Предложенытиенопиридиновыесоединенияформулы (I) иихфармацевтическиприемлемыесоли. Вэтихсоединенияходиниз X, Xи Xпредставляетсобой S икаждыйиздвухостальныхнезависимопредставляетсобой CR, гдезначения R ивсехостальныхпеременныхявляютсятакими, какопределенов настоящемдокументе. Показано, чтосоединенияингибируютактивностькиназы HPK1 иобладаютпротивоопухолевойактивностью in vivo. Предложенатакжефармацевтическаякомпозициядлялечениярака, содержащаясоединениеи фармацевтическиприемлемыйносительилиразбавитель. Предложеноприменениесоединенияилиегофармацевтическиприемлемойсоли, атакжеихкомбинациис антителомк PD-1 длялечениярака. Такжепредложенспособлеченияракау субъекта.
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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：HUE054159T2
公开(公告)日：2021-08-30
申请号：HUE16813437
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 , A61K39/00 , A61K45/06 , A61P35/00 , C07K16/28
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公开(公告)号：RS61919B1
公开(公告)日：2021-06-30
申请号：RSP20210675
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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