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公开(公告)号:MX2018000048A
公开(公告)日:2018-06-06
申请号:MX2018000048
申请日:2016-06-23
Applicant: UNIV HEALTH NETWORK
Inventor: LAUFER RADOSLAW , SAMPSON PETER BRENT , LIU YONG , LI SZE-WAN , PAULS HEINZ W , GRACE NG , NARENDRA KUMAR B PATEL , YUNHUI LANG
IPC: C07D495/04 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K39/395 , A61P35/00
Abstract: Se describen compuesto de tienopiridinona de la Fórmula (I) y sus sales farmacéuticamente aceptables; en estos compuestos, uno de X1; X2 y X3 es S y los otros dos son cada uno independientemente CR, en donde R y demás variables son como se define en el presente; los compuestos muestran inhibir la actividad de quinasa HPK1 y tener actividad anti-tumoral in vivo; los compuestos pueden ser eficazmente combinados con portadores farmacéuticamente aceptables y también con otros enfoques inmunomoduladores, tales como la inhibición del punto de control o inhibidores de oxidación de triptófano. (ver Fórmula).
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公开(公告)号:MA42456A
公开(公告)日:2018-05-23
申请号:MA42456
申请日:2016-06-23
Applicant: UNIV HEALTH NETWORK
Inventor: LAUFER RADOSLAW , LANG YUNHUI , LI SZE-WAN , LIU YONG , NG GRACE , PATEL NARENDRA KUMAR B , PAULS HEINZ W , SAMPSON PETER BRENT
IPC: A61K31/4355 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K31/551 , A61K39/00 , A61K39/395 , A61K45/06 , A61P35/00 , C07D495/04 , C07K16/28
Abstract: L'invention concerne des composés de thiénopyridinone de formule (i) et des sels de ceux-ci pharmaceutiquement acceptables. Dans ces composés, l'un de x1, x2, et x3 est s et les deux autres sont chacun indépendamment cr, r et toutes les autres variables sont telles que définies dans la description. Ces composés sont connus pour inhiber l'activité de la kinase hpk1 et pour avoir une activité antitumorale in vivo. Ces composés peuvent être efficacement combinés avec des vecteurs pharmaceutiquement acceptables, ainsi qu'avec d'autres techniques immunomodulatrices, telles qu'une inhibition de points de contrôle ou des inhibiteurs de l'oxydation du tryptophane. Formule (i).
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公开(公告)号:AU2013344716B2
公开(公告)日:2018-03-01
申请号:AU2013344716
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:CA2694724C
公开(公告)日:2017-09-12
申请号:CA2694724
申请日:2008-08-01
Applicant: UNIV HEALTH NETWORK
Inventor: FEHER MIKLOS , FORREST BRYAN T , LANG YUNHUI , LAUFER RADOSLAW , LIU YONG , PAN GUOHUA , PAULS HEINZ W , SAMPSON PETER BRENT , YAO YI
IPC: C07D211/58 , A61K31/17 , A61K31/397 , A61K31/40 , A61K31/445 , A61P3/10 , A61P35/00 , C07C275/32 , C07D205/04 , C07D207/50 , C07D211/56
Abstract: A CPT1 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:RS55471B1
公开(公告)日:2017-04-28
申请号:RSP20160997
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
IPC: C07D413/14 , A61K31/5377 , A61P35/00 , C07D403/04 , C07D403/10 , C07D403/14
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公开(公告)号:ES2603613T3
公开(公告)日:2017-02-28
申请号:ES11764988
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
IPC: C07D413/14 , A61K31/5377 , A61P35/00 , C07D403/04 , C07D403/10 , C07D403/14
Abstract: Un compuesto representado por la fórmula estructural siguiente:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: Ra es -F, metoxi, metilo o etilo; R4 es -H o metilo; y R6 es -CH>=CH-(fenilo sustituido opcionalmente), en donde el fenilo en -CH>=CH-(fenilo) está sustituido opcionalmente con uno o más sustituyentes seleccionados independientemente del grupo que consiste en halógeno, alquilo C1-6, haloalquilo C1-6, (aminoalquilo C1-6), (alquilamino C1-6)alquilo C1-6, (fenil)alquilo C1-6, amino, alquilamino C1-6, dialquilamino C1-6, -(CH2)0-3-N-piperidinilo, -(CH2)0-3-N-morfolinilo, -(CH2)0-3-N-pirrolidinilo, -(CH2)0-3-Npiperazinilo y -(CH2)0-3-N-oxazepanilo, en donde el N-piperazinilo está sustituido opcionalmente en N' con alquilo C1-6 o acilo C1-6.
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公开(公告)号:DK2556071T3
公开(公告)日:2016-12-12
申请号:DK11764988
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
IPC: C07D413/14 , A61K31/5377 , A61P35/00 , C07D403/04 , C07D403/10 , C07D403/14
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公开(公告)号:CA2709536C
公开(公告)日:2016-05-31
申请号:CA2709536
申请日:2008-12-19
Applicant: UNIV HEALTH NETWORK
Inventor: PAULS HEINZ W , FORREST BRYAN T , LAUFER RADOSLAW , FEHER MIKLOS , SAMPSON PETER BRENT , PAN GUOHUA , LI SZE-WAN , LIU YONG
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
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.
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公开(公告)号:CA2964282A1
公开(公告)日:2016-05-06
申请号:CA2964282
申请日:2015-10-09
Applicant: UNIV HEALTH NETWORK
Inventor: BRAY MARK R , BROKX RICHARD , LAUFER RADOSLAW , LI SZE-WAN , MASON JACQUELINE M , NG GRACE , PAULS HEINZ W
IPC: C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00 , A61P37/06
Abstract: The invention is a compound represented by Structural Formula (I): (I); or a pharmaceutically acceptable salt thereof. Values for the variables are provided herein. Also included is a pharmaceutical composition comprising the compound represented by Structural Formula (I) and a pharmaceutically acceptable carrier or diluent and methods of treating a subject with cancer with the compound of Structural Formula (I).
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公开(公告)号:CA2850394A1
公开(公告)日:2013-04-18
申请号:CA2850394
申请日:2012-10-12
Applicant: UNIV HEALTH NETWORK
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: C07D401/00 , A61K31/416 , A61P35/00 , C07D231/56 , C07D401/02 , C07D401/14 , C07D403/02 , C07D405/14 , C07D409/14 , C07D451/06 , C07D491/107
Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
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