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公开(公告)号:AU2011238384B2
公开(公告)日:2015-02-19
申请号:AU2011238384
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: C07D403/04 , A61K31/5377 , A61P35/00 , C07D413/14
Abstract: The invention is directed to a compound represented by the following structural formula and 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:AU2008340991B2
公开(公告)日:2012-02-23
申请号:AU2008340991
申请日:2008-12-19
Applicant: UNIV HEALTH NETWORK
Inventor: PAN GUOHUA , FORREST BRYAN T , LAUFER RADOSLAW , FEHER MIKLOS , PAULS HEINZ W , SAMPSON PETER BRENT , LI SZE-WAN , LIU YONG
IPC: C07D401/14 , A61K31/416 , A61K31/4192 , A61P35/00 , C07D403/06 , 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:AU2008340991A1
公开(公告)日:2009-07-02
申请号:AU2008340991
申请日:2008-12-19
Applicant: UNIV HEALTH NETWORK
Inventor: PAN GUOHUA , FORREST BRYAN T , LAUFER RADOSLAW , FEHER MIKLOS , PAULS HEINZ W , SAMPSON PETER BRENT , LI SZE-WAN , LIU YONG
IPC: C07D401/14 , A61K31/416 , A61K31/4192 , A61P35/00 , C07D403/06 , 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 thereof. 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:MX386480B
公开(公告)日:2025-03-18
申请号:MX2018000048
申请日:2018-01-08
Applicant: UNIV HEALTH NETWORK
Inventor: NG GRACE , LAUFER RADOSLAW , LI SZE-WAN , LIU YONG , PATEL NARENDRA KUMAR B , PAULS HEINZ W , SAMPSON PETER BRENT , LANG YUNHUI
IPC: C07D495/04 , A61K31/4355 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K31/551 , A61K39/395 , A61P35/00 , C07K16/28
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:ES2872555T3
公开(公告)日:2021-11-02
申请号:ES16813437
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: Un compuesto representado por la fórmula (I-A): **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en el que: R es H, -F, -CI, -Br, -OH, -alquilo (C1-C4), -haloalquilo (C1-C4), -alcoxilo (C1-C4), -alquilen (C1-C4)-OH o heterociclilo monocíclico de 4-7 miembros opcionalmente sustituido con 1-3 grupos seleccionados de -F, - CI, -Br, -OH, -alquilo (C1-C4), -haloalquilo (C1-C4) o -alcoxilo (C1-C4); R1 es -NRaRb o -ORa1; Ra en cada aparición es independientemente -H, -alquilo (C1-C6), -(CH2)n-cicloalquilo (C3-C7), -(CH2)n- heterociclilo monocíclico de 3-7 miembros, -(CH2)n-cicloalquilo (C6-C12) en puente, -(CH2)n-heteroarilo de 5- 10 miembros opcionalmente sustituido; o -(CH2)n-heterociclilo en puente de 6-12 miembros, en el que el - alquilo (C1-C6), -(CH2)n-cicloalquilo (C3-C7), -(CH2)n-heterociclilo monocíclico de 3-7 miembros, -(CH2)n- cicloalquilo (C6-C12) en puente, -(CH2)n-heteroarilo de 5-10 miembros o -(CH2)n-heterociclilo en puente de 6- 12 miembros está opcionalmente sustituido con 1-3 grupos seleccionados de -F, -CI, -Br, -CN, -NH2, -OH, oxo, -alquilo (C1-C4), -haloalquilo (C1-C4), -alcoxilo (C1-C4), -haloalcoxilo (C1-C4), -alquilen (C1-C4)-OH o - alquilen (C1-C4)-NH2; Rb en cada aparición es independientemente -H o -alquilo (C1-C6); o Ra y Rb, junto con el nitrógeno al que están unidos, forman -heterociclilo (C3-C10); Ra1 en cada aparición es independientemente -H, alquilo (C1-C6), cicloalquilo (C3-C10), heterociclilo de 3-10 miembros, arilo (C6-C10) o heteroarilo de 3-10 miembros; R4 y R5, junto con el nitrógeno al que están unidos, forman heterociclilo monocíclico de 4-7 miembros o heterociclilo en puente de 6-12 miembros, en el que el heterociclilo monocíclico de 4-7 miembros o heterociclilo en puente de 6-12 miembros está opcionalmente sustituido con 1-3 grupos seleccionados de - F, -CI, -Br, -CN, -NH2, -OH, oxo, -alquilo (C1-C4), -haloalquilo (C1-C4), -alcoxilo (C1-C4), -haloalcoxilo (C1-C4), -alquilen (C1-C4)-OH o -alquilen (C1-C4)-NH2; R6 en cada aparición es independientemente -F, -CI, -Br, -CN, -NH2, -OH, -alquilo (C1-C6), - haloalquilo (C1- C6), -alquenilo (C2-C6), -alquinilo (C2-C6), cicloalquilo (C3-C6), -alcoxilo (C1-C6), -haloalcoxilo (C1-C6), - alquilen (C1-C6)-OH o -alquilen (C1-C6)-NH2; m es 0, 1, 2 o 3; y n es 0, 1 o 2.
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公开(公告)号:SG10202105964RA
公开(公告)日:2021-07-29
申请号:SG10202105964R
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
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 a checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).
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公开(公告)号:DK3322711T3
公开(公告)日:2021-04-26
申请号:DK16813437
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:HK1255833A1
公开(公告)日:2019-08-30
申请号:HK18114909
申请日:2018-11-21
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: C07D20060101 , A61K20060101 , A61P20060101 , C07K20060101
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公开(公告)号:CA2850394C
公开(公告)日:2019-05-21
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 , SAMPSON PETER BRENT , FEHER MIKLOS , AWREY DONALD E , NG GRACE
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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公开(公告)号:RS57481B1
公开(公告)日:2018-10-31
申请号:RSP20180775
申请日:2014-11-14
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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