公开(公告)号：WO2011123946A8

公开(公告)日：2011-12-08

申请号：PCT/CA2011000386

申请日：2011-04-06

Applicant: UNIV HEALTH NETWORK ,  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

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

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: (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.

Abstract translation: 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐：（I）。 由该结构式表示的化合物是激酶抑制剂，因此在此公开用于治疗癌症。 本文提供了结构式中变量的定义。

公开(公告)号：WO2012000103A1

公开(公告)日：2012-01-05

申请号：PCT/CA2011000776

申请日：2011-07-04

Applicant: UNIV HEALTH NETWORK ,  PAN GUOHUA ,  MASON JACQUELINE M ,  WEI XIN ,  FEHER MIKLOS

Inventor： PAN GUOHUA ,  MASON JACQUELINE M ,  WEI XIN ,  FEHER MIKLOS

IPC: A61K31/496 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4439 ,  A61P35/00

CPC classification number: A61K31/416 ,  A61K31/4439 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377

Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation, hi particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.

Abstract translation: 本文提供用于治疗癌症患者的方法，用途和组合物，其中癌症的特征在于PTEN基因突变。在具体实施方案中，所述方法包括向患者施用包含治疗有效量的PLK4拮抗剂的组合物，以及鉴定 如果存在PTEN基因突变，则可能对PLK4拮抗剂治疗有反应的患者。

公开(公告)号：WO2008109991A8

公开(公告)日：2008-12-18

申请号：PCT/CA2008000440

申请日：2008-03-06

Applicant: UNIV HEALTH NETWORK ,  PAULS HEINZ W ,  SAMPSON PETER BRENT ,  FORREST BRYAN T ,  LAUFER RADOSLAW ,  LIU YONG ,  FEHER MIKLOS ,  YAO YI ,  PAN GUOHUA

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

CPC classification number: C07D409/06 ,  C07C1/26 ,  C07C17/10 ,  C07C2529/40 ,  C07D207/325 ,  C07D213/71 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D263/34 ,  C07D277/48 ,  C07D295/215 ,  C07D307/24 ,  C07D307/68 ,  C07D307/82 ,  C07D333/34 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07C9/00 ,  C07C19/075

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.

Abstract translation: CPT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。

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.

公开(公告)号：EP2556071A4

公开(公告)日：2013-09-04

申请号：EP11764988

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

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.

公开(公告)号：EP3057965A4

公开(公告)日：2017-05-24

申请号：EP14854037

申请日：2014-10-17

Applicant: UNIV HEALTH NETWORK

Inventor： SAMPSON PETER BRENT ,  FEHER MIKLOS ,  PAULS HEINZ W

IPC: C07D413/14 ,  A61K31/5377 ,  A61P35/00

CPC classification number: C07D413/14

Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer. Compound (I)

Abstract translation: 公开了由以下结构式表示的化合物（I）的富马酸盐和马来酸盐及其相应的药物组合物。 1：1化合物（I）延胡索酸盐和1：1化合物（I）马来酸盐的特定单晶形式的特征在于各种性质和物理测量。 还公开了制备1：1化合物（I）富马酸盐和1：1化合物（I）马来酸盐的特定结晶形式的方法。 本发明还提供了治疗患有癌症的受试者的方法。 化合物（I）

公开(公告)号：EP2588110A4

公开(公告)日：2014-04-16

申请号：EP11800027

申请日：2011-07-04

Applicant: UNIV HEALTH NETWORK

Inventor： PAN GUOHUA ,  MASON JACQUELINE M ,  WEI XIN ,  FEHER MIKLOS

IPC: A61K31/496 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4439 ,  A61P35/00

CPC classification number: A61K31/416 ,  A61K31/4439 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377

Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.

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。

公开(公告)号：EP2417127A4

公开(公告)日：2012-08-29

申请号：EP10761154

申请日：2010-04-06

Applicant: UNIV 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 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/14

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：EP2235004A4

公开(公告)日：2011-05-04

申请号：EP08865534

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 ,  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