公开(公告)号：WO2012000103A8

公开(公告)日：2012-01-05

申请号：PCT/CA2011/000776

申请日：2011-07-04

Applicant: UNIVERSITY 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

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：WO2015054793A1

公开(公告)日：2015-04-23

申请号：PCT/CA2014/051001

申请日：2014-10-17

Applicant: UNIVERSITY 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，以及它们相应的药物组合物。 1：1富马酸化合物（I）和马来酸化合物（I）的特殊单晶形式的特征在于各种性能和物理测量。 还公开了制备1：1富马酸化合物（I）和1:1化合物（I）马来酸酯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：WO2014056083A1

公开(公告)日：2014-04-17

申请号：PCT/CA2013/000859

申请日：2013-10-11

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： LIU, Yong ,  LANG, Yunhui ,  NG, Grace ,  LI, Sze-Wan ,  PAULS, Heinz W. ,  LAUFER, Radoslaw ,  PATEL, Narendra Kumar B. ,  SAMPSON, Peter Brent ,  FEHER, Miklos ,  AWREY, Donald E.

IPC: C07D451/06 ,  A61K31/416 ,  A61K31/4439 ,  A61P35/00 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D498/08

CPC classification number: C07D498/08 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D451/06

Abstract: The invention is a compound represented by Structural Formula (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).

Abstract translation: 本发明是由结构式（I）表示的化合物或其药学上可接受的盐。 这里提供了变量的值。 还包括药物组合物，其包含由结构式（I）表示的化合物和药学上可接受的载体或稀释剂以及用结构式（I）的化合物治疗患有癌症的受试者的方法。

公开(公告)号：WO2011123937A1

公开(公告)日：2011-10-13

申请号：PCT/CA2011/000366

申请日：2011-04-06

Applicant: UNIVERSITY HEALTH NETWORK ,  LAUFER, Radoslaw ,  PAULS, Heinz W. ,  FEHER, Miklos ,  NG, Grace ,  LIU, Yong ,  EDWARDS, Louise G. ,  PATEL, Narendra Kumar B. ,  PAN, Guohua ,  MAK, Tak W.

Inventor： LAUFER, Radoslaw ,  PAULS, Heinz W. ,  FEHER, Miklos ,  NG, Grace ,  LIU, Yong ,  EDWARDS, Louise G. ,  PATEL, Narendra Kumar B. ,  PAN, Guohua ,  MAK, Tak W.

IPC: C07D231/56 ,  A61K31/416 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

CPC classification number: C07D231/56 ,  A61K31/00 ,  A61K31/517 ,  A61K31/522 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present teachings provide a compound represented by Strutural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.

Abstract translation: 本发明提供由式（I）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：WO2014075168A1

公开(公告)日：2014-05-22

申请号：PCT/CA2013/000957

申请日：2013-11-15

Applicant: UNIVERSITY 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：WO2011123946A1

公开(公告)日：2011-10-13

申请号：PCT/CA2011/000386

申请日：2011-04-06

Applicant: UNIVERSITY 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 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：WO2010115279A1

公开(公告)日：2010-10-14

申请号：PCT/CA2010/000518

申请日：2010-04-06

Applicant: UNIVERSITY HEALTH NETWORK ,  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

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 ,  C07D409/14 ,  C07D413/14

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

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.

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：由该结构式表示的化合物是激酶抑制剂，因此本文公开了用于治疗癌症的化合物。 本文提供了结构式中变量的定义。

公开(公告)号：WO2009079767A9

公开(公告)日：2009-07-02

申请号：PCT/CA2008/002227

申请日：2008-12-19

Applicant: UNIVERSITY HEALTH NETWORK ,  PAULS, Heinz, W. ,  FORREST, Bryan, T. ,  LAUFER, Radoslaw ,  FEHER, Miklos ,  SAMPSON, Peter, Brent ,  PAN, Guohua

Inventor： PAULS, Heinz, W. ,  FORREST, Bryan, T. ,  LAUFER, Radoslaw ,  FEHER, Miklos ,  SAMPSON, Peter, Brent ,  PAN, Guohua

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.

公开(公告)号：WO2013053051A1

公开(公告)日：2013-04-18

申请号：PCT/CA2012/000955

申请日：2012-10-12

Applicant: UNIVERSITY 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

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 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.

Abstract translation: 本教导提供由结构式（I）或（I'）表示的吲唑化合物或其药学上可接受的盐。 还描述了作为蛋白激酶抑制剂的药物组合物及其使用方法，例如对乳腺癌细胞，结肠癌细胞和卵巢癌细胞具有抗癌活性的TTK蛋白激酶，polo样激酶4（PLK4）和Aurora激酶。

公开(公告)号：WO2009079767A1

公开(公告)日：2009-07-02

申请号：PCT/CA2008/002227

申请日：2008-12-19

Applicant: UNIVERSITY HEALTH NETWORK ,  PAULS, Heinz, W. ,  FORREST, Bryan, T. ,  LAUFER, Radoslaw ,  FEHER, Miklos ,  SAMPSON, Peter, Brent ,  PAN, Guohua

Inventor： PAULS, Heinz, W. ,  FORREST, Bryan, T. ,  LAUFER, Radoslaw ,  FEHER, Miklos ,  SAMPSON, Peter, Brent ,  PAN, Guohua

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

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.

Abstract translation: 本发明涉及由结构式（A）表示的化合物或其药学上可接受的盐。 本发明还涉及包含由上述结构式（A）表示的化合物或其药学上可接受的盐和药学上可接受的载体或稀释剂的药物组合物。 还公开了治疗患有癌症的受试者的方法，其中所述方法包括施用治疗有效量的由上述结构式（A）表示的化合物或其药学上可接受的盐。