公开(公告)号：US20190040074A1

公开(公告)日：2019-02-07

申请号：US16155846

申请日：2018-10-09

Applicant: University Health Network

Inventor： Yong Liu ,  Heinz W. Pauls ,  Radoslaw Laufer ,  Sze-Wan Li ,  Peter Brent Sampson ,  Miklos Feher ,  Grace Ng ,  Narendra Kumar B. Patel ,  Yunhui Lang

IPC: C07D487/04 ,  C07D519/00

Abstract: The present teachings provide a compound represented by structural formula (I-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.

公开(公告)号：US10392374B2

公开(公告)日：2019-08-27

申请号：US15886104

申请日：2018-02-01

Applicant: University Health Network

Inventor： Peter Brent Sampson ,  Miklos Feher ,  Heinz W. Pauls

IPC: 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.

公开(公告)号：US09573954B2

公开(公告)日：2017-02-21

申请号：US14443072

申请日：2013-11-15

Applicant: University Health Network

Inventor： Yong Liu ,  Heinz W. Pauls ,  Radoslaw Laufer ,  Sze-Wan Li ,  Peter Brent Sampson ,  Miklos Feher ,  Grace Ng ,  Narendra Kumar B. Patel ,  Yunhui Lang

IPC: C07D487/04 ,  C07D519/00

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：US09402828B2

公开(公告)日：2016-08-02

申请号：US14592968

申请日：2015-01-09

Applicant: University Health Network

Inventor： Guohua Pan ,  Jacqueline M. Mason ,  Xin Wei ,  Miklos Feher

IPC: A61K31/553 ,  A61K31/00 ,  A61K31/535 ,  C07D273/00 ,  C07D211/00 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377

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

Abstract: Provided herein are methods and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation and/or a PI3K gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist.

Abstract translation: 本文提供了用于治疗癌症患者的方法和组合物，其中癌症的特征在于PTEN基因突变和/或PI3K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。

公开(公告)号：US20150299203A1

公开(公告)日：2015-10-22

申请号：US14443072

申请日：2013-11-15

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Yong Liu ,  Heinz W. Pauls ,  Radoslaw Laufer ,  Sze-Wan Li ,  Peter Brent Sampson ,  Miklos Feher ,  Grace Ng ,  Narendra Kumar B. Patel ,  Yunhui Lang

IPC: C07D487/04 ,  C07D519/00

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：US08999968B2

公开(公告)日：2015-04-07

申请号：US13935016

申请日：2013-07-03

Applicant: University Health Network

Inventor： Peter Brent Sampson ,  Yong Liu ,  Sze-Wan Li ,  Bryan T. Forrest ,  Heinz W. Pauls ,  Louise G. Edwards ,  Miklos Feher ,  Narendra Kumar B. Patel ,  Guohua Pan

IPC: A61K31/551 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4427 ,  A61K31/416 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  A61K31/437 ,  A61K45/06 ,  C07D471/10

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：US20140371202A1

公开(公告)日：2014-12-18

申请号：US14351381

申请日：2012-10-12

Applicant: University Health Network

Inventor： Heinz W. Pauls ,  Radoslaw Laufer ,  Yong Liu ,  Sze-Wan Li ,  Bryan T. Forrest ,  Yunhui Lang ,  Narendra Kumar B. Patel ,  Louise G. Edwards ,  Grace Ng ,  Peter Brent Sampson ,  Miklos Feher ,  Donald E. Awrey

IPC: C07D231/56 ,  C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D409/12 ,  C07D409/14

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：US20140045838A1

公开(公告)日：2014-02-13

申请号：US13935021

申请日：2013-07-03

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Peter Brent Sampson ,  Yong Liu ,  Sze-Wan Li ,  Bryan T. Forrest ,  Heinz W. Pauls ,  Louise G. Edwards ,  Miklos Feher ,  Narendra Kumar B. Patel ,  Radoslaw Laufer ,  Guohua Pan

IPC: C07D403/04 ,  A61K45/06 ,  C07D413/14 ,  A61K31/5377

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.

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：US20140045822A1

公开(公告)日：2014-02-13

申请号：US13935016

申请日：2013-07-03

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Peter Brent Sampson ,  Yong Liu ,  Sze-Wan Li ,  Bryan T. Forrest ,  Heinz W. Pauls ,  Louise G. Edwards ,  Miklos Feher ,  Narendra Kumar B. Patel ,  Guohua Pan

IPC: A61K31/553 ,  C07D403/04 ,  A61K31/437 ,  C07D471/10 ,  A61K45/06 ,  C07D401/14 ,  A61K31/5377 ,  C07D409/14 ,  C07D471/04 ,  A61K31/416 ,  A61K31/496

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：US20210269428A1

公开(公告)日：2021-09-02

申请号：US17172511

申请日：2021-02-10

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Peter Brent Sampson ,  Miklos Feher ,  Heinz W. Pauls

IPC: 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.