公开(公告)号：US09657025B2

公开(公告)日：2017-05-23

申请号：US14926977

申请日：2015-10-29

Applicant: University Health Network

Inventor： Radoslaw Laufer ,  Grace Ng ,  Sze-Wan Li ,  Heinz W. Pauls ,  Yong Liu ,  Narendra Kumar B. Patel

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

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

公开(公告)号：US09139563B2

公开(公告)日：2015-09-22

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

IPC: A61K31/5377 ,  C07D403/04 ,  C07D413/14 ,  C07D231/56 ,  C07D403/10 ,  C07D403/14 ,  A61K45/06

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：US20220089601A1

公开(公告)日：2022-03-24

申请号：US17459725

申请日：2021-08-27

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Sze-Wan Li ,  Heinz W. Pauls ,  Peter Brent Sampson

IPC: C07D487/04 ,  A61P35/00 ,  C30B29/58 ,  C30B7/14 ,  C30B7/02 ,  A61K31/519

Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is bisphosphate hemihydrate, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the treatment of cancer and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of such a co-crystal.

公开(公告)号：US11104681B2

公开(公告)日：2021-08-31

申请号：US16806392

申请日：2020-03-02

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： Sze-Wan Li ,  Heinz W. Pauls ,  Peter Brent Sampson

IPC: A61K31/519 ,  A61P35/00 ,  C07D487/04 ,  C30B29/58 ,  C30B7/14 ,  C30B7/02

Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is bisphosphate hemihydrate, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the treatment of cancer and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of such a co-crystal.

公开(公告)号：US20190322669A1

公开(公告)日：2019-10-24

申请号：US16225970

申请日：2018-12-19

Applicant: University Health Network

Inventor： Radoslaw Laufer ,  Grace Ng ,  Sze-Wan Li ,  Heinz W. Pauls ,  Yong Liu ,  Narendra Kumar B. Patel

IPC: C07D487/04 ,  C07D519/00

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

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：US10167289B2

公开(公告)日：2019-01-01

申请号：US15598402

申请日：2017-05-18

Applicant: University Health Network

Inventor： Radoslaw Laufer ,  Grace Ng ,  Sze-Wan Li ,  Heinz W. Pauls ,  Yong Liu ,  Narendra Kumar B. Patel

IPC: C07D487/04 ,  C07D519/00

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

公开(公告)号：US20180282335A1

公开(公告)日：2018-10-04

申请号：US15521895

申请日：2015-10-09

Applicant: University Health Network

Inventor： Radoslaw Laufer ,  Grace Ng ,  Richard Brokx ,  Heinz W. Pauls ,  Sze-wan Li ,  Jacqueline M. Mason ,  Mark R. Bray

IPC: C07D487/04 ,  A61P35/00 ,  A61P29/00 ,  A61P37/06

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  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).

公开(公告)号：US20180105511A1

公开(公告)日：2018-04-19

申请号：US15790847

申请日：2017-10-23

Applicant: University Health Network

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

IPC: C07D403/10 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D403/10 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/56 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14

Abstract: The present invention is directed to novel synthetic methods for preparing cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.

公开(公告)号：US09796703B2

公开(公告)日：2017-10-24

申请号：US15440548

申请日：2017-02-23

Applicant: University Health Network

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

IPC: C07D403/10 ,  C07D403/14 ,  C07D413/14

CPC classification number: C07D403/10 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/56 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14

Abstract: The present invention is directed to novel synthetic methods for preparing cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.