公开(公告)号：US20220002313A1

公开(公告)日：2022-01-06

申请号：US17372717

申请日：2021-07-12

Applicant: UNIVERSITY HEALTH NETWORK

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

IPC: C07D495/04 ,  A61K31/496 ,  A61K39/395 ,  C07K16/28 ,  A61K31/4355 ,  A61K31/5355 ,  A61K31/551 ,  A61P35/00 ,  A61K31/5377 ,  A61K45/06

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).

公开(公告)号：US10106545B2

公开(公告)日：2018-10-23

申请号：US15434275

申请日：2017-02-16

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

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：US11059832B2

公开(公告)日：2021-07-13

申请号：US16705458

申请日：2019-12-06

Applicant: University Health Network

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

IPC: C07D495/04 ,  A61K31/496 ,  A61K39/395 ,  C07K16/28 ,  A61K31/4355 ,  A61K31/5355 ,  A61K31/551 ,  A61P35/00 ,  A61K31/5377 ,  A61K45/06 ,  A61K39/00

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 checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).

公开(公告)号：US10570143B2

公开(公告)日：2020-02-25

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 (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.

公开(公告)号：US20180179221A1

公开(公告)日：2018-06-28

申请号：US15738286

申请日：2016-06-23

Applicant: University Health Network

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

IPC: C07D495/04 ,  A61K45/06 ,  A61P35/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551

CPC classification number: C07D495/04 ,  A61K31/4355 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/551 ,  A61K39/395 ,  A61K45/06 ,  A61K2039/505 ,  A61P35/00 ,  C07K16/2818 ,  A61K2300/00

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 checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).

公开(公告)号：US20170217966A1

公开(公告)日：2017-08-03

申请号：US15434275

申请日：2017-02-16

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

CPC classification number: 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：US09580390B2

公开(公告)日：2017-02-28

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 ,  C07D413/14 ,  C07D409/12 ,  C07D409/14 ,  C07D405/14 ,  C07D451/06 ,  C07D491/107 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D413/04 ,  C07D413/10 ,  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 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: 本发明提供由结构式（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：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：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：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。