IP Library Granted Patent US 12,617,811
Granted Patent B2
US 12,617,811 · App. 18/013,402 · Granted May 5, 2026

HPK1 inhibitors and uses thereof

Inventors: Wenge Zhong (Thousand Oaks, CA); Xiaotian Zhu (Newton, MA); Song Feng (Shanghai, CN); Lei Wu (Shanghai, CN); Wei Huang (Shanghai, CN); Hao Liu (San Diego, CA); Rongqiang Liu (Kendall Park, NJ); Kate Xin Wen (Shanghai, CN); Hua Zhou (Shanghai, CN)
Assignee: Regor Pharmaceuticals, Inc.
C07F9/6561A61K45/06A61P35/00C07D401/14C07D405/14C07D471/04C07D473/32C07D487/04C07D491/107C07D498/04C07D519/00C07F9/65583
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Quick Facts
Patent No.
US 12,617,811
App. No.
18/013,402
Filed
Dec 28, 2022
Granted
May 5, 2026
Kind
B2
Art Unit
1627
USPC
514/275
Abstract

The invention provides a compound represented by structural formula (I) or formula (II), or a pharmaceutically acceptable salt or a stereoisomer thereof useful for treating diseases (such as cancer) that are treatable by inhibiting HPK1 activity.

Claims (30)

1 . A compound represented by Formula I,

or a pharmaceutically acceptable salt, or a stereoisomer thereof.

2 . The compound of claim 1 , represented by Formula IA,

or a pharmaceutically acceptable salt.

3 . Ne compound of claim 1 , represented by Formula IB,

or a pharmaceutically acceptable salt.

4 . A compound represented by Formula IIA,

or a pharmaceutically acceptable salt.

5 . A compound represented by Formula IIB,

or a pharmaceutically acceptable salt.

6 . A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt or a stereoisomer thereof, and a pharmaceutically acceptable carrier.

7 . A combination comprising a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof, and one or more therapeutically active co-agents.

8 . A method for treating a subject with cancer, comprising administering to the subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, or a stereoisomer thereof.

9 . The method of claim 8 , wherein the cancer is selected from breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

10 . A method of inhibiting HPK1 activity in a subject in need thereof, said method comprising administering to the subject an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof.

11 . The method of claim 10 , wherein the subject has a cancer, and wherein the cancer is treated.

12 . The method of claim 11 , wherein the cancer is selected from breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

13 . A method for treating a subject with cancer, comprising administering to the subject a therapeutically effective amount of the compound of claim 1 in combination with an immune checkpoint inhibitor, wherein the immune checkpoint inhibitor is a PD-1 inhibitor, a PD-L1 inhibitor, or a CTLA-4 inhibitor.

14 . The method of claim 13 , wherein the immune checkpoint inhibitor is a bispecific monoclonal antibody or an antigen binding fragment thereof specific for PD-1 and PD-L1, or CTLA-4.

15 . The method of claim 14 , wherein the cancer is selected from breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

16 . A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 5 or a pharmaceutically acceptable salt or a stereoisomer thereof, and a pharmaceutically acceptable carrier.

17 . A combination comprising a therapeutically effective amount of the compound of claim 5 or a pharmaceutically acceptable salt or a stereoisomer thereof, and one or more therapeutically active co-agents.

18 . A method for treating a subject with cancer, comprising administering to the subject an effective amount of a compound of claim 5 , or a pharmaceutically acceptable salt, or a stereoisomer thereof.

19 . The method of claim 18 , wherein the cancer is selected from breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

20 . A method of inhibiting HPK1 activity in a subject in need thereof, said method comprising administering to the subject an effective amount of compound of claim 5 , or a pharmaceutically acceptable salt or a stereoisomer thereof.

21 . A method of claim 20 , wherein the subject has cancer, and wherein the cancer is treated.

22 . A method of claim 21 , wherein the cancer is selected from that of breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

23 . A method for treating a subject with cancer, comprising administering to the subject a therapeutically effective amount of the compound of claim 5 in combination with an immune checkpoint inhibitor, wherein the immune checkpoint inhibitor is a PD-1 inhibitor, a PD-L1 inhibitor, or a CTLA-4 inhibitor.

24 . The method of claim 23 , wherein the immune checkpoint inhibitor is a bispecific monoclonal antibody or an antigen binding fragment thereof specific for PD-1 and PD-L1, or CTLA-4.

25 . The method of claim 24 , wherein the cancer is selected from breast cancer, colorectal cancer, lung cancer, ovarian cancer, and pancreatic cancer.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 24, 2023
From: QILU REGOR THERAPEUTICS INC.
To: REGOR PHARMACEUTICALS, INC.
Reel/Frame 065322/0727 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 27, 2023
From: ZHONG, WENGE; ZHU, XIAOTIAN; FENG, SONG; WU, LEI; HUANG, WEI; LIU, HAO; LIU, RONGQIANG; WEN, KATE XIN; ZHOU, HUA
To: QILU REGOR THERAPEUTICS INC.
Reel/Frame 062514/0086 →
Priority Claims (1)
WO PCT/CN2020/100134 · Jul 3, 2020 · international
Continuity (1)
Related Publication 20230339896A1 · Oct 26, 2023
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