IP Library › Granted Patent US 12,419,874
Granted Patent B2
US 12,419,874 · App. 19/054,180 · Granted Sep 23, 2025

GLP-1R agonist compound and use thereof

Inventors: Wei Nie (Chongqing, CN); Xiaolong Kerri Yan (Chongqing, CN); Haoying Xu (Chongqing, CN); Qiang Liu (Chongqing, CN); Zhichao Xu (Chongqing, CN); Hongkun Qin (Chongqing, CN); Xiang Li (Chongqing, CN); Hongyi Liu (Chongqing, CN); Yaming Cao (Chongqing, CN); Xiaoqing Bai (Chongqing, CN)
Assignees: Chongqing Pharmaceutical Research Institute Co., Ltd.; Yaopharma Co., Ltd.
A61K31/437C07D471/10
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Quick Facts
Patent No.
US 12,419,874
App. No.
19/054,180
Granted
Sep 23, 2025
Kind
B2
Abstract

The present disclosure relates to a GLP-1R agonist compound and use thereof, and specifically provides a compound represented by Formula I, or an isotope-labelled compound, a stereoisomer, or a pharmaceutically acceptable salt thereof, and use thereof as a medicament. The compound exhibits excellent agonistic effects and pharmacodynamic properties on GLP-1R and, as a modulator, is useful for manufacturing a medicament for the treatment, amelioration, or prevention of metabolic diseases and related diseases, thus having broad application prospects.

Claims (29)

1. A compound, wherein the compound is selected from the group consisting of:

or an isotopic compound or stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

5. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

6. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

7. The compound according to claim 1 , wherein the compound is:

or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition, comprising the compound of claim 1 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

9. A pharmaceutical composition, comprising the compound of claim 3 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

10. A pharmaceutical composition, comprising the compound of claim 4 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

11. A pharmaceutical composition, comprising the compound of claim 5 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

12. A pharmaceutical composition, comprising the compound of claim 6 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

13. A pharmaceutical composition, comprising the compound of claim 7 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

14. A method for treating disease or condition in a subject in need thereof, the method comprising: administering to the subject an effective amount of the compound of claim 1 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, wherein the disease or condition is diabetes or obesity.

15. A compound having the structure of:

or an isotopic compound or stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition, comprising the compound of claim 15 or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

17. A method for treating disease or condition in a subject in need thereof, the method comprising: administering to the subject an effective amount of the compound of claim 15 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, wherein the disease or condition is diabetes or obesity.

18. A compound having the structure of:

or an isotopic compound or stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

19. A pharmaceutical composition, comprising the compound of claim 18 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

20. A method for treating disease or condition in a subject in need thereof, the method comprising: administering to the subject an effective amount of the compound of claim 18 , or the isotopic compound or stereoisomer thereof, or the pharmaceutically acceptable salt thereof, wherein the disease or condition is diabetes or obesity.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 20, 2026
From: CHONGQING PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.; YAOPHARMA CO. LTD.
To: YAOPHARMA CO. LTD.
Reel/Frame 075323/0347 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 14, 2025
From: NIE, WEI; YAN, XIAOLONG KERRI; XU, HAOYING; LIU, QIANG; XU, ZHICHAO; QIN, HONGKUN; LI, XIANG; LIU, HONGYI; CAO, YAMING; BAI, XIAOQING
To: CHONGQING PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.; YAOPHARMA CO., LTD.
Reel/Frame 070223/0470 →
Continuity (2)
Continuation PCTCN2024105741 · Jul 16, 2024
Related Publication 20250195481A1 · Jun 19, 2025
References Cited (28)
US 10858356B2 · Yoshino · 2020 [cited by applicant]
US 12234236B1 · Liang · 2025 [cited by applicant]
US 12291530B1 · Liang · 2025 [cited by applicant]
CN 116003403A · 2023 [cited by applicant]
CN 117069743A · 2023 [cited by applicant]
CN 119306743A · 2025 [cited by applicant]
CN 119431365A · 2025 [cited by applicant]
CN 119528907A · 2025 [cited by applicant]
JP 2019099571A · 2019 [cited by applicant]
WO 2018056453A1 · 2018 [cited by applicant]
WO 2021155841A1 · 2021 [cited by applicant]
WO 2022017338A1 · 2022 [cited by applicant]
WO 2022048665A1 · 2022 [cited by applicant]
WO 2022052958A1 · 2022 [cited by applicant]
WO 2023016546A1 · 2023 [cited by applicant]
WO 2023169456A1 · 2023 [cited by applicant]
WO 2024153070A1 · 2024 [cited by applicant]
WO 2024169952A1 · 2024 [cited by applicant]
WO 2025002250A1 · 2025 [cited by applicant]
WO 2025002326A1 · 2025 [cited by applicant]
WO 2025006921A1 · 2025 [cited by applicant]
WO 2025011664A1 · 2025 [cited by applicant]
WO 2025026436A1 · 2025 [cited by applicant]
WO 2025045208A1 · 2025 [cited by applicant]
WO 2025057134A2 · 2025 [cited by applicant]
WO 2025026270A1 · 2025 [cited by applicant]
Kawai T, Sun B, Yoshino H, et al. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proc Natl Acad Sci U S A. 2020; 117(47):29959-29967. [cited by applicant]
International Search Report issued Sep. 19, 2024 in PCT/CN2024/105741. [cited by applicant]