IP Library › Granted Patent US 12,357,626
Granted Patent B2
US 12,357,626 · App. 16/636,758 · Granted Jul 15, 2025

Anthranilic acid-based compound, and Pin1 inhibitor, therapeutic agent for inflammatory diseases and therapeutic agent for cancer that use the same

Inventors: Tomoichiro Asano (Hiroshima, JP); Yusuke Nakatsu (Hiroshima, JP); Hisanaka Ito (Hachioji, JP); Takayoshi Okabe (Tokyo, JP)
Assignee: Amenis Bioscience, Inc.
A61K31/47A61K31/24A61P1/16A61P35/00C07C233/81C07C311/21C07D215/48
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Quick Facts
Patent No.
US 12,357,626
App. No.
16/636,758
Granted
Jul 15, 2025
Kind
B2
Abstract

The purpose of the invention is to develop, as drug-candidate compounds, a group of novel compounds having the activity of inhibiting functions of Pin1. The invention provides: a compound represented by formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for cancer, and a therapeutic or prophylactic agent for adiposity that use said compound/salt.

Claims (28)

1. A compound represented by the Formula (I), or a salt thereof:

wherein at least one of the R 1 or R 2 represents an optionally substituted naphthyl group, an optionally substituted quinolyl group, or an optionally substituted phenoxy phenyl group;

either R 1 or R 2 represents, if not any of the above-described groups, an optionally substituted aryl group, or an optionally substituted monocyclic heterocyclic group;

R 3 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and

X represents a single bond, —CO— group, —CO—O—CH 2 — group, —CO—CH 2 —O— group, —SO 2 — group, —CH 2 —CO—NH— group, —CH 2 —CO— group, or —CH 2 — group.

2. The compound or a salt thereof according to claim 1 , wherein at least one of R 1 or R 2 represents an optionally substituted naphthyl group.

3. The compound or a salt thereof according to claim 2 , wherein R 1 represents an optionally substituted naphthyl group.

4. The compound or a salt thereof according to claim 1 , wherein R 3 represents a hydrogen atom or a methyl group.

5. A Pin1 inhibitor comprising the compound or a salt thereof according to claim 1 .

6. A pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof according to claim 1 and a pharmaceutically acceptable carrier.

7. A therapeutic or prophylactic agent for the treatment or prevention of an inflammatory disease associated with fibrosis, comprising the compound or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.

8. The therapeutic or prophylactic agent according to claim 7 , wherein the inflammatory disease associated with fibrosis is non-alcoholic steatohepatitis, inflammatory bowel disease, or pulmonary fibrosis.

9. The therapeutic or prophylactic agent according to claim 7 , further comprising an active ingredient of at least one additional drug for the treatment or prevention of the inflammatory disease associated with fibrosis.

10. A method of treating or preventing an inflammatory disease associated with fibrosis, comprising administering the therapeutic or prophylactic agent according to claim 7 , in combination with at least one additional drug for the treatment or prevention of the inflammatory disease associated with fibrosis.

11. A therapeutic or prophylactic agent for the treatment or prevention of cancer, comprising the compound or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.

12. The therapeutic or prophylactic agent according to claim 11 , wherein the cancer is colon cancer or prostate cancer.

13. The therapeutic or prophylactic agent according to claim 11 , further comprising an active ingredient of at least one additional drug for the treatment or prevention of cancer.

14. A method of treating or preventing cancer, comprising administering the therapeutic or prophylactic agent according to claim 11 , in combination with at least one additional drug for the treatment or prevention of cancer.

15. A method of preparing a medicament for the treatment or prevention of cancer, comprising combining a pharmaceutically acceptable carrier and a therapeutic or prophylactic amount of the compound or a pharmaceutically acceptable salt thereof according to claim 1 .

16. A method of treating or preventing cancer, comprising administering the compound or a pharmaceutically acceptable salt thereof according to claim 1 to a patient in need thereof.

17. A therapeutic or prophylactic agent for the treatment or prevention of obesity, comprising the compound or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.

18. A therapeutic or prophylactic agent according to claim 17 , further comprising an active ingredient of at least one additional drug for the treatment or prevention of obesity.

19. A method of treating or preventing obesity, comprising administering the therapeutic or prophylactic agent according to claim 17 , in combination with at least one additional drug for the treatment or prevention of obesity.

20. A method of preparing a medicament for the treatment or prevention of obesity, comprising combining a pharmaceutically acceptable carrier and a therapeutic or prophylactic amount of the compound or a pharmaceutically acceptable salt thereof according to claim 1 .

21. A method of treating or preventing obesity, comprising administering the compound or a pharmaceutically acceptable salt thereof according claim 1 to a patient in need thereof.

22. A method of preparing a medicament for the treatment or prevention of an inflammatory disease associated with fibrosis, comprising combining a pharmaceutically acceptable carrier and a therapeutic or prophylactic amount of the compound or a pharmaceutically acceptable salt thereof according to claim 1 .

23. A method of treating or preventing an inflammatory disease associated with fibrosis, comprising administering the compound or a pharmaceutically acceptable salt thereof according to claim 1 to a patient in need thereof.

24. The compound or a salt thereof according to claim 2 , wherein R 2 represents an optionally substituted naphthyl group.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2024
From: HIROSHIMA UNIVERSITY; THE UNIVERSITY OF TOKYO; TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES
To: AMENIS BIOSCIENCE, INC.
Reel/Frame 066781/0504 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2020
From: ASANO, TOMOICHIRO; NAKATSU, YUSUKE
To: HIROSHIMA UNIVERSITY
Reel/Frame 053243/0062 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2020
From: ITO, HISANAKA
To: TOKYO UNIVERSITY OF PHARMACY & LIFE SCIENCES
Reel/Frame 053243/0111 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2020
From: OKABE, TAKAYOSHI
To: THE UNIVERSITY OF TOKYO
Reel/Frame 053243/0152 →
Priority Claims (1)
JP 2017-152808 · Aug 7, 2017 · national
Continuity (1)
Related Publication 20200383967A1 · Dec 10, 2020
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