IP Library › Granted Patent US 11,071,738
Granted Patent B2
US 11,071,738 · App. 16/636,752 · Granted Jul 27, 2021

Therapeutic agent for fatty liver diseases and therapeutic agent for adiposity

Inventors: Tomoichiro Asano (Hiroshima, JP); Yusuke Nakatsu (Hiroshima, JP); Hisanaka Ito (Hachioji, JP); Takayoshi Okabe (Tokyo, JP)
Assignees: Hiroshima University; Tokyo University of Pharmacy & Life Sciences; The University of Tokyo
A61K31/5377A61K31/341A61K31/403A61K31/415A61K31/4184A61K31/4439A61P1/16A61P3/04A61K45/06
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Quick Facts
Patent No.
US 11,071,738
App. No.
16/636,752
Granted
Jul 27, 2021
Kind
B2
Abstract

The purpose of the invention is to develop a novel therapeutic agent for fatty liver diseases such as NASH or NAFLD. The invention provides a therapeutic or prophylactic agent for fatty liver diseases that comprises, as an active ingredient, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a therapeutic or prophylactic agent for adiposity that comprises, as an active ingredient, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.

Claims (33)

1. A therapeutic or prophylactic agent for the treatment or prevention of fatty liver disease, comprising a compound represented by the Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:

wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;

a ring A represents a benzene ring and forms a naphthyl group with adjacent benzene ring;

X represents —O—CO— group;

Y represents a single bond, —NH— group, —CH 2 —O— group, —CH 2 — group, or —CH(NH—Boc)—CH 2 — group;

Z represents a hydrogen atom;

R 1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;

R 2 represents an optionally substituted aryl group, an optionally substituted heterocyclic group, an optionally substituted cycloalkyl group, or a group represented by the following Formula (II):

wherein rings B and C independently represent an optionally substituted aryl group, an optionally substituted heterocyclic group, or an optionally substituted cycloalkyl group, and R 7 represents a single bond, —O— group, —CO— group, —NH— group, —SO 2 — group, —CO—NH— group, an optionally substituted C 1-3 alkylene group, an optionally substituted C 2-3 alkenylene group, —S—R 8 — group wherein R 8 represents an optionally substituted C 1-2 alkylene group, —CO—R 8 — group, —O—R 8 — group, or —SO 2 —R 8 —group, and Y is attached to any of the ring B, ring C, and R 7 ; and

R 3 represents 0 to 4 identical or different substituents.

2. The therapeutic or prophylactic agent according to claim 1 , wherein the fatty liver disease is non-alcoholic steatohepatitis.

3. The therapeutic or prophylactic agent according to claim 1 , wherein m is 1 and n is 0.

4. The therapeutic or prophylactic agent according to claim 1 , wherein R 2 represents an optionally substituted polycyclic aryl group or an optionally substituted polycyclic heterocyclic group.

5. The therapeutic or prophylactic agent according to claim 1 , wherein Y represents a single bond, —CH 2 — group, or —CH 2 —O— group.

6. The therapeutic or prophylactic agent according to claim 1 , wherein R 1 represents a hydrogen atom.

7. The therapeutic or prophylactic agent according to claim 1 , further comprising an active ingredient of at least one additional drug for the treatment or prevention of fatty liver disease.

8. A method of treating or preventing fatty liver disease, comprising administering the therapeutic or prophylactic agent according to claim 1 , in combination with at least one additional drug for the treatment or prevention of fatty liver disease.

9. A therapeutic or prophylactic agent for the treatment or prevention of obesity, comprising a compound represented by the Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:

wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;

a ring A represents a benzene ring and forms a naphthyl group with adjacent benzene ring;

X represents —O—CO— group;

Y represents a single bond, —NH— group, CH 2 —O— group, —CH 2 — group, or —CH(NH—Boc)—CH 2 — group;

Z represents a hydrogen atom;

R 1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;

R 2 represents an optionally substituted aryl group, an optionally substituted heterocyclic group, an optionally substituted cycloalkyl group, or a group represented by the following Formula (II):

wherein rings B and C independently represent an optionally substituted aryl group, an optionally substituted heterocyclic group, or an optionally substituted cycloalkyl group, and R 7 represents a single bond, —O— group, —CO— group, —NH— group, —SO 2 — group, —CO—NH— group, an optionally substituted C 1-3 alkylene group, an optionally substituted C 2-3 alkenylene group, —S—R 8 — group wherein R 8 represents an optionally substituted C 1-2 alkylene group, —CO—R 8 — group, —O—R 8 — group, or —SO 2 —R 8 — group, and Y is attached to any of the ring B, ring C, and R 7 ; and

R 3 represents 0 to 4 identical or different substituents.

10. The therapeutic or prophylactic agent according to claim 9 , wherein m is 1 and n is 0.

11. The therapeutic or prophylactic agent according to claim 9 , wherein R 2 represents an optionally substituted polycyclic aryl group or an optionally substituted polycyclic heterocyclic group.

12. The therapeutic or prophylactic agent according to claim 9 , wherein Y represents a single bond, —CH 2 — group, or —CH 2 —O— group.

13. The therapeutic or prophylactic agent according to claim 9 , wherein R 1 represents a hydrogen atom.

14. The therapeutic or prophylactic agent according to claim 9 , further comprising an active ingredient of at least one additional drug for the treatment or prevention of obesity.

15. A method of treating or preventing obesity, comprising administering the therapeutic or prophylactic agent according to claim 9 in combination with at least one additional drug for the treatment or prevention of obesity.

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 053242/0932 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2020
From: ITO, HISANAKA
To: TOKYO UNIVERSITY OF PHARMACY & LIFE SCIENCES
Reel/Frame 053242/0965 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2020
From: OKABE, TAKAYOSHI
To: THE UNIVERSITY OF TOKYO
Reel/Frame 053243/0009 →
Priority Claims (1)
JP JP2017-152807 · Aug 7, 2017 · national
Continuity (1)
Related Publication 20200383989A1 · Dec 10, 2020