IP Library Granted Patent US 10,045,977
Granted Patent B2
US 10,045,977 · App. 15/492,198 · Granted Aug 14, 2018

Use of nalmefene in non-alcoholic steatohepatitis

Inventors: Edwin S C Wu (Research Triangle Park, NC); Peter J. S. Chiu (Mill Creek, WA); May Mei-chi Hsu (Zhubei, TW)
Assignee: TAIWANJ PHARMACEUTICALS CO., LTD.
A61K31/485A61K9/0053
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Quick Facts
Patent No.
US 10,045,977
App. No.
15/492,198
Granted
Aug 14, 2018
Kind
B2
Abstract

The present invention relates to new medical uses of morphinans such as nalmefene and naltrexone and their related derivatives, pharmaceutical formulations thereof, and use thereof for prevention and treatment of NASH, NAFLD, and/or ASH.

Claims (30)

1. A method of treating, NASH, which comprises administering to a human or animal in need thereof a therapeutic amount of a compound of the formula (I), wherein:

A is OH or OCH3, R is H, CH3, or cyclopropylmethyl;

X is the oxygen atom, Y is CH2 or oxygen, Z is H or OH, said compounds being administered as a racemic mixture or as enantiomers, diastereoisomers, or pharmaceutically acceptable salts.

2. The method of claim 1 , wherein the compound of Formula (I) has one of the following structures:

3. The method of claim 1 , wherein the compound of Formula (I) has one of the following structures:

4. A method as claimed in claim 1 , wherein said compound is Compound A (nalmefene).

5. A method as claimed in claim 1 , wherein said compound is Compound B (naltrexone).

6. A method of treating NAFLD, which comprises administering to a human or animal in need thereof a therapeutic amount of a compound of the formula (I), wherein:

A is OH or OCH3, R is H, CH3, or cyclopropylmethy;

X is the oxygen atom, Y is CH2 or oxygen, Z is H or OH, said compounds being administered as a racemic mixture or as enantiomers, diastereoisomers, or pharmaceutically acceptable salts.

7. A method of treating-ASH, which comprises administering to a human or animal in need thereof a therapeutic amount of a compound of the formula (I), wherein:

A is OH or OCH3, R is H, CH3, or cyclopropylmethyl;

X is the oxygen atom, Y is CH2 or oxygen, Z is H or OH, said compounds being administered as a racemic mixture or as enantiomers, diastereoisomers, or pharmaceutically acceptable salts.

8. The method of claim 1 , wherein the compound is administered orally.

9. The method of claim 1 , wherein the compound is administered parenterally.

10. A method as claimed in claim 1 wherein said compound is administered in a daily dose of from 1 mg to 100 mg.

11. The method of claim 6 , wherein the compound of Formula (I) has one of the following structures:

12. The method of claim 6 , wherein the compound of Formula (I) has one of the following structures:

13. A method as claimed in claim 6 , wherein said compound is Compound A (nalmefene).

14. A method as claimed in claim 6 , wherein said compound is Compound B (naltrexone).

15. The method of claim 6 , wherein the compound is administered orally.

16. The method of claim 6 , wherein the compound is administered parenterally.

17. A method as claimed in claim 6 wherein said compound is administered in a daily dose of from 1 mg to 100 mg.

18. The method of claim 7 , wherein the compound of Formula (I) has one of the following structures:

19. The method of claim 7 , wherein the compound of Formula (I) has one of the following structures:

20. A method as claimed in claim 7 , wherein said compound is Compound A (nalmefene).

21. A method as claimed in claim 7 , wherein said compound is Compound B (naltrexone).

22. The method of claim 7 , wherein the compound is administered orally.

23. The method of claim 7 , wherein the compound is administered parenterally.

24. A method as claimed in claim 7 wherein said compound is administered in a daily dose of from 1 mg to 100 mg.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 5, 2017
From: WU, EDWIN SC; CHIU, PETER J.S.; HSU, MAY MEI-CHI
To: TAIWANJ PHARMACEUTICALS CO., LTD.
Reel/Frame 043785/0609 →
Continuity (3)
Provisional Application 62326435 · Apr 22, 2016
Provisional Application 62395436 · Sep 16, 2016
Related Publication 20170304294A1 · Oct 26, 2017
Cited By (11)
US 12,241,090 US 12,258,584 US 12,281,334 US 12,297,457 US 12,379,372 US 12,414,967 US 12,421,500 US 12,428,622 US 12,497,597 US 12,534,709 US 12,600,943