IP Library Granted Patent US 11,931,335
Granted Patent B2
US 11,931,335 · App. 16/983,367 · Granted Mar 19, 2024

Enhancing autophagy or increasing longevity by administration of urolithins or precursors thereof

Inventors: Christopher L. Rinsch (Morges, CH); William Blanco-Bose (La Croix, CH); Bernard Schneider (Pully, CH); Laurent Mouchiroud (Morges, CH); Dongryeol Ryu (Renens, CH); Penelope Andreux (Eclepens, CH); Johan Auwerx (Buchillon, CH)
Assignee: Amazentis SA
A61K31/37A61K31/00A61K31/366A61K31/7048A61K45/06C07D311/80
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Quick Facts
Patent No.
US 11,931,335
App. No.
16/983,367
Granted
Mar 19, 2024
Kind
B2
Abstract

Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.

Claims (45)

1. A method of improving or increasing autophagy, comprising conjointly administering to a healthy human in need thereof an effective amount of L-carnitine or a pharmaceutically acceptable salt thereof, and a urolithin represented by Formula I or a pharmaceutically acceptable salt thereof;

wherein:

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of H and OR; and

R is independently for each occurrence H, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

2. The method of claim 1 , wherein the urolithin is selected from the group consisting of urolithin A, urolithin B, urolithin C, urolithin D, and any combination thereof.

3. The method of claim 1 , wherein the urolithin is urolithin A.

4. The method of claim 1 , wherein the urolithin is urolithin B.

5. The method of claim 1 , wherein the autophagy is mitophagy.

6. The method of claim 1 , wherein the conjoint administration is oral.

7. The method of claim 1 , wherein the human is elderly.

8. The method of claim 1 , wherein said conjoint administration is sequential.

9. The method of claim 1 , wherein said conjoint administration is simultaneous.

10. A method of treating a disease selected from the group consisting of muscle degenerative disorder, sarcopenia, muscular dystrophy, cardiomyopathy, Ulrich myopathy, obesity, cardiovascular disease, atherosclerosis, a mitochondria-related disease associated with altered mitochondrial function or a reduced mitochondrial density; or disease related to a metabolic function, comprising:

conjointly administering to a vertebrate in need thereof an effective amount of L-carnitine or a pharmaceutically acceptable salt thereof, and a urolithin represented by Formula I or a pharmaceutically acceptable salt thereof;

wherein:

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of H and OR; and

R is independently for each occurrence H, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

11. A method of treating a condition selected from the group consisting of frailty, muscular atrophy, muscle disuse atrophy, skeletal muscle atrophy or impaired muscle strength associated with aging, and skeletal muscle damage, a mitochondria-related condition associated with altered mitochondrial function or a reduced mitochondrial density, and a condition related to a metabolic function, comprising:

conjointly administering to a vertebrate in need thereof an effective amount of L-carnitine or a pharmaceutically acceptable salt thereof, and a urolithin represented by Formula I or a pharmaceutically acceptable salt thereof;

wherein:

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of H and OR; and

R is independently for each occurrence H, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

12. The method of claim 10 , wherein the disease is sarcopenia, muscular dystrophy, cardiomyopathy, Ulrich myopathy, obesity, cardiovascular disease, or atherosclerosis.

13. The method of claim 12 , wherein the vertebrate is a human.

14. The method of claim 11 , wherein the condition is frailty, muscular atrophy, muscle disuse atrophy, or skeletal muscle atrophy.

15. The method of claim 14 , wherein the vertebrate is a human.

16. A method of protecting against muscle damage or injury; protecting or maintaining cardiac muscle; improving muscle function, muscle strength, muscle mass, muscle endurance, or muscle recovery following exercise; improving balance or coordination; improving mitochondrial function; or weight management, comprising:

conjointly administering to a healthy human an effective amount of L-carnitine or a pharmaceutically acceptable salt thereof, and a urolithin represented by Formula I or a pharmaceutically acceptable salt thereof;

wherein:

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of H and OR; and

R is independently for each occurrence H, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

17. The method of claim 16 , wherein the method protects against muscle damage or injury.

18. The method of claim 16 , wherein the method protects or maintains cardiac muscle.

19. The method of claim 16 , wherein the method improves muscle function, muscle strength, muscle mass, muscle endurance, or muscle recovery following exercise.

20. The method of claim 16 , wherein the method improves balance or coordination.

21. The method of claim 16 , wherein the method improves mitochondrial function.

22. The method of claim 16 , wherein the method manages weight.

23. The method of claim 11 , wherein the urolithin is urolithin A.

24. The method of claim 13 , wherein the urolithin is urolithin A.

25. The method of claim 15 , wherein the urolithin is urolithin A.

26. The method of claim 16 , wherein the urolithin is urolithin A.

27. The method of claim 23 , wherein the conjoint administration is oral.

28. The method of claim 24 , wherein the conjoint administration is oral.

29. The method of claim 25 , wherein the conjoint administration is oral.

30. The method of claim 26 , wherein the conjoint administration is oral.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 4, 2020
From: SCHNEIDER, BERNARD; MOUCHIROUD, LAURENT; RYU, DONGRYEOL; ANDREUX, PENELOPE; AUWERX, JOHAN
To: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
Reel/Frame 053395/0900 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 4, 2020
From: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
To: AMAZENTIS SA
Reel/Frame 053395/0954 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 4, 2020
From: RINSCH, CHRISTOPHER L.; BLANCO-BOSE, WILLIAM
To: AMAZENTIS SA
Reel/Frame 053395/0988 →
Continuity (6)
Division 15701057 · Sep 11, 2017
Continuation 13929455 · Jun 27, 2013
Provisional Application 61791137 · Mar 15, 2013
Provisional Application 61712886 · Oct 12, 2012
Provisional Application 61665137 · Jun 27, 2012
Related Publication 20200397748A1 · Dec 24, 2020
Cited By (3)
US 12,544,358 US 12,576,064 US 12,576,065