IP Library › Granted Patent US 12,398,122
Granted Patent B2
US 12,398,122 · App. 18/730,722 · Granted Aug 26, 2025

Resolvin analogs compounds, methods and uses thereof

Inventors: Mohamed Benderdour (Pierrefonds, CA); Julio Fernandes (Montréal, CA); René Maltais (Québec, CA); Jean-Yves Sancéau (Québec, CA)
Assignee: VALORISATION RECHERCHE HSCM LIMITED PARTNERSHIP
C07D405/06C07D233/64
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Quick Facts
Patent No.
US 12,398,122
App. No.
18/730,722
Granted
Aug 26, 2025
Kind
B2
Abstract

The present application relates to resolvin analogs having anti-inflammatory and antioxidant properties, uses and methods using the same. More specifically, the present application relates to compounds of formula (I) or an enantiomer, isomer, salt or solvate thereof.

Claims (40)

1. A compound of Formula (I):

wherein

R 1 is selected from the group consisting of H and C 1-8 alkyl;

R 2 , R 3 and R 4 are independently selected from the group consisting of H, C 1-8 alkyl, and a suitable protecting group; wherein R 2 and R 3 may be joined to form, together with the atom therebetween, an heterocyclyl group;

R 5 and R 6 are independently selected from the group consisting of H and C 1-8 alkyl;

R 7 is selected from the group consisting of linear or branched C 1-10 alkyl and linear or branched C 2-10 alkenyl, wherein the alkyl and alkenyl may be interrupted by 1 to 3 heteroatoms selected from O, N and S, and may be substituted with one or more group selected from halogen, —OH, —CF 3 , —CN, —NH 2 , —SH and phenyl,

is absent or represents a bond,

wherein R 4 is absent when is a bond,

or an enantiomer, isomer, salt or solvate thereof.

2. A compound of Formula (IA):

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and are as defined in claim 1 , and n and m are independently an integer from 0 to 7,

or an enantiomer, isomer, salt or solvate thereof.

3. The compound of claim 1 , wherein R 7 is pentyl, propyl, octyl or benzyl.

4. The compound of claim 1 , wherein R 1 is H, methyl, ethyl or propyl.

5. The compound of claim 1 , wherein R 1 is H or methyl.

6. The compound of claim 1 , wherein R 2 , R 3 and R 4 are independently selected from the group consisting of H, methyl, ethyl, and propyl.

7. The compound of claim 1 , wherein R 2 and R 3 are joined to form, together with the atom therebetween, an acetal group.

8. The compound of claim 1 , wherein R 2 , R 3 and R 4 are each H.

9. The compound of claim 1 , wherein R 5 and R 6 are each H, methyl or ethyl.

10. The compound of claim 1 , wherein R 5 and R 6 are each methyl.

11. The compound of claim 1 having the structure of Formula (I-2):

or an enantiomer, isomer, salt or solvate thereof.

12. The compound of claim 1 having the structure of Formula (I-1):

or an enantiomer, isomer, salt or solvate thereof.

13. The compound of claim 1 having the structure of Formula (IB)

or an enantiomer, isomer, salt or solvate thereof.

14. The compound of claim 1 having the structure of Formula (IC)

or an enantiomer, isomer, salt or solvate thereof.

15. A pharmaceutical composition comprising a compound as defined in claim 1 , or an enantiomer, isomer, salt or solvate thereof, and a pharmaceutically acceptable excipient, diluent or carrier.

16. A pharmaceutical composition comprising a compound as defined in claim 11 , or an enantiomer, isomer, salt or solvate thereof, and a pharmaceutically acceptable excipient, diluent or carrier.

17. A pharmaceutical composition comprising a compound as defined in claim 12 , or an enantiomer, isomer, salt or solvate thereof, and a pharmaceutically acceptable excipient, diluent or carrier.

18. A pharmaceutical composition comprising a compound as defined in claim 13 , or an enantiomer, isomer, salt or solvate thereof, and a pharmaceutically acceptable excipient, diluent or carrier.

19. A pharmaceutical composition comprising a compound as defined in claim 14 , or an enantiomer, isomer, salt or solvate thereof, and a pharmaceutically acceptable excipient, diluent or carrier.

20. A method for treating an inflammatory disease or disorder, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

21. The method of claim 20 , wherein the inflammatory disease or disorder is selected from arthritis, osteoarthritis, inflammatory bowel disease or disorder, and skin inflammatory disease and disorder.

22. A method for inhibiting monocytes/macrophages differentiation, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

23. A method for inhibiting osteoclasts recruitment, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

24. A method for inhibiting MMP-13 production, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

25. A method for inhibiting ultraviolet-induced hyaluronic acid degradation, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

26. A method for inhibiting COX-2 expression, comprising administering an effective amount of a compound as defined in claim 1 in a subject in need thereof.

Assignments (4)
NUNC PRO TUNC ASSIGNMENT Recorded Sep 5, 2024
From: MALTAIS, RENÉ; SANCÉAU, JEAN-YVES
To: UNIVERSITÉ LAVAL
Reel/Frame 068498/0850 →
NUNC PRO TUNC ASSIGNMENT Recorded Sep 5, 2024
From: UNIVERSITÉ LAVAL
To: VALORISATION RECHERCHE HSCM LIMITED PARTNERSHIP
Reel/Frame 068499/0174 →
NUNC PRO TUNC ASSIGNMENT Recorded Sep 5, 2024
From: FERNANDES, JULIO; BENDERDOUR, MOHAMED
To: CENTRE INTÉGRÉ UNIVERSITAIRE DE SANTÉ ET DE SERVICES SOCIAUX DU-NORD-DE-L'ÎLE-DE-MONTRÉAL
Reel/Frame 068499/0375 →
NUNC PRO TUNC ASSIGNMENT Recorded Sep 5, 2024
From: CENTRE UNIVERSITAIRE DE SANTÉ ET DE SERVICES SOCIAUX DU-NORD-DE-L'ÎLE-DE-MONTRÉAL
To: VALORISATION RECHERCHE HSCM LIMITED PARTNERSHIP
Reel/Frame 068499/0597 →
Continuity (2)
Provisional Application 63301450 · Jan 20, 2022
Related Publication 20250115588A1 · Apr 10, 2025
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