IP Library › Granted Patent US 10,744,181
Granted Patent B2
US 10,744,181 · App. 16/482,040 · Granted Aug 18, 2020

Glycopeptide derivatives for use in the treatment and/or prevention and/or attenuation of fibrosis diseases

Inventors: Géraldine Deliencourt-Godefroy (Bois d'Ennebourg, FR); Jocelyne Legoedec (Sotteville-les-Rouen, FR)
Assignee: TFCHEM
A61K38/14A61K9/0014A61K31/70A61P17/02
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Quick Facts
Patent No.
US 10,744,181
App. No.
16/482,040
Granted
Aug 18, 2020
Kind
B2
Abstract

The present invention relates to a compound of the following formula (I), as well as to a pharmaceutical composition comprising at least one compound of following formula (I) and at least one pharmaceutically acceptable excipient, for use in the treatment and/or prevention and/or attenuation of fibrosis diseases, in particular excessive scars such as keloids or hypertrophic scars.

Claims (51)

1. A method of treating and/or preventing and/or attenuating a fibrosis disease, comprising the administration to a person in need thereof of an effective amount of a compound of following formula (I):

or a salt thereof, a solvate, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions,

in which:

n represents an integer from 1 to 6,

m represents 0 or 1,

p represents 0 or 1

R represents H, F, CH 3 , CH 2 F, or CH 2 OH,

R 1 , R 2 and R 3 represent, independently from one another, H, F, or OH,

R 4 represents a hydrogen, a halogen, or OH, and

R 6 and R 7 represent, independently from each other, a hydrogen, a (C 1 -C 6 )alkyl, an aryl, or an aryl-(C 1 -C 6 )alkyl.

2. The method according to claim 1 , wherein the fibrosis disease is excessive scars.

3. The method according to claim 2 , wherein the excessive scars are keloids or hypertrophic scars.

4. The method according to claim 1 , wherein the compound of formula (I) has one of the following formulas (Ia), (Ib), (Ic):

5. The method according to claim 1 , wherein n represents an integer from 2 to 6.

6. The method according to claim 1 , wherein R represents a CH 2 OH group.

7. The method according to claim 1 , wherein R 1 , R 2 and R 3 each represent a OH group.

8. The method according to claim 1 , wherein R 4 represents a OH group.

9. The method according to claim 1 , wherein R 6 and R 7 represent, independently from each other, a (C 1 -C 6 )alkyl, an aryl or an aryl-(C 1 -C 6 )alkyl.

10. The method according to claim 1 , wherein the compound of formula (I) is chosen among the following compounds:

and the salts and/or solvates thereof.

11. A method of treating and/or preventing and/or attenuating a fibrosis disease, comprising the administration to a person in need thereof of an effective amount of a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and at least one compound of following formula (I):

or a salt thereof, a solvate, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions,

in which:

n represents an integer from 1 to 6,

m represents 0 or 1,

p represents 0 or 1

R represents H, F, CH 3 , CH 2 F, or CH 2 OH,

R 1 , R 2 and R 3 represent, independently from one another, H, F, or OH,

R 4 represents a hydrogen, a halogen, or OH, and

R 6 and R 7 represent, independently from each other, a hydrogen, a (C 1 -C 6 )alkyl, an aryl, or an aryl-(C 1 -C 6 )alkyl.

12. The method according to claim 11 , wherein the fibrosis disease is excessive scars.

13. The method according to claim 12 , wherein the excessive scars are keloids or hypertrophic scars.

14. The method according to claim 11 , wherein n represents an integer from 2 to 6; R represents a CH 2 OH group; R 1 , R 2 and R 3 each represent a OH group; R 4 represents a OH group; and R 6 and R 7 represent, independently from each other, a (C 1 -C 6 )alkyl, an aryl or an aryl-(C 1 -C 6 )alkyl.

15. The method according to claim 11 , wherein the compound of formula (I) is chosen among the following compounds:

and the salts and/or solvates thereof.

16. The method according to claim 11 , wherein the pharmaceutical composition is administered topically in combination with or after a laser or surgical treatment.

17. A dressing comprising a pad, compress or sponge impregnated with a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and at least one compound of following formula (I):

or a salt thereof, a solvate, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions,

in which:

n represents an integer from 1 to 6,

m represents 0 or 1,

p represents 0 or 1

R represents H, F, CH 3 , CH 2 F, or CH 2 OH,

R 1 , R 2 and R 3 represent, independently from one another, H, F, or OH,

R 4 represents a hydrogen, a halogen, or OH, and

R 6 and R 7 represent, independently from each other, a hydrogen, a (C 1 -C 6 )alkyl, an aryl, or an aryl-(C 1 -C 6 )alkyl.

18. The dressing according to claim 17 , wherein n represents an integer from 2 to 6; R represents a CH 2 OH group; R 1 , R 2 and R 3 each represent a OH group; R 4 represents a OH group; and R 6 and R 7 represent, independently from each other, a (C 1 -C 6 )alkyl, an aryl or an aryl-(C 1 -C 6 )alkyl.

19. The dressing according to claim 17 , wherein the compound of formula (I) is chosen among the following compounds:

and the salts and/or solvates thereof.

20. A method of treating and/or preventing and/or attenuating a fibrosis disease, comprising the application to a person in need thereof of a dressing according to claim 17 .

21. The method according to claim 20 , wherein the dressing is applied in combination with or after a laser or surgical treatment.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 27, 2020
From: DELIENCOURT-GODEFROY, GÉRALDINE; LEGOEDEC, JOCELYNE
To: TFCHEM
Reel/Frame 051631/0442 →
Continuity (1)
Related Publication 20190388501A1 · Dec 26, 2019