Granted Patent B2

US 7,381,707 · App. 11/171,785 · Granted Jun 3, 2008

Abstract

Claims (27)

1. A method to treat dry eye in a mammal in need of such treatment comprising intraocularly administering to said eye a composition comprising a carrier and a peptide of the formula

wherein:

A 1 is Val, Leu, Ile, or Cha;

A 2 is Val, Leu, Ile, or Cha;

A 3 is Gly or Ala;

A 4 is Lys, Arg, or Har;

each R 1 and R 2 , independently, is H, C 1-12 alkyl, C 7-10 phenylalkyl, or C(═O)E 1 , where E 1 is C 1-20 alkyl, C 3-20 alkenyl, C 3-20 alkynyl, phenyl, 3,4-dihydroxyphenylalkyl, naphthyl, or C 7-10 phenylalkyl; provided that when either R 1 or R 2 is C(═O)E 1 , the other must be H; and

R 3 is OH, NH 2 , C 1-12 alloxy, C 7-10 phenylalkoxy, C 11-20 naphthylalkoxy, C 1-12 alkylamino, C 7-10 phenylalkylamino, or C 11-20 naphthylalkylamino;

or a cosmetically acceptable salt thereof.

2. The method of claim 1 , wherein R 1 is H, R 2 is H or C(═O)E 1 where E 1 is C 1-20 alkyl, and R 3 is OH or NH 2 .

3. The method of claim 1 , wherein A 1 is Leu, A 2 is Ile, A 3 is Gly, and A 4 is Arg or Lys.

4. The method of claim 2 , wherein A 1 is Leu, A 2 is Ile, A 3 is Gly, and A 4 is Arg or Lys.

5. The method of claim 1 , wherein said peptide is H2-Leu-Ile-Gly-Arg-NH 2 (SEQ.ID.NO: 1), H 2 -Leu-Ile-Gly-Lys-NH 2 (SEQ.ID.NO: 2), H 2 -Leu-Ile-Gly-Arg-OH (SEQ.ID.NO: 3), H 2 -Leu-Ile-Gly-Lys-OH (SEQ.ID.NO: 4), Palmitoyl-Leu-Ile-Gly-Arg-NH 2 (SEQ.ID.NO: 5), Palmitoyl-Leu-Ile-Gly-Lys-NH 2 (SEQ.ID.NO: 6), Palmitoyl-Leu-Ile-Gly-Arg-OH (SEQ.ID.NO: 7), Palmitoyl-Leu-Ile-Gly-Lys-OH (SEQ.ID.NO: 8) Stearoyl-Leu-Ile-Gly-Arg-NH 2 (SEQ.ID.NO: 9), Stearoyl-Leu-Ile-Gly-Lys-NH 2 (SEQ.ID.NO: 10), Stearoyl-Leu-Ile-Gly-Arg-OH (SEQ.ID.NO: 11), and Stearoyl-Leu-Ile-Gly-Lys-OH (SEQ.ID.NO: 12), or a cosmetically-acceptable salt thereof.

6. The method of claim 1 , wherein said peptide is H 2 -Leu-Ile-Gly-Arg-NH 2 (SEQ.ID.NO: 1)or a cosmetically-acceptable salt thereof.

7. The method of claim 1 , wherein said peptide is H 2 -Leu-Ile-Gly-Arg-OH (SEQ.ID.NO: 3)or a cosmetically-acceptable salt thereof.

8. A The method of claim 1 , wherein said composition is administered by topical administration.

9. A The method of claim 1 , wherein said composition is administered by intraocular injection.

10. The method of claim 1 , wherein said composition is administered by intraocular implantation.

11. The method of claim 3 , wherein said composition is administered by topical administration.

12. The method of claim 3 , wherein said composition is administered by intraocular injection.

13. The method of claim 3 , wherein said composition is administered by intraocular implantation.

14. The method of claim 4 , wherein said composition is administered by topical administration.

15. The method of claim 4 , wherein said composition is administered by intraocular injection.

16. The method of claim 4 , wherein said composition is administered by intraocular implantation.

17. The method of claim 6 , wherein said composition is administered by topical administration.

18. The method of claim 6 , wherein said composition is administered by intraocular injection.

19. The method of claim 6 , wherein said composition is administered by intraocular implantation.

Assignments (8)