Potent thymopentin analogs
AssigneeOrtho Pharmaceutical Corporation
InventorsGideon Goldstein, George Heavner, Daniel Kroon, Tapan Audhya
Life of this patent
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Abstract
Immunoregulating peptides are disclosed which are more potent than thymopentin or splenin and are useful for their effects on the immune system, especially the treatment of thymic deficiencies.
Claims14
A peptide having the formula:
- R-V-W-X-Y-Z-R.sup.1
- or a pharmaceutically-acceptable acid- or base-addition salt thereof, wherein:
- R is H, loweralkyl, formyl, or loweralkanoyl;
- V is ARG or D-ARG;
- W is [LYS, D-LYS,] PRO, dehydro-PRO, or AIB;
- X is ASP, D-ASP, GLU, or D-GLU;
- Y is VAL, LYS, LEU, ILE, GLU, ALA, GLN, D-VAL, D-LYS, D-LEU, D-ILE, D-GLU, D-ALA, or D-GLN;
- Z is PHE, HIS, TRP, D-PHE, D-HIS, or D-TRP;
- and R.sup.1 is OH or NR.sup.2 R.sup.3 ;
- and R.sup.2 and R.sup.3 are each independently selected from H or loweralkyl[;
- provided that when W is LYS, X is D-ASP, GLU, or D-GLU, and Y is VAL, Z is other than PHE].
A peptide having the formula .alpha.-acetyl-ARG-PRO-ASP-VAL-PHE-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula .alpha.-formyl-ARG-PRO-ASP-VAL-PHE-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula .alpha.-(loweralkanoyl)-ARG-PRO-ASP-VAL-PHE-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula H-ARG-PRO-ASP-VAL-PHE-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula H-ARG-PRO-ASP-VAL-HIS-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula H-ARG-LYS-ASP-VAL-HIS-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
A peptide having the formula H-ARG-LYS-ASP-VAL-PHE-OH or a pharmaceutically-acceptable acid- or base-addition salt thereof.
Dependencies are inferred from the claim text.