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EP0166612A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Potent thymopentin analogs

Assignee: Ortho Pharmaceutical Corp
•
Filing: 1985-06-26
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Granted: —
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Expires: 2005-06-26
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Abstract

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.

Inventors

  • 👤 Gideon Goldstein
  • 👤 George Heavner
  • 👤 Daniel Kroon
  • 👤 Tapan Audhya

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-09 03:52
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/06; C07K14/00; C07K14/435; C07K14/575; C07K14/66; C07K14/662; A; A61; A61P; A61P37/00; A61P37/02; A61P37/04; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/18

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 116 words
A peptide having the formula: R-V-W-X-Y-Z-R 1 or a pharnaceutically-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; R 1 is OH or NR 2 R 3 ; and R 2 and R 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.
Claim 2
Dependent Claim 116 words
A peptide having the formula: R-V-W-X-Y-Z-R 1 or a pharnaceutically-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; R 1 is OH or NR 2 R 3 ; and R 2 and R 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.
Claim 3
Dependent Claim 13 words
The peptide of claim 1 wherein Z is PHE, HIS, D-PHE, or D-HIS.
Claim 4
Dependent Claim 23 words
The peptide of claim 1 wherein R is hydrogen or loweralkyl, V is ARG, X is ASP, and Z is PHE or HIS.
Claim 5
Dependent Claim 14 words
The peptide of any one of claims 1 to 3 wherein W is PRO.
Claim 6
Dependent Claim 23 words
A peptide having the formula: α-acetyl-ARG-PRO-ASP-VAL-PHE-OH; d _-formyl-ARG-PRO-ASP-VAL-PHE-OH; α-(loweralkanoyl)-ARG-PRO-ASP-VAL-PHE-OH; H-ARG-PRO-ASP-VAL-PHE-OH; H-ARG-PRO-ASP-VAL-HIS-OH ; H-ARG-LYS-ASP-VAL-HIS-OH; or H-ARG-LYS-ASP-VAL-PHE-OH; or a pharmaceutically-acceptable acid- or base-addition salt thereof.
Claim 7
Dependent Claim 23 words
A peptide having the formula: α-acetyl-ARG-PRO-ASP-VAL-PHE-OH; d _-formyl-ARG-PRO-ASP-VAL-PHE-OH; α-(loweralkanoyl)-ARG-PRO-ASP-VAL-PHE-OH; H-ARG-PRO-ASP-VAL-PHE-OH; H-ARG-PRO-ASP-VAL-HIS-OH ; H-ARG-LYS-ASP-VAL-HIS-OH; or H-ARG-LYS-ASP-VAL-PHE-OH; or a pharmaceutically-acceptable acid- or base-addition salt thereof.
Claim 8
Dependent Claim 31 words
A pharmaceutical composition comprising an effective T cell or B cell inducing amount of a peptide of any one of claims 1 to 5 in admixture with a pharmaceutically acceptable carrier.
Claim 9
Dependent Claim 39 words
A peptide of any one of claims 1 to 5 or a composition of claim 6 for treatment of a condition resulting from relative or absolute T cell or B cell deficiency in a subject having such a condition.
Claim 10
Dependent Claim 35 words
A peptide of any one of claims 1 to 5 or a composition of claim 6 for inducing lymphopoietic stem cells of a subject to develop the characteristics of thymus-derived lymphocytes or for inducing precursor
Claim 11
Dependent Claim 13 words
B cells of a subject to develop the characteristics of mature B cells.
Claim 12
Dependent Claim 13 words
B cells of a subject to develop the characteristics of mature B cells.
Claim 13
Dependent Claim 24 words
The use of peptide synthesis techniques to produce a peptide of any one of claims 1 to 5 from its constituent amino acid residues.
Claim 14
Dependent Claim 37 words
A process for producing a composition according to claim 6 comprising admixing an effective T cell or B cell inducing amount of a peptide of any one of claims 1 to 5 with a pharmaceutically acceptable carrier.

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