# US 4,395,404 A · Synthetic thymosin .beta..sub.3 and .beta..sub.4 analogues

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- Number: US 4,395,404 A
- Document ID: US4395404A
- Status: Granted
- Kind: A
- Application number: 06/378,463
- Filed: 1982-05-14
- Granted: 1983-07-26
- Earliest claimed: 1982-05-14
- Assignees: The George Washington University
- Inventors: Teresa L. K. Low; Allan L. Goldstein
- Web page: https://patentgrep.com/patent/US4395404A

## CPC

- C07K 5/1005: {and aliphatic}
- A61P 37/04: Immunostimulants
- C07K 5/0806: {the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala}
- C07K 14/57581: {Thymosin; Related peptides}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- Y10S 530/837: Lymph; lymph-glands; thymus
- Y10S 930/18: Thymus derived hormone or factor; related peptides
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

## Abstract

Novel peptides representing fragments of thymosin .beta..sub.3 and .beta..sub.4 have been synthesized and are active agents affecting regulation, differentiation and function of thymus dependent lymphocytes and macrophages.

## Claims

### Claim 1

A peptide of the formula
R-Gly-Glu-Ser-R.sub.1
wherein R represents H-Q, Q-Ala-, Q-Gln-Ala, Q-Glu-Lys-Gln-Ala, Q-Gln-Glu-Lys-Gln-Ala-, Q-Glu-Gln-Glu-Lys-Gly-Ala, Q-Ile-Glu-Gln-Glu-Lys-Gin-Ala, Q-Thr-Ile-Glu-Gln-Glu-Lys-Gln-Ala-, Q-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gin-Ala, or Q-Gln-Sar-wherein Q represents H or acyl; and R.sub.1 represents -OH, -A-C or -A-B-C wherein A represents Asp or Asn, B represents -Glu-Ile-Thr- and C represents -Ala-Lys-Thr-Oh.
and the pharmaceutically acceptable acid or base addition salts thereof.

### Claim 2 (depends on 1)

A peptide according to claim 1 which is H-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser-OH.

### Claim 3 (depends on 1)

A peptide according to claim 1 which is H-Ile-Glu-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser-OH.

### Claim 4 (depends on 1)

A peptide according to claim 1 which is H-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser-OH.

### Claim 5 (depends on 1)

A peptide according to claim 1 which is H-Gln-Ala-Gly-Glu-Ser-OH.

### Claim 6 (depends on 1)

A peptide according to claim 1 which is H-Ala-Gly-Glu-Ser-OH.

### Claim 7 (depends on 1)

A peptide according to claim 1 which is H-Gly-Glu-Ser-OH.

### Claim 8 (depends on 1)

A peptide according to claim 1 which is H-Gln-Ala-Gly-Glu-Ser-Asp-Ala-Lys-Thr-OH.

### Claim 9 (depends on 1)

A peptide according to claim 1 which is H-Gln-Ala-Gly-Glu-Ser-Asn-Ala-Lys-Thr-OH.

### Claim 10 (depends on 1)

A peptide according to claim 1 which is CH.sub.3 CO-Gln-Sar-Gly-Glu-Ser-Asp-Ala-Lys-Thr-OH.

### Claim 11 (depends on 1)

A peptide according to claim 1 which is CH.sub.3 CO-Gln-Sar-Gly-Glu-Ser-Asn-Ala-Lys-Thr-OH.

### Claim 12 (depends on 1)

A peptide according to claim 1 which is H-Gln-Ala-Gly-Glu-Ser-Asp-Glu-Ile-Thr-Ala-Lys-Thr-OH.

### Claim 13 (depends on 1)

A method for stimulating the production of TdT positive prothymocytes, for inhibiting macrophage migration, or restoring immune responses of steroid suppressed mammalian subject, said method comprising administering to said subject an effective amount of a peptide of claim 1.