# US 4,399,066 A · Novel peptide, process for preparation thereof and use thereof

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- Number: US 4,399,066 A
- Document ID: US4399066A
- Status: Granted
- Kind: A
- Application number: 06/341,056
- Filed: 1982-01-20
- Granted: 1983-08-16
- Earliest claimed: 1981-01-29
- Assignees: Fujisawa Pharmaceutical Co., Ltd.
- Inventors: Osamu Nakaguchi; Satoshi Okada; Masashi Hashimoto
- Web page: https://patentgrep.com/patent/US4399066A

## CPC

- C07K 5/0215: {containing natural amino acids, forming a peptide bond via their side chain functional group, e.g. epsilon-Lys, gamma-Glu}
- 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)
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- 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)
- 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)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms, having the structure: ##STR1## wherein R.sup.1 is hydrogen or acyl, R.sup.2 is lower alkyl, R.sup.3 is carboxy or protected carboxy, R.sup.4 is hydroxy(lower) alkyl, R.sup.5 is carboxy or protected carboxy, R.sup.6 is carboxy or protected carboxy, and R.sup.7 is hydrogen or an amino protective group and their therapeutically acceptable salts.

## Claims

### Claim 1

A compound of the following formula or its pharmaceutically acceptable salt: ##STR10## wherein R.sup.1 is hydrogen or acyl,
wherein acyl is selected from the group consisting of alkanoyl and aralkanoyl either of which may be substituted with halogen, hydroxy, protected hydroxy, carboxy, or amino,
R.sup.2 is lower alkyl,
R.sup.3 is carboxy or protected carboxy,
R.sup.4 is hydroxy(lower) alkyl,
R.sup.5 is carboxy or protected carboxy,
R.sup.6 is carboxy or protected carboxy, and
R.sup.7 is hydrogen or an amino protective group.

### Claim 2 (depends on 1)

A compound according to claim 1, wherein R.sup.1 is hydroxy(lower)alkanoyl, or protected hydroxy(lower)alkanoyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are each as defined in claim 1.

### Claim 3 (depends on 1, 2)

A compound according to claim 2, wherein R.sup.1 is 2-hydroxypropionyl or 2-acetoxypropionyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.7 are each as defined in claim 1.