# US 4,399,065 A · D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof

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- Number: US 4,399,065 A
- Document ID: US4399065A
- Status: Granted
- Kind: A
- Application number: 06/337,288
- Filed: 1982-01-05
- Granted: 1983-08-16
- Earliest claimed: 1981-01-13
- Assignees: Patentbureau Danubia
- Inventors: Sandor Bajusz; Erzsebet Szell nee Hasenohrl; Eva Barabas; Daniel Bagdy
- Web page: https://patentgrep.com/patent/US4399065A

## CPC

- C07K 5/06078: {and aromatic or cycloaliphatic}
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

The invention relates to D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, highly stable in aqueous solution, and to a process for preparing it from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate is isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anticoagulant activity.

## Claims

### Claim 1

D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate highly stable in aqueous solution.

### Claim 2

A pharmaceutical composition for use as an anticoagulant which comprises a pharmaceutically acceptable carrier and/or diluent and an effective amount of D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate.