SIALIC ACID-BONDED PHYSIOLOGICALLY ACTIVE PEPTIDE AND PRODUCTION THEREOF

SIALIC ACID-BONDED PHYSIOLOGICALLY ACTIVE PEPTIDE AND PRODUCTION THEREOF

NEW MATERIAL:A sialic acid-bond physiologically active peptide of formula I (R is H or acetyl; Pep is peptide residue). EXAMPLE:N-(5-Acetamido-2,4,7,8,9-penta-O-acetyl-3,5-dideoxy-beta-D-gly cero-D- galacto-nonuropyranosonyl)-gamma-glutamyl-cystinyl-glycine. USE:Medicines with the activity inherent...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: TANAKA MAKOTO, SUGIMOTO MAMORU, BAN CHIEKO, GOTOU MOTOAKI, SUGAI HIROSHI
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SUGARS
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Beschreibung
Zusammenfassung:NEW MATERIAL:A sialic acid-bond physiologically active peptide of formula I (R is H or acetyl; Pep is peptide residue). EXAMPLE:N-(5-Acetamido-2,4,7,8,9-penta-O-acetyl-3,5-dideoxy-beta-D-gly cero-D- galacto-nonuropyranosonyl)-gamma-glutamyl-cystinyl-glycine. USE:Medicines with the activity inherent in physiologically active peptide further enhanced and biological half-life extended. PREPARATION:For example, a 3,5-dideoxy-beta-D-glycero-D-galacto- nonuropyranosonic acid of formula II (Ac is acetyl) is reacted with pentafluorophenol in the presence of a condensation agent into a pentafluorophenyl ester of formula III, which is then reacted with a peptide using e.g. a peptide automatically synthesizing machine, thus obtaining the objective compound of formula I.