Cyclopeptides and their use as absorption promoters when applied to the mucosa

US5565423A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Jurgen K. Sandow · Königstein, DE
• Walter Durckheimer · Hattersheim, DE
• Günter Ditzinger · Hellerup, DK
• Hans P. Merkle · Zürich, CH

Key dates

• Filing date: Apr 7, 1995
• Grant date: Oct 15, 1996
• Expiry date: Apr 7, 2015

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Cyclopeptides and their use as absorption promoters when applied to the mucosa The invention relates to a compound of the formula I ##STR1## or a physiologically tolerated salt thereof, in which X is a basic L- or D-amino acid, PA1 Y is a neutral or basic L- or D-amino acid, PA1 Z is a neutral or basic L- or D-amino acid, which can be identical to or different from Y, PA1 R.sup.1 is an N-bonded acyl radical of the formula II ##STR2## in which Ar is a phenyl radical, which is optionally substituted by 1, 2 or 3 identical or different radicals from the series comprising hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, amino, carboxyl, (C.sub.1 -C.sub.4)-alkylamino and halogen, or is a 2-aminothiazol-4-yl radical, p is an integer from zero to 4 and q, n, m and 1 independently of one another are zero or 1. The invention additionallly relates to the use of compounds of the formula I and physiologically tolerated salts thereof for promoting the absorption of peptides and proteins when applied to the mucosa, and pharmaceutical formulations which contain a pharmacologically active amount of one or more peptides or proteins and a compound of the formula I or physiologically tolerated salts thereof.