Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use

US4496543A · kind A · utility

Assignee

• Sandoz AG · CH

Inventors

• Wilfried Bauer · Lampenberg, CH
• Janos Pless · Basel, CH

Key dates

• Filing date: Aug 18, 1983
• Grant date: Jan 29, 1985
• Expiry date: Aug 18, 2003

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/26
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Straight-chain or mono-cyclicpolypeptides comprising a heptapeptide moiety, said moiety having in the 1-position (N-terminal) an .alpha.-N-phenylalkylated, optionally ring-substituted phenylalanine residue, in the 2-position a cysteine residue, in the 3-position an optionally ring-substituted phenylalanine residue, in the 4-position an optionally benzene-ring-substituted tryptophan residue, in the 5-position an optionally .epsilon.-N-alkylated lysine residue and in the 7-position (C-terminal) a cysteine or cysteinol residue the S-atoms of the cysteine residue at the 2-position and the cysteine or cysteinol residue at the 7-position being linked together in the case of the mono-cyclic polypeptides to form an -S-S-bridge, whereby the residues at the 1-, 2-, 4-, 6-, and 7-positions of said heptapeptide moiety may each be in the (L)- or (D)-configuration and the residues at the 4-, 5- and 6-positions of said heptapeptide moiety may each be optionally .alpha.-N-alkylated, said polypeptides being in free or protected form, as well as salt forms and complexes thereof. Subject compounds are useful as pharmaceuticals, e.g. as GH-secretion inhibitors.