EP0505680B1 — Octapeptide or heptapeptide derivatives, a process for preparing them as well as medicaments containing these compounds and the use of them

USPTO Abstract

A subject matter of the invention are octapeptide or heptapeptide amide derivatives of formula <CHEM> wherein X1 stands for an aromatic D-amino acid rest; or a D-phenylglycyl, p-hydroxyphenylglycyl, o-aminobenzoyl, m-aminobenzoyl, D-tetrahydroisoquinolylcarbonyl or sarcosylalanyl; or a <CHEM> group, in which latter A1 means the rest of an amine or means an amino group or means an alkoxy, aryloxy or aralkyloxy group; X2 represents an aromatic amino acid rest or a histidyl group; X3 means a D-tryptophyl, o-aminobenzoyl, m-aminobenzoyl, aspartyl, D-aspartyl, beta -aspartyl, beta -D-aspartyl or aminosuccinyl group; or a group indicated for X1; X4 stands for an amino acid rest bearing an alkyl or aralkyl side chain; or a prolyl or beta -alanyl group; or a valence bond; X5 means an aromatic amino acid rest or a threonyl group; R1 represents hydrogen or a <CHEM> group, in which latter A2 means hydrogen or an alkyl group; R2 means hydrogen, -S- or a -S-acetamidomethyl, phenyl or p-hydroxyphenyl group; R3 stands for hydrogen or hydroxyl; R4 means a phenyl or p-hydroxyphenyl group; or -S-or a -S-acetamidomethyl group when the meaning of R2 is the same group; or a methyl group when R3 is hydroxyl and n is 1, 2, 3 or 4 and acid addition salts thereof. o