Polypeptides, processes for their production, pharmaceutical com

Details Polypeptides, processes for their production, pharmaceutical com Polypeptides, processes for their production, pharmaceutical com

1983-08-18

1985-01-29

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125S, 514 16, A61K 3700, C07C10352

Patent

active

044965435

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.

REFERENCES:
patent: 4235886 (1980-11-01), Freidinger et al.
patent: 4282143 (1981-08-01), Sarantakis
patent: 4360516 (1982-11-01), Freidinger et al.
patent: 4395403 (1983-07-01), Bauer et al.

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