Novel cyclopeptides

Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Reduced antigenicity – reduced ability to bind complement – or...

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26011255, A61K 3700, C07C10352

Patent

active

042384818

ABSTRACT:
Sulphur-free cyclopeptides with somatostatin-analogous aminoacid partial sequences, of the formula ##STR1## in which R is Asn, Ala or de-R, trp is D-Trp or L-Trp, which can be substituted in the benzene ring by halogen atoms or nitro groups, W is a free or etherified hydroxyl group or halogen atom present as a substituent on the benzene ring of the L-phenylalanine radical, or is hydrogen, X is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-X and Y is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-Y, and also acid addition salts and complexes thereof have biological properties similar to those of somatostatin and can be used, especially in the form of pharmaceutical preparations, for the treatment of excessive secretion of somatotropin, insulin and/or glucagon. The compounds according to the invention are obtained by cyclising a corresponding linear peptide compound in which the .epsilon.-amino group of the lysine radical and, if desired, also the hydroxyl group of the threonine radical are protected and detaching the protective groups which are present.

REFERENCES:
patent: 3988304 (1976-10-01), Garsky
patent: 4000259 (1976-12-01), Garsky
patent: 4054558 (1977-10-01), Garsky
patent: 4115554 (1978-09-01), Veber
patent: 4146612 (1979-03-01), Veber
J.A.C.S. 98, 1976, pp. 2367-2369.

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