Alkyl esters of somatostatin and process therefor

C - Chemistry – Metallurgy – 07 – C

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530/7.26

C07C 103/52 (1980.01)

Patent

CA 1062248

ALKYL ESTERS OF SOMATOSTATIN AND PROCESS THEREFOR Abstract of the Disclosure Alkyl esters of somatostatin and of its linear reduced form, and pharmaceutically acceptable salts thereof, in which the alkyl group contains from 1-14 carbon atoms in a straight or branched chain are disclosed. The compounds are prepared by coup- ling according to the azide method an appropriately protected first heptapeptide hydrazide containing the amino acid residues 1-7 of somatostatin with an appropriately protected second hepta- peptide alkyl ester containing the amino acid residues 8-14, said second heptapeptide having a terminal free amino group and the appropriate terminal carboxylic acid ester group. The resulting linear protected tetradecapeptide alkyl ester is transformed into the corresponding alkyl ester of somatostatin or of the linear reduced form thereof by deprotecting and/or oxidizing procedures. The alkyl esters of somatostatin and of its linear reduced form have somatostatin-like pharmacological activities, and compositions and methods for their use are also disclosed. - 1 -

255846

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