C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/7.26
C07K 14/655 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1111841
Novel cyclopeptides Abstract of the Disclosure Sulphur-free cyclopeptides with somatostatin- analogous aminoacid partial sequences, of the formula Image (I) 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 ben- zene 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.
312129
Kamber Bruno
Rink Hans
Sieber Peter
Fetherstonhaugh & Co.
Novartis Ag
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