Chemical compounds

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.1, 167/103

C07K 14/585 (2006.01) A61K 38/23 (2006.01) C07K 14/575 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2001094

- 26 - A B S T R A C T Novel analogues of calcitonin gene related peptide comprise analogues of natural CGRPs modified at at least two of positions 3, 22 and 25. These compounds are of general formula NH2-Ala-Cys-A-aa.alpha.-B-C-Lys-D-aa.beta.-CONH2 wherein A is a carboxylate or amide substituted amino acid or amino acid analogue; aa.alpha. is substantially the amino acid sequence of a CGRP from position 4 to position 21; B is a hydrocarbyl or thio substituted amino acid or amino acid analogue; C is valine or glycine; D is an amine or hydroxyl substituted amino acid or amino acid analogue. The novel analogues may comprise natural amino acid residues. Preferably A is aspartate or asparagine, B is valine or methionine, C is valine and D is asparagine or serine. The analogues exhibit desirable cardiovascular properties and are potentially useful in therapy, e.g. for treatment of deficiencies in cerebral blood supply.

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