Peptide and a method of obtaining it

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/08 (2006.01) C07K 5/02 (2006.01) C07K 5/027 (2006.01) C07K 5/033 (2006.01) C07K 5/072 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) C07K 5/09 (2006.01) C07K 5/093 (2006.01) C07K 5/097 (2006.01) C07K 5/10 (2006.01) C07K 5/103 (2006.01) C07K 5/107 (2006.01) C07K 5/113 (2006.01) C07K 5/117 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2214410

The invention relates to medicine, specifically, to methods of obtaining biologically active substances with immuno-regulating properties, and can be used in medicine and veterinary science and in experimental biochemistry. The fundamental problem addressed by the invention is that of producing a novel synthetic biologically active peptide with immuno-regulating properties and of the formula: X-Glu-Trp-Y, in which X is H or Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, D- Trp, .gamma.-aminobutyric acid, -aminocaproic acid; Y is Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D- Tyr, D-Phe, D-Trp, .gamma.-aminobutyric acid, - aminocaproic acid, -OH, mono- or di-substituted amide (C1-C3). Peptide synthesis takes place in a solution by successive growth of a chain from the C termination of the molecules, using a strategy of maximum blocking of functional groups, starting from amino acid alkyl ether, using the method of activating the ethers and the method of mixed anhydrides using tributyloxicarbonyl amino acid.

L'invention concerne la médecine, spécifiquement des procédés d'obtention de substances biologiquement actives présentant des propriétés immuno-régulatrices, et peut être utilisée en médecine ainsi qu'en science vétérinaire et en biochimie expérimentale. Le problème fondamental abordé par l'invention est celui de la production d'un nouveau peptide synthétique biologiquement actif présentant des propriétés immuno-régulatrices et de la formule: X-Glu-Trp-Y, dans laquelle X représente H ou Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, D-Trp, acide .gamma.-aminobutyrique, acide ?-aminocaproïque; Y représente Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, D-Trp, acide .gamma.-aminobutyrique, acide ?-aminocaproïque, -OH, un amide (C¿1?-C¿3?) à mono ou disubstitution. La synthèse du peptide a lieu en solution par la croissance successive d'une chaîne tirée de la terminaison C des molécules, à l'aide d'une stratégie de blocage maximum des groupes fonctionnels, partant d'alkyle éther d'acide aminé, selon le procédé d'activation des éthers et le procédé d'anhydrides mélangés utilisant un acide aminé de tributyloxicarbonyle.

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