Alpha-msh-antagonist didpeptide conjugates

Details Alpha-msh-antagonist didpeptide conjugates Alpha-msh-antagonist didpeptide conjugates

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 8/64 (2006.01) A61K 38/05 (2006.01) A61Q 19/08 (2006.01) A23L 1/305 (2006.01)

Patent

CA 2566478

The invention relates to a dipeptide conjugate having general formula I, AA2-AA1-NH2, wherein A represents the radical corresponding to a monocarboxylic acid with general formula II, HOOC-R, in which: R represents a linear or branched aliphatic radical at C1-C24, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, and/or which can comprise a phenyl group or lipoic acid or the reduced form thereof, dihydrolipoic acid or N-lipoyllysine; and AA1 and AA2 represent identical or different amino acids which are selected from the group containing Ala, Asn, Cys, Gln, Gly, Ile, Leu, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, Asp, Glu, Arg, His, Lys, Orn, Dap, Dab, the corresponding homo-amino acids and the corresponding beta-amino acids in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.

La présente invention concerne un conjugué dipeptidique de formule générale (I) suivante A-AA2-AAI-NH2 dans laquelle A représente le radical correspondant à un acide monocarboxylique de formule générale (II) suivante HOOC-R, dans laquelle R représente un . radical aliphatique en C1-C24 linéaire ou ramifié, éventuellement substitué par un groupe hydroxyle, pouvant comporter une ou plusieurs insaturations, avantageusement de 1 à 6 insaturations, et/ou pouvant comporter un groupe phényle ou l'acide lipoique ou sa forme réduite l'acide dihydrolipoique ou la N-lipoyl~lysine,, AA1 et AA2 représentent des acides aminés identiques ou différents choisis dans le groupe constitué par Ala, Asn, Cys, Gln, Gly, Ile, Leu, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, Asp, Glu, Arg, His, Lys, Orn, Dap, Dab les homoacides aminés correspondants et les béta- acides aminés correspondants sous forme d'énantiomères ou de diastéréoisomères ainsi que leurs mélanges, y compris les mélanges racémiques.

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