Novel multimeric cd40 ligands, method for preparing same and...

C - Chemistry – Metallurgy – 07 – K

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C07K 14/525 (2006.01) A61K 38/04 (2006.01) C07K 14/705 (2006.01)

Patent

CA 2591035

The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H-Xa-Xb-Xc-Xd-Xe-(Xf)i-, wherein i represents 0 or 1, Xa is in particular selected among lysine, arginine, ornithine residues, Xb is in particular selected among glycine, asparagine, L-proline or D-proline residues, Xc et Xd are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe et Xf are in particular selected among the following amino acid residues: NH2-(CH2)n-COOH, n ranging from 1 to 10 or NH2-(CH2-CH2-O)m-CH2CH2COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr- Tyr146 fragment

La présente invention concerne un composé répondant à la formule (I), dans laquelle Y représente un macrocycle dont le cycle comprend de 9 à 36 atomes, et est fonctionnalisé par trois fonctions aminés ou COOH ; Rc représente un groupe de formule H-Xa-Xb-Xc-Xd-Xe-(Xf)i-, dans laquelle i représente 0 ou 1, Xa est notamment choisi parmi les résidus de lysine, d'arginine, d'ornithine, Xb est notamment choisi parmi les résidus de glycine, d'asparagine, de L- proline ou de D-proline, Xc et Xd sont notamment choisis parmi les résidus de tyrosine, de phénylalanine ou de 3-nitro-tyrosine, Xe et Xf sont notamment choisis parmi les résidus d'acides aminés suivants : NH2-(CH2)n-COOH, n variant de 1 à 10 ou NH2-(CH2-CH2-O)m-CH2CH2COOH, m variant de 3 à 6, sous réserve que l'un au moins des résidus d'acides aminés X3, Xb, Xc et Xd soit différent de l'acide aminé correspondant dans la séquence du fragment143Lys- Gly-Tyr- Tyr146 de CD40L naturel.

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