Synthesis and characterization of novel systems for guidance...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 9/00 (2006.01) A61K 38/04 (2006.01) C07K 7/64 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2499496

The invention relates to a method for preparing a grafted homodetic cyclopeptde forming a frame defining two surfaces, one surface being known as the upper surface and the other surface being known as the lower surface, both surfaces being grafted, characterized in the a linear peptide is synthesized, said synthesis being carried out on modified amino acids or not, some of which includeorthogonal protector groups, intramolecular cylization of the protected linear peptide thus obtained is performed, all or part of the orthogonal protector groups are substituted by a protected precursor, and at least one molecule of therapeutic interest is grafted on one and/or the other surface of the frame by means of an oxime link.

La présente invention concerne un procédé de préparation d'un cyclopeptide homodétique greffé formant un châssis définissant deux faces, une face dite supérieure et une face dite inférieure, lesdites deux faces étant toutes les deux greffées, caractérisé en ce que l'on synthétise un peptide linéaire, ladite synthèse étant effectuée à partir d'acides aminés modifiés ou non, certains d'entre eux portant des groupes protecteurs orthogonaux, on effectue une cyclisation intramoléculaire du peptide protégé linéaire obtenu, on substitue tout ou partie des groupes protecteurs orthogonaux par un précurseur protégé, on greffe sur l'une et/ou l'autre face dudit châssis, par une liaison oxime, au moins une molécule d'intérêt.

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