20(s) camptothecin glycoconjugates

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 9/00 (2006.01) A61K 31/70 (2006.01) A61K 38/14 (2006.01) C07D 491/22 (2006.01) C07H 15/203 (2006.01) C07H 15/26 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2291436

The invention relates to 20(S) camptothecin glycoconjugates, wherein a 3-O- methylated .beta.-L-fucose element is bonded to the 20-hydroxyl group of a camptothecin derivative by means of a thiourea-modified peptide spacer. The invention also relates to a method for the production of the inventive compounds and to the use thereof as medicaments, specially in the field of cancer diseases.

L'invention concerne des glycoconjugués de 20(S)-camptothécine, dans lesquels un motif .beta.-L-Fucose 3-O-méthylé est réticulé, par l'intermédiaire d'un espaceur peptidique modifié par une thio-urée, avec le groupe 20-hydroxyle d'un dérivé de camptothécine. L'invention concerne également des procédés pour préparer ces composés ainsi que leur utilisation comme médicaments, notamment dans le cadre des pathologies cancéreuses.

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