High penetration prodrug compositions of peptides and...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/16 (2006.01) A61P 17/00 (2006.01) A61P 25/00 (2006.01) C07K 1/04 (2006.01) C07K 7/08 (2006.01) C07K 14/00 (2006.01)

Patent

CA 2761489

Provided is a high penetration composition or high penetration prodrugs of peptide or peptide-related compound comprising functional unit, linker, and transportational unit. The functional unit is covalently linked to the transportational unit via the linker, and comprises a moiety of the peptide or the peptide-related compound. The transportational unit comprises protonatable amine group. The linker comprises chemical bond that is capable of being cleaved after the composition penetrates across a biological barrier.

La présente invention concerne une composition à pénétration élevée ou des promédicaments à pénétration élevée, composé(e) d'un peptide ou d'un composé apparenté à un peptide comprenant une unité fonctionnelle, un lieur, et une unité de transport. L'unité fonctionnelle est liée par covalence à l'unité de transport par l'intermédiaire du lieur, et contient une fraction du peptide ou du composé apparenté à un peptide. L'unité de transport contient un groupe amine protonable. Le lieur comporte une liaison chimique capable d'être coupée après la pénétration de la composition à travers une barrière biologique.

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