Amide-based insulin prodrugs

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/62 (2006.01) A61K 38/28 (2006.01) A61P 3/10 (2006.01) C07K 1/107 (2006.01)

Patent

CA 2744558

Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.

Préparations de promédicaments insuliniques et d'analogues insuliniques dans lesquels le peptide de l'insuline à été modifié par une liaison d'un élément de promédicament dipeptidique. Les promédicaments de l'invention ont des demi-vies accrues d'au moins 10 heures, plus généralement de plus de 2 heures, de 20 heures et moins de 70 heures, et sont convertis en forme active en conditions physiologiques par l'intermédiaire d'une réaction non enzymatique commandée par instabilité chimique.

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