Reversible boronate complexes of 1,2-cis-diol cyclic-peptides

Details Reversible boronate complexes of 1,2-cis-diol cyclic-peptides Reversible boronate complexes of 1,2-cis-diol cyclic-peptides

C - Chemistry, Metallurgy

07

K

C07K 7/56 (2006.01) A61K 38/12 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2340647

Reversible borate or boronate complexes of 1,2-cis-diol cyclic-peptides and their use as a means for purification, isolation, stabilization and/or water solubilization of their respective parent 1,2-cis-diol cyclic-peptide is described. A method for forming the boronate adducts is also described. The method is particularly useful for forming boronate adducts of hydrophobic Echinocandin compounds to increase their water solubility. Pharmaceutical formulations and treatments based on the reversible borate or boronate complexes of active 1,2-cis-diol cyclic-peptides (e.g., Echinocandin antifungal compounds) are also described.

L'invention concerne des complexes de borates ou boronates réversibles et de peptides cycliques à 1,2-cis-diol, ainsi que l'utilisation de ceux-ci pour purifier, isoler, stabiliser, et/ou solubiliser dans l'eau, leur parent respectif, le peptide cyclique à 1,2-cis-diol. L'invention concerne également un procédé de formation d'adduits, ce procédé étant notamment utile pour former des adduits de boronates/composés d'Echinocandine hydrophobes, afin d'augmenter la solubilité de ceux-ci dans l'eau. L'invention concerne encore des formulations pharmaceutiques ainsi que des traitements à base de ces complexes de borates ou boronates/peptides cycliques à 1,2-cis-diol actifs (par exemple des composés antifongiques d'Echinocandine).

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