Formulation of boronic acid compounds

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 5/02 (2006.01) A61K 31/69 (2006.01) A61K 38/05 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07F 5/04 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2435146

The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of formula (1) in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.

L'invention concerne des composés stables préparés à partir d'acide boronique, et des composés lyophilisés de ces derniers, de formule (1) dans laquelle Z?1¿ et Z?2¿ sont des fractions dérivées du sucre. L'invention concerne également des procédés de préparation de ces composés. La lyophilisation d'un mélange renfermant un composé d'acide boronique et une fraction dérivée du sucre produit une composition stable qui libère promptement le composé d'acide boronique lors de sa dissolution dans un milieu aqueux.

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