Acid addition salts of 5-aminolevulinic acid or its derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 229/22 (2006.01) A61K 31/195 (2006.01)

Patent

CA 2561050

The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

La présente invention concerne un sel d'addition acide d'acide 5-aminolévulinique (5-ALA) ou d'un dérivé de 5-ALA (p. ex. un ester de 5-ALA), dont l'acide présente un pKa d'environ 5 au plus, de préférence environ 3 au plus, à condition que l'acide soit différente de l'acide chlorhydrique. Des sels particulièrement préférés sont des sels dérivés d'acides sélectionnés dans le groupe constitué par l'acide sulfonique et ses dérivés, l'acide bromhydrique, l'acide sulfurique, l'acide nitrique et l'acide phosphorique. Les sels de l'invention sont particulièrement utiles comme agents de photosensibilisation intervenant dans le diagnostic et la photochimiothérapie de troubles ou d'anomalies des surfaces extérieures ou intérieures du corps.

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