Sulphonated meso-tetraphenyl chlorins and their use as...

A - Human Necessities – 61 – K

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A61K 41/00 (2006.01)

Patent

CA 2457856

The present invention provides photosensitizing agents obtained by reducing a single double bond in the porphyrin macrocycle of a sulphonated meso- tetraphenylporphyrin, preferably a disulphonated meso-tetraphenylporphyrin such as TPPS2a. The resulting sulphonated meso-tetraphenyl chlorins include compounds of formula (I) (wherein X is -SO3H; n, p, q and r are each independently 0 or 1; and the sum of n, p, q and r is an integer from 1 to 4, preferably at least 2, e.g. 2 or 4) isomers and isomer mixtures thereof. The compounds of the invention and their pharmaceutically acceptable salts find particular use as photosensitizing agents in the photochemical internalization of molecules and in photodynamic therapy.

La présente invention concerne des agents de photosensibilisation obtenus par réduction d'une seule double liaison au niveau du macrocycle de prophyrine d'une méso-tétraphénylporphyrine sulfonée, de préférence, une méso-tétraphénylporphyrine disulfonée telle que la TPPS¿2a?. Les méso-tétraphénylchlorines sulfonées ainsi obtenues comprennent des composés de formule (I) (où X représente -SO¿3?H; n, p, q et r représentent chacun indépendamment 0 ou 1; et la somme de n, p, q et r représente un entier compris entre 1 et 4, de préférence au moins 2, par exemple 2 ou 4), des isomères et des mélanges d'isomères. Les composés selon l'invention et leurs sels pharmaceutiquement acceptables sont notamment utilisés en tant qu'agents de photosensibilisation dans l'internalisation photochimique de molécules et dans la thérapie photodynamique.

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