Boronated metalloporphyrins and therapeutic methods

Details Boronated metalloporphyrins and therapeutic methods Boronated metalloporphyrins and therapeutic methods

C - Chemistry, Metallurgy

07

F

C07F 5/02 (2006.01) A61K 31/69 (2006.01) C07D 487/22 (2006.01) C07F 1/08 (2006.01) C07F 5/05 (2006.01) C07F 13/00 (2006.01) C07F 15/06 (2006.01)

Patent

CA 2172415

Carborane substituted porphyrin compounds complexed with a metal or transition metal have a variety of therapeutic uses. These compounds have been found, for example, selectively to inhibit vial aspartyl proteases. The transition metal complexes are useful both therapeutically in BNCT (boron neutron capture therapy) as well as for MR contrast enhancement. Particularly preferred compounds in accordance with the invention use the dipotassium salt of 2,4-bis-[.alpha.,.beta.-(1,2-dicarbaclosododecaborane carboxy)ethyl]deuteroporphyrin, which is complexed with a metal or a transition metal. These compounds arc well solubilized in water, and are suitable for oral administration.

Les composés de porphyrine substitués par carborane décrits ici, complexés avec un métal ou un métal de transition, ont une variété d'utilisations thérapeutiques. Par exemple, on a découvert que ces composés inhibent sélectivement des protéases d'aspartyle virale. Les complexes de métaux de transition sont utiles à la fois sur un plan thérapeutique (thérapie de capture neutronique du bore), ainsi que dans l'amélioration du contraste en résonance magnétique (RM). Les composés préférés de l'invention utilisent notamment le sel dipotassium de 2,4-bis-[.alpha.,.beta.-(1,2-dicarbaclosododécaborane carboxy)éthyl]deutéroporphyrine, qui est complexé avec un métal ou un métal de transition. Ces composés se solubilisent parfaitement dans l'eau, et sont appropriés pour être administrés oralement.

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