Agents for treatment of glaucomatous retinopathy and optic...

A - Human Necessities – 61 – K

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A61K 31/497 (2006.01) A61K 31/05 (2006.01) A61K 31/26 (2006.01) A61K 31/352 (2006.01) A61K 31/353 (2006.01) A61K 31/366 (2006.01) A61K 31/40 (2006.01) A61K 31/404 (2006.01) A61K 45/00 (2006.01) A61P 27/02 (2006.01)

Patent

CA 2547852

Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating glaucomatous retinopathy or optic neuropathy. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2- dithiole-3-thione, butylated hydroxyanisole, flavonoid, an isothiocyanate, 3,5- di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.

L'invention concerne des agents qui stimulent la translocation nucléaire de la protéine Nrf2 et améliorent les produits des gènes qui détoxifient et éliminent des métabolites cytotoxiques, ainsi qu'un procédé pour traiter une rétinopathie glaucomateuse ou une neuropathie optique. Les agents à structures diverses qui agissent sur le passage Nrf2/ARE induisent l'expression des enzymes et des protéines qui possèdent des propriétés cytoprotectrices versatiles et ils sont une défense contre les métabolites toxiques et les xénobiotiques. Les agents comprennent certains électrophiles et des oxydants tels qu'un accepteur d'addition de Michaël, le diphénol, le thiocarbamate, le quinone, le 1,2-dithiole-3-thione, l'hydroxyanisole butylé, un flavonoïde, un isothiocyanate, un 3,5-di-tert-butyl-4-hydroxytoluène, l'éthoxyquinine, la coumarine, leurs combinaisons, ou un de leurs dérivés ou analogues actifs de manière pharmacologique.

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