Use of breakers of advanced glycation endproducts for...

A - Human Necessities – 61 – K

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A61K 31/155 (2006.01) A61K 31/192 (2006.01) A61K 31/196 (2006.01) A61K 31/197 (2006.01) A61K 31/198 (2006.01) A61K 31/606 (2006.01) A61P 39/00 (2006.01)

Patent

CA 2405411

Advanced glycation endproducts (AGEs) have been implicated in the pathogenesis of a variety of debilitating diseases such as diabetes, atherosclerosis, Alzheimer's and rheumatoid arthritis, as well as in the normal aging process. Five compounds are here reported to be active in breaking AGE-protein cross- links. These compounds are L-bis-[4-(4-chlorobenzamido- phenoxyisobutyryl)cystine] (LR20); 4-(3,5- dichlorophenylureido)phenoxyisobutyryl-1-amido-cyclohexane-1-carboxylic acid (LR23); methylene bis [4,4'-(2-chlorophenylureido-phenoxyisobutyric acid)] (LR90); 5-aminosalicylic acid (5-ASA); and metformin. These compounds may be used to reverse the debilitating effects of those diseases in which AGEs are formed.

La présente invention concerne des produits finaux de glycation avancée (AGEs) qui jouent un rôle dans la pathogénèse d'une variété de maladies débilitantes comme le diabète, l'athérosclérose, la maladie d'Alzheimer et la polyarthrite rhumatoïde ainsi que dans le processus de veillissement normal. Cinq composés sont décrits ici comme permettant de rompre les réticulations de la protéine-AGE. Il s'agit de L-bis-[4-(4-chlorobenzamido-phénoxyisobutyryl)cystine] (LR20); acide 4-(3,5-dichlorophénylureido)phénoxyisobutyryl-1-amido-cyclohéxane-1-carboxylique ; (LR23); acide méthylène bis [4,4'-(2-chlorophénylureido-phénoxyisobutyrique)] (LR90) acide 5-aminosalicylique (5-ASA); and metformine. Ces composés peuvent être utilisés pour inverser les effets débilitants de ces maladies au cours desquelles se forment des produits finaux de glycation avancée.

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