Substituted indole-2-carboxylic acids as glucosyl...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/42 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2243882

Disclosed is a substituted indole-2-carboxylic acid of the formula: (see fig. I) wherein R1 is hydrogen or (C1-C6) alkyl; and R2 is (C1-C6) alkyl, (C3-C7) cycloalkyl, phenyl or phenyl substituted with one to three groups independently selected from (C1-C3) alkyl, (C1-C3) alkoxy, halogen, cyano or nitro; or a pharmaceutically acceptable salt thereof, useful as an inhibitor of uridine diphosphate glucose : glycoprotein glucosyltransferase (UGG Tase).

Divulgation d'un acide indole-2-carboxylique substitué, ou d'un sel de cet acide utilisable en pharmacie, de formule (voir figure I), dans laquelle : R1 est un atome d'hydrogène ou un alkyle en C1-C6; R2 est un alkyle en C1-C6, un cycloalkyle en C3-C7, un phényle ou un phényle substitué par un à trois groupements choisis, de manière indépendante, parmi un alkyle en C1-C3, un alcoxy en C1-C3, un atome d'halogène, un cyano ou un nitro. Ces composés sont utiles comme inhibiteur de la glucosyltransférase (UGGTase) dans le cas des glycoprotéines contenant de l'uridine-diphosphate-glucose.

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