Protein tyrosine phosphatase inhibitor

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/53 (2006.01) A61P 3/10 (2006.01) A61P 35/00 (2006.01) C07D 487/00 (2006.01) C12P 17/18 (2006.01)

Patent

CA 2421718

Use of a compound of formula (I), wherein each R, which are the same or different, is H or C1-C6 alkyl, and X completes a ring which is a substituted triazine having one of the following formulae (II) to (IV), wherein R' is H or C1-C6 alkyl; or an enol tautomer of a compound of formula (I) in which any of the groups R or R' is hydrogen; in the manufacture of a medicament for use as a protein tyrosine phosphatase (PTP) inhibitor. Formula (I) embraces 2- methylfervenulone, which can be produced by fermentation of a novel microbial strain. Fermentation of the said strain also produces novel precursors to 2- methylfervenulone having utility as prodrugs.

Composé de formule (I) dans laquelle chacun des R, qui sont identiques ou différents, représentent H ou alkyle C¿1?-C¿6?, et X complète un noyau qui est une triazine substituée répondant à l'une des formules (II) à (IV). Dans ces formules, R' représente H ou alkyle C¿1?-C¿6? ou un tautomère énol d'un composé de formule (I) dans laquelle l'un quelconque des groupes R ou R' représente hydrogène. Ledit composé est utilisé dans la préparation d'un médicament destiné à être utilisé en tant qu'inhibiteur de protéine tyrosine phosphatase (PTP). La formule (I) englobe la 2-méthylfervenulone qui peut être produite par fermentation d'une nouvelle souche microbienne. La fermentation de ladite souche produit également de nouveaux précurseurs de 2-méthylfervenulone utiles en tant que promédicaments.

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