Tyrosine phosphatase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 207/333 (2006.01) A61K 31/402 (2006.01) A61P 3/10 (2006.01) A61P 43/00 (2006.01) C07D 209/12 (2006.01)

Patent

CA 2410338

Compounds of the general formula (|) or salts thereof exhibit a protein tyrosine phosphatase inhibiting activity and are useful as preventive and therapeutic drugs for diabetes or the like: (|)wherein X1 and X2 are each a free valency or a spacer having a C1-20 main chain; one of R1 and R2 is a cyclic group which bears a substituent selected from among (1) carboxylated C1- 6 alkoxy groups which may be substituted and (2) carboxylated C1-6 aliphatic hydrocarbon groups which may be substituted and may further have other substituent, and the other is an optionally substituted cyclic group or hydrogen; and R3, R4 and R5 are each hydrogen or a substituent, or alternatively R4 together with R3 or R5 may form an optionally substituted ring, with the proviso that some compounds of the general formula (|) are excepted.

L'invention concerne des composés représentés par la formule générale (I) ou leurs sels, présentant une activité d'inhibition de la protéine tyrosine phosphatase et utilisés comme médicaments préventifs et thérapeutiques contre le diabète ou autres maladies semblables. Dans ladite formule (I), X¿1? et X¿2? sont chacun une valence libre ou un bras espaceur comprenant une chaîne principale C¿1-20 ?; un élément parmi R¿1? ou R¿2 ?est un groupe cyclique comportant un substituant sélectionné dans (1) des groupes alkoxy carboxylés C¿1-6 ?pouvant être substitués et (2) des groupes hydrocarbures aliphatiques carboxylés C¿1-6 ?pouvant être substitués et pouvant également comprendre un autre substituant, et l'autre est un groupe cyclique substitué ou hydrogène ; et R3, R4, et R5 sont chacun hydrogène ou un substituant ou, en variante, R4 avec R3 ou R5 peuvent former un anneau éventuellement substitué, à condition que certains composés de la formule générale (I) soient exclus.

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