Sulfotransferase inhibitor

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/7028 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/08 (2006.01) A61P 43/00 (2006.01) C07H 15/04 (2006.01) C12N 9/99 (2006.01)

Patent

CA 2526022

The hexuronic acid derivative represented by the following formula 1 or a salt thereof is used as an active ingredient of a heparin/heparan sulfate sulfotransferase inhibitor. [Chemical formula 1] (see formula 1) In the formula, each of R1, R2, and R3 independently represent(s) SO3- or H which may have a substituent, provided that at least one thereof represents SO3-; X represents OR4, SR4, N(R4)2, or C(R4)3, R4 independently represents H, alkyl, alkenyl, alkynyl, acyl, aryl, or aralkyl group; one of R5 and R6 represents COOH while the other represents H; and the wavy line represents .alpha.-glycosidic bond or .beta.-glycosidic bond.

La présente invention a trait à un dérivé de l'acide hexuronique caractérisé en ce qu'il est de formule (1) ou un sel de celui-ci utilisé comme principe actif dans un inhibiteur de transférase de groupe sulfate d'héparine/héparane sulfate. Dans la formule (1) : chacun parmi R¿1?, R¿2? et R¿3? est indépendamment SO¿3??-¿ ou H à condition qu'au moins un parmi ceux-ci soit SO¿3??-¿ et que ceux-ci peuvent être substitués ou non substitués ; X est OR¿4?, SR¿4?, N(R¿4?)¿2? ou C(R¿4?)¿3? où chacun des R¿4? est indépendamment H, alkyle, alcynyle, acyle, aryle ou aralkyle ; un parmi R¿5? et R¿6? est COOH tandis que l'autre est H ; et la ligne ondulée est une liaison .alpha.-glycosidique ou une liaison .beta.-glycosidique.

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