2-n-substituted or...

Details 2-n-substituted or... 2-n-substituted or...

C - Chemistry, Metallurgy

07

D

C07D 211/56 (2006.01) A61K 31/445 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2362082

This invention relates to (2R,3S,4R,5R)-2-amino-5- methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted- 2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): (see formula I) wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower .omega.-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-- protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4- tetraol by multi-steps of reactions.

L'invention concerne des (2R, 3S, 4R, 5R)-2-amino-5-méthylpipéridine-3,4-diols et des (2S, 3S, 4R, 5R)-2-amino-5-méthylpipéridine-3,4-diols avec substitution 2-N, de formule générale (I), y compris les sels pharmaceutiquement acceptables de ces produits, qui ont un puissant effet inhibiteur sur la glycosidase. Dans ladite formule, R<1> et R<2> sont chacun hydrogène; ou R<1> est hydrogène tandis que R<2> est alkanoyle inférieur ou alkanoyle inférieur omega -trihalogéné; ou R<1> et R<2> sont ensemble phtaloyle. Les composés considérés peuvent être élaborés suivant des processus à plusieurs phases à partir de (2S, 3S, 4R)-5-N-protégés-2,3,4-O-triprotégés-5-aminopentane-1,2,3,4-tétraols.

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