Steroidal glycoside compounds as core 2 glcnac- t inhibitors

Details Steroidal glycoside compounds as core 2 glcnac- t inhibitors Steroidal glycoside compounds as core 2 glcnac- t inhibitors

A - Human Necessities

61

K

A61K 31/704 (2006.01) A61K 31/7048 (2006.01) A61K 31/706 (2006.01) A61P 1/04 (2006.01) A61P 1/06 (2006.01) A61P 1/16 (2006.01) A61P 3/10 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2614017

Treatments for conditions involving detrimental activity of the enzyme core 2 GIcNAc - T are provided using compounds of the formula (I) wherein R1 is H, - OH, C1-6 alkoxy, -NR5R6, or Sac 1; R2is H, -OH, C1-6 alkoxy or Sac 2; R 3 is H, -OH, C1-6 alkoxy or Sac 3; R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6- alkoxy- C1-6 -alkyl; R5 is H, C1-6 alkyl or C1-6 acyl; R6 is H, C1-6 alkyl or C1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof

L'invention se rapporte à des traitements de troubles faisant intervenir l'activité nuisible du core enzyme 2 GicNAc-T, qui font appel à des composés représentés par la formule (I), ou à un sel pharmaceutiquement acceptable, un éther ou un ester desdits composés. Dans ladite formule, R1 représente H, -OH, alcoxy C1-6, -NR5R6 ou Sac 1 ; R2 représente H, -OH, alcoxy C1-6 ou Sac 2 ; R 3 représente H, -OH, alcoxy C1-6 ou Sac 3 ; R4 représente H, alkyle C1-6, hydroxyalkyle C1-6 ou alcoxy-C1-6-alkyle-C1-6 ; R5 représente H, alkyle C1-6 ou acyle C1-6 ; R6 représente H, alkyle C1-6 ou acyle C1-6 ; Sac 1, Sac 2 et Sac 3 sont des groupes fonctionnels saccharide sélectionnées indépendamment ; et Z représente un groupe fonctionnel stéroïde.

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