Compounds useful as modulators of the proteasome activity

Details Compounds useful as modulators of the proteasome activity Compounds useful as modulators of the proteasome activity

A - Human Necessities

61

K

A61K 31/407 (2006.01) A01N 43/38 (2006.01) A61K 8/49 (2006.01) A61K 31/405 (2006.01) A61P 9/00 (2006.01) A61P 17/02 (2006.01) A61P 21/00 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01) A61P 31/18 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) A61Q 19/08 (2006.01)

Patent

CA 2604133

The present invention relates to the use of compounds of the following general formula (I): wherein no is 0 or 1, and when no is 1, X = CH2 or X = NCH2C6H5; R1 is OH, or a OR10 group, or a group of formula NH-(CH2)n1-R11; R2 is H, or an alkyl group, or a group of formula (CH2)n2-(CO)n3-NR13R14; R3 is H, or an alkyl group; R4 is H, or Boc, or Z; R5 is H, or Boc, or Z ; R6 is a OR16 group; R7 and R8 are H, or a halogen atom, as modulators of the proteasome activity, in the frame of the preparation of a medicament useful for the prevention or treatment of diseases wherein the proteasome is involved, or the preparation of cosmetic compositions, or of phytosanitary compositions.

La présente invention concerne des composés représentés par la formule générale (I): dans laquelle no vaut 0 ou 1, et, dans le cas où no vaut 1, X = CH2 ou X = NCH2C6H5; R1 est OH, ou un groupe OR10, ou un groupe de formule NH-(CH2)n1-R11; R2 est H, ou un groupe alkyle, ou un groupe de formule (CH2)n2-(CO)n3-NR13R14; R3 est H, ou un groupe alkyle; R4 est H, ou Boc, ou Z; R5 est H, ou Boc, ou Z; R6 est un groupe OR16; R7 et R8 sont H, ou un atome d'halogène, ceci sous l'angle de leur utilisation en tant que modulateurs de l'activité du protéasome dans le cadre de la fabrication d'un médicament utile pour la prévention ou le traitement de maladies dans lesquelles le protéasome est impliqué, ou bien de compositions cosmétiques, ou bien encore de compositions phytosanitaires.

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