C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/04 (2006.01) A01N 43/16 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01) A61P 35/00 (2006.01) C07D 309/30 (2006.01) C07D 309/32 (2006.01) C07D 309/36 (2006.01)
Patent
CA 2547229
The present invention relates to compounds of formula (1) and salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 is a glycosyl moiety, hydroxyl-protected acetate derivatives thereof or amino derivatives thereof; R2, R3 an R4 are, each independently, selected from the group comprising hydrogen, C1-6alkyl, C2- 20alkenyl, C6-20arylalkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl, C6-20aryl aralkyl, akylcarbonyloxy, arylcarbonyloxy, alkyloxy, alklylthio, alkylamino, alkyloxyalkyl,. alkanoyl, alkylcarbonylalkyl, optionally substituted by one or more substituents independently selected from the group comprising alkyl, aralkyl, aryl, cycloalkyl, alkyloxycarbonyl, carboxyl, aminocarbonyl, hydroxy, cyano, halogen or amino optionally mono- or disubstituted wherein the substituents are independently selected from the group comprising alkyl, aryl, aralkyl, aryloxy, arylamino, aryloxyalkyl, arylaminoalkyl, aralkoxy, alkoxy.
La présente invention concerne des composés représentés par la formule (I) et certains de leurs sels, stéréoïsomères, mélanges racémiques, promédicaments, esters et métabolites. Dans cette formule, R¿1? est groupe fonctionnel glycosyle, l'un de ses dérivés acétate à protection hydroxyle, ou l'un de ses dérivés aminés. R¿2?, R¿3? et R¿4? sont chacun indépendamment choisis dans le groupe comprenant hydrogène, C¿1-6?alkyle, C¿2-20?alcényle, C¿6-20?arylalkyle, C¿3-7?cycloalkyle, C¿3-7?cycloalkyle-C¿1-6?alkyle, C¿6-20?aryle-aralkyle, akylcarbonyloxy, arylcarbonyloxy, alkyloxy, alklylthio, alkylamino, alkyloxyalkyle, alcanoyle, alkylcarbonylalkyle, éventuellement substitué par un ou plusieurs substituants indépendamment choisi dans le groupe comprenant alkyle, aralkyle, aryle, cycloalkyle, alkyloxycarbonyle, carboxyle, aminocarbonyle, hydroxy, cyano, halogène ou amino éventuellement mono- ou disubstitué auquel cas les substituants sont indépendamment choisi dans le groupe comprenant alkyle, aryle, aralkyle, aryloxy, arylamino, aryloxyalkyle, arylaminoalkyle, aralcoxy, alcoxy.
de Hoffmann Edmond
Mathieu Benoit
Van Hove Charles
Smart & Biggar
Universite Catholique de Louvain
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