C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 15/24 (2006.01) A61K 31/485 (2006.01) A61K 31/70 (2006.01) A61P 25/04 (2006.01) A61P 29/00 (2006.01) C07D 489/02 (2006.01) C07H 7/06 (2006.01) C07H 17/00 (2006.01) C07H 17/04 (2006.01)
Patent
CA 2746429
The invention relates to derivatives of morphine-6-glucuronide having formula (I) wherein R1 is a 5-membered heteroaromatic group optionally substituted by one or more substituents selected from among halogen atoms and (C1-C4)alkyl, halogen, hydroxyl, halo(C1-C4)alkyl, halo(C1-C4)alkyloxy, (C1-C4)alkyloxy, aryl(C1-C4)alkyl and aryl groups, said aryl group being optionally substituted by one or more groups selected from among (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxyl and (C1-C4)alkyloxy groups, in the form of a base or acid addition salt, as well as in hydrate or solvate form. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
La présente invention concerne des dérivés du morphine-6-glucuronide de formule (I) suivante dans laquelle : R1 est un groupe hétéroaromatique à 5 chaînons éventuellement substitué par un ou plusieurs substituants choisis parmi les atomes d'halogène et les groupes (C1-C4)alkyle, halogène, hydroxyle, halo(C1- C4)alkyle, halo(C1-C4)alkyloxy, (C1-C4)alkyloxy, aryl(C1- C4)alkyle et aryle, ledit groupe aryle étant éventuellement substitué par un ou plusieurs groupes choisis parmi les groupes (C1- C4)alkyle, halo(C1-C4)alkyle, hydroxyle et (C1-C4)alkyloxy, à l'état de base ou de sel d'addition à un acide ainsi qu'à l'état d'hydrate ou de solvate. La présente invention vise également leur procédé de préparation et leur application en thérapeutique.
Dlubala Alain
Ripoche Isabelle
Trecant Claire
Robic
Sanofi
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