Triazolopyrimidine derivatives as glycogen synthase kinase 3...

Details Triazolopyrimidine derivatives as glycogen synthase kinase 3... Triazolopyrimidine derivatives as glycogen synthase kinase 3...

C - Chemistry, Metallurgy

07

D

C07D 487/00 (2006.01)

Patent

CA 2531232

This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6 alkylcarbonyl; C1-6 a]kyl; C1-6 alkyloxycarbonyl; C1-6 alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonytoxy; or optionally substituted C1-6 alkyloxyCl-6alkylcarbonyl; X1 represents a direct bond; -(CH2)n3- or -(CH2)n4-X1a-X1b-; R2 represents optionally substituted C3- 7CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X2 represents a direct bond; -NR1-NR1-(CH2)N3 -; -0- ; -0-(CH2)n3-; -C(=O)-; -C(=O)- (CH2)n3-; -C(=O)-NR5-(CH2)n3-; -C(=S)-; -S-; - S(=O)n1-; -(CH2)n3-; -(CH2)n4-X1a-X1b-; -X1a.-X1b-(CH2)n4-; -S(=O)n1-NR5- (CH2)n3-NR5_ or -S(=O)n1,-NR5 -(CH2)n3-; R3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; optionally substituted C2-4alkenyl or C2-4alkynyl; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1- 3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR9R10; C(=O)NR9R10;- NR5_C(=O)-NR9R10; -NR5-C(=O)-R5; -S(=O) n1,-R11 -NR5-S(=O)n1,-R11 -S-CN; -NR5 - CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

Composé de formule (I), <I>N</I>-oxyde, sel d'addition acceptable sur le plan pharmaceutique, amine quaternaire et forme stéréochimiquement isomère dudit composé. Dans ladite formule, le noyau A représente phényle, pyridyle, pyrimidinyle, pyridazinyle ou pyrazinyle; R?1¿ représente hydrogène; aryle; formyle; C¿1-6?alkylcarbonyle; C¿1-6?alkyle; C¿1-6?alkyloxycarbonyle; C¿1-6?alkyle substitué par formyle, C¿1-6?alkylcarbonyle, C¿1-6?alkyloxycarbonyle, C¿1-6?alkylcarbonyloxy; ou C¿1-6?alkyloxyC¿1-6?alkylcarbonyle éventuellement substitué; X¿1? représente une liaison directe; -(CH¿2?)¿n3?- ou -(CH¿2?)¿n4?-X¿1a?-X¿1b?-; R?2¿ représente C¿3-7?cycloalkyle éventuellement substitué; phényle; un hétérocycle monocyclique à 4, 5, 6 ou 7 éléments contenant au moins un hétéroatome choisi parmi O, S ou N; benzoxazolyle ou un radical de formule (a-1); X¿2? représente une liaison directe; -NR?1¿-; NR?1¿-(CH¿2?)¿n3?-; -O-; -O-(CH¿2?)¿n3?-; -C(=O)-; -C(=O)-(CH¿2?)¿n3?-; -C(=O)-NR?5¿-(CH¿2?)¿n3?-; -C(=S)-; -S-; -S(=O)¿n1?-; -(CH¿2?)¿n3?-; -(CH¿2?)¿n4?-X¿1a?-X¿1b?-; -X¿1a?-X¿1b?-(CH¿2?)¿n4?-; -S(=O)¿n1?-NR?5¿-(CH¿2?)¿n3?-NR?5¿- ou -S(=O)¿n1?-NR?5¿-(CH¿2?)¿n3?-; R?3¿ représente un hétérocycle monocyclique à 5 ou 6 éléments éventuellement substitué contenant au moins un hétéroatome choisi parmi O, S ou N, ou un hétérocycle bicyclique à 9 ou 10 éléments contenant au moins un hétéroatome choisi parmi O, S ou N; R?4¿ représente hydrogène; halo; hydroxy; C¿1-4?alkyle éventuellement substitué; C¿2-4?alcényle ou C¿2-4?alcynyle éventuellement substitué; polyhaloC¿1-3?alkyle; C¿1-4?alkyloxy éventuellement substitué; polyhaloC¿1-3?alkyloxy; C¿1-4?alkylthio; polyhaloC¿1-3?alkylthio; C¿1-4?alkyloxycarbonyle; C¿1-4?alkylcarbonyloxy; C¿1-4?alkylcarbonyle; polyhaloC¿1-4?alkylcarbonyle; nitro; cyano; carboxyle; NR?9¿R?10¿; C(=O)NR?9¿R?10¿; -NR?5¿-C(=O)-NR?9¿R?10¿; -NR?5¿-C(=O)-R?5¿; -S(=O)¿n1?-R?11¿; -NR?5¿-S(=O)¿n1?-R?11¿; -S-CN; -NR?5¿-CN. La présente invention concerne également l'utilisation desdits composés, des compositions pharmaceutiques les contenant et des procédés de préparation desdits composés.

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