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 487/04 (2006.01) A61K 31/519 (2006.01) A61P 3/10 (2006.01) A61P 25/24 (2006.01) C07D 235/00 (2006.01) C07D 249/00 (2006.01)

Patent

CA 2531333

This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary arnine and a stereochernic ally isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyI; Cl.6alkylcarbonyl, C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylearbonyl, C1-~6alkyloxycarbonyl, C1- 6alkylcarbonyloxy; or C1-6alkyloxyC1-6alkylcarbonyl optionally substituted with C1-6alkyloxycarbonyl; X represents a direct bond; -(CH2)n3~or -(CH2)m4- X1a-X1b-; R2 represents C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom. selected from 0, S or N; benzoxazolyl or a radical of formula (a-1), wherein said R2 substituent may optionally be substituted; R3 represents halo; hydroxy; optionally substituted C1-.6alkyl; C2-6a]kenyl or C2-6alkynyl, each optionally substituted; optionally substituted polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted polyhaloC1-~6alkyloxy; C1-6alkylthio; polyhaloC1-6a]kylthio; C1-6a]kyloxycarbonyl; C1-6alkylcarbonyloxy; C1- 6alkylearbonyl; polyhaloC1-6alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR6b R7b; C(=O)-NR 6b R7b; -NR5-C(=O)R5;'-S(=O)nl-R8a; - NR5S(=O)nl -R 8a;-NR 5 -S(=O)nl-R 8a ; -S-CN; -NR5 -CN;R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; C2-4alkenyl or C2-4alkynyl, each optionally substituted; polyha]oC1-3alkyl; optionally substituted C1- 4alkyloxy; polyhalo-C1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio~ C1- 4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhatoC1- 4alkyl~carbonyl; nitro; cyano; carboxyl; NR10 R11; C(=O)NR10-R11;NR5-C(=O)- NR10R11;-NR5 -C(=O)-R5; -S(=O)nl,-R12 -NR5-S(=O)nI-R12 ; -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 par C¿1-6?alkyloxycarbonyle; X représente une liaison directe; -(CH¿2?)¿n3?- ou -(CH¿2?)¿n4?-X¿1a?-X¿1b?-; R?2¿ représente C¿3-7?cycloalkyle; 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), ce substituant de R?2¿ pouvant éventuellement être substitué; R?3¿ représente halo; hydroxy; C¿1-6?alkyle éventuellement substitué; C¿2-6?alcényle ou C¿2-6?alcynyle, chacun étant éventuellement substitué; polyhaloC¿1-6?alkyle éventuellement substitué; C¿1-6?alkyloxy éventuellement substitué; polyhaloC¿1-6?alkyloxy éventuellement substitué; C¿1-6?alkylthio; polyhaloC¿1-6?alkylthio; C¿1-6?alkyloxycarbonyle; C¿1-6?alkylcarbonyloxy; C¿1-6?alkylcarbonyle; polyhaloC¿1-6?alkylcarbonyle; cyano; carboxyle; aryloxy; arylthio; arylcarbonyle; NR?6b¿R?7b¿; C(=O)-NR?6b¿R?7b¿; -NR?5¿-C(=O)-NR?6b¿R?7b¿; -NR?5¿-C(=O)-R?5¿; ? ¿-S(=O)¿n1?-R?8a¿; -NR?5¿-S(=O)¿n1?-R?8a¿; -S-CN; -NR?5¿-CN; R?4¿ représente hydrogène; halo; hydroxy; C¿1-4?alkyle éventuellement substitué; C¿2-4?alcényle ou C¿2-4?alcynyle, chacun étant 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?10¿R?11¿; C(=O)NR?10¿R?11¿; -NR?5¿-C(=O)-NR?10¿R?11¿; -NR?5¿-C(=O)-R?5¿; -S(=O)¿n1?-R?12¿; -NR?5¿-S(=O)¿n1?-R?12¿; -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.

Affiliated with

Also associated with

Rating

Triazolopyrimidine derivatives as glycogen synthase kinase 3... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Triazolopyrimidine derivatives as glycogen synthase kinase 3..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Triazolopyrimidine derivatives as glycogen synthase kinase 3... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1722050