Tetralines

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C - Chemistry, Metallurgy

07

C

C07C 217/74 (2006.01) A61K 31/135 (2006.01) A61K 31/16 (2006.01) A61K 31/255 (2006.01) A61K 31/275 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) C07C 211/42 (2006.01) C07C 215/64 (2006.01) C07C 225/20 (2006.01) C07C 237/48 (2006.01) C07C 255/58 (2006.01) C07C 309/65 (2006.01) C07C 311/39 (2006.01) C07C 317/32 (2006.01) C07C 323/31 (2006.01) C07D 295/033 (2006.01) C07D 295/073 (2006.01) C07D 295/096 (2006.01)

Patent

CA 2217855

Compounds of formula (I) wherein R1 and R2, independently, are hydrogen (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio, halogen, trifluoromethyl, trifluoromethoxy, cyano, (C2-5)alkanoyl, (C1-4)alkylsulfonyl or sulfamoyl; R3 is hydrogen, hydroxy, (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, (C2-5)alkanoyl, carbamoyl, (C1-4)alkylsulfonyloxy or trifluoromethylsulfonyloxy; and R4 and R5, independently, are hydrogen, (C1-4)alkyl, hydroxy(C2-4)alkyl or phenyl(C1-4)alkyl, or form together with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino or piperazinyl group, in free base or acid addition salt form. Compounds according to formula (1) are useful in the treatment of epilepsy, stroke and brain or spinal trauma.

Cette invention concerne des composés correspondant à la formule (I), où R1 et R2 représentent indépendamment hydrogène, alkyle (C1-4), alcoxy (C1-4), alkylthio (C1-4), halogène, trifluorométhyle, trifluorométhoxy, cyano, alcanoyle (C2-5), alkyl (C1-4) sulfonyle, ou sulfamoyle; R3 représente hydrogène, hydroxy, alkyle (C1-4), alcoxy (C1-4), halogène, cyano, alcanoyle (C2-5), carbamoyle, alkyl (C1-4) sulfonyloxy ou trifluorométhylsulfonyloxy; et R4 et R5 représentent indépendamment hydrogène, alkyle (C1-4), hydroxyalkyle (C2-4), ou phényle-alkyle (C1-4), ou encore forment avec l'atome d'azote auquel ils sont attachés un groupe pyrrolidinyle, pipéridino ou pipérazinyle, en base libre ou sous forme de sel d'addition d'acide. Les composés correspondant à la formule (I) sont utiles dans le traitement de l'épilepsie, des accidents cardiovasculaires et des traumatismes du cerveau ou de la moelle épinière.

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