Indole derivatives as 5-ht2a ligands and as serotonine...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/14 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2330796

Pharmaceutical compounds of formula (I) in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R1 and R2 are each hydrogen, C1-4 alkyl, C1-4 alkoxy, HO-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C1-4 alkythio, halo, optionally substituted phenyl, optionally substituted phenyl-C1-4 alkyl, or R1 and R2 together with the carbon atom to which they are attached form a C3-6 cycloalkyl group, C=O, C=NOR' where R' is hydrogen or C1-4 alkyl, R3, R4 and R5 are each hydrogen, halo, nitro, C1-4 alkyl, C1-4 alkoxy, C1-4 alkyl-CO-, where m is 0, 1 or 2, R'R''N-SO2-, -COOR', -CONR'R'', -NR'R''-N(OR')COOR'', -COR', -NHSO2R', where R' and R'' are each hydrogen or C1-4 alkyl, R6 and R7 are each hydrogen or C1- 4 alkyl, X is oxygen or sulphur, the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

L'invention concerne des composés pharmaceutiques ayant la formule (I) dans laquelle n est compris entre 1 et 6, m est 1 ou 2 et p est 1 ou 2. R?1¿ et R?2¿ sont chacun hydrogène, alkyle C¿1-4?, alcoxy C¿1-4?, alkyle HO-C¿1-4?, alkyle C¿1-4? - alcoxy C¿1-4?, alkylthio C¿1-4?, halo, phényle éventuellement substitué, phényle - alkyle C¿1-4? éventuellement substitué, ou R?1¿ et R?2¿ sont pris conjointement avec l'atome de carbone auquel ils sont attachés pour former un groupe cycloalkyle C¿3-6?, ?C=O, C=NOR', où R' est hydrogène ou alkyle C¿1-4? ; R?3¿, R?4¿ et R?5¿ sont chacun hydrogène, halo, nitro, alkyle C¿1-4?, alcoxy C¿1-4?, -CO- alkyle C¿1-4?, où m est 0, 1 ou 2, R'R''N-SO¿2?-, -COOR', -CONR'R'', -NR'R'', -N(OR')COOR'', -COR', -NHSO¿2?R', où R' et R'' sont chacun hydrogène ou alkyle C¿1-4? ; R?6¿ et R?7¿ sont chacun hydrogène ou alkyle C¿1-4?, x est oxygène ou soufre, la ligne en pointillé représente une éventuelle liaison double dans les positions 6- et 7-. L'invention concerne également les sels de ces compositions.

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