Fused indolecarboxamides: dopamine receptor subtype specific...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/88 (2006.01) C07D 209/94 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2263340

Disclosed are compounds of formula (I) or the pharmaceutically acceptable acid addition salts thereof wherein (a) represents an aromatic or alicyclic ring; R1 and R2 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1- C6 alkoxy, -O2CR', -NHCOR', -COR', -SOmR', where R' is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1 and R2 independently represent -CONR'R'', or -NR'R'' where R' and R'' independently represent hydrogen or C1-C6 alkyl; R3 is hydrogen, C1-C6 alkyl, or -COR''' where R''' is C1-C6 alkyl; R4 is hydrogen or C1-C6 alkyl; and R represents an azacycloalkylalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention are useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

L'invention concerne des composés utiles pour le tratiemetn de troubles affectifs, (schizophrénie, dépression, maladie d'Alzheimer, par exemple), troubles de la fonction motrice (parkinsonisme ou dystonie, par exemple) ou d'autres troubles qui réagissent au blocage dopaminergique comme l'abus d'intoxicants ou les troubles obsessivo-compulsifs. Les composés de l'invention sont en outre utiles pour le traitement des effets secondaires extrapyramidaux associés à l'utilisation d'agents neuroleptiques classiques. Lesdits composés sont de la formule (I) and laquelle (a) représente un noyau aromatique ou alicyclique; R¿1? et R¿2? sont égaux ou différents et représentent hydrogène, alkyle C¿1?-C¿6?, halogène, hydroxy, amino, cyano, nitro, trifluorométhyle, trifluorométhoxy, alcoxy C¿1?-C¿6?, -O¿2?CR', -NHCOR', -COR', -SO¿m?R', R' étant alkyle C¿1?-C¿6?, m étant égal à 0, 1 ou 2; ou R¿1? et R¿2? représentent, indépendamment, -CONR'R'', ou -NR'R'', R' et R'' représentant indépendamment hydrogène ou alkyle C¿1?-C¿6?; R¿3? is hydrogène, alkyle C¿1?-C¿6?, ou -COR''', R''' étant alkyle C¿1?-C¿6?; R¿4? est hydrogène, alkyle C¿1?-C¿6?, et R répresente un groupe azacycloalkyalkyle.

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