C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 519/00 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2254755
This invention concerns the compounds of formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; R1 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl; R2, R3 and R4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, C1-6alkylthio, mercapto, amino, mono- and di(C1-6alkyl)amino, carboxyl, C1- 6alkyloxycarbonyl or C1-6alkylcarbonyl; R5 is hydrogen, C1-6alkyl, phenyl or phenylC1-6alkyl; R6 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1- 6alkylthio, or a radical of formula -NR8R9, wherein R8 and R9 are each independently selected from hydrogen C1-6alkyl, phenyl or phenylC1- 6alkyl; R7 is hydrogen or C1-6alkyl; or R6 and R7 taken together may form a bivalent radical of formula -R6-R7-; having central dopamine and serotonin antagonistic activity; their preparation, compositions containing them and their use as a medecine.
L'invention concerne des composés de formule (I), leurs sels d'addition pharmaceutiquement acceptables et leurs formes isomériques du point de vue stéréochimique, dans laquelle Alk est alcanediyle C1-6; R<1> est hydrogène, alkyle C1-6, aryle ou aryl-alkyle C1-6; R<2>, R<3> et R<4> sont choisis indépendamment entre hydrogène, halo, hydroxy, nitro, cyano, alkyle C1-6, alkyloxy C1-6, trifluorométhyle, alkylthio C1-6, mercapto, amino, mono et di(alkyle C1-6)amino, carboxyle, alkyloxycarbonyle C1-6 ou akylcarbonyle C1-6; R<5> est hydrogène, alkyle C1-6, phényle ou phényl-alkyle C1-6; R<6> est hydrogène, alkyle C1-6, alkyloxy C1-6, alkylthio C1-6, ou un radical de formule NR<8>R<9>, dans laquelle R<8> et R<9> sont choisis indépendamment entre hydrogène, alkyle C1-6, phényle ou phényl-alkyle C1-6; R<7> est hydrogène ou alkyle C1-6; ou R<6> et R<7> ensemble peuvent former un radical bivalent de formule R<6>-R<7>. Ces composés ont une activité centrale antagoniste de la dopamine et de la sérotonine. L'invention concerne également leur préparation, ainsi que des compositions les contenant et leur utilisation comme médicaments.
Kennis Ludo Edmond Josephine
Mertens Josephus Carolus
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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