Antipsychotic 4-(1h-indolyl-1-yl)-1-substituted piperidine...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 513/04 (2006.01) A61K 31/445 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) C07D 401/14 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2210913

The present invention concerns the compounds of formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R1 and R2 are each independently hydrogen, halogen, C1-6alkyl or C1-6alkyloxy; R3 and R4 are each independently hydrogen, C1- 6alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C1- 6alkyl, C1-6alkyloxy, C1-6alkylthio, mercapto, amino, mono- and di(C1-6alkyl)-amino, carboxyl, C1-6alkyloxycarbonyl and C1-6alkylcarbonyl; Alk is C1-4alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.

L'invention concerne les composés de la formule (I), leurs sels d'addition pharmaceutiquement acceptables ainsi que leurs formes stéréochimiquement isomères, formule dans laquelle la ligne pointillée désigne une liaison optionnelle, R<1> et R<2> représentent chacun indépendamment hydrogène, halogène, alkyle C1-6 ou alkyloxy C1-6; R<3> et R<4> représentent chacun indépendamment hydrogène, alkyle C1-6, phényle ou phényle présentant 1, 2 ou 3 substituants choisis parmi halo, hydroxy, nitro, cyano, triflurométhyle, alkyle C1-6, alkyloxy C1-6, alkylthio C1-6, mercapto, amino, mono et di(alkyle C1-6)-amino, carboxyle, alkyloxycarbonyle C1-6 et alkylcarbonyle C1-6; Alk représente alcanediyle C1-4; D représente une pyrimidinone, une piperidone ou une benzimidozolidinone. Ces composés présentent une activité neuroleptique. L'invention concerne également leur préparation, des compositions les contenant ainsi que leur utilisation en tant que médicaments.

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