Substituted 1-piperazinylacylpiperidine derivatives, their...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/14 (2006.01) A61K 31/497 (2006.01) A61P 25/28 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2487840

The invention concerns 1-substitued piperazinylacylpiperidine derivatives of general formula (I) (see formula I) wherein: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom, a trifluoromethyl radical, C1-C4 alkyl, a C1-C4 alkoxy, a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom, an -OR5 group, a - CH2OR5 group, a -NR6R7 group; a -NR8COR9 group; a -NR8CONR10R11 group; a -CH2NR12R13 group; a - CH2NR8CONR14R15 group; a C1-C4 alkoxycarbonyl; a -CONR16R17 group; or R3 forms a double bond between the carbon atom whereto it is bound and the neighbouring carbon atom of the piperidine cycle; R4 represents an aromatic group selected among (see formula II); (see formula III); (see formula IV); (see formula V); (see formula VI); (see formula VII); said aromatic groups being unsubstituted, monosubstituted or disubstituted by a substituent selected independently among a halogen atom, a C1-C4 alkyl, a C1- C4 alkoxy, a trifluoromethly radical. The invention also concerns a method for preparing said compounds and their therapeutic use.

L'invention concerne des dérivés de 1-piperazinylacylpipéridine substitués, de formule générale (I), dans laquelle: n est 1 ou 2; p est 1 ou 2; R1 représente un atome d'halogène; un radical trifluorométhyle; un (C1-C4)alkyle; un (C1- C4)alcoxy; un radical trifluorométhoxy; R2 représente un atome d'hydrogène ou un atome d'halogène; R3 représente un atome d'hydrogène; un groupe -OR5; un groupe -CH2OR5; un groupe -NR6R7; un groupe -NR8COR9; un groupe -NR8CONR10R11; un groupe -CH2NR12R13; un groupe -CH2NR8CONR14R15; un (C1-C4)alcoxycarbonyle; un groupe -CONR16R17; ou bien R3 constitue une double liaison entre l'atome de carbone auquel il est lié et l'atome de carbone voisin du cycle pipéridine; R4 représente un groupe aromatique choisi parmi (II); lesdits groupes aromatiques étant non subtitués, mono- ou disubstitués par un substituant choisi indépendamment parmi un atome d'halogène; un (C1-C4)alkyle; un (C1-C4)alcoxy; un radical trifluorométhyle. Procédé de préparation et application en thérapeutique.

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