C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/08 (2006.01) A61K 31/55 (2006.01) A61P 25/18 (2006.01) A61P 25/20 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 25/32 (2006.01)
Patent
CA 2751866
The invention relates to N-[(6-azabicyclo[3.2.1]oct-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C1-C6)alkyl group, (C3-C7)-cycloalkyl, optionally substituted by one or more fluorine, (C3-C7)-cycloalkyl, (C2-C4)alkenyl, phenyl, (C1-C6)alkoxy, hydroxy; R2 is phenyl or naphtyl optionally substituted by one or more halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo-(C1C6)alkyl, NR4R5, (C1-C6)alkylthio, (C1-C6)alkyl-SO2, phenyl or heteroaryl,; R2 is one or more hydrogen or halogen atom, halo-(C1-C6)alkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)alkyl; R3, R4 and R5 are independently a hydrogen atom or a (C1-C6)alkyl group; R6 is a (C1-C6)alkyl group; R4 and R5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C1-C6)alkyl group. The invention also relates to the therapeutic use thereof and to a method for synthesizing same.
La présente invention se rapporte à des dérivés de N-[(6-aza-bicyclo[3.2.1]oct- 1-yl)-aryl-méthyl]-benzamide de formule (I). R représente un atome d'hydrogène ou un groupe (C1-C6)alkyle, (C3-C7)- cycloalkyle, éventuellement substitué par un ou plusieurs fluor, (C3-C7)-cycloalkyle, (C2-C4)alcényle, phényl, (C1-C6)alcoxy, hydroxy; R1 représente un phényle ou naphtyle, éventaellement substitué par un ou plusieurs halogène, (C1-C6)alkyle, (C1- C6)alcoxy, halo-(C1-C6)alkyle, NR4R5, (C1-C6)alkyle-thio, (C1-C6)alkyle-SO2, phényle ou hétéroaryle; R2 représente un ou plusieurs atomes d'hydrogène, d'halogène, halo-(C1-C6)alkyle, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)-cycloalkyl-(C1-C3)alkyle; R3, R4 et R5 représentent indépendamment l'un de l'autre un atome d'hydrogène ou un groupe (C1-C6)alkyle; R6 représente un groupe (C1- C6)alkyle; R4 et R5 peuvent former ensemble un cycle choisi parmi les cycles azétidine, pyrrolidine, pipéridine, morpholine, thiomorpholine, pipérazine, azépine, éventuellement substitué par un groupe (C1-C6)alkyle. Utilisation en thérapeutique et procédé de synthèse.
Dargazanli Gihad
Estenne-Bouhtou Genevieve
Medaisko Florence
Robic
Sanofi
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