2-alkyl-(2-amino-3-aryl-propionyl)-piperazine derivatives...

Details 2-alkyl-(2-amino-3-aryl-propionyl)-piperazine derivatives... 2-alkyl-(2-amino-3-aryl-propionyl)-piperazine derivatives...

C - Chemistry, Metallurgy

07

D

C07D 403/12 (2006.01) C07D 241/04 (2006.01) C07D 241/08 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2501231

The present invention relates to compounds which comprise a nitrogen- containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1-C12 linear or branched alkyl, C3-C8 cyclic alkyl, C2- C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3- alkylpiperazines having the formula (I): wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, -CO2H, - CONH2, -CONHCH3, and -CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl..

La présente invention se rapporte à des composés qui possèdent un squelette sous forme de cycle contenant de l'azote, substitué par une unité alkyle R?1¿ sélectionnée parmi alkyle C¿1?-C¿12? linéaire ou ramifié, alkyle C¿3?-C¿8? cyclique, alcényle C¿2?-C¿12? linéaire ou ramifié, ou haloalkyle, c'est-à-dire, par exemple, aux 2-kéto-3-alkylpipérazines représentées par la formule (I). Dans ladite formule : R est sélectionné parmi phényle, 3-fluorophényle, 4-fluorophényle, 3,5-difluorophényle, et 4-chlorophényle ; R?1¿ est sélectionné parmi méthyle, éthyle, propyle, iso-propyle, butyle, iso-butyle, sec-butyle, tert-butyle, cyclopropyle, cyclopropylméthyle, cyclopentyle, cyclopentylméthyle, cyclohexyle, clohexylméthyle, benzyle, allyle, 1-méthylallyle, 2-méthylallyle, but-2-ényle, et propargyle ; R?7a¿ est sélectionné parmi hydrogène, -CO¿2?H, -CONH¿2?, -CONHCH¿3?, and -CON(CH¿3?)¿2?; R?8¿ représente benzyle, benzyle substitué, ou naphthalén-2-ylméthyle.

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