New classes of gabaa/bzr ligands

C - Chemistry – Metallurgy – 07 – D

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C07D 513/04 (2006.01) A61K 31/4355 (2006.01) A61K 31/4365 (2006.01) A61K 31/437 (2006.01) A61P 25/00 (2006.01) A61P 25/08 (2006.01) A61P 25/20 (2006.01) A61P 25/22 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2720461

The present invention relates to novel GABA A /BzR ligands of the general formulas (I), (II) and (III) wherein R1 is selected from the group consisting of hydrogen, halogen, haloalkyl having 1-2 carbon atoms, alkoxy having 1 to 3 carbon atoms in the alkyl chain, alkyl having 1 to 3 carbon atoms, and nitro, and R2 is selected from the group consisting of hydrogen, halogen and alkyl having 1 to 2 carbon atoms, as well as the use of these compounds for treating anxiolytic, anticonvulsant, sedative- hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals including pharmaceutical compositions comprising the same

Cette invention a pour objet de nouveaux ligands GABAA/BzR de formules générales (I), (II) et (III). Dans lesdites formules, R1 est choisi dans le groupe constitué par un atome d'hydrogène, un atome d'halogène, un groupe halogénoalkyle ayant de 1 à 2 atomes de carbone, un groupe alcoxy ayant de 1 à 3 atomes de carbone dans la chaîne alkyle, un groupe alkyle ayant de 1 à 3 atomes de carbone, et un groupe nitro, et R2 est choisi dans le groupe constitué par un atome d'hydrogène, un atome d'halogène et un groupe alkyle ayant de 1 à 2 atomes de carbone. L'invention concerne également l'utilisation de ces composés ayant des effets anxiolytiques, anticonvulsifs, sédatifs, hypnotiques, et de relaxation musculaire, et permettant de traiter les états anxiogènes, insomniaques et épileptiques chez les mammifères, et notamment, des compositions pharmaceutiques les contenant.

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