Compounds for inhibition of 5-hydroxytryptamine and...

C - Chemistry – Metallurgy – 07 – C

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C07C 215/42 (2006.01) A61K 31/222 (2006.01) A61P 25/00 (2006.01) C07C 217/60 (2006.01) C07C 219/24 (2006.01)

Patent

CA 2612413

Compounds of the general formula (I), optical isomers, pharmaceutically acceptable salts, preparation process and uses thereof in which R1, R2, R3 and R4 are as defined in specification are disclosed. Such compounds can be optical isomers or racemic mixtures and can be metabolically transformated into 1-[2-dimethylamine-1-(4-hydroxyphenyl)-ethyl]cyclohexanol with new pharmaceutically active in vivo after administration, which can be used for treating diseases associated central nervous system such as depression et al. by interrupting reuptake of 5-hydroxytryptamine (5-HT ) and norepinephrine (NA ) .

La présente invention concerne des composés de la formule générale (I), des isomères optiques, des sels pharmaceutiquement acceptables, un procédé de préparation et leurs utilisations, dans laquelle R1, R2, R3 et R4 sont tels que définis dans la description. De tels composés peuvent être des isomères optiques ou des mélanges racémiques pouvant être transformés métaboliquement en 1-[2-diméthylamine-1-(4-hydroxyphényl)-éthyl]cyclohexanol présentant une nouvelle activité pharmaceutique in-vivo après administration, permettant une utilisation dans le traitement de pathologies associées au système nerveux central telles que la dépression et al. en interrompant le recaptage de la 5-hydroxytryptamine (5-HT) et de la norépinéphrine (NA ).

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