Novel benzo [d] [1,3]-dioxol derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 295/00 (2006.01)

Patent

CA 2616383

The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents.

La présente invention concerne un isotopologue du composé 1 substitué avec du deutérium au niveau du carbone de méthylène du noyau benzodioxol. Les isotopologues de l'invention sont des inhibiteurs sélectifs du recaptage de la sérotonine (ISRS) et présentent des propriétés biopharmaceutiques et métaboliques uniques par comparaison avec le composé 1. Ils peuvent en outre être utilisés pour déterminer avec précision la concentration du composé 1 dans des liquides biologiques et pour déterminer des profils métaboliques du composé 1 et de ses isotopologues. L'invention concerne en outre des compositions comprenant ces isotopologues deutérés ainsi que des méthodes de traitement de maladies et d'affections sensibles à une transmission sérotoninergique neuronale accrue, ces composés étant utilisés de manière isolée ou en combinaison avec des agents additionnels.

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