Tetrahydrocarbazole derivatives with biological action and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/82 (2006.01) A61K 31/403 (2006.01) A61P 15/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2565850

The present invention provides novel tetrahydrocarbazole derivatives of formula (I) which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathoblochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human. (see formula I)

La présente invention concerne de nouveaux dérivés de tétrahydrocarbazole améliorés du point de vue de leurs propriétés, lesquels dérivés peuvent être utilisés comme inhibiteurs de récepteurs couplés aux protéines G (RCPGs). Ces nouveaux composés permettent ainsi de traiter des états pathologiques dont la manifestation dépend de l'effet pathobiochimique de RCPGs. En particulier, les composés selon l'invention ont un effet sur une inhibition antagoniste du récepteur de LHRH. Cette invention concerne également des médicaments contenant comme principe actif un ou plusieurs de ces nouveaux composés. Ces médicaments sont particulièrement appropriés pour être utilisés sur l'homme ou sur des mammifères sous une forme pour administration orale.

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