Heterocyclyl-ergoline derivatives as 5-ht1a receptor ligands

C - Chemistry – Metallurgy – 07 – D

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C07D 457/02 (2006.01) A61K 31/48 (2006.01) C07D 457/00 (2006.01)

Patent

CA 2243992

Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in .alpha. or .beta. configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.

Dérivé d'ergoline représenté par la formule (I) dans laquelle R¿1? représente un atome d'hydrogène ou un groupe alkyle C¿1?-C¿4?, ou un atome de brome, un groupe méthyle ou alkylthio C¿1?-C¿4?; n est 0, 1 ou 2; le substituant à la position 8 est situé dans une configuration .alpha. ou .beta.; Het représente une chaîne hétérocyclique aromatique à cinq éléments, ladite chaîne possédant trois hétéroatomes qui sont semblables ou différents et qui sont sélectionnés dans le groupe constitué par un atome de soufre, d'oxygène et d'azote et X représente un atome d'hydrogène, de chlore, de brome ou de fluor, ou sel d'apport acide acceptable sur le plan pharmaceutique, efficaces au niveau du système nerveux central. Procédé servant à les préparer et compositions pharmaceutiques les contenant.

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