Anellated .beta.-carbolines

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/14 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) A61K 31/695 (2006.01) C07D 471/04 (2006.01) C07D 491/147 (2006.01) C07D 495/14 (2006.01) C07D 498/14 (2006.01) C07D 513/14 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2217719

Described are compounds of formula (I), wherein A is a 5-6 membered unsaturated ring in which 1-2 C atoms can be substituted by N, O and/or S and which can be substituted with R5 and R6, and the method for preparing them. Because of their affinity for benzodiazepine receptors, the compounds of formula (I) as well as their salts can be used as drugs. They have different intrinsic efficacy (i.e. agonistic, antagonistic and/or inversely agonistic efficacy) with different isoforms of the GABA benzodiazepine receptor.

L'invention concerne des composés de la formule (I) dans laquelle A désigne un composé cyclique insaturé à 5 ou 6 chaînons, dans lequel 1 à 2 atomes de C peuvent être substitués par N, O et/ou S, et qui peut être substitué par R?5¿ et R?6¿. L'invention concerne également leur procédé de préparation. Les composés de la formule (I) et leurs sels s'utilisent comme médicaments en raison de leur affinité envers les récepteurs de benzodiazépine. Ces composés présentent une efficacité intrinsèque différenciée (c.-à-d. efficacité agoniste, antagoniste et/ou inversement agoniste) sur diverses isoformes du récepteur de GABA-benzodiazépine.

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