Compounds which are derivatives of the beta - carbolines ligands of the receiver with an agonist effect of benzodiazepines and other screw - to - of benzodiazepines and medicinal products containing them.

摘要

New compounds derived from beta -carbolines and which are ligands of the benzodiazepine receptor having an antagonist and reverse agonist effect with respect to benzodiazepines. These compounds correspond to the formulae: …IMAGE… in which: … …  X is O, S, …IMAGE… …  or else …IMAGE… …  represents the radical -N(R6)-C(=O)-CH2-X, …  R1 is a hydroxyl or alkoxy radical or an alkyl radical substituted by a hydroxyl or alkoxy radical, …  R2 is a hydrogen atom or an alkyl, hydroxyl, alkoxy, acyloxy or benzyloxy radical, it being possible for the said radicals to be optionally substituted, …  R3, R4, R5 and R6 are chosen from the hydrogen atom or an alkyl radical, optionally substituted by a hydroxyl, alkoxy or alkoxycarbonylmethyl radical, … as well as the corresponding tetrahydro derivatives of beta -carboline and the pharmaceutically acceptable salts or quaternary ammonium derivatives of these compounds.