Indolo-(3,2-b)-quinuclidine derivs. - are useful as antidepressants and anxiolytics

摘要

Quinuclidine derivs. for formula (I) and their salts with acids and bases are new, (R1=H, opt. branched, opt. substd. alkyl or opt. branched 4-14C cycloalkylalkyl(in both cases an alkyl CH2 can be replaced by O and/or opt. substd. N and/or CO), or opt. branched aralkyl or aralkenyl (in the alkylene chain a CH2 can be replaced by O, CO or opt. substd. N), or R1 is opt. substd. aryl or opt. branched, opt. substd. heterocyclyl=alkyl having 3-8 ring members with 1 or 2 of them S, O or opt..substd. N. R21R31R4 and R5=H, opt. branched and opt. substd. lower alkyl or alkoxy, 3-7C cyclo=alkyl, opt. substd. aryl, halo NO2, lower alkylthio, OH, opt. substd. aryloxy or aralkoxy a 3-7 membered heterocycle with 1 or 2 hetero=atoms, COOH (opt. substd. by alkyl, aralkyl, aryl or cycloalkyl) or is carbamido or sulphonomido both opt. substd. by alkyl, aralkyl, aryl or cycloalkyl). They are made by reacting the appropriate phenylhydrazine hydrochloride with 3-quinuclidinone. (I) have CNS, esp antidepressant and anxiolytic, activity and are more effective and less toxic than e.g. nomifensin. They are administered at 0.3-3, esp. 1-2, mg/kg per day in unit doses of esp. 0.3-0.6 mg/kg.