Pyrazolo (3,4-c) and thiazolo (5,4-c) isoquinolines, methods for preparing them, these compounds for use as antiinflammatory, CNS-depressant and anti-anxiety agents and pharmaceutical compositions thereof

摘要

New tricyclic ortho-fused heterocyclic compounds of formula IMAGE I wherein A is the group IMAGE (a) or the group IMAGE (b) in which R represents hydrogen, (C1-4)alkyl, phenyl or tolyl and R1 and may be (C1-4)alkyl, phenyl or tolyl, R2 is selected from (C1-4)alkyl, (C2-4)alkanoylmethyl, carbo(C1-3)alkoxymethyl, hydroxy(C2-4)alkyl, halo(C2-4)alkyl and a group IMAGE wherein R3 is an alkylene group from 2 to 4 carbon atoms and R4 and R5 independently represent hydrogen or (C1-4)alkyl or, taken together with the nitrogen atom, a fully hydrogenated 5 or 6 membered heterocyclic radical which may contain a further heteroatom selected from O, N and S and be optionally substituted by a (C1-4)alkyl or phenyl group, or R2 may represent, nil the dotted lines x and y may represent nil or additional bonds; with the proviso that, when the symbol R2 linked to the oxygen atom is different from nil, x is an additional bond and y and the other symbol R2 represent nil; with the further proviso that, when the symbol R2 linked to the nitrogen atom is different from nil, y is an additional bond and x and the other symbol R2 represent nil; and salts therewith of pharmaceutically acceptable acids. The compounds possess antiinflammatory, CNS-depressent and anti-anxiety utility.