2,3A-DIAZAHYDRINDANONE AND 3H-PYRIDO-(1,2-C)PYRIMIDIN-3-ONE DERIVATIVES

摘要

Novel compounds of general formula FORM:1114397/C2/1 and salts thereof, wherein n is 0 or 1 and R is C1- 7 alkyl, optionally substituted by one or more OH,NH2, mono or dialkylamino, halo or heterocyclic substituents, or is aryl or aralkyl either of which groups may be substituted by one or more halo, NO2, NH2, OH, C1- 7 alkyl, C1- 7 alkoxy, C1- 7 aminoalkyl which may be N-substituted by one or two alkyl groups, CF3, C2- 7 alkoxycarbonyl, acyl or C2- 7 alkanoylamido substituents, are prepared by reacting an amide of general formula FORM:1114397/C2/2 with formaldehyde and introducing or modifying the group R if desired and optionally converting any base into a salt. The amides of the last general formula above or salts thereof are obtained by condensing an acid of general formula FORM:1114397/C2/3 with ammonia or an amine of formula RNH2 and removing the N-benzyloxycarbonyl group. Pharmaceutical compositions having analgesic, antiphlogistic, inflammation-inhibiting and anti-allergic activity and in conventional forms for oral, rectal, topical, percutaneous or parenteral administration comprise an above novel compound and a compatible pharmaceutical carrier, optionally with usual additives.