Deutsche Gold- Und Silber-scheideanstalt Vormals Roessler

Asta Medica, Aktiengesellschaft

Karl-Heinz Klingler

Jurgen Engel

Bernhard Kutscher

Stefan Szelenyi

Hans-Reinhold Dieter

Erich Bickel

Jurgen Schmidt

Peter Metzenauer

Ute Achterath-Tuckermann

Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R.sub.1 is C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.3 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkanoyloxy, benzoyloxy, morpholinocarbonyloxy, C.sub.1 -C.sub.6 -alkyloxycarbonyloxy, C.sub.1 -C.sub.6 -alkylaminocarbonyloxy, C.sub.1 -C.sub.6 -dialkylaminocarbonyloxy or the group -Alk-A, where Alk represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -hydroxyalkyl or C.sub.3 -C.sub.6 -cycloalkyl and the symbol A represents hydrogen or other substituents. R.sub.2, R.sub.3 and R.sub.4 represent various substituents, where R.sub.1 may also be hydrogen, when R.sub.2 is the group ##STR2## and R.sub.5 represents phenyl, C.sub.1 -C.sub.4 -alkoxyphenyl or diphenylmethyl and R.sub.3 and R.sub.4 are hydrogen and their salts. The compounds provide anti-allergic, anti-asthmatic, anxiolytic and hypotensive effects.

4,5-dihydro-4-oxo-pyrrolo[1,2-a]quinoxalinones and corresponding aza

Basic substituted alkyl theophylline derivatives of the formula ##STR1## in which Alk is a straight or branched chain alkylene group with 2 to 4 carbon atoms and R is hydrogen or a methyl group are produced by catalytic hydrogenation of compounds of the formula ##STR2## where the phenolic hydroxyl groups and/or the secondary basic nitrogen atom can contain protective groups using as the solvent a compound of the formula ##STR3## where R', R' and R'' are the same or different and are alkyl groups of 1 to 2 carbon atoms and R' together with R'' can also be an alkylene bridge with 3 to 4 carbon atoms and in a given case the protective groups present are split off.

Process for the production of basic substituted alkyl theophylline

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Langen, Germany

Karl-Heinz Klingler