Boehringer Mannheim Gmbh

Michael Schultz

Wolfgang Bartsch

Helmut Michel

Herbert Simon

Christos Tsaklakidis

Elmar Bosies

Dieter Herrmann

Wulf Pahlke

Rainer Haag

The present invention provides anti-angina pharmaceutical compositions containing at least one compound of the formula: ##STR1## wherein n is 1 or 2, R is a hydrogen atom or an H--(C.sub.1 -C.sub.8)-alkylene, hydroxy-(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N--(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N--(C.sub.1 -C.sub.8)-alkylene-CO--, R.sup.1 R.sup.2 N--CO--NR.sup.3 --(C.sub.1 -C.sub.8)-alkylene or R.sup.1 R.sup.2 N--CO-- radical, A is a valency bond or an --NR.sup.4 --CO-- or --CO-- NR.sup.4 -- radical, R.sup.4 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated or cyclic alkyl radical containing up to 6 carbon atoms and B is a valency bond or a straight-chained or branched alkylene chain containing up to 8 carbon atoms, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms.

Cyclic azaaliphatic compounds with a nitroxy function, processes for the

The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.3 is a hydrogen atom or a lower-alkyl radical, when X is an --NR.sup.3 --CO-- radical, R.sup.3, together with the nitrogen atom and a carbon atom of the group A, bridge a heterocyclic ring containing 4 to 6 carbon atoms or R.sup.3, together with R.sup.2, A and the two nitrogen atoms, bridge a heterocyclic ring containing 3 to 5 carbon atoms; and the optically-active forms and physiologically acceptable salts thereof.

Pharmaceutical compositions containing nitroxyalkylamines, novel

The present invention provides anti-angina pharmaceutical compositions containing at least one compound of the formula: ##STR1## wherein n is 1 or 2, R is a hydrogen atom or an H-(C.sub.1 -C.sub.8)-alkylene, hydroxy-(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N-(C.sub.1 -C.sub.8)-alkylene, R.sup.1 R.sup.2 N-(C.sub.1 -C.sub.8)-alkylene-CO--, R.sup.1 R.sup.2 N-CO-NR.sup.3 -(C.sub.1 -C.sub.8)-alkylene or R.sup.1 R.sup.2 N-CO-- radical, A is a valency bond or an --NR.sup.4 --CO-- or --CO--NR.sup.4 -- radical, R.sup.4 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated of cyclic alkyl radical containing up to 6 carbon atoms and B is a valency bond or a straight-chained or branched alkylene chain containing up to 8 carbon atoms, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms.

The present invention provides compounds of the general formulae: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.5 -alkyl radicals, C.sub.3 -C.sub.5 -alkenyl radicals or phenyl radicals or, together with the carbon atom to which they are attached, form a saturated or unsaturated C.sub.3 -C.sub.7 ring, R.sub.3 and R.sub.4, which can be the same or different, are hydrogen atoms, straight-chained or branched C.sub.1 -C.sub.10 -alkyl radicals, straight-chained or branched C.sub.3 -C.sub.7 -alkenyl radicals, C.sub.3 -C.sub.7 -cycloalkyl radicals, C.sub.3 -C.sub.7 -cycloalkenyl radicals, phenyl, arylalkyl or hetarylalkyl radicals, R.sub.5 is a hydrogen atom or a lower alkyl radical and X is an oxygen or sulphur atom or an imino group. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions with immunosuppressive action containing them.

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Mannheim, Germany

Michael Schultz