Boehringer Mannheim Gmbh

Boehringer Mannehim Gmbh

Wulf Pahlke

Elmar Bosies

Uwe Bicker

Rudi Gall

Gunter Weimann

Dieter Herrmann

Christos Tsaklakidis

Rainer Haag

Michael Schultz

Richard Endele

The present invention provides [3-(C.sub.16 -C.sub.18)-alkaesulphinyl- and -sulphonyl-2-methoxy-methylpropyl]-(2-trimethylammonioethyl) phosphates having superior anti-tumor activity.

[3-(C.sub.16 -C.sub.18)-alkanesulphinyl and

A method of selectively suppressing the excess immune reaction produced iatrogenically or autochthonously by administering 0.1 to 100 mg of ciamexone per kg of body weight.

Ciamexone as a selective immunosuppressant

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.

Imidazolidine derivatives as immunosuppressives

The present invention is concerned with N- substituted aziridine-2-carboxylic acid derivatives, with pharmaceutical compositions containing these compounds and their immuno-stimulating and immuno-modulating activities.

N-substituted aziridine-2-carboxylic acid derivatives, processes for the

The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.3 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, which can also be part of a cycloalkane ring system and is optionally substituted one or more times by hydroxyl, halogen, alkylthio, alkanesulphinyl, alkanesulfonyl, nitrile, alkoxycarbonyl, carboxamido optionally substituted by alkyl radicals, cycoalkyl, optionally substituted phenyl or alkoxy, which in turn is optionally substituted by phenyl, hydroxyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, optionally acylated amino, alkoxycarbonyl, nitrile or carboxamido optionally substituted by alkyl radicals, Z is an oxygen or sulfur atom, R.sub.4 is a straight-chained or branched alkylene radical containing 2 to 5 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl radical, with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together represent an unsubstituted, straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon chain containing up to 18 carbon atoms, Y, R.sub.4 and R.sub.5 have the above-given meanings and Z is an oxygen atom, R.sub.3 cannot be a propylene or 2-methylpropylene chain optionally substituted by hydroxyl, alkoxy or benzyloxy and with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together signify an alkyl radical containing up to 18 carbon atoms and substituted by halogen or phenyl, Y and Z are oxygen atoms and R.sub.4 and R.sub.5 have the above-given meanings, R.sub.3 cannot be a propylene or 2-hydroxypropylene chain; and the pharmacologically acceptable salts thereof. The invention also provides pharmaceutical compositions containing such compounds, having cancerostatic action without inducing thrombocyte aggregation.

Phospholipid compound

Sulfur-containing phospholipid compounds of the formula ##STR1## pharmaceutical compositions having anti-tumor activity which include said phospholipid compounds, and the method of use for combating tumors, of said phospholipid compounds.

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Mannheim, Germany

Wulf Pahlke