Sulphur-containing phospholipids, their preparation and use

C - Chemistry – Metallurgy – 07 – F

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260/460.2, 260/4

C07F 9/09 (2006.01) C07F 9/10 (2006.01) C07F 9/165 (2006.01)

Patent

CA 1174244

ABSTRACT The present invention provides alkanol phosphoric acid monoammonium alkyl esters of the general formula: Image (I) wherein X is a valency bond, an oxygen or sulphur atom, a sulphinyl or sulphonyl group, an aminocarbonyl, carbonylamino or ureido group or a cycloalkylene or phenylene radical, Y is an oxygen or sulphur atom, R1 is a hydrogen atom, a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which can be substit- uted one or more times by aryl, halogen, lower alkoxy, alkylthio, alkoxycarbonyl, alkanesulphiny or alkane- sulphony, R2 is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing up to 18 carbon atoms, which can be sub- stituted one or more times by halogen, aryl, lower alkoxy, alkoxycarbonyl, alkylthio, alkanesuphinyl or alkanesulphonyl, R3 is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing 2 - 0 carbon atoms, which can also be part of a cycloalkane ring and can be substituted one or more times by hydroxyl, halogen, nitrile, cycloalkyl, phenyl, alkoxycarbonyl, optionally alkylated carbamoyl, alkylthio, alkanesulphinyl, alkanesulphonyl, optionally acylated amino or by alkoxy which, in turn, can be substituted by aryl, alkylthio, alkanesulphinyl, alkanesulphonyl, optionally acylated amino, alkoxy- carbonyl, nitrile, hydroxyl, alkoxy or optionally alkylated carbamoyl, R4 is a straight-chained or branched alkylene chain containing 2 to 4 carbon atoms, R5 is a hydrogen atom or a lower alkyl radical and n is 0, 1 or 2; as well as the pharmacologically accept- able salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for combating cancer.

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