Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1987-05-21
1988-10-18
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
A61U 31685
Patent
active
047787880
DESCRIPTION:
BRIEF SUMMARY
The invention concerns the use of compounds of the lysolecithine type as an agent against multiple sclerosis.
In DE-OS 20 09 342 and DE-OS 20 09 343, the use of synthetic lysolecithine compounds is described to increase resistance and an immunological adjuvants. Moreover, from DE-OS 26 19 686 the effectiveness of such compounds as antitumor agents is known. In addition, after the application of lysophosphatides there is a formation of activated cells which are capable of increasing the resistance of the body to harmful influences.
It has now surprisingly been found that lysolecithine analogues having the general formula I demonstrate good effectiveness in the treatment of multiple sclerosis.
The subject of the invention is therefore the use of a compound of the general formula I ##STR2## in which R.sub.1 is alkyl having from 12 to 18, and in particular from 16 to 18 carbon atoms, R.sub.2 is alkyl having from 1 to 8 carbon atoms, R.sub.3 is H or alkyl having from 1 to 3 carbon atoms, as an agent against multiple sclerosis.
An alkyl group R.sub.1, R.sub.2 and/or R.sub.3 can be branched, and is prefereably straight-chained.
In a compound of the general formula I, R.sub.2 is preferably an alkyl radical with from 1 to 3 carbon atoms, and especially methyl, and/or R.sub.3 is preferably H.
Preferred compounds are, in particular, the compound of formula I where R.sub.1 =n-hexadecyl, and R.sub.2 =methyl and where R.sub.3 =H (compound II) and primarily the compound of the formula I where R.sub.1 =n-octadecyl, and R.sub.2 =methyl and R.sub.3 =H (compound III).
The preparation of the compounds according to formula I can be performed in one of the ways which have been described in the literature; compare, for example, D. Arnold et al, Liebig's Ann. Chem. 709, 234-239 (1967); H. U. Weltzien and O. Westphal, Liebig's Ann. Chem. 709, 240-243 (1967); and H. Eibl and O. Westphal, Liebig's Ann. Chem. 709, 244-247 (1967).
Multiple sclerosis (MS), one of the most frequent nerve diseases, is an autoimmune illness in which T-lymphocytes penetrate into the nerve substance decompose the myelin there.
MS can be artificially generated in animal tests, in that the so-called basic protein is extracted from myelin, and this basic protein is injected into test animals (mice) with complete Freund adjuvant. After from 5 to 7 days, lymphocytes are extracted from the animals. The lymphocytes which are extracted from the animal can initiate MS when they are administered to a test animal, in which process at least 10.sup.6 -T-cells per animal must be administered (compare Ben-Nun A., Wekerle and Cohen I. R. The rapid isolation of clonable antigen specific T-lymphocyte capable of mediating autoimmune encephalomyletitis Eur. J. Immunology (1981), 11 195).
If now a compound according to the invention having general formula I, for example the compound III, is administered to the animals, the MS symptoms can be removed. Hence it can be concluded that the compounds in accordance with the invention evidently de-activate those T-cell clones in some way which have developed the specificity which causes the MS symptoms against myelin or basic protein.
Moreover, in the case of humans suffering from MS, after the administration of the compound III, a clear improvement of the MS symptoms was observed: in the case of oral administration (solution of compound III in liquids containing lipoprotein, for example in milk), after a daily administration of 200 .mu.g for a period of several weeks and subsequent transition to administration only every second day of 200 .mu.g, there was complete freedom from the complaint which could be maintained, which, for example, was expressed in the capability for completely normal motion, driving automobiles etc.
The application of the substances according to the invention can, as a rule, be carried out in the conventional manner, for example by means of the administration of such compounds as antitumor agents, i.e. for example intravenously, perorally or as an infusion; oral administration is, as a rule, the preferred type o
Friedman Stanley J.
Max-Planck-Gesellschaft zur Foerderung der Wissenschaften
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