Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1995-09-20
1998-01-13
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514863, A61K 3120
Patent
active
057080283
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
This application is a 371 of PCT/EP94/00941 Mar. 24, 1994.
The invention relates to new uses of cis-9-heptadecenoic acid.
Saturated and unsaturated fatty acids are constituents of the cell membrane of cells. The concentration of unsaturated fatty acids plays a role in the barrier properties of the skin and in the reactivity of calls in inflammatory processes.
An anti-inflammatory and oedema-inhibiting action has been described for the monounsaturated fatty acid cis-9-heptadecenoic acid in German Auslegeschriften 1 195 296 and 1 147 221. It is said to have an activity in cases of acute and chronic dermatitis, in particular on burn wounds and in the treatment of "Ulcera cruris". A reduction of an induced granuloma tissue in the rat under the influence of cis-9-heptadecenoic acid and an inactivity of oleic acid in this test set-up has been reported. This is in contrast to the findings of Gor'kova et al. (Chemical Abstracts Vol. 68, (1968) 1909 u), who found an activity of oleic acid and an increased cellular infiltrate in an induced granuloma in the rat under the influence of cis-9-heptadecenoic acid.
Surprisingly, it has now been found that cis-9-hepta-1-decenoic acid is active on psoriasis, allergies and autoimmune diseases.
The invention relates to the use of cis-9-heptadecenoic acid and/or its salts for the prophylaxis and treatment of psoriasis, allergies and autoimmune diseases.
cis-9-Heptadecenoic acid is known and is obtainable by known processes or by isolation from animal tissue. Physiologically tolerated salts of cis-9-heptadecenoic acid are preferred.
The term psoriasis means this skin disease in all its manifestations.
Allergies are, in particular, atopy and contact allergies. Atopy manifests itself, for example, as allergic conjunctivitis, allergic rhinitis, allergic asthma or neurodermatitis.
Autoimmune diseases are, in particular, the diseases of the rheumatic type.
Surprisingly, the active compounds according to the invention are active against diseases which are so different in principle, such as psoriasis, allergies and autoimmune diseases.
For prophylaxis, the active compounds are administered to lessen the incidence and intensity of manifestations of the diseases. Treatment in the manifest stage leads to shortening thereof and to alleviation of the symptoms. cis-9-Heptadecenoic acid can suppress or reduce the release of important triggering mediators, such as TNF.alpha..
Water-soluble salts of cis-9-heptadecenoic acid, in particular the alkali metal salts, for example the sodium salt or the potassium salt, and also the ammonium salt, are preferred. The calcium, magnesium and aluminium salt and also the salts of organic bases, for example amines, such as ethanolamine, ethylenediamine and morpholine, are also suitable.
Pharmaceutical preparations, agents or compositions which comprise the compound according to the invention or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable diluent or carrier are also provided according to the invention.
The compounds of the present invention can be used on humans orally or parenterally, for example in a dosage of 0.05 to 500 mg, preferably 0.5 to 50 mg, particularly preferably 0.1 to 10 mg per day, and in particular also in subdivided doses, for example two to four times daily.
The compounds according to the invention can also be incorporated without problems into customary pharmaceutical and cosmetic bases for topical applications, and the corresponding topical pharmaceutical and cosmetic formulations or compositions are thus obtained. They are preferably employed in amounts of 0.001 to 10% by weight, in particular in amounts of 0.01 to 1% by weight, in each case based on the total weight of the topical composition. The formulations can be used several times daily in the customary manner.
The invention also relates to the use of the active compounds according to the invention for the preparation of pharmaceutical compositions and topical pharmaceutical and cosmetic compositions for the prophylaxis and tr
REFERENCES:
HCAPLUS Abstract 1993: 66867, Martin (1992).
Degwert Joachim
Jacob Jurgen
Steckel Friedhelm
Beiersdorf AG
Cintins Marianne M.
Moezie M.
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