Drug – bio-affecting and body treating compositions – Topical body preparation containing solid synthetic organic... – Anti-inflammatory or anti-irritant
Reexamination Certificate
2000-04-17
2003-07-08
Dees, Jose′ G. (Department: 1619)
Drug, bio-affecting and body treating compositions
Topical body preparation containing solid synthetic organic...
Anti-inflammatory or anti-irritant
C424S401000, C424S078020, C424S078030, C514S887000, C514S937000
Reexamination Certificate
active
06589520
ABSTRACT:
The invention relates to novel compounds of cis-6-hexadec-1-enoic acid or its derivatives. It is also called cis-hexadec-6-enoic acid or delta-6-hexadecenoic acid.
BACKGROUND OF THE INVENTION
Saturated and unsaturated fatty acids are constituents of the cell membrane of cells. The concentration of unsaturated fatty acids plays a part in the barrier properties of the skin and in the reactivity of cells in inflammatory processes.
Thus it is already known to use cis-9-heptadecenoic acid for the treatment of psoriasis, allergies and auto-immune disorders (DE-A-4309512).
cis-6-Hexadecenoic acid has already been proposed for softening the skin in cosmetic and dermatological preparations (U.S. Pat. No. 4,036,991). It has also already been described in the literature that cis-hexadecenoic acid is a constituent of human sebaceous matter and psoriasis flakes (Jacob et al., Z. Klin. Chem. Klin. Biochem., 11th year, (1973), 297-300). A combination of neutral lipids with cis-6-hexadecenoic acid can be used for the treatment of dry skin (DE-A-4131940).
Surprisingly, it has been found that cis-6-hexadec-1-enoic acid is effective in psoriasis, allergies and auto-immune disorders as well as on dry skin and on sensitive skin.
SUMMARY OF THE INVENTION
The invention relates to the use of cis-6-hexadecenoic acid or its derivatives as an active compound for the prophylaxis and treatment of psoriasis, allergies and auto-immune disorders as well as on dry skin and on sensitive skin.
Topical application is preferred.
DETAILED DESCRIPTION
Highly suitable derivatives are the salts and esters of cis-6-hexadecenoic acid, which are preferred, and natural substances which contain this acid and its derivatives, which are also called derivatives here.
Preferred esters are the mono-, di- or trglycerides of cis-hexadecenoic acid, mixed glycerides which contain at least one further carboxylic acid or fatty acid, the mono- or di-cis-6-hexadecenoic acid esters with ethylene glycol and/or propylene glycol, where in each case one or more moles of glycol per mole or two moles of cis-hexadecenoic acid can be contained and cis-6-hexadecenoic acid esters with straight-chain or branched mono-alcohols having, for example, 1 to 22 carbon atoms, in particular 12 to 20 carbon atoms, in the alkyl radical.
Further carboxylic acids or fatty acids of the mixed triglycerides can contain, for example, 1 to 22, preferably 12 to 22, carbon atoms and can be saturated or unsaturated and then have, for example, 1 to 5, preferably 1 to 3, double bonds.
Suitable mono- or diesters with ethylene glycol and/or propylene glycol can contain, for example, 1 to 50, preferably 5 to 40, in particular 10 to 30, mol of glycol per mole of the respective ester.
cis-6-Hexadecenoic acid is the main constituent (85% by weight as the triglyceride) of the oil obtained from the seeds of Thunbergia alata, “black-eyed Susan” (G.F. Spencer et al., Lipids, Vol. 6, No. 10 and U.S. Pat. No. 4,036,991).
According to the invention, the natural triglycerides of the seed oil of Thunbergia alata with cis-6-hexadecenoic acid can preferably be used.
According to the invention, the seed oil of Thunbergia alata can also advantageously be used as a natural substance. It is thus, for example, not necessary to isolate the cis-6-hexadecenoic acid or its derivatives. It is also possible to use the active compounds according to the invention and in particular the seed oil of Thunbergia alata in pure form without further additives.
The oil can be obtained from the seeds in a simple manner, e.g. as described in the respected literature. The cis-6-hexadecenoic acid can then be obtained from the oil according to known processes, for example by ester cleavage, and from this in turn the derivatives according to the invention can be obtained by known processes.
The name psoriasis means this skin disorder of all types.
Allergies are, in particular, atopy and contact allergies. Atopy is manifested, for example, as allergic conjunctivitis, allergic rhinitis, allergic asthma or in particular neurodermatitis.
Auto-immune disorders are, in particular, the disorders of the rheumatic type.
Surprisingly, the active compounds according to the invention are effective against very different diseases such as psoriasis, allergies and auto-immune disorders, and on dry skin and on sensitive skin.
The active compounds according to the invention are distinguished by a strong anti-inflammatory action.
For prophylaxis, the active compounds are administered in order to decrease manifestations of the disease in frequency and strength. Treatment in the manifest stage leads to its curtailment and to the alleviation of the symptoms.
Even in the case of dry and sensitive skin, the active compounds can be used prophylatically and for the treatment of the disorders.
Dry skin is, on the one hand, skin which lacks an adequate or normal moisture content, but on the other hand also skin which suffers from structural damage and functional disorders in the epidermis and dermis, e.g. in addition to dryness with chapping and formation of dryness folds, pruritus and decreased refatting by sebaceous glands (for example after washing). The term “dry skin” also includes “senile xerosis”.
The active compounds according to the invention can also be used in the case of sensitive skin, in particular against neurosensory phenomena, e.g. “stinging”.
The epidermis is richly equipped with nerves and peripheroceptors such as Vater-Pacini lamellated corpuscles, Merkel cell neurite complexes and free nerve endings for sensation of pain, cold, heat and itching.
In humans with sensitive or easily injured skin, a neurosensory phenomenon called “stinging” (“sting=injure, bum, hurt) can therefore be observed. This “sensitive skin” differs basically from “dry skin” with thickened and indurated horny layers.
Typical reactions of “stinging” on sensitive skin are reddening, tautening and burning of the skin and also itching.
A further neurosensory phenomenon is to be regarded as itching in the case of atopic skin, and also itching in the case of skin disorders.
According to the invention, it is therefore possible to make available active compounds and preparations containing those active compounds which, in particular, prevent neurosensory phenomena or alleviate them or rapidly make them fade, i.e. are suitable for prophylaxis and/or treatment.
“Stinging” phenomena can be regarded as disorders to be treated cosmetically. Severe itching, however, in particular in the case of atopy, in particular neurodermatitis and severe itching of the skin occurring, can also be regarded as a relatively serious dermatological disorder.
The active compounds according to the invention can in particular also be used on skin superficially appearing to be healthy, e.g. in the case of psoriasis and atopy, i.e. also in addition to the diseased skin areas and, in particular, here too in the case of dry and sensitive skin.
Preferred salts are water-soluble salts of cis-9-heptadecenoic acid, in particular the alkali metal salts, e.g. the sodium salt or the potassium salt, and also the ammonium salt. Also suitable are the calcium, magnesium and aluminium salts and the salts of organic bases, e.g. amines such as ethanolamine, ethylenediamine and morpholine.
According to the invention, pharmaceutical preparations, agents or compositions are also provided which contain the compound according to the invention or its pharmaceutically tolerable salt together with a pharmaceutically tolerable diluent or vehicle.
The compounds of the present invention can be used orally or parenterally in man, e.g. in a dosage of 0.05 to 500 mg, preferably 0.5 to 50 mg, particularly preferably 0.1 to 10 mg per day, in particular also in subdivided doses, for example twice to four times daily.
The active compounds according to the invention can also be incorporated without problems into customary pharmaceutical, in particular dermatological, and cosmetic bases for preferred topical applications and the corresponding pharmaceutical, in particular dermatological, and cosmetic topical prep
Hoppe Udo
Jacob Jurgen
Beiersdorf AG
Dees Jose′ G.
George Konata M
Norris & McLaughlin & Marcus
LandOfFree
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