Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-09-04
2001-06-19
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S577000
Reexamination Certificate
active
06248749
ABSTRACT:
The present invention relates to a use of at least one inhibitor of the activity of retinoid acid in a cosmetic composition or for the manufacture of a pharmaceutical composition, the inhibitor of the activity of retinoid acid or the pharmaceutical composition being intended for treating sensitive skins and/or the acute damage induced by UV radiation.
It is known that some skins are more sensitive than others.
The symptoms of sensitive skins have until now been poorly characterized and the problem of these skins have been poorly defined because of this; no-one knew exactly the process implicated in the sensitivity of the skin. Some thought that a sensitive skin was a skin which reacted to cosmetic products, others that it was a skin which reacted to several external factors, not necessarily linked to cosmetic products.
Some tests have been evaluated in order to try to understand sensitive skins, for example tests based on lactic acid and DMSO which are known to be irritant substances: see for example the article by K. Lammintausta et al., Dermatoses, 1988, 36, pages 45-49; and the article by T. Agner and J. Serup, Clinical and Experimental Dermatology, 1989, 14, pages 214-217. However, these tests do not make it possible to characterize sensitive skins.
Moreover, sensitive skins have been assimilated with allergic skins.
Because the characteristics of sensitive skins were poorly known, it has up until now been very difficult to treat them, and they have been treated indirectly, for example by limiting, in cosmetic or dermatological compositions, the use of products with an irritant character such as surfactants, preservatives, solvents, propellants or perfumes.
Numerous clinical tests have since been performed and the symptoms linked to sensitive skins have thus been determined. These symptoms are in particular subjective signs, which are essentially dysaesthetic sensations. Dysaesthetic sensations are understood to mean sensations which are painful to a greater or lesser degree and which are felt in a cutaneous zone such as pricking, formication, itching or pruritus, inflammation, discomfort, twitching and the like.
It has been possible to show, in addition, that a sensitive skin was not an allergic skin. Indeed, an allergic skin is a skin which reacts to an external agent, an allergen, which triggers an allergic reaction. It is an immunological process which occurs only when an allergen is present and which affects only sensitized subjects. The essential characteristic of the sensitive skin is, according to the applicant, on the contrary, a mechanism of response to external factors, which can affect any individual, even though the individuals said to have sensitive skin react thereto more quickly than others. This mechanism is not immunological, it is aspecific.
Sensitive skins can be divided into two large clinical forms, the irritable and/or reactive skins and the intolerant skins.
An irritable and/or reactive skin is a skin which reacts through a pruritus, that is to say through itching, or through pricking, to various factors such as the environment (exposure to excessive UV rays), emotions, food, wind, rubbing, razors, soap, surfactants, hard water with a high chalk concentration, temperature variations or wool.
An intolerant skin is a skin which reacts to sensations of inflammation, twitching, formication and/or reddening, to various factors such as the environment (exposure to excessive UV rays), emotion and food.
Excessive exposure of the skin to UV rays can lead to acute cutaneous damage, such as an erythematous and/or irritated and/or red and/or swollen and/or oedematous and/or desquamatory skin. This acute cutaneous damage leads to what is commonly called “sunburn”. This acute damage is to be distinguished from chronic damage, such as cancerous pathologies or a photoaged skin, which corresponds mainly to dermal damage, and subsidiarily to epidermal damage. “Sensitive” scalps have a more univocal clinical semiology: the sensations of pruritus and/or pricking and/or inflammation are essentially triggered by local factors such as rubbing, soap, surfactants, hard water with a high chalk concentration, shampoos or lotions. These sensations are also sometimes triggered by factors such as the environment, emotion and/or food.
Moreover, in some anatomical regions such as the large folds (inguinal, genital, axillary, popliteal, anal, submammary or elbow bend regions) and the feet, sensitive skin is manifested by pruriginous sensations and/or dysaesthetic sensations (inflammation, pricking) linked in particular to sweating, rubbing, wool, surfactants, hard water with a high chalk concentration and/or variations in temperature.
The products having an irritant character can be used in cosmetic or pharmaceutical compositions, and more particularly dermatological compositions, quite obviously for other effects. Thus, they are generally used as active agents, surfactants, preservatives, perfumes, solvents or propellants for the said compositions.
However, because of this undesirable effect, these products are generally used in very low doses. The use of these products in a small quantity may then prove to be of little advantage compared with the use of other less active but less irritant or not irritant products which are therefore used in a larger quantity.
Consequently, there is a need in the cosmetic and pharmaceutical field to find a means which makes it possible to use these products, without the latter exhibiting an irritant character which can be criticized by the user.
It is known, in general, that all-trans- retinoic acid acts on the differentiation and/or the proliferation of cells by interacting with nuclear receptors or RARs (retinoic acid receptors) contained in the cell nucleus. Numerous synthetic structural analogues of all-trans-retinoic acid or of 9-cis-retinoic acid, commonly called “retinoids”, have been described so far in the literature. There are so far three identified sub-types of RAR receptors called &agr;-RAR, &bgr;-RAR and &ggr;-RAR, respectively. These receptors, after binding of the ligand (i.e. of all-trans-retinoic acid), interact with the promoter region of genes regulated by retinoic acid at the level of specific response elements (RARE).
Some analogues can bind and activate a particular RAR (&agr;, &bgr; or &ggr;) receptor sub-type. Finally, other analogues exhibit no particular selective activity towards these various receptors. To this end, and for example, all-trans-retinoic acid activates the RARs (RAR specific agonist ligand), all sub-types taken into consideration.
Retinoic acid and retinoids in general have been claimed for treating the following disorders or conditions: acne vulgaris, comedo-type acne, polymorphic acne, acne rosacea, nodulocystic acne, acne conglobata, senile acne, secondary acne such as solar acne, acne medicamentosa or occupational acne; other keratinization types of disorders, in particular ichthyosis, ichthyosiform states, Darrier's disease, keratosis palmaris et plantaris, leucoplakia and leucoplakia-like states, skin or mucosal (buccal) lichen; other dermatological conditions linked to a keratinization disorder with an inflammatory and/or immunoallergic component and in particular all forms of psoriasis whether cutaneous, mucosal or ungual, and even psoriatic rheumatism, or alternatively skin atopy, such as eczema or respiratory atopy or alternatively gingival hypertrophy; damage induced by UV radiation; skin ageing, whether photoinduced or chronologic or actinic keratoses and pigmentations or any pathology associated with chronologic or actinic ageing; healing disorders or vibices; disorders of sebaceous function such as hyperseborrhoea of acne or simple seborrhoea.
The combination of compounds which are agonists of the &agr;-RARs and &ggr;-RARs with &agr;-RAR antagonists for treating photoaged skins has also been described in patent application WO 96/30009, specifying that the &agr;-RAR antagonists alone are not active for this type of treatment.
Retinoic acid and retinoids in general, by binding with the R
Demarchez Michel
Jomard Andre
Burns Doane Swecker & Mathis L.L.P.
Centre International de Recherches Dermatologiques Galderma
Jarvis William R. A.
Kim Vickie
LandOfFree
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