Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2001-01-31
2003-08-05
Dees, Jose′ G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S059000, C424S060000, C424S063000, C424S064000, C424S070700, C424S070900, C424S400000, C424S401000, C514S398000, C514S399000, C514S844000, C514S937000
Reexamination Certificate
active
06602514
ABSTRACT:
The invention relates to the use of one or more compounds chosen from compounds of the formulae Ia and Ib
the physiologically compatible salts of the compounds of the stereoisomeric forms of the compounds of the formulae Ia and Ib, where
R
1
is H or alkyl,
R
2
is H, COOH, COO-alkyl or CO—NH—R
5
,
R
3
and R
4
are in each case independently of one another H or OH,
n is 1, 2 or 3,
alkyl is an alkyl radical having 1 to 4 carbon atoms, and
R
5
is H, alkyl, an amino acid radical, dipeptide radical or tripeptide radical
for the preparation of a cosmetic formulation
for protecting human skin from stress factors, in particular from dryness as a result of high temperatures or very low temperatures with low atmospheric humidity and/or from high salt concentration on the skin,
for protecting cells, proteins and/or biomembranes of human skin,
for protecting the microflora of human skin and/or for stabilizing the skin barrier.
Healthy human skin is colonized on its surface, the Stratum corneum, by a large number of microorganisms which live commensally. From the great diversity of these microorganisms, only a few live continually on the skin and thus form the resident skin flora. The main representatives of the resident flora on the human skin are Staphylococci, Micrococci, coryneform bacteria and Pityrospora. These live in small colonies on the surface of the Stratum corneum and in the outer epidermis. A second group of microorganisms, which settles temporarily from the outside, in particular on exposed areas of skin, is referred to as transient flora and cannot settle permanently on healthy skin whose microenvironment is heavily determined by the resident microflora. In various regions of the body, the composition of the skin flora varies depending on the microenvironment of the skin. The density of the microorganisms adapts to the respective skin environment so that the ecology of these regions of the body is not unbalanced by excessive settlement by microorganisms. Compared with the normal state of the skin, the number of microorganisms decreases in the case of dry skin, while the number of microorganisms increases in the case of moist skin, e.g. as a result of inflammatory changes in the case of eczema, by up to 1000-fold.
Being the barrier layer and surface of the human body, the skin is exposed to a large number of external stress factors. The human skin is an organ which, having diverse specialized cell types—keratinocytes, melanocytes, Langerhans cells, Merkel cells and intercalated sensory cells—protects the body against external influences. A differentiation should be made here between external physical, chemical, and biological influences on the human skin. External physical influences include thermal and mechanical influences, and the effect of radiation. External chemical influences are, in particular, the effect of toxins and allergens. External biological influences include the effect of foreign organisms and the metabolic products thereof.
The surface of the human skin is covered by a fatty film which, depending on the given ratios, is to be considered as an oil-in-water or a water-in-oil emulsion and contains numerous active ingredients, such as e.g. enzymes and vitamins, e.g. vitamin D. This fatty film, which has been formed from the lipids released from the sebaceous glands and keratinocytes, preserves the moisture of the skin and protects the body as a skin barrier against unfavorable environmental factors. This sensitive equilibrium of the skin barrier is disturbed by external or internal factors.
The microorganisms of human skin are subjected to various stress factors. For example, they can be damaged by drying out or by high salt concentrations on the surface of the skin, e.g. after perspiring, which can lead to damage of the skin barrier. However, some of these microorganisms—Staphylococci, Micrococci, Corynebacteria and Brevibacteria—usually have the ability to form compatible solutes in order to protect against drying out or high salt concentration and thus contribute to the formation of an intact skin barrier. The compatible solutes, which are also referred to as stress protection substances, are low molecular weights of substances in cytoplasm.
Hitherto, it has, for example, been attempted to effect care or protection of human skin by hydrophilic substances which themselves bind water (E. A. Galinski, Experientia 49 (1993) 487-496). However, these hydrophilic substances bind water molecules of the water of hydration as well as free water molecules. Although this leads to a binding of water molecules, it does not lead, for example, to a protection of the hydration sheaths of cells, proteins and cell membranes.
The object was therefore to provide cosmetic formulations, the use of which overcome [sic] or at least reduce [sic] the abovementioned skin problems and in particular are [sic] suitable.
for protecting human skin against stress factors, in particular against dryness as a result of high temperatures or very low temperatures at low atmospheric humidity and/or against high salt concentration on the skin,
for protecting cells, proteins and/or biomembranes of the human skin,
for protecting the microflora of the human skin, and/or
for stabilizing the skin barrier.
Surprisingly, we have now found that this object is achieved by the use of one or more compounds chosen from compounds of the formulae Ia and Ib
the physiologically compatible salts of the compounds of the formulae Ia and Ib, and the stereoisomeric forms of the compounds of the formulae Ia and Ib, where
R is H or alkyl,
R
2
is H, COOH, COO-alkyl or CO—NH—R
5
,
R
3
and R
4
are in each case independently of one another H or OH,
n is 1, 2 or 3,
alkyl is an alkyl radical having 1 to 4 carbon atoms, and
R
5
is H, alkyl, an amino acid radical, dipeptide radical or tripeptide radical in cosmetic formulations.
Within the scope of the present invention, all compounds above and below chosen from the compounds of the formulae Ia and Ib, the physiologically compatible salts of the compounds of formulae Ia and Ib, and the stereoisomeric forms of the compounds of the formulae Ia and Ib are referred to as “ectoin or ectoin derivatives”.
Ectoin-containing cosmetic formulations protect cells, protein, enzymes, vitamins, DNA, cell membranes and biomembranes of the skin against damage as a result of drying out and the withdrawal of water. The hydration effect of ectoin stabilizes the water equilibrium of the Stratum corneum and the skin barrier. Ectoin prevents dry and flaky skin.
In addition, ectoin-containing cosmetic formulations protect the microflora of the skin, which is important for an intact skin barrier, against stress as a result of drying out and high ion concentration after perspiring. The stabilization of the resident skin flora by ectoin or its derivatives is an important prerequisite for the equilibrium of the microenvironment of the skin and the formation of an intact skin barrier.
Ectoin and the ectoin derivatives are low molecular weight cyclic amino acid derivatives which can be obtained from various halophilic microorganisms. Both ectoin and hydroxyectoin have the advantage that they do not react with the cell metabolism.
DE 43 42 560 describes the use of ectoin and ectoin derivatives as moisture-donors in cosmetic products.
The compounds chosen from the compounds of the formulae Ia and Ib, the physiologically compatible salts of the compounds of the formulae Ia and Ib and the stereoisomeric forms of the compounds of the formulae Ia and Ib can be present in the cosmetic preparations as optical isomers, diastereomers, racemates, zwitterions, cations or as a mixture of these. Of the compounds chosen from the compounds of the formulae Ia and Ib, the physiological compatible salts of the compounds of the formulae Ia and Ib and the stereoisomeric forms of the compounds of the formulae Ia and Ib, preference is given to those in which R
1
is H or CH
3
, R
2
is H or COOH, R
3
and R
4
in each case independently of one another are H or OH and n is 2. Of the compound
Bünger Joachim
Driller Hans-Jürgen
Martin Roland
Dees Jose′ G.
Lamm Marina
Merck Patent GmbH
Millen White Zelano & Branigan P.C.
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