Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
1998-09-23
2001-10-02
Williamson, Michael A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C514S017400, C514S844000
Reexamination Certificate
active
06296857
ABSTRACT:
The present invention relates to cosmetic or dermatological preparations comprising oligopeptides, for using active ingredients known per se, for cosmetic and topical dermatological lightening of the skin or for preventing tanning of the skin, in particular tanning of the skin caused by UV radiation.
In a preferred embodiment, the present invention relates to cosmetic and dermatological preparations for the prophylaxis and treatment of cosmetic or dermatological changes in the skin such as, for example, undesired pigmentation, for example local hyperpigmentations and malpigmentations (for example lentigo, freckles), but also for the purely cosmetic lightening of large areas of skin whose pigmentation is quite adequate for the individual skin type.
The factors which are responsible for skin pigmentation are the melanocytes which are found in the lowest layer of the epidermis, the stratum basale, next to the basal cells, as pigment-forming cells which occur either singly or more or less in clusters, depending on the skin type. Melanocytes contain melanosomes as characteristic cell organelles, and these form melanin at higher rates when stimulated by UV radiation. The melanin is transported into the keratinocytes and leads to a more or less pronounced tan or brown skin colour.
Melanin is the end product of an oxidative process in which tyrosine is converted with the aid of the enzyme tyrosinase via 3,4-dihydroxyphenylalanine (dopa), dopaquinone, leucodopachrome, dopachrome, 5,6-dihydroxyindole and indole-5,6-quinone to give, finally, melanin.
Hyperpigmentation problems of the skin have a multiplicity of causes and/or accompanying symptoms of a large number of biological processes, for example UV radiation (for example, freckles, ephelides), genetic predisposition, malpigmentation of the skin in the course of wound healing and/or wound scarring or skin ageing (for example
lentigines seniles
).
Active ingredients and preparations which counteract skin pigmentation are known. Products which are essentially used in practice are based on hydroquinone but, on the one hand, only become effective after several weeks' use and, on the other hand, unduly long use of such products is unacceptable for toxicological reasons. Inhibition of tyrosinase by substances such as kojic acid, ascorbic acid and azelaic acid and their derivatives is also well known, but has cosmetic and dermatological disadvantages.
It was an object of the present invention to remedy these shortcomings.
The publication WO-97/00892 describes the depigmenting action of the signal proteins of agoutis (rodent family of the Dasyproctidae, occurrence: approx. 20 species in the woodlands of Central America).
Surprisingly, the object is achieved by cosmetic or pharmaceutical preparations which are distinguished by an effective content of one or more monomeric or homo- or heterodimeric or homo- or heterotrimeric or homo- or heterotetrameric oligopeptides,
(1) where these oligopeptides are based on a structure Asn-Ser-Leu-Asp-Phe (or NSLDF) SEQ ID NO: 1 as homo- or heteromonomer,
(2) where structures as mentioned above are present in the monomeric or homo- or heterodimeric or homo- or heterotrimeric or homo- or heterotetrameric oligopeptides, with the difference that the C-terminus and/or the N-terminus is complemented by up to 5 amino acids, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids,
(3) or where amino acid sequences shown under items (1) and (2) occur as single or repetitive structural motifs in monomeric or homo-/hetero-di-, -tri- or -tetrameric oligopeptides or proteins with a molecular weight of between approx. 0.5 and 100 kdalton,
(4) or where the monomeric or homo-/hetero-di-, -tri, or -tetrameric oligopeptides or proteins are acylated on the C-terminus, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids and R represents a branched or unbranched, saturated or unsaturated hydrocarbon radical, in particular an alkyl radical having 1 to 30 carbon atoms,
(5) or where the monomeric or homo-/hetero-di-, -tri-, or -tetrameric oligopeptides or proteins are amidated on the C-terminus, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids and where R′ and R″ independently of one another may be selected from the group consisting of hydrogen and the branched or unbranched, saturated or unsaturated hydrocarbon radicals, in particular the alkyl radical having 1 to 30 carbon atoms,
(6) or where the monomeric or homo-/hetero-di-, -tri-, or -tetrameric oligopeptides or proteins are amidated on the C-terminus and acylated on the N-terminus, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids, R represents a branched or unbranched saturated or unsaturated hydrocarbon radical, in particular an alkyl radical having 1 to 30 carbon atoms, and where R′ and R″ independently of one another may be selected from the group consisting of hydrogen and the branched or unbranched, saturated or unsaturated hydrocarbon radicals, in particular the alkyl radical having 1 to 30 carbon atoms,
(7) or where amino acid sequences occur in monomeric or homo-/hetero-di-, -tri- or -tetrameric oligopeptides or proteins as single or repetitive structural motifs, as shown by the structures
where &PSgr; may represent a single bond or an amino acid sequence of up to 5 amino acids, &OHgr; may represent an amino acid sequence of up to 15 amino acids, n represents a number from 1 to 25, R represents a branched or unbranched saturated or unsaturated hydrocarbon radical, in particular an alkyl radical of 1 to 30 carbon atoms, and where R′ and R″ independently of one another may be selected from the group consisting of hydrogen and the branched or unbranched, saturated or unsaturated hydrocarbon radicals, in particular the alkyl radical having 1 to 30 carbon atoms.
Also considered to be an advantageous embodiment of the present invention is the use of one or more monomeric or homo- or heterodimeric or homo- or heterotrimeric or homo- or heterotetrameric oligopeptides,
(1) where these oligopeptides are based on a structure Asn-Ser-Leu-Asp-Phe (or NSLDF) SEQ ID NO: 1 as homo- or heteromonomer,
(2) where, in the sequence Asn-Ser-Leu-Asp-Phe, in each case one valine may be replaced by an amino acid selected from the group consisting of glycine, alanine, leucine, isoleucine, serine, threonine and methionine, preferably alanine, while the remainder of the sequence is retained,
(3) or where structures as mentioned above are present in the monomeric or homo- or heterodimeric or homo- or heterotrimeric or homo- or heterotetrameric oligopeptides, with the difference that the C-terminus and/or the N-terminus is complemented by up to 5 amino acids, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids,
(4) or where amino acid sequences shown under items (1) and (2) occur as single or repetitive structural motifs in monomeric or homo-/hetero-di-, tri- or -tetrameric oligopeptides or proteins with a molecular weight of between approx. 0.5 and 100 kdalton,
(5) or where the monomeric or homo-/hetero-di-, Tri-, or -tetrameric oligopeptides or proteins are acylated on the N-terminus, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5 amino acids and R represents a branched or unbranched saturated or unsaturated hydrocarbon radical, in particular an alkyl radical having 1 to 30 carbon atoms,
(6) or where the monomeric or homo-/hetero-di-, tri-, or -tetrameric oligopeptides or proteins are amidated on the C-terminus, as shown by the structure
where &PSgr; and &OHgr; independently of one another may represent amino acid sequences of 0 up to 5
Hearing Vincent J.
Max Heiner
Schonrock Uwe
Beiersdorf Aktiengesellschaft
Norris & McLaughlin & Marcus
Williamson Michael A.
LandOfFree
Cosmetic or dermatological preparations comprising... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cosmetic or dermatological preparations comprising..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cosmetic or dermatological preparations comprising... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2572596