US2005118119A1PendingUtilityA1
Use of a compound inactivating the kinase a protein in a composition containg a cosmetically acceptable medium in order to lighten the skin
Priority: Jan 25, 2002Filed: Jan 22, 2003Published: Jun 2, 2005
Est. expiryJan 25, 2022(expired)· nominal 20-yr term from priority
A61P 17/00A61K 31/00A61K 8/44C07C 233/49A61K 31/55A61K 2800/782A61Q 19/02C07C 233/51A61Q 17/04A61K 31/41
45
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Claims
Abstract
A method of using a compound to lighten the skin by inactivating protein kinase A. The compound may be in a composition with either a pharmacologically or cosmetically acceptable medium. Depending upon the medium and concentration of the compound, the composition may be used either therapeutically or non-therapeutically.
Claims
exact text as granted — not AI-modified1 - 26 . (canceled)
27 . A method of lightening skin comprising inactivating the protein kinase A with a composition comprising:
a) a cosmetically acceptable medium; and b) a compound.
28 . A method of lightening skin comprising inactivating the protein kinase A with a composition comprising:
a) a cosmetically acceptable medium; and b) a compound of general formula (I): or salts thereof, wherein:
1) R 1 represents the characterizing chain of a fatty acid comprising:
i) about 3 to about 30 carbon atoms; and
ii) a characteristic comprising at least one member selected from the group consisting of:
aa) saturated;
bb) unsaturated;
cc) linear; and
dd) branched;
2) R 2 represents the characterizing chain of an amino acid; and
3) m is between about 1 and about 50.
29 . The method of claim 28 , wherein said compound comprises a radical of general formula (II):
R 1 —C(═O)— (II)
wherein said radical comprises about 7 to about 22 carbon atoms.
30 . The method of claim 29 , wherein said radical comprises at least one member selected from the group consisting of:
a) octanoyl; b) decanoyl; c) undecylenoyl; d) dodecanoyl; e) tetradecanoyl; f) hexadecanoyl; g) octadecanoyl; h) eicosanoyl; i) docosanoyl; j) 8-octadecenoyl; k) eicosenoyl; l) 13-docosenoyl; m) 9,12-octadecadienoyl; and n) 9,12,15-octadecatrienoyl radical.
31 . The method of claim 30 , wherein said radical comprises at least one member selected from the group consisting of:
a) octanoyl; b) ω-undecylenoyl; c) dodecanoyl; d) hexadecanoyl; e) 8-octadecenoyl; f) 13-docosenoyl; g) 9,12-octadecadienoyl; and h) 9,12,15-octadecatrienoyl.
32 . The method of claim 31 , wherein said R 2 further comprises at least one member selected from the group consisting of:
a) glycine; b) alanine; c) serine; d) aspartic acid; e) glutamic acid; f) valine; g) threonine; h) arginine; i) lysine; j) proline leucine; k) phenylalanine; l) isoleucine; m) histidine; n) tyrosine; o) tryptophan; p) asparagine; q) glutamine; r) cysteine; s) cystine; t) methionine; u) hydroxyproline; v) hydroxylysine; w) sarcosine; and x) ornithine.
33 . The method of claim 32 , further comprising a residue, said residue comprising at least one member selected from the group consisting of:
a) a residue of general formula (IIIa) —HN—CH(R 2 )—C(═O)— (IIIa), and b) a residue of general formula (IIIb)
34 . The method of claim 33 , wherein said R 2 comprises at least one member selected from the group consisting of:
a) phenylalanine; b) tyrosine; c) histidine; d) methionine; e) cysteine; and f) tryptophan.
35 . The method of claim 34 , wherein said m is less than about 5.
36 . The method of claim 35 , wherein said m is less than or equal to about 2.
37 . The method of claim 36 , wherein said m is less than or equal to about 1.4.
38 . The method of claim 37 , wherein said m is equal to about 1.
39 . A method which may be used for treating skin comprising lightening said skin non-therapeutically with a composition, wherein said composition comprises:
a) a cosmetically acceptable medium; and b) an effective amount of at least one compound that inactivates protein kinase A.
40 . The method of claim 39 , wherein said composition comprises between about 0.01 % and about 10% of its total weight of said compound.
41 . The method of claim 40 , wherein said composition comprises between about 0.1% and about 5% of its total weight of said compound.
42 . The method of claim 41 , wherein said composition comprises between about 1% and about 5% of its total weight of said compound.
43 . A composition which may be used for lightening the skin comprising:
a) a pharmaceutically acceptable medium; and b) an effective amount of at least one compound that inactivates protein kinase A.
44 . The composition of claim 43 , wherein:
a) said composition is pharmaceutical; and b) said composition is suitable for therapeutic use.
45 . The method of claim 44 , wherein said composition comprises between about 0.01 % and about 10% of its total weight of said compound.
46 . The method of claim 45 , wherein said composition comprises between about 0.1% and about 5% of its total weight of said compound.
47 . The method of claim 46 , wherein said composition comprises between about 1% and about 5% of its total weight of said compound.
48 . The method of claim 27 , wherein said compound also inactivates adenylate cyclase.
49 . The method of claim 33 , wherein:
a) said radical comprises at least one member selected from the group consisting of:
1) octanoyl radicals; and
2) ω-undecylenoyl radicals; and
b) said residue comprises at least one member selected from the group consisting of: wherein said R 2 represents the characterizing chain of phenylalanine.
50 . The method of claim 48 , wherein:
a) said radical comprises at least one member selected from the group consisting of:
1) octanoyl radicals; and
2) ω-undecylenoyl radicals; and
b) said residue comprises at least one member selected from the group consisting of: wherein said R 2 represents the characterizing chain of phenylalanine.
51 . The method of claim 42 , wherein said compound also inactivates adenylate cyclase.
52 . The composition of claim 47 , wherein said compound also inactivates adenylate cyclase.
53 . The method of claim 38 , wherein said compound further comprises an affinity for the melanocyte specific hormone (α-MSH) receptor.
54 . The method of claim 51 , wherein said compound further comprises an affinity for the melanocyte specific hormone (α-MSH) receptor.
55 . The composition of claim 52 , wherein said compound further comprises an affinity for the melanocyte specific hormone (α-MSH) receptor.
56 . A composition comprising N-(ω-undecylenoyl)phenylalanine of formula (Ia):
57 . The composition of claim 56 , wherein said composition is used cosmetics.
58 . A pharmaceutical composition comprising:
a) a pharmaceutically acceptable medium; and b) an effective amount of the compound N-(ω-undecylenoyl)phenylalanine of formula (Ia):
59 . A composition comprising an emulsion, wherein said emulsion comprises between about 0.01% and about 10% of its total weight, the compound N-(ω-undecylenoyl)phenylalanine of formula (Ia):
60 . The composition of claim 59 , wherein said emulsion comprises between about 0.1% and about 5% of its total weight of said compound.
61 . The composition of claim 60 , wherein said emulsion further comprises between about 1% and about 5% of its total weight of said compound.Join the waitlist — get patent alerts
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