# US 2012/0058140 A1 · Topical compositions for inhibiting matrix metalloproteases and providing antioxidative activities

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- Number: US 2012/0058140 A1
- Document ID: US20120058140A1
- Status: Published application
- Kind: A1
- Application number: 12/874,884
- Filed: 2010-09-02
- Published: 2012-03-08
- Earliest claimed: 2010-09-02
- Assignees: Bath & Body Works Brand Management, Inc.
- Inventors: Joseph D. Ceccoli; Brian Costello; James A. Hayward; Konstantinos M. Lahanas
- Web page: https://patentgrep.com/patent/US20120058140A1

## CPC

- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61K 8/9728: Fungi, e.g. yeasts
- A61K 8/9767: Pinaceae [Pine family], e.g. pine or cedar
- A61K 8/9771: Ginkgophyta, e.g. Ginkgoaceae [Ginkgo family]
- A61K 8/9789: Magnoliopsida [dicotyledons]
- A61K 8/9794: Liliopsida [monocotyledons]
- A61Q 19/08: Anti-ageing preparations
- A61K 2800/782: Enzyme inhibitors; Enzyme antagonists
- A61Q 19/005: {Preparations for sensitive skin}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

A topical composition according to the present invention for use in a skin care regimen that provides matrix metalloprotease (MMP) inhibiting activity, tissue inhibitor of metalloprotease (TIMP) inducing activity, and immediate and delayed antioxidative activity. Preferably, the topical composition comprises at least one MMP inhibitor, a TIMP inducing agent, Tremella fuciformis (snow fungus) extract, Camellia sinensis (green tea) leaf extract, and Eugenia caryophyllus (clove) extract. The compositions are useful in anti-wrinkle and anti-aging products, providing elasticity, firmness, tone and texture to the skin, ameliorating fine lines and preventing skin damage.

## Claims

### Claim 1

A topical skin composition for providing short-term and long-term antioxidant and matrix metalloprotease inhibiting activities to the skin, comprising:
a matrix metalloprotease inhibitor component;
a tissue inhibitor of matrix metalloproteases inducing agent; and
an antioxidant comprising at least one natural extract.

### Claim 2 (depends on 1)

A composition according to claim 1, wherein said composition is effective for inhibiting MMP-1, MMP-3 and MMP-9.

### Claim 3 (depends on 1)

A composition according to claim 1, wherein said matrix metalloprotease inhibitor component comprises soybean seed extract.

### Claim 4 (depends on 1)

A composition according to claim 1, wherein said matrix metalloprotease inhibitor component is selected from the group consisting of (2S,3R)—N-hydroxy-N′-[(1S)-1-(methylcarbamoyl)-2-phenyl-ethyl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide), N-[2,2-dimethyl-1-(methylcarbamoyl)propyl]-2-[hydroxy-(hydroxycarbamoyl)methyl]-4-methyl-pentanamide), N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide), palmitoyl tripeptide-5, N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide, and a mixture thereof.

### Claim 5 (depends on 1)

A composition according to claim 1, wherein said matrix metalloprotease inhibitor component is present in the amount of from about 0.001% to about 1.0% by weight.

### Claim 6 (depends on 1)

A composition according to claim 1, wherein said tissue inhibitor of matrix metalloproteases inducing agent comprises acetyl hexapeptide-20.

### Claim 7 (depends on 1)

A composition according to claim 1, wherein said tissue inhibitor of matrix metalloproteases inducing agent is present in the amount of from about 0.01% to about 2.0% by weight.

### Claim 8 (depends on 1)

A composition according to claim 1, wherein said natural extract is effective to provide matrix metalloprotease inhibiting activities.

### Claim 9 (depends on 1)

A composition according to claim 1, wherein said natural extract comprises at least one selected from the group consisting of a plant extract, a fruit extract, and a fungus extract.

### Claim 10 (depends on 1)

A composition according to claim 1, wherein said natural extract comprises snow fungus extract, clove extract, and green tea leaf extract.

### Claim 11 (depends on 1)

A composition according to claim 1, wherein said natural extract comprises apple fruit extract, cinnamon bark extract, and Chinese rhubarb extract.

### Claim 12 (depends on 1)

A composition according to claim 1, wherein said natural extract is selected from the group consisting of snow fungus extract, clove extract, green tea leaf extract, apple fruit extract, cinnamon bark extract, Chinese rhubarb extract, ginkgo biloba extract, black chokeberry extract, cantaloupe melon extract, bilberry extract, French maritime pine extract, milk thistle extract, caper extract, culcitium reflexum leaf extract, krameria triandra root extract, peach flower extract, great burnet root extract, autumn joy leaf extract, pueraria lobata extract, lemon grass extract, basil extract, grape seeds extract, rosemary extract, sage extract, thyme extract, chamomile extract, lavender extract, horse chestnut extract, and lemon extract, red oak bark extract, Japanese Horse Chestnut extract, argania spinosa leaf extract, pariparoba root extract, marine eelgrass extract, pomegranate extract, calaguala extract, blackberry extract, raspberry extract, muscadine grapes extract, rooibos extract, pine pollen extract, blackberry leaf extract, and combinations thereof.

### Claim 13 (depends on 1)

A composition according to claim 1, wherein said natural extract is present in the amount of from about 1.0% to about 25% by weight.

### Claim 14 (depends on 1)

A composition according to claim 1, wherein said composition is prepared in a form selected from the group consisting of gel, lotion, oil-in-water or water-in-oil emulsions, water-in-silicone emulsions, hydroalcoholic systems, aerosol, spray and anhydrous form.

### Claim 15

A topical short-term and long-term anti-aging composition comprising:
a soybean seed extract for inhibiting matrix metalloprotease in the skin;
an acetyl hexapeptide-20 for inducing tissue inhibitors of matrix metalloprotease in the skin; and
a natural extract for providing antioxidant activities to the skin.

### Claim 16 (depends on 15)

A composition according to claim 15, wherein said natural extract comprises snow fungus extract, clove extract, and green tea leaf extract.

### Claim 17 (depends on 16)

A composition according to claim 16, wherein said natural extract further comprises apple fruit extract, cinnamon bark extract, and Chinese rhubarb extract.

### Claim 18

A topical skin composition for providing short-term and long-term antioxidant and matrix metalloprotease inhibiting activities to the skin, comprising:
from about 0.001% to about 1.0% by weight of a matrix metalloprotease inhibitor component;
from about 0.01% to about 2.0% by weight of a tissue inhibitor of matrix metalloproteases inducing agent; and
from about 1.0% to about 25% by weight of at least one natural extract.

### Claim 19 (depends on 18)

A composition according to claim 18, wherein said composition is effective for inhibiting MMP-1, MMP-3 and MMP-9.

### Claim 20 (depends on 18)

A composition according to claim 18, wherein said matrix metalloprotease inhibitor component is selected from the group consisting of soybean seed extract, (2S,3R)—N-hydroxy-N′-[(1S)-1-(methylcarbamoyl)-2-phenyl-ethyl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide), N-[2,2-dimethyl-1-(methylcarbamoyl)propyl]-2-[hydroxy-(hydroxycarbamoyl)methyl]-4-methyl-pentanamide), N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide), palmitoyl tripeptide-5, N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide, and a mixture thereof.

### Claim 21 (depends on 18)

A composition according to claim 18, wherein said tissue inhibitor of matrix metalloproteases inducing agent comprises acetyl hexapeptide-20.

### Claim 22 (depends on 18)

A composition according to claim 18, wherein said natural extract comprises at least one selected from the group consisting of a plant extract, a fruit extract, and a fungus extract.

### Claim 23 (depends on 18)

A composition according to claim 18, wherein said natural extract comprises snow fungus extract, clove extract, and green tea leaf extract.

### Claim 24 (depends on 23)

A composition according to claim 23, wherein said natural extract further comprises apple fruit extract, cinnamon bark extract, and Chinese rhubarb extract.

### Claim 25 (depends on 18)

A composition according to claim 18, wherein said natural extract is selected from the group consisting of snow fungus extract, clove extract, green tea leaf extract, apple fruit extract, cinnamon bark extract, Chinese rhubarb extract, ginkgo biloba extract, black chokeberry extract, cantaloupe melon extract, bilberry extract, French maritime pine extract, milk thistle extract, caper extract, culcitium reflexum leaf extract, krameria triandra root extract, peach flower extract, great burnet root extract, autumn joy leaf extract, pueraria lobata extract, lemon grass extract, basil extract, grape seeds extract, rosemary extract, sage extract, thyme extract, chamomile extract, lavender extract, horse chestnut extract, and lemon extract, red oak bark extract, Japanese Horse Chestnut extract, argania spinosa leaf extract, pariparoba root extract, marine eelgrass extract, pomegranate extract, calaguala extract, blackberry extract, raspberry extract, muscadine grapes extract, rooibos extract, pine pollen extract, blackberry leaf extract, and combinations thereof.

### Claim 26

A method for providing short-term and long-term antioxidant and matrix metalloprotease inhibiting activities to the skin, comprising the steps of:
topically applying a composition comprising:
a matrix metalloprotease inhibitor component;
a tissue inhibitor of matrix metalloproteases inducing agent; and
an antioxidant comprising at least one natural extract.

### Claim 27 (depends on 26)

A method according to claim 26, wherein said composition is effective for inhibiting MMP-1, MMP-3 and MMP-9.

### Claim 28 (depends on 26)

A method according to claim 26, wherein said matrix metalloprotease inhibitor component comprises soybean seed extract.

### Claim 29 (depends on 26)

A method according to claim 26, wherein said matrix metalloprotease inhibitor component is selected from the group consisting of (2S,3R)—N-hydroxy-N′-[(1S)-1-(methylcarbamoyl)-2-phenyl-ethyl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide), N-[2,2-dimethyl-1-(methylcarbamoyl)propyl]-2-[hydroxy-(hydroxycarbamoyl)methyl]-4-methyl-pentanamide), N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide), palmitoyl tripeptide-5, N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide, and a mixture thereof.

### Claim 30 (depends on 26)

A method according to claim 26, wherein said matrix metalloprotease inhibitor component is present in the amount of from about 0.001% to about 1.0% by weight.

### Claim 31 (depends on 26)

A method according to claim 26, wherein said tissue inhibitor of matrix metalloproteases inducing agent comprises acetyl hexapeptide-20.

### Claim 32 (depends on 26)

A method according to claim 26, wherein said tissue inhibitor of matrix metalloproteases inducing agent is present in the amount of from about 0.01% to about 2.0% by weight.

### Claim 33 (depends on 26)

A method according to claim 26, wherein said natural extract is effective to provide matrix metalloprotease inhibiting activities.

### Claim 34 (depends on 26)

A method according to claim 26, wherein said natural extract comprises at least one selected from the group consisting of a plant extract, a fruit extract, and a fungus extract.

### Claim 35 (depends on 26)

A method according to claim 26, wherein said natural extract comprises snow fungus extract, clove extract, and green tea leaf extract.

### Claim 36 (depends on 26)

A method according to claim 26, wherein said natural extract comprises apple fruit extract, cinnamon bark extract, and Chinese rhubarb extract.

### Claim 37 (depends on 26)

A method according to claim 26, wherein said natural extract is selected from the group consisting of snow fungus extract, clove extract, green tea leaf extract, apple fruit extract, cinnamon bark extract, Chinese rhubarb extract, ginkgo biloba extract, black chokeberry extract, cantaloupe melon extract, bilberry extract, French maritime pine extract, milk thistle extract, caper extract, culcitium reflexum leaf extract, krameria triandra root extract, peach flower extract, great burnet root extract, autumn joy leaf extract, pueraria lobata extract, lemon grass extract, basil extract, grape seeds extract, rosemary extract, sage extract, thyme extract, chamomile extract, lavender extract, horse chestnut extract, and lemon extract, red oak bark extract, Japanese Horse Chestnut extract, argania spinosa leaf extract, pariparoba root extract, marine eelgrass extract, pomegranate extract, calaguala extract, blackberry extract, raspberry extract, muscadine grapes extract, rooibos extract, pine pollen extract, blackberry leaf extract, and combinations thereof.

### Claim 38 (depends on 26)

A method according to claim 26, wherein said natural extract is present in the amount of from about 1.0% to about 25% by weight.

### Claim 39

A method for providing short-term and long-term antioxidant and matrix metalloprotease inhibiting activities to the skin, comprising:
topically applying a composition to the skin comprising:
a soybean seed extract for inhibiting matrix metalloprotease in the skin,
an acetyl hexapeptide-20 for inducing tissue inhibitors of matrix metalloprotease; and
a natural extract for providing antioxidant activities to the skin.

### Claim 40

A topical skin composition for providing short-term and long-term antioxidant and matrix metalloprotease inhibiting activities to the skin, comprising:
a matrix metalloprotease inhibitor component derived from soybean seed extract;
a tissue inhibitor of matrix metalloproteases inducing agent comprising acetyl hexapeptide-20; and
a natural extract component comprising snow fungus extract, clove extract, and green tea leaf extract.

### Claim 41 (depends on 40)

A composition according to claim 40, wherein said composition is effective for inhibiting MMP-1, MMP-3 and MMP-9.

### Claim 42 (depends on 40)

A composition according to claim 40, wherein said natural extract component further comprises apple fruit extract, cinnamon bark extract, and Chinese rhubarb extract.

### Claim 43 (depends on 40)

A composition according to claim 40, wherein said matrix metalloprotease inhibitor component further comprises at least one selected from the group consisting of (2S,3R)—N-hydroxy-N′-[(1S)-1-(methylcarbamoyl)-2-phenyl-ethyl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide), N-[2,2-dimethyl-1-(methylcarbamoyl)propyl]-2-[hydroxy-(hydroxycarbamoyl)methyl]-4-methyl-pentanamide), N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide), palmitoyl tripeptide-5, N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide, and a mixture thereof.

### Claim 44 (depends on 40)

A composition according to claim 40, wherein said matrix metalloprotease inhibitor component is present in the amount of from about 0.001% to about 1.0% by weight.

### Claim 45 (depends on 40)

A composition according to claim 40, wherein said tissue inhibitor of matrix metalloproteases inducing agent is present in the amount of from about 0.01% to about 2.0% by weight.

### Claim 46 (depends on 40)

A composition according to claim 40, wherein said natural extract further comprises at least one selected from the group consisting of apple fruit extract, cinnamon bark extract, Chinese rhubarb extract, ginkgo biloba extract, black chokeberry extract, cantaloupe melon extract, bilberry extract, French maritime pine extract, milk thistle extract, caper extract, culcitium reflexum leaf extract, krameria triandra root extract, peach flower extract, great burnet root extract, autumn joy leaf extract, pueraria lobata extract, lemon grass extract, basil extract, grape seeds extract, rosemary extract, sage extract, thyme extract, chamomile extract, lavender extract, horse chestnut extract, and lemon extract, red oak bark extract, Japanese Horse Chestnut extract, argania spinosa leaf extract, pariparoba root extract, marine eelgrass extract, pomegranate extract, calaguala extract, blackberry extract, raspberry extract, muscadine grapes extract, rooibos extract, pine pollen extract, blackberry leaf extract, and combinations thereof.

### Claim 47 (depends on 40)

A composition according to claim 40, wherein said natural extract is present in the amount of from about 1.0% to about 25% by weight.

### Claim 48

An effective short-term and long-term antioxidant and matrix metalloprotease inhibiting complex composition for incorporation into topical composition comprising:
from about 0.05% to about 1.50% soybean seed extract;
from about 0.50% to about 2.50% acetyl hexapeptide-20;
from about 0.05% to about 1.50% snow fungus extract;
from about 0.50% to about 3.00% clove extract;
from about 0.50% to about 2.50% green tea leaf extract;
from about 0.05% to about 1.50% cinnamon bark extract;
from about 1.50% to about 3.00% apple fruit extract; and
from about 0.05% to about 1.50% Chinese rhubarb extract.

### Claim 49 (depends on 48)

A composition according to claim 48, wherein said complex composition is present in said topical composition in the amount of from about 0.1% to about 10% by weight.

### Claim 50 (depends on 48)

A composition according to claim 48, wherein said complex composition is present in said topical composition in the amount of from about 1.0% to about 8.0% by weight.

### Claim 51 (depends on 48)

A composition according to claim 48, wherein said complex composition is present in said topical composition in the amount of from about 2.0% to about 6.0% by weight.

### Claim 52 (depends on 48)

A composition according to claim 48, wherein said topical composition is prepared in a form selected from the group consisting of gel, lotion, oil-in-water or water-in-oil emulsions, water-in-silicone emulsions, hydroalcoholic systems, aerosol, spray and anhydrous form.