Melanin decomposition inhibitor

• US 10,966,911 B2
• Filed: 02/10/2017
• Issued: 04/06/2021
• Est. Priority Date: 02/12/2016
• Status: Active Grant

• Current Assignee: KAO Corporation
• Original Assignee: KAO Corporation
• Inventors: Murase, Daiki, Hachiya, Akira, Oya, Naoki, Takano, Kei, Kawasaki, Akiko, Kawabata, Keigo
• Primary Examiner(s): Howell, Theodore R.
• Assistant Examiner(s): Kosturko, George W
• Application Number:
  US16/075,828
• Publication Number:
  US 20190053994A1
• Time in Patent Office: 1,516 Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 2800/782 Enzyme inhibitors; Enzyme antagonists
• CPC Class Codes: A61K 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 31/4375 the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
• CPC Class Codes: A61K 31/4741 condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
• CPC Class Codes: A61K 36/29 Berberidaceae (Barberry family), e.g. barberry, cohosh or mayapple
• CPC Class Codes: A61K 36/71 Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
• CPC Class Codes: A61K 36/718 Coptis (goldthread)
• CPC Class Codes: A61K 36/756 Phellodendron, e.g. corktree
• CPC Class Codes: A61K 36/87 Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
• CPC Class Codes: A61K 8/41 Amines
• CPC Class Codes: A61K 8/43 Guanidines
• CPC Class Codes: A61K 8/49 containing heterocyclic compounds
• CPC Class Codes: A61K 8/4926 having six membered rings
• CPC Class Codes: A61K 8/97 from algae, fungi, lichens or plants; from derivatives thereof
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: A61Q 19/02 for chemically bleaching or whitening the skin
• CPC Class Codes: A61Q 5/00 Preparations for care of the hair
• CPC Class Codes: A61Q 5/10 Preparations for permanently dyeing the hair
• CPC Class Codes: Y02A 50/30 : Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

To provide an inhibitor of melanin decomposition, which inhibits decomposition of melanin in keratinocytes to accelerate accumulation of melanin in skin and hair.

An inhibitor of melanin decomposition in keratinocytes, comprising at least one selected from the group consisting of a plant extract containing berberine or a salt thereof, berberine or a salt thereof, proguanil or a salt thereof and phenformin or a salt thereof, as an active ingredient.

Claims

1. A method for inhibiting melanin decomposition in a subject'"'"'s keratinocytes, comprising externally applying, to a site on the subject'"'"'s skin at which the subject desires to inhibit melanin decomposition, an effective amount of an external preparation that comprises proguanil or a salt thereof and inhibiting melanin decomposition at the site as a result of the applying.

5. The method according to claim 1, wherein the amount of proguanil that is applied per adult, is 0.1 to 5,000 mg per day.

9. The method according to claim 1, wherein the dose of proguanil per area of 100 cm² per application is from 0.01 to 10 mg.

2. A method for inhibiting autophagy in a subject'"'"'s keratinocytes, comprising externally applying, to a site on the subject'"'"'s skin at which the subject desires to inhibit the autophagy, an effective amount of an external preparation that comprises proguanil or a salt thereof and inhibiting autophagy at the site as a result of the applying.

6. The method according to claim 2, wherein the amount of proguanil that is applied per adult, is 0.1 to 5,000 mg per day.

10. The method according to claim 2, wherein the dose of proguanil per area of 100 cm² per application is from 0.01 to 10 mg.

3. A method for darkening a subject'"'"'s skin or hair color, comprising externally applying, to a site on the subject'"'"'s skin or hair at which the subject desires to darken the subject'"'"'s skin or hair color, an effective amount of an external preparation that comprises proguanil or a salt thereof and darkening the subject'"'"'s skin or hair color at the site as a result of the applying.

7. The method according to claim 3, wherein the amount of proguanil that is applied per adult, is 0.1 to 5,000 mg per day.

11. The method according to claim 3, wherein the dose of proguanil per area of 100 cm² per application is from 0.01 to 10 mg.

4. A method for improving a subject'"'"'s gray hair, comprising externally applying to a site on the subject'"'"'s skin or hair at which the subject desires to improve gray hair, an effective amount of an external preparation that comprises proguanil or a salt thereof and improving the subject'"'"'s gray hair at the site as a result of the applying.

8. The method according to claim 4, wherein the amount of proguanil that is applied per adult, is 0.1 to 5,000 mg per day.

12. The method according to claim 4, wherein the dose of proguanil per area of 100 cm² per application is from 0.01 to 10 mg.