IP Library › Granted Patent US 9,155,690
Granted Patent B2
US 9,155,690 · App. 14/504,445 · Granted Oct 13, 2015

Compound having skin-whitening, anti-oxidizing and PPAR activities and medical use thereof

Inventors: Hae Young Chung (Busan, KR); Min Hi Park (Busan, KR); Young Mi Ha (Busan, KR); Yu Kyeong Han (Busan, KR); Ji Young Park (Busan, KR); Yun Jung Park (Busan, KR); Jin Ah Kim (Busan, KR); Ji Yeon Lee (Gyeongsangnam-do, KR); Yu Min Song (Busan, KR); Hyung Ryong Moon (Busan, KR)
Assignee: PUSAN NATIONAL UNIVERSITY INDUSTRY-UNIVERSITY COOPERATION FOUNDATION
A61K8/49A61K8/4946A61K31/426A61Q19/02C07D235/18C07D277/06C07D277/66A61K2800/78A61Q19/06
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Quick Facts
Patent No.
US 9,155,690
App. No.
14/504,445
Granted
Oct 13, 2015
Kind
B2
Abstract

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

Claims (11)

1. A skin-whitening method, comprising:

administering to a subject a compound of Formula I,

wherein R 1 to R 4 are identical to or different from each other, and are any one of H, OH, a C 1 to C 4 alkoxy, and bromine,

wherein X is any one of Cl and CF 3 .

2. The skin-whitening method of claim 1 , wherein the compound is selected from the group consisting of 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 28), 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)benzene-1,2-diol (Compound 29), 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)benzene-1,3-diol (Compound 30), 2-methoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 31), 2-ethoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 32), 2-(4-methoxyphenyl)-5-(trifluoromethyl)benzo[d]thiazol (Compound 34), 2-(2,4-dimethoxyphenyl)-5-(trifluoromethyl)benzo[d]thiazol (Compound 37), and 2,6-dimethoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 40).

3. The skin-whitening method of claim 2 , wherein the compound is administered to the subject in a range of 0.001 to 100 mg/kg daily.

4. The skin-whitening method of claim 1 , wherein the compound is selected from the group consisting of 4-(5-chlorobenzo[d]thiazol-2-yl)phenol (Compound 82), 4-(5-chlorobenzo[d]thiazol-2-yl)benzene-1,2-diol (Compound 83), 4-(5-chlorobenzo[d]thiazol-2-yl)benzene-1,3-diol (Compound 84), 4-(5-chlorobenzo[d]thiazol-2-yl)-2-ethoxyphenol (Compound 86), 2-bromo-4-(5-chlorobenzo[d]thiazol-2-yl)phenol (Compound 95), 2,6-dibromo-4-(5-chlorobenzo[d]thiazol-2-yl)phenol (Compound 96), and 4-(5-chlorobenzo[d]thiazol-2-yl)-2,6-dimethoxyphenol (Compound 126).

5. The skin-whitening method of claim 4 , wherein the compound is administered to the subject in a range of 0.001 to 100 mg/kg daily.

6. A skin-whitening method, comprising:

administering to a subject a compound selected from the group consisting of 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 28), 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)benzene-1,2-diol (Compound 29), 4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)benzene-1,3-diol (Compound 30), 2-methoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 31), 2-ethoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 32), 2-(4-methoxyphenyl)-5-(trifluoromethyl)benzo[d]thiazole (Compound 34), 2-(2,4-dimethoxyphenyl)-5-(trifluoromethyl)benzo[d]thiazole (Compound 37), and 2,6-dimethoxy-4-(5-(trifluoromethyl)benzo[d]thiazol-2-yl)phenol (Compound 40).

7. The skin-whitening method of claim 6 , wherein the compound is administered to the subject in a range of 0.001 to 100 mg/kg daily.

Priority Claims (1)
KR 10-2011-0011544 · Feb 9, 2011 · national
Continuity (2)
Continuation 13984567
Related Publication 20150017111A1 · Jan 15, 2015