Inhibitors of melanocyte tyrosinase as topical skin lighteners
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-008/02
A01N-043/00
출원번호
UP-0206290
(2008-09-08)
등록번호
US-7858105
(2011-02-24)
발명자
/ 주소
Dooley, Thomas P.
Curto, Ernest V.
출원인 / 주소
Mediquest Therapeutics, Inc.
대리인 / 주소
Connolly Bove Lodge & Hutz LLP
인용정보
피인용 횟수 :
0인용 특허 :
2
초록▼
Methods and formulations are provided to reduce pigmentation in skin, using an array of compounds selected from benzimidazoles, phenylthioureas, phenylthiols, phenylamines, bi- and multicyclic phenols, thiopheneamines, and benzothiamides. The compounds preferably inhibit pigment synthesis in melanoc
Methods and formulations are provided to reduce pigmentation in skin, using an array of compounds selected from benzimidazoles, phenylthioureas, phenylthiols, phenylamines, bi- and multicyclic phenols, thiopheneamines, and benzothiamides. The compounds preferably inhibit pigment synthesis in melanocytes through the tyrosinase pathway. The methods can be used for lightening skin, and for treating uneven skin complexions which result from hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo. The compounds can be used medically or cosmetically.
대표청구항▼
What is claimed is: 1. A method of reducing pigmentation of skin for cosmetic effects in a mammal comprising administering to the mammal an effective amount of a compound defined by structure (I), or a pharmaceutically acceptable salt or ester thereof: wherein: R1 is H; R2 is selenium; R″
What is claimed is: 1. A method of reducing pigmentation of skin for cosmetic effects in a mammal comprising administering to the mammal an effective amount of a compound defined by structure (I), or a pharmaceutically acceptable salt or ester thereof: wherein: R1 is H; R2 is selenium; R″ is C or CH; when R″ is C, R′ is C(R8)2 or NR3 and forms a bond with R″; when R″ is CH, R′ is CH3 or NH2; R4, R5, R6, and R7 are independently CR8, or N; R3 is (i) substituted or unsubstituted alkyl, alkenyl, aryl, or heterocycle, (ii) —C1-5 alkoxy, (iii) —OH, (iv) hydrogen, (v) C(O)—C1-3 alkyl, or (vi) —(CH2)1-5SC(O)NR9R10; R8 is (i) hydrogen, (ii) halogen, (iii) NO2, (iv) —CN, (v) —OR10, (vi) —NHSO2—C1-3alkyl, (vii) —NHCO—C1-5 alkyl, (viii) oxime, (ix) hydrazine, (x) —NR9R10, (xi) HSO2, (xii) HSO3, (xiii) thio-C1-5 alkyl, (xiv) C1-5 acyloxy, (xv) H2PO3, (xvi) thiol, (xvii) —COOR9, (xiii) C1-5 alkynyl, or (xix) —C1-5 alkyl, —C1-5 alkenyl, aryl, heteroaryl, or heterocycle, optionally substituted with one or more of —OH, —SH, C(O)H, COOR9, C1-5 acyloxy, halogen, NR9R10, C1-5 thioether, or C1-5 alkoxy; R9 is hydrogen or C1-3 alkyl; and R10 is hydrogen, or C1-5 alkyl optionally substituted with —OH. 2. The method of claim 1 wherein R″ is C or CH, R4, R5, R6, and R7 are independently CR8, R8 is (i) hydrogen, (ii) halogen, (iii) —OR9, (iv) —OH, (v) —NR9R9, (vi) or (vii) —C1-5 alkyl or alkenyl optionally substituted with one or more of —OH, —SH, halogen, NH2, 2 or 3 of R4, R5, R6, and R7 are CH. 3. The method of claim 1 wherein R4, R5, R6, and R7 are independently selected from CR8, R8 is OR9, and 2 or 3 of R4, R5, R6, and R7 are CH. 4. The method of claim 1 wherein the compound has an IC50 against mammalian tyrosinase activity of less than or equal to 300 uM. 5. The method of claim 1 wherein the compound has an IC50 against melanin production in mammalian melanocytic cells of less than or equal to 300 uM. 6. The method of claim 1 wherein the compound absorbs ultraviolet radiation. 7. The method of claim 1 wherein the compound is an antioxidant. 8. The method of claim 1 wherein the mammal is a human. 9. The method of claim 1 wherein the administration is through a topical formulation or an occlusive patch. 10. The method of claim 1 wherein the method is for lightening skin pigmentation. 11. The method of claim 1 wherein R′ is NR3, R3 is H, R″ is C, each R4, R5, R6, and R7 is CR8, and R8 is H.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (2)
Tuloup, Remy; Blaise, Christian, Composition for topical application comprising at least one iminophenol compound.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.