KR970701685A - 피부 미백 조성물(skin lightening compositions) - Google Patents

피부 미백 조성물(skin lightening compositions)

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Publication number
KR970701685A
KR970701685A KR1019960704858A KR19960704858A KR970701685A KR 970701685 A KR970701685 A KR 970701685A KR 1019960704858 A KR1019960704858 A KR 1019960704858A KR 19960704858 A KR19960704858 A KR 19960704858A KR 970701685 A KR970701685 A KR 970701685A
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South Korea
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alkyl
group
hydrogen
iii
hydroxy
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KR1019960704858A
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칼라 린 크발네스
미첼 안토니 델롱
바톤 제임스 브래드버리
커티스 보비 모틀리
존 데이비드 카터
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레이서 제이코버스 코넬리스
더 프록터 앤드 갬블 캄파니
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Publication of KR970701685A publication Critical patent/KR970701685A/ko

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Abstract

본 발명은 하기 구조식(Ⅰ) 또는 (Ⅱ)를 갖는 활성 화합물을 사용하여 피부를 미백시키는 조성물, 화합물 및 방법, 및 이들 화합물의 약학적으로 허용가능한 염, 다른 거울이성질체 또는 입체이성질체를 갖지 않거나 또는 이들과 혼합된 그의 입체이성질체 및 거울이성질체; 및 환자의 피부를 미백시키는 활성성분 안전 효과량을 포함하는, 약학적으로 허용되는 담체와의 조성물을 이루는 이들 화합물에 관한 것이다.
상기 식에서, (ⅰ) 각각의 X는 독립적으로 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R 및 NRR로 이루어진 군으로부터 선택되고, X는 페놀 하이드록시에 대해 오르토 위치에 결합되는 경우 하이드록시, 아미노 및 티오가 아니며; (ⅱ) m은 0 내지 4의 정수이고; (ⅲ) 각각의 R' 및 R"은 독립적으로 수소, 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, OCRROR, COR, CR(OR), OR, CONRR, COOR, CRROR, CN, SR 및 NRR로 이루어진 군으로부터 선택되며, 존재하는 경우 할로는 하이드록시와 동일한 탄소상에 존재하지 않고; (ⅳ) R은 알킬 또는 치환된 알킬이고, R이 존재하고 R'이 또한 수소인 경우 R"은 수소, 하이드록시, 할로, 티오, 시아노 및 아미노가 아니며; (ⅴ) 각각의 R은 독립적으로 수소, 알킬, 치환된 알킬 및 아릴로 이루어진 군으로부터 선택되고; (ⅵ) n은 1 내지 약 5의 정수이고, (C)n중 하나 이상의 탄소는 치환기로서 알킬 또는 하이드록시 이외의 것을 갖고, Z에 인접한 (C)n은 R'으로서 아미노, SH, CN 또는 하이드록시 이외의 것을 가지며; (ⅶ) Z는 O, NR, S, SO, SO2, PO2R 및 POR로 이루어진 군으로부터 선택되고; (ⅷ) 하이드록시, 아미노, 시아노 및 티올로 이루어진 군으로부터 선택되는 하나의 치환제를 갖는 임의의 탄소는 이치환되는 경우 이 치환기가 R' 또는 R"인지에 관계없이 수소, 알킬 및 아릴로 이루어진 군으로부터 선택되는 다른 치환기를 갖는다.

Description

피부 미백 조성물(SKIN LIGHTENING COMPOSITIONS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. a) 하기 구조를 갖는 피부 미백 활성 화합물 유효량; 및 b) 약학적으로 허용가능한 담체를 포함하는 것을 특징으로 하는 피부 미백 조성물;
    상기 식에서, (ⅰ) 각 X는 독립적으로 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R 및 NRR로 이루어진 군으로부터 선택되고, X는 페놀 하이드록시에 대해 오르토 위치에 결합되는 경우 X는하이드록시, 아미노 또는 티오가 아니며; (ⅱ) m은 0 내지 4의 정수이고; (ⅲ) 각각의 R' 및 R"은 독립적으로 수소, 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, OCRROR, COR, CR(OR), OR, CONRR, COOR, CRROR, CN, SR 및 NRR로 이루어진 군으로부터 선택되고, 존재하는 경우 할로는 하이드록시, NH2또는 SH와 동일한 탄소상에 존재하지 않고; (ⅳ) R은 알킬 또는 치환된 알킬이고, R이 존재하고 R'이 또한 수소이면, R"은 수소, 하이드록시, 할로, 티오, 시아노 및 아미노가 아니며; (ⅴ) 각 R은 독립적으로 수소, 알킬, 치환된 알킬 및 아릴로 이루어진 군으로부터 선택되고; (ⅵ) n은 1 내지 약 5의 정수이고, (C)n의 하나 이상의 탄소는 치환기로서 알킬 또는 하이드록시 이외의 것을 갖고, Z에 인접한 (C)n은 R'으로서 아미노, SH, CN 또는 하이드록시 이외의 것을 가지며; (ⅶ) Z는 O, NR, S, SO, SO2, PO2R 및 POR로 이루어진 군으로부터 선택되고; (ⅷ) 하이드록시, 아미노, 시아노 및 티올로 이루어진 군으로부터 선택되는 하나의 치환체를 갖는 임의의 탄소는 이치환되는 경우 이 치환기가 R' 또는 R"인지에 관계없이 수소, 알킬 및 아릴로 이루어진 군으로부터 선택되는 다른 치환기를 갖는다.
  2. 제1항에 있어서, 활성성분이 4-〔(테트라하이드로-2H-피란-2-일)옥시〕페놀, 4-〔(1-에톡시에틸)옥시〕페놀, 4-〔(테트라하이드로-2H-티오피란-2-일)옥시〕페놀, 2-플루오로-4-〔(테트라하이드로-2H-피란-2-일)옥시〕페놀, 4-〔(테트라하이드로푸란-2-일)옥시〕페놀로 이루어진 군으로부터 선택되는 피부 미백 조성물.
  3. 하기 구조를 갖는 피부 미백 활성 화합물 :
    상기 식에서, (ⅰ) 각각의 X는 독립적으로 F, Cl, Br, C1-C4알킬, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R 및 NRR로 이루어진 군으로부터 선택되고, X는 페놀 하이드록시에 대해 오르토 위치에 있을 때 하이드록시, 아미노 또는 티오가 아니며; (ⅱ) m은 0 내지 4의 정수이고; (ⅲ) 각 R' 및 R"은 독립적으로 수소, 할로, C1-C10알킬, C1-C10치환된 알킬, 아릴, OR, OCOR, OCRROR, COR, CR(OR), OR, CONRR, COOR, CRROR, CN, SR 및 NRR로 이루어진 군으로부터 선택되며, 적어도 하나의 R'은 수소이고; (ⅳ) 각 R은 독립적으로 수소, C1-C10알킬, C1-C|10치환된 알킬 및 아릴로 이루어진 군으로부터 선택되고; (ⅵ) n은 1 내지 약 5의 정수이고, Z에 인접한 임의의 (C)n은 R'으로서 아미노, SH, CN 또는 하이드록시 이외의 것을 갖고; (ⅶ) Z는 NR, S, SO, SO2로 이루어진 군으로부터 선택되고; (ⅷ) 하나의 치환기로서 하이드록시, 아미노, 시아노 및 티올로 갖는 임의의 탄소는 이치환되는 경우 이 치환기가 R' 또는 R"인지에 상관없이 수소, 알킬, 치환된 알킬 및 아릴로 이루어진 군으로부터 선택되는 다른 치환제를 가지며; (ⅸ) R' 또는 R"으로서 존재하는 할로 또는 시아노는 하이드록시와 동일한 탄소상에 존재하지 않는다.
  4. 하기 구조를 갖는 피부 미백 활성 화합물 :
    상기 식에서, (ⅰ) X는 독립적으로 할로, 아릴, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R 및 NRR로 이루어진 군으로부터 선택되고, X가 페놀 하이드록시에 대해 오르토 위치에 있는 경우 하이드록시, 아미노 또는 티오가 아니며; (ⅱ) m은 0 내지 4의 정수이고; (ⅲ) 각 R' 및 R"은 독립적으로 수소, 알킬, 아릴, 알콕시, 아릴옥시, OCOR, COR, CONRR, COOR, OCRROR, CRROR로 이루어진 군으로부터 선택되고, R'이 수소인 경우 R"은 수소가 아니며; (ⅳ) R은 알킬 또는 치환된 알킬이고; (ⅴ) 각각의 R은 독립적으로 수소, 알킬, 치환된 알킬 및 아릴로 구성된 군으로부터 선택되고; (ⅵ) Z는 O, NR, S, SO, SO2, PO2R 및 POR로 이루어진 군으로부터 선택되고; (ⅶ) 하나의 치환기로서 하이드록시, 아미노, 시아노 및 티올로 갖는 임의의 탄소는 이치환되는 경우 수소, 알킬, 치환된 알킬 및 아릴로 이루어진 군으로부터 선택되는 다른 치환제를 갖는다.
  5. 하기 구조를 갖는 피부 미백 활성 화합물 :
    상기 식에서, (ⅰ) 각각의 X는 독립적으로 할로, 알킬, 아릴, OR, OCOR, COR, CONRR, COOR, CN, SR, SOR, SO2R, SO3R 및 NRR로 이루어진 군으로부터 선택되고, X가 페놀 하이드록시에 대해 오르토 위치에 있는 경우 하이드록시, 아미노 또는 티오가 아니며; (ⅱ) m은 0 내지 4의 정수이고; (ⅲ) 각각의 R" 및 R' 은 독립적으로 수소, 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, COR, CONRR, COOR, CN, SR 및 NRR로 이루어진 군으로부터 선택되고, (C)n중 하나 이상의 탄소는 수소로서의 R'을 갖고 약 3개 이하의 R'은 수소가 아니고, 존재하는 경우 할로는 하이드록시, NH2또는 SH와 동일한 탄소상에 존재하지 않으며; (ⅳ) 각각의 R은 독립적으로수소, 알킬 및 아릴로 이루어진 군으로부터 선택되고; (ⅴ) n은 1 내지 5의 정수이고, (C)n중 하나 이상의 탄소는 치환기로서 알킬 또는 하이드록시 이외의 것을 가지며, O에 인접한 (C)n은 R'으로서 아미노, SH, CN 또는 하이드록시 이외의 것을 갖는다.
  6. 제5항에 있어서, 하기 구조를 갖는 피부 미백 화합물.
    로 이루어진 군으로부터 선택되고; (ⅱ) R"은 수소, C1-C4알콕시, F, Cl, Br, CN이고, (ⅲ) 각각의 R'은 독립적으로 수소, 할로, 알킬, 치환된 알킬, 아릴, OR, OCOR, COR, CONRR, COOR, OCRROR, CRROR, CN, SR 및 NRR로 이루어진 군으로부터 선택되고, 고리에서 O와 동일한 탄소상에 존재하는 R'은 수소, 알킬, 할로알킬 및 아릴로부터 선택되며; (ⅳ) 각 R은 독립적으로 수소, 알킬 및 아릴로 이루어진 군으로부터 선택된다.
  7. 제1항 내지 제6항 중 어느 한 항에 있어서, 활성성분이 4-〔(1-에톡시에틸)옥시〕페놀, 4-〔(테트라하이드로-2H-티오피란-2-일)옥시〕페놀, 2-플루오로-4-〔(테트라하이드로-2H-피란-2-일)옥시〕페놀, 4-〔(테트라하이드로푸란-2-일)옥시〕페놀로 이루어진 군으로부터 선택되는 피부 미백 활성 화합물.
  8. 제1항 내지 제7항 중 어느 한 항에 있어서, 피부 미백 활성성분이 약 2㎛/㎠/h 이상의 Jmax를 갖는 피부 미백 조성물.
  9. 포유동물의 피부를 미색시키는 조성물을 제조하는데 제1항 내지 제8항 중 어느 한 항에 따른 화합물을 사용하는 용도.
  10. 피부 ㎠당 약 30㎍ 내지 약 750㎍의 화합물을 전달하는, 포유동물의 피부를 미백시키는 국부 조성물을 제조하는데 제1항 내지 제9항 중 어느 한 항에 따른 화합물을 사용하는 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960704858A 1994-03-04 1995-03-01 피부 미백 조성물(skin lightening compositions) KR970701685A (ko)

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CA2184478A1 (en) 1995-09-08
DE69524577T2 (de) 2002-10-31
WO1995023780A3 (en) 1995-09-28
ATE210623T1 (de) 2001-12-15
CN1112343C (zh) 2003-06-25
ES2164763T3 (es) 2002-03-01
JP3124460B2 (ja) 2001-01-15
AU1939995A (en) 1995-09-18
CZ257496A3 (en) 1997-01-15
EP0748307A1 (en) 1996-12-18
MX9603879A (es) 1997-09-30
CN1146196A (zh) 1997-03-26
EP0748307B1 (en) 2001-12-12
WO1995023780A2 (en) 1995-09-08
US6537527B1 (en) 2003-03-25
US6068834A (en) 2000-05-30
AU701828B2 (en) 1999-02-04
JPH0848620A (ja) 1996-02-20
DE69524577D1 (de) 2002-01-24

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