CAS: 72584-75-9; (S)-2,9-Diacetyloxy-5,6,6A,7-Tetrahydro-1,10-Dimethoxy-6-Methyl-4H-Dibenzo[de,G]Quinoline

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    专利号:CN-110831934-B
    优先权日:2017-05-12
    标 题:Method for the synthesis of N-acyl compounds without the use of organic solvents or acid chlorides

    专利号:US-2011236330-A1
    优先权日:2008-12-09
    标 题:Skin Whitening
    发明人:MOUSSOU PHILIPPE; SABADOTTO MELANIE; RATHJENS ANDREAS
    权利人:MOUSSOU PHILIPPE; SABADOTTO MELANIE; RATHJENS ANDREAS
    摘要:Methods for reducing pigmentation or hyperpigmentation of skin comprising applying to the skin a substance of formula (I) in the D-form, L-form or racemic form (D,L) are disclosed: n n n n n n n n n n whereinn R 1 is selected from the group consisting of a hydrogen group (—H), a methyl group (—CH 3 ), an ethyl group (—CH 2 CH 3 ), a C3 alkyl group, a C4 alkyl group, an acetyl group (—C(O)CH 3 ), a propanoyl group (—C(O)CH 2 CH 3 ), an n-butanoyl group (—C(O)CH 2 CH 2 CH 3 ), and a 2-methyl-propanoyl group (—C(O)CH(CH 3 ) 2 ), R 2 is selected from the group consisting of a hydrogen group (—H), an ethyl group (CH 2 CH 3 ), a C3 alkyl group, a C4 alkyl group, an acetyl group (—C(O)CH 3 ), a propanoyl group (—C(O)CH 2 CH 3 ), an n-butanoyl group (—C(O)CH 2 CH 2 CH 3 ), and a 2-methyl-propanoyl group (—C(O)CH(CH 3 ) 2 ), R 3 is selected from the group consisting of a hydroxyl group (—OH), an amino group (NH 2 ), a methoxy group (OCH 3 ), an ethoxy group (—OCH 2 CH 3 ), a C3 alkoxy group, a C4 alkoxy group, and a benzyloxy group (—OCH 2 C 6 H 5 ), and X and Y are independently selected from the group consisting of a hydrogen group (—H), a methyl group (—CH 3 ), an ethyl group (—CH 2 CH 3 ), a C3 group alkyl, a C4 alkyl group, a halogen group, a methoxy group (—OCH 3 ), an ethoxy group (—OCH 2 CH 3 ), a C3 alkoxy group, a C4 alkoxy group, and a benzyloxy group (—OCH 2 C 6 H 5 ), provided that at least one of X and Y is not a hydrogen group (—H). nn Cosmetic compositions and/or topical compositions comprising the substance are useful for (i) lightening of the skin and/or (ii) whitening of the skin and/or (iii) reduction of pigmentation of the skin and/or (iv) reduction of hyperpigmentation of the skin and/or (v) inhibition of melanogenesis in the skin and/or (vi) prevention and/or retardation of signs of ageing and/or improving the skin appearance of an aged skin. Such composition are also useful for treatment of pigmentation or hyperpigmentation of the skin due to abnormal melanin synthesis and/or secretion.

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    1: Pratchyapurit WO. Combined use of two formulations containing diacetyl boldine, TGF-β1 biomimetic oligopeptide-68 with other hypopigmenting/exfoliating agents and sunscreen provides effective and convenient treatment for facial melasma. Either is equal to or is better than 4% hydroquinone on normal skin. J Cosmet Dermatol. 2016 Jun;15(2):131-44. doi: 10.1111/jocd.12201. Epub 2016 Feb 2. Epub 2006 Aug 21.
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