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    • 2. 发明申请
    • Skin Lightening Compositions
    • US20140154190A1
    • 2014-06-05
    • US14175360
    • 2014-02-07
    • Yoko NikiMasaki YoshidaMasamitsu IchihashiHideya AndoDaniel B. YaroshMary S. Matsui
    • Yoko NikiMasaki YoshidaMasamitsu IchihashiHideya AndoDaniel B. YaroshMary S. Matsui
    • A61K8/49A61Q17/04A61Q19/02
    • A61K8/4946A61K8/49A61K2800/782A61Q17/04A61Q19/02
    • Compositions and methods for lightening and/or depigmenting skin are provided, the compositions comprising compounds having the structure: wherein: R1 and R2 are same or different and are each selected from the group consisting of hydrogen, alkyl, carbomethoxy, carboethoxy, alkoxy, and alkanoyl, any of which may be halogen-substituted, and halogen; R6 is selected from the group consisting of hydrogen, methyl, and ethyl; and R3, R4 and R5 are the same or different and are each selected from the group consisting of hydrogen, methyl, methoxy, ethoxy, methoxyethoxy, ethoxyethoxy, propoxy, propoxymethoxy, and the like, any of which may be halogen-substituted; or having the structure: wherein: R2 is hydrogen, lower alkyl or hydroxy lower alkyl; R3 is lower alkyl, —CH2CN, hydroxy lower alkyl, —NO, —CH2N═C or (wherein R6 and R7 are independently selected from the group consisting of hydrogen and lower alkyl) or hydrogen provided R2 is not hydrogen; R4 is Z-T-W wherein Z represents —O—, —NH— or a single bond; T represents a straight- or branched-chain lower-alkylene group; when Z is a single bond, T also represents an ethenylene or a propenylene group wherein the unsaturated carbon is at the single bond; when Z is —O—, T also represents an allylene group wherein the saturated carbon is at the oxygen; and W represents hydrogen, when T is allylene and Z is —O—, and Ar, wherein Ar is selected from thienyl, pyridinyl, furanyl, phenyl and substituted phenyl wherein there are one or more substituents on the phenyl independently selected from halogen or lower alkyl; and R5 is hydrogen, halogen or lower alkyl; or pharmaceutically-, cosmetically- and dermatologically-acceptable salts, solvates, and bioprecursors, and stereoisomers and enantiomers of these compounds, free from or mixed with other enantiomers or stereoisomers; and such compounds in compositions with a pharmaceutically-, cosmetically- or dermatologically-acceptable carrier thereof comprising a safe and effective amount of the skin lightening or depigmenting compound.