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    • 3. 发明授权
    • Peptides or peptidic conjugate derivatives of MSH and the use thereof for cosmetically fighting against canities
    • MSH的肽或肽结合物衍生物及其用于美容防御的方法
    • US07785577B2
    • 2010-08-31
    • US11596288
    • 2005-05-10
    • Michel HocquauxAnne-Marie PinelJean MartinezGilles Subra
    • Michel HocquauxAnne-Marie PinelJean MartinezGilles Subra
    • A61K8/64
    • A61K47/54
    • The invention relates to a peptide of formula W-DPhe-Arg-Z (I) and to a conjugate thereof of a formula A-W-DPhe-Arg-Z (II), wherein A is a radical corresponding to a monocarboxylic acid of general formula HOOC—R (III), wherein R is an linear or branched possibly substituted by a hydroxy group aliphatic C1-C24 radical which can comprise one or several unsaturations, preferably from 1 to 6 unsaturations, a lipoic acid or the reduced form thereof, a dihydrolipoic acid, N-lipoyl-lysine or a phenylbutyric acid, W is His, Ala-His, Ala-Ala-His, Nle-Ala-His, DTrp-Ala-His, Nle-Trp-His, Lys, Ala-Lys, Nle-Ala-Lys, Orn, Ala-Orn, Nle-Ala-Orn, Ala, Nle-Ala-Ala, Arg, Ala-Arg. Nle-Ala-Arg, Nle-Ala-DTrp or a bond in case of compounds of formula (II), Z is NH2, OH and OR, wherein R is a linear or branched aliphatic C1-C24 radical, TrpNH2, NapNH2, TpiNH2, TicNH2, AlaNH2i TrpOH, NapOH, TpiOH, TicOH, AlaOH, PheNH2, or PheOH, exempting a peptidic conjugate for which A is a radical corresponding to an acetic acid, W is Nle-Ala-His and Z is TrpNH2 in the form of enantiomers or diastereoisomer and the mixtures thereof including racemic mixtures. The use of the inventive compounds for cosmetically fighting against canities is also disclosed.
    • 本发明涉及式W-DPhe-Arg-Z(I)的肽及其与式AW-DPhe-Arg-Z(II)的结合物,其中A是相应于通式 HOOC-R(III),其中R是可以被羟基脂族C 1 -C 24基取代的直链或支链,其可以包含一个或多个不饱和基团,优选1至6个不饱和基团,硫辛酸或其还原形式, 二氢硫辛酸,N-脂酰赖氨酸或苯丁酸,W是His,Ala-His,Ala-Ala-His,Nle-Ala-His,DTrp-Ala-His,Nle-Trp-His,Lys,Ala-Lys ,Nle-Ala-Lys,Orn,Ala-Orn,Nle-Ala-Orn,Ala,Nle-Ala-Ala,Arg,Ala-Arg。 Nle-Ala-Arg,Nle-Ala-DTrp或在式(II)化合物的情况下为键,Z为NH 2,OH和OR,其中R为直链或支链脂族C 1 -C 24基团,TrpNH 2,NapNH 2,TpiNH 2 ,TicNH2,AlaNH2i TrpOH,NapOH,TpiOH,TicOH,AlaOH,PheNH2或PheOH,免除其中A是对应于乙酸的基团的肽结合物,W是Nle-Ala-His,Z是TrpNH2,其形式为 对映异构体或非对映异构体及其混合物,包括外消旋混合物。 还公开了本发明化合物用于美容化妆品的用途。
    • 4. 发明申请
    • Peptides or Peptidic Conjugate Derivatives of Msh and the Use Thereof for Cosmetically Fighting Against Canities
    • Msh的肽或肽结合物衍生物及其用于化妆品抗争的用途
    • US20080200396A1
    • 2008-08-21
    • US11596288
    • 2005-05-10
    • Michel HocquauxAnne-Marie PinelJean MartinezGilles Subra
    • Michel HocquauxAnne-Marie PinelJean MartinezGilles Subra
    • A61K8/64A61Q5/00
    • A61K47/54
    • The invention relates to a peptide of formula W-DPhe-Arg-Z (I) and to a conjugate thereof of a formula A-W-DPhe-Arg-Z (II), wherein A is a radical corresponding to a nionocarboxylic acid of general formula HOOC—R (III), wherein R is an linear or branched possibly substituted by a hydroxy group aliphatic C1-C24 radical which can comprise one or several unsaturations, preferably from 1 to 6 unsaturations, a lipoic acid or the reduced form thereof, a dihydrolipoic acid, N-lipoyl-lysine or a phenylbutyric acid, W is His, Ala-His, Ala-Ala-His, Nle-Ala-His, DTrp-Ala-His, Nle-Trp-His, Lys, Ala-Lys, Nle-Ala-Lys, Orn, Ala-Orn, Nle-Ala-Orn, Ala, Nle-Ala-Ala, Arg, Ala-Arg. Nle-Ala-Arg, Nle-Ala-DTrp or a bond in case of compounds of formula (II), Z is NH2, OH and OR, wherein R is a linear or branched aliphatic C1-C24 radical, TrpNH2, NapNH2, TpiNH2, TicNH2, AlaNH2i TrpOH, NapOH, TpiOH, TicOH, AlaOH, PheNH2, or PheOH, exempting a peptidic conjugate for which A is a radical corresponding to an acetic acid, W is Nle-Ala-His and Z is TrpNH2 in the form of enantiomers or diastereoisomer and the mixtures thereof including racemic mixtures. The use of the inventive compounds for cosmetically fighting against canities is also disclosed.
    • 本发明涉及式W-DPhe-Arg-Z(I)的肽及其与式AW-DPhe-Arg-Z(II)的共轭物,其中A是相应于通式 HOOC-R(III),其中R是可以被羟基脂族C 1 -C 24 - 基团取代的直链或支链,其可以包含一个或几个不饱和基团,优选 1至6个不饱和键,硫辛酸或其还原形式,二氢硫辛酸,N-脂酰赖氨酸或苯丁酸,W是His,Ala-His,Ala-Ala-His,Nle-Ala-His,DTrp -Ale-His,Nle-Trp-His,Lys,Ala-Lys,Nle-Ala-Lys,Orn,Ala-Orn,Nle-Ala-Orn,Ala,Nle-Ala-Ala,Arg,Ala-Arg。 Nle-Ala-Arg,Nle-Ala-DTrp或在式(II)化合物的情况下为键,Z为NH 2,OH和OR,其中R为直链或支链脂族C 1, N,N,N,N,N,N,N,N,N, 2 N,AlaNH 2,TrpOH,NapOH,TpiOH,TicOH,AlaOH,PheNH 2 H或PheOH,可以免除A为 对应于乙酸的基团,W是Nle-Ala-His,Z是对映异构体或非对映异构体形式的TrpNH 2 H 2,其混合物包括外消旋混合物。 还公开了本发明化合物用于美容化妆品的用途。