CONJUGUES TRIPEPTIDIQUES AGONISTES DE LA MSH
    5.
    发明公开
    CONJUGUES TRIPEPTIDIQUES AGONISTES DE LA MSH 有权
    CONJUGUES TRIPEPTIDIQUQUES AGONISTES DE LA MSH

    公开(公告)号:EP1745071A2

    公开(公告)日:2007-01-24

    申请号:EP05770969.3

    申请日:2005-05-10

    IPC分类号: C07K14/685

    CPC分类号: A61K47/542

    摘要: The invention relates to a tripeptide conjugate having general formula I, A-AA1-AA2-AA3-NH2, wherein A represents the radical corresponding to a monocarboxylic acid with general formula II, HOOC-R, in which: R represents a linear or branched aliphatic radical at C1-C24, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, lipoic acid or the reduced form thereof, dihydrolipoic acid, N- lipoyllysine, or phenylbutyric acid; and AA1, AA2 and AA3, which may be identical or different, represent independently of each other an amino acid selected from His, Phe, Ala, Arg, Lys, Orn, Trp, Nap, Tpi and Tic, on the condition that at least one of AA1, AA2 or AA3 represent Phe, preferably Dphe in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.

    摘要翻译: 本发明涉及具有通式I,A-AA1-AA2-AA3-NH2的三肽缀合物,其中A表示对应于具有通式II的一元羧酸HOOC-R的基团,其中:R表示直链或支链 脂族酸或其还原形式,二氢硫辛酸,N-硫辛酰赖氨酸或苯丁酸;以及任选地被羟基取代的C1-C24脂族基团,其可以包含一个或多个不饱和度,优选1-6个不饱和度, 并且AA1,AA2和AA3可以相同或不同,彼此独立地表示选自His,Phe,Ala,Arg,Lys,Orn,Trp,Nap,Tpi和Tic的氨基酸,条件是至少 AA1,AA2或AA3中的一个代表Phe,优选Dphe,其为对映异构体或非对映异构体及其混合物形式,包括外消旋混合物。

    CONJUGUES DIPEPTIDIQUES ANTAGONISTES DE L'ALPHA-MSH

    公开(公告)号:EP1750528A2

    公开(公告)日:2007-02-14

    申请号:EP05770970.1

    申请日:2005-05-10

    IPC分类号: A23L1/305

    摘要: The invention relates to a dipeptide conjugate having general formula I, AA2-AA1-NH2, wherein A represents the radical corresponding to a monocarboxylic acid with general formula II, HOOC-R, in which: R represents a linear or branched aliphatic radical at C1-C24, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, and/or which can comprise a phenyl group or lipoic acid or the reduced form thereof, dihydrolipoic acid or N-lipoyllysine; and AA1 and AA2 represent identical or different amino acids which are selected from the group containing Ala, Asn, Cys, Gln, Gly, Ile, Leu, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, Asp, Glu, Arg, His, Lys, Orn, Dap, Dab, the corresponding homo-amino acids and the corresponding beta-amino acids in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.

    摘要翻译: 本发明涉及具有通式I的二肽缀合物AA2-AA1-NH2,其中A代表对应于具有通式II的一元羧酸HOOC-R的基团,其中:R表示C1上的直链或支链脂族基团 -C24,其任选被羟基取代并且可以包含一个或多个不饱和度,优选1至6个不饱和度,和/或可以包含苯基或硫辛酸或其还原形式,二氢硫辛酸或N- 硫辛酰赖氨酸; 并且AA1和AA2代表选自Ala,Asn,Cys,Gln,Gly,Ile,Leu,Met,Phe,Pro,Ser,Thr,Trp,Tyr,Val,Asp,Glu的相同或不同的氨基酸 Arg,His,Lys,Orn,Dap,Dab,对应的同型氨基酸和对应的β-氨基酸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。