Compounds which inhibit neuronal exocytosis (III)

Compounds which inhibit neuronal exocytosis (III)

  • CN 104,334,156 A
  • Filed: 04/12/2013
  • Published: 02/04/2015
  • Est. Priority Date: 04/13/2012
  • Status: Active Application
First Claim
Patent Images

1. general formula (I) compound:

  • R 1-W n-X m-AA 1-AA 2-AA 3-AA 4-AA 5-AA 6-AA 7-AA 8-AA 9-Y p-Z q-R 2(I) Its stereoisomer, its mixture and/or its cosmetically or pharmaceutically acceptable salt, it is characterized in that;

    AA 1be selected from the group of following formation ;

    -Arg-,-His-,-Lys-,-Gln-,-Asn-,-Glu-and-Asp-;

    AA 2be selected from the group of following formation ;

    -Arg-,-His-,-Lys-,-Gln-,-Asn-,-Glu-and-Asp-;

    AA 3be selected from the group of following formation ;

    -Leu-,-Ile-,-Val-,-Met-,-MetO-,-MetO 2-,-Glu-,-Asp-,-Phe-,-Trp-and-Tyr-;

    AA 4be selected from the group of following formation ;

    -Lys-,-His-,-Glu-and-Asp-;

    AA 5be selected from the group of following formation ;

    -Arg-,-His-,-Lys-,-Gln-,-Asn-,-Glu-and-Asp-;

    AA 6be selected from the group of following formation ;

    -Met-,-MetO-,-MetO 2-,-Ile-,-Leu-,-Val-,-His-,-Lys-and-Arg-;

    AA 7be selected from the group of following formation ;

    -Met-,-MetO-and-MetO 2-;

    AA 8be selected from the group of following formation ;

    -Glu-,-Asp-,-Gly-,-Ala-and-Pro-;

    AA 9be selected from the group of following formation ;

    -Gln-,-Asn-or key;

    W, X, Y, Z are aminoacid and are select independently among themselves;

    N, m, p and q be among themselves select independently and there is the value of 0 or 1;

    N+m+p+q is less than or equal to 2;

    Condition is if AA 1-Arg-, AA 2-Gln-, AA 3-Leu-, AA 4-Glu-, AA 5-His-, AA 6-Val-and AA 9key, so AA 8be selected from the group of following formation ;

    -Glu-,-Gly-,-Ala-and-Pro-;

    With condition be if AA 1-Lys-, AA 2-Arg-, AA 3-Phe-, AA 4-His-, AA 5-Asn-, AA 6-Ile-, AA 8-Gly-and AA 9be key, so n+m+p+q equals 0;

    R 1be selected from by the following group formed;

    H, derived from the polymer of Polyethylene Glycol, that non-annularity replaces or be unsubstituted aliphatic group, that replace or be unsubstituted alcyl, that replace or be unsubstituted heterocyclic radical, that replace or the heteroaryl alkyl that is unsubstituted, replacement or the aryl that is unsubstituted, replacement or the aralkyl that is unsubstituted and R 5-CO-, wherein R 5be selected from the group of following formation;

    H, that non-annularity replaces or be unsubstituted aliphatic group, that replace or be unsubstituted alcyl, that replace or be unsubstituted aryl, that replace or the aralkyl that is unsubstituted, replacement or the heterocyclic radical that is unsubstituted and replacement or the heteroaryl alkyl that is unsubstituted;

    R 2be selected from by the following group formed ;

    -NR 3r 4,-OR 3with-SR 3, wherein R 3and R 4group independently selected from following formation;

    H, derived from the polymer of Polyethylene Glycol, that non-annularity replaces or be unsubstituted aliphatic group, that replace or be unsubstituted alcyl, that replace or be unsubstituted heterocyclic radical, that replace or the heteroaryl alkyl that is unsubstituted, replacement or the aryl that is unsubstituted, and replace or the aralkyl that is unsubstituted;

    With R 1and R 2it not a-amino acid.

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