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GIP-GLP-1 dual agonist compounds and methods

  • US 10,093,713 B2
  • Filed: 11/06/2014
  • Issued: 10/09/2018
  • Est. Priority Date: 11/06/2013
  • Status: Active Grant
First Claim
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1. A GIP analogue having the general Formula I:


  • R1-Tyr-X2-Glu-Gly-Thr-Phe-Thr-Ser-Asp-X10-Ser-Ile-X13-Leu-X15-X16-Ψ

    -Ala-X19-X20-X21-Phe-X23-X24-Trp-Leu-X27-X28-X29-X30-R2



    (SEQ ID NO;

         56) (I)whereinR1 is H, C1-4 alkyl, acetyl, formyl, benzoyl, trifluoroacetyl or pGlu;

    X2 is selected from Aib and D-Ala;

    X10 is selected from Tyr and Leu;

    X13 is selected from Ala, Tyr and Aib;

    X15 is selected from Asp and Glu;

    X16 is selected from Glu and Lys;

    X19 is selected from Gln and Ala;

    X20 is selected from Lys and Arg;

    X21 is selected from Ala and Glu;

    X23 is selected from Val and Ile;

    X24 is selected from Asn and Glu;

    X27 is selected from Leu, Glu and Val;

    X28 is selected from Ala, Ser and Arg;

    X29 is selected from Aib, Ala, and Gln;

    X30 is selected from Lys, Gly and Y1, or is absent;

    Y1 (when present) is selected from Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser (SEQ ID NO;

         57), Lys-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser (SEQ ID NO;

         58), Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser (SEQ ID NO;

         59), Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser (SEQ ID NO;

         60) and Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser (SEQ ID NO;

         61);

    Ψ

    is a residue of Lys, Arg, Orn or Cys in which the side chain is conjugated to a substituent having the formula —

    Z2-Z1, wherein Z2-Z1 is;

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