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Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases

  • US 10,023,614 B2
  • Filed: 12/04/2017
  • Issued: 07/17/2018
  • Est. Priority Date: 07/17/2014
  • Status: Active Grant
First Claim
Patent Images

1. A peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt thereof, comprising an amino acid sequence consisting of Formula (Xa):


  • X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-X19-X20 



    (Xa),whereinX1 is absent;

    X2 is absent;

    X3 is Glu, (D)Glu, Arg, (D)Arg, Phe, (D)Phe, 2-Nal, Thr, Leu, (D)Gln, or absent;

    X4 is Pen;

    X5 is Dap, Dap(Ac), Gly, Lys, Gln, Arg, Ser, Thr, or Asn;

    X6 is Thr;

    X7 is Trp;

    X8 is Gln;

    X9 is Pen;

    X10 is 2-Nal, a Phe analog, Tyr, or a Tyr analog;

    X11 is 1-Nal, 2-Nal, Phe(3,4-dimethoxy), or Phe(3,4-Cl2);

    X12 is Acpc, Acbc, Acvc, Achc, Aib, α

    -DiethylGly, α

    -MeLys, α

    -MeLys(Ac), α

    -MeLeu, α

    -MeOrn, α

    -MeSer, α

    -MeVal, Cha, Cit, hLeu, Lys, Leu, Arg, or 4-amino-4-carboxy-tetrahydropyran;

    X13 is Cit, Asp, Glu, Lys, Lys(Ac), Asn, or Gln;

    X14 is Dab(Ac), Dap(Ac), His, Lys(Ac), Asn, Gln, or Tyr;

    X15 is Ala, betaAla, Gly, Asn, Gln, or Ser;

    X16 is any amino acid or absent;

    X17 is any amino acid or absent;

    X18 is any amino acid or absent;

    X19 is any amino acid or absent; and

    X20 is any amino acid or absent, wherein the peptide inhibitor is cyclized via a disulfide bond between X4 and X9 of the amino acid sequence, andwherein 2-Nal is L-2-Naphthylalanine, Pen is L-Penicillamine, Dap is L-Diaminopropionic acid, Dap(Ac) is L-Diaminopropionic acid(Ac), 1-Nal is L-1-Naphthylalanine,Acpc is 1-aminocyclopropylcarboxylic acid, Acbc is 1-aminocyclobutanecarboxylic acid, Acvc is 1-aminocyclopentanecarboxylic acid, Achc is 1-aminocyclohexanecarboxylic acid, Aib is 2-aminoisobutyric acid, α

    -MeLys is alpha-methyl-L-Lysine, α

    -MeLys(Ac) is alpha-methyl-L-Lysine(Ac), α

    -MeLeu is alpha-methyl-L-Leucine, α

    -MeOrn is alpha-methyl-L-Ornathine, α

    -MeSer is alpha-methyl-L-Serine, α

    -MeVal is alpha-methyl-L-Valine, Cha is Cyclohexyl-L-alanine, Cit is L-Citrulline, hLeu is L-homoLeucine, Dab(Ac) is L-Diaminobutyric acid(Ac), and betaAla is Beta-alanine.

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