GLP-2 compounds, formulations, and uses thereof
First Claim
Patent Images
1. A peptide comprising the amino acid sequence of formula I His-X2-X3-Gly-X5-Phe-X7-X8-X9-X10-X1-X12-X13-X14-X15-X16-X17-X18-Ala-Arg-X21-Phe-Ile-X24-Trp-Leu-Ile-X28-Thr-Arg-Ile-Thr-X33
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(formula I);
wherein X2 is Ala, Val, or Gly;
X3 is Asp or Glu;
X5 is Ser or Lys;
X7 is Ser or Lys;
X8 is Asp, Glu, or Lys;
X9 is Asp, Glu, or Lys;
X10 is Met, Lys, Leu, Ile, or Nor-Leucine;
X11 is Asn or Lys;
X12 is Thr or Lys;
X13 is Ile or Lys;
X14 is Leu or Lys;
X15 is Asp or Lys;
X16 is Asn or Lys;
X17 is Leu or Lys;
X18 is Ala or Lys;
X21 is Asp or Lys;
X24 is Asn or Lys;
X28 is Gin or Lys;
X33 is Asp, Glu, or Lys.
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Abstract
The present invention relates to novel human glucagon-like peptide-2 (GLP-2) peptides and human glucagon-like peptide-2 derivatives which have a protracted profile of action as well as polynucleotide constructs encoding such peptides, vectors and host cells comprising and expressing the polynucleotide, pharmaceutical compositions, uses and methods of treatment.
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Citations
81 Claims
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1. A peptide comprising the amino acid sequence of formula I
His-X2-X3-Gly-X5-Phe-X7-X8-X9-X10-X1-X12-X13-X14-X15-X16-X17-X18-Ala-Arg-X21-Phe-Ile-X24-Trp-Leu-Ile-X28-Thr-Arg-Ile-Thr-X33 -
(formula I);
wherein X2 is Ala, Val, or Gly;
X3 is Asp or Glu;
X5 is Ser or Lys;
X7 is Ser or Lys;
X8 is Asp, Glu, or Lys;
X9 is Asp, Glu, or Lys;
X10 is Met, Lys, Leu, Ile, or Nor-Leucine;
X11 is Asn or Lys;
X12 is Thr or Lys;
X13 is Ile or Lys;
X14 is Leu or Lys;
X15 is Asp or Lys;
X16 is Asn or Lys;
X17 is Leu or Lys;
X18 is Ala or Lys;
X21 is Asp or Lys;
X24 is Asn or Lys;
X28 is Gin or Lys;
X33 is Asp, Glu, or Lys. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 80)
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41. A GLP-2 derivative comprising a GLP-2 parent peptide, wherein a lipophilic substituent is attached to one or more amino acid residues of the GLP-2 parent peptide at a position relative to the amino acid sequence of SEQ ID NO:
- 1 independently selected from the group consisting of S5, S7, D8, E9, M10, N11, T12, 113, L14, D15, N16, L17, A18, D21, N24, and Q28, with the proviso that said lipophilic substituent is not attached at the N-terminal amino acid residue or the C-terminal amino acid residue of the GLP-2 parent peptide.
- View Dependent Claims (42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79)
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81. A GLP-2 peptide comprising the amino acid sequence of formula I
His-X2-X3-Gly-X5-Phe-X7-X8-X9-X10-X1-X12-X13-X14-X15-X16-X17-X18-Ala-Arg-X21-Phe-Ile-X24-Trp-Leu-Ile-X28-Thr-Arg-Ile-Thr-X33 -
(formula I);
or a fragment thereof;
wherein X2 is Ala, Val, or Gly;
X3 is Asp or Glu;
X5 is Ser or Lys;
X7 is Ser or Lys;
X8 is Asp, Glu, or Lys;
X9 is Asp, Glu, or Lys;
X10 is Met, Lys, Leu, Ile, or Nor-Leucine;
X11 is Asn or Lys;
X12 is Thr or Lys;
X13 is Ile or Lys;
X14 is Leu or Lys;
X15 is Asp or Lys;
X16 is Asn or Lys;
X17 is Leu or Lys;
X18 is Ala or Lys;
X21 is Asp or Lys;
X24 is Asn or Lys;
X28 is Gln or Lys;
X33 is Asp, Glu, or Lys.
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Specification