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US 6,458,924 B2Granted
Derivatives of GLP-1 analogs
AssigneeNovo Nordisk A/S
InventorsLiselotte Bjerre Knudsen, Per Olaf Huusfeldt, Per Franklin Nielsen
Life of this patent
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Abstract
The present invention relates to a pharmaceutical composition comprising a GLP-1 derivative having a lipophilic substituent; and a surfactant.
Claims20
A glucagon-like peptide-1 (GLP-1) derivative of formula I (SEQ ID NO:2):
- 7 8 9 10 11 12 13 14 15 16 17 His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser- 18 19 20 21 22 23 24 25 26 27 28 Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe- 29 30 31 32 33 34 35 36 37 Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Glu
- wherein
- (a) the ε-amino group of Lys at position 26 is substituted with a lipophilic substituent optionally via a spacer, and
- (b) the lipophilic substituent is (i) CH3(CH2)nCO— wherein n is 6, 8, 10, 12, 14, 16, 18, 20 or 22 (ii) HOOC(CH2)mCO— wherein m is 10, 12, 14, 16, 18, 20 or 22, or (iii) lithocholyl, and
- (c) the spacer is an amino acid residue except Cys, or the spacer is γ-aminobutanoyl.
2 more elements
Dependencies are inferred from the claim text.