Patent ID: 6458924
Filing Date: 2002-10-01
Classification: A61K,C07K,C11D

Abstract:
A glucagon-like peptide-1 (GLP-1) derivative of formula I (SEQ ID NO:2):â€ƒ7â€ƒâ€ƒâ€ƒ8â€ƒâ€ƒâ€ƒ9â€ƒâ€ƒâ€ƒ10â€ƒâ€ƒ11â€ƒâ€ƒ12â€ƒâ€ƒ13â€ƒâ€ƒ14â€ƒâ€ƒ15â€ƒâ€ƒ16â€ƒâ€ƒ17His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser- 18â€ƒâ€ƒ19â€ƒâ€ƒ20â€ƒâ€ƒ21â€ƒâ€ƒ22â€ƒâ€ƒ23â€ƒâ€ƒ24â€ƒâ€ƒ25â€ƒâ€ƒ26â€ƒâ€ƒ27â€ƒâ€ƒ28Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe- 29â€ƒâ€ƒ30â€ƒâ€ƒ31â€ƒâ€ƒ32â€ƒâ€ƒ33â€ƒâ€ƒ34â€ƒâ€ƒ35â€ƒâ€ƒ36â€ƒâ€ƒ37Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gluwherein(a) the &egr;-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)nCOâ€” wherein n is 6, 8, 10, 12, 14, 16, 18, 20 or 22 (ii) HOOC(CH2)mCOâ€” 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 &ggr;-aminobutanoyl.