Patent ID: 6268343
Filing Date: 2001-07-31
Classification: A61K,A61P,C07K,C11D

Abstract:
A GLP-1 derivative of formula I (SEQ ID NO:2):7 8 9 10 11 12 13 14 15 16 17 His-Xaa-Xaa-Gly-Xaa-Phe-Thr-Xaa-Asp-Xaa-Xaa- 18 19 20 21 22 23 24 25 26 27 28 Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Phe- 29 30 31 32 33 34 35 36 37 Ile-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-XaawhereinXaa at position 8 is Ala,Xaa at position 9 is Glu,Xaa at position 11 is Thr,Xaa at position 14 is Ser,Xaa at position 16 is Val,Xaa at position 17 is Ser,Xaa at position 18 is Ser,Xaa at position 19 is Tyr,Xaa at position 20 is Leu,Xaa at position 21 is Glu,Xaa at position 22 is Gly,Xaa at position 23 is Gln,Xaa at position 24 is Ala,Xaa at position 25 is Ala,Xaa at position 26 is Lys,Xaa at position 27 is Glu,Xaa at position 30 is Ala,Xaa at position 31 is Trp,Xaa at position 32 is Leu,Xaa at position 33 is Val,Xaa at position 34 is Arg,Xaa at position 35 is Gly,Xaa at position 36 is Arg, andXaa at position 37 is Gly,wherein(a) the .epsilon.-amino group of Lys at position 26 is substituted with a lipophilic substituent, optionally via a spacer,(b) the lipophilic substituent is (i) CH.sub.3 (CH.sub.2).sub.n CO-- wherein n is 6, 8, 10, 12, 14, 16, 18, 20 or 22, (ii) HOOC(CH.sub.2).sub.m CO-- wherein m is 10, 12, 14, 16, 18, 20 or 22, or (iii) lithochoyl, and(c) the spacer is (i) an unbranched alkane .alpha.,.omega.-dicarboxylic acid group having from 1 to 7 methylene groups, (ii) an amino acid residue except Cys, or (iii) .gamma.-aminobutanoyl.