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US 12,703,731 B2Granted
Long-acting GLP-1 compound
AssigneeGan & Lee Pharmaceuticals
InventorsZhongru Gan, Wei Chen, Yining Zhang, Fangkai Xue, Lingyu Cai, Jianghong Niu, Bin Mu
Life of this patent
Estimating the term…
Abstract
A novel GLP-1 derivative, compared with GLP-1 derivatives such as liraglutide and semaglutide which are on the market, has comparable or better effect, potency or efficacy, longer or comparable duration of action in vivo or half-life in vivo, has better or comparable GLP-1 receptor binding affinity and has better or comparable DPP-IV stability.
Claims11
A compound of formula (B):
- or a pharmaceutically acceptable salt, amide or ester thereof,
- wherein
- G1 is a [Gly8, Arg34]GLP-1-(7-37) peptide of SEQ ID NO:
- 2;
- [Acy-(L1)r-(L2)q] is a substituent linked to the ε amino group of the Lys residue at position 26 of the [Gly8, Arg34]GLP-1-(7-37) peptide;
- r is 1;
- q is 1 or 2;
- Acy is a fatty diacid comprising 20, 21 or 22 carbon atoms, wherein formally, a hydroxyl group has been removed from one of the carboxyl groups in the fatty diacid;
- L1 is the amino acid residue of γGlu;
- L2 is-HN-(CH2)2-O-(CH2)2-O-CH2-CO-;
- Acy, L1 and L2 are linked by amide bonds;
- and
- the C-terminus of L2 is linked to the ε amino group of the Lys residue at position 26 of the [Gly8, Arg34]GLP-1-(7-37) peptide.
10 more elements
A compound selected from the group consisting of:
- N-ε26-[2-(2-[2-(4-[19-carboxynonadecanoylamino]-4 (S)-carboxybutanoylamino)ethoxy]ethoxy) acetyl][Gly8, Arg34]GLP-1-(7-37) peptide;
- and
- N-ε26-[2-(2-[2-(2-[2-(2-[4-(21-carboxyheneicosanoylamino)-4 (S)-carboxybutanoylamino]ethoxy)ethoxy]acetylamino)ethoxy]ethoxy) acetyl][Gly8, Arg34]GLP-1-(7-37) peptide,
- or a pharmaceutically acceptable salt, amide or ester thereof.
1 more element
A compound having the structure:
- wherein the amino acid sequence in the compound is that of SEQ ID NO:
- 2.
A compound having the structure:
- wherein the amino acid sequence in the compound is that of SEQ ID NO:
- 2.
Dependencies are inferred from the claim text.