The invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
本发明涉及一种可选择 C 端延伸的 GLP-1 类似物的衍
生物,该衍
生物包括以 C20 或 C22 二酸基形式存在的第一和第二延伸分子、双
氨基支链连接体,以及第一和第二进一步连接体,每个连接体均包括 O
EG 样连接体元件;其中这些元件通过酰胺键相互连接,并连接到 GLP-1 类似物的赖
氨酸残基上。本发明还涉及掺入本发明衍
生物中的新型 GLP-1 类似物形式的中间产物,以及衍
生物的药物组合物和医疗用途。这些衍
生物具有很长的半衰期,同时又能保持令人满意的药效,因此可能适用于每月给药一次。