申请人:Garibay Patrick William
公开号:US20080171695A1
公开(公告)日:2008-07-17
The present invention is related to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of B chain or to an ε-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethyleneglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH
2
and —COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.
本发明涉及胰岛素衍生物,其侧链通过酰胺键连接到B链的N-末端氨基酸残基的α-氨基基团或存在于亚基B中的Lys残基的ε-氨基基团上,该侧链独立地包含一种或多种乙二醇,丙二醇和/或丁二醇残基,其在每个末端分别包含从—NH2和—COOH中选择的基团;一种含有4到22个碳原子的脂肪二酸基团,其中至少有一个自由羧酸基团或在中性pH下带负电的基团;以及可能的连接剂,通过酰胺或醚键将侧链中的各个组分连接在一起,其中连接剂可以包括一个自由羧酸基团。