TAGMOSE, Tina Møller,MADSEN, Peter,KJELDSEN, Thomas Børglum
申请号：
ES09727247
公开号：
ES2563553T3
申请日:
2009.03.31
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound of formula II: M-Zn-Yo-Ins, or formula III: Alb-M-Zn-Yo-Ins in said formulas Ins represents insulin analogue, wherein said insulin analogue has a lysine residue at the C-terminal A chain, including the C-terminal extension of the chain, wherein said extension , compared with the A21 amino acid residue, consists of a single amino acid residue is lysine or a lysine residue at the C-terminal extension of amino acids in the chain consisting of 2-5 amino acid residues and optionally, wherein in said insulin analogue to six amino acid residues A1-A21 in and B1-B30 positions of human insulin have been deleted or replaced by another amino acid residue and M represents the thiol reactive group designated M after reaction with a thiol group of Alb (albumin) M represents a Michael acceptor represented by a malimido group, vinylsulfone, a thiol reactive group represented by iodide, pyridyldisulfide, methoxy or ethoxycarbonyl disulfide and o-nitrofenildisulfuro where M and M are connected, through the connector Zn-I, the epsilon-amino group of the lysine residue C-terminal A chain, where said epsilon-amino group has been removed a hydrogen atom Z is a covalent bond, or represents a portion of one of the following six formulas: -NH- (CH2-CH2-O) p-CH2- CO- -NH- (CH2) q-CH2-CO- -NH- (CH2-CH2-O) r-CH2-CH2-CO- -HN-CH2-CH2-NH-CO- -NH-CH2-CH2-O-CH2-CH2-CH2-CH2-NHCO- CO- and -NH-C6H4-CO- wherein p is 0 (zero) or an integer in the range from 1 to 24 q is 0 (zero) or an integer in the range from 1 to 24 r is 0 (zero) or an integer in the range from 1 to 24 and -C6H4- is para-phenylene n represents an integer in the range from 1 to 10 And it has one of the meanings given for Z o is 0 to 10 and Alb is selected from the group consisting of Albagen and human serum albumin.Un compuesto de fórmula II: M-Zn-Yo-Ins, o de fórmula III: Alb-M-Zn-Yo-Ins en dichas fórmulas Ins representa un análogo de la insulina, donde dicho análogo de la insulina tiene un residuo de lisina en el extremo C
