发明名称 Novel Insulin Derivatives
摘要 The novel insulin derivates delivers, after administration to humans, insulin as a function of the glucose concentration in the tissue.
申请公布号 US2016229902(A1) 申请公布日期 2016.08.11
申请号 US201615131672 申请日期 2016.04.18
申请人 Novo Nordisk A/S 发明人 Hoeg-Jensen Thomas;Jakobsen Palle;Sensfuss Ulrich;Fledelius Christian;Ribel-Madsen Ulla
分类号 C07K14/62 主分类号 C07K14/62
代理机构 代理人
主权项 1. An insulin derivative of formula I: (Z1—Y1—X1)m-Ins-(X—Y—Z)n wherein n is zero or 1; m is zero or 1; with the proviso that not both n and m are zero; Ins represents insulin or an insulin analogue optionally having an A22 lysine, each Ins having an A chain and a B chain having a B29 lysine residue, from which a hydrogen atom has been removed from an ε amino group present in the B29 lysine residue, from an ε amino group present in the optional A22 lysine residue, or from the ε amino groups present in both the B29 and optional A22 lysine residues, and wherein the amino group present in the N terminal amino acid residue in the A chain, B chain, or both A and B chains, optionally, is substituted by one or two alkyl groups, and wherein —X—Y—Z or —X1—Y1—Z1 is independently attached to the ε amino group in one or both of the B29 lysine or A22 lysine residues in the insulin or insulin analogue; X and X1, independently of each other, is a bond, a moiety of formula —CO—(C1-C3-alkylene)-CH(COOH)—NH— wherein the amino group is connected to the Y/Y1 moiety or a moiety of formula —CO—(C1-C3-alkylene)-SO2—NH—, wherein the amino group is connected to the Y/Y1 moiety; Y and Y1, independently of each other, is ω-amino alkanoyl group is a straight or branched alkyl group containing 6 to 22 carbon atoms and wherein a hydrogen atom has been removed from the ω-amino group; and Z and Z1, independently of each other, is —SO2—Ar or —CO—Ar, wherein Ar is a phenyl group substituted by one or more —B(OH)2 groups and, optionally, substituted by one or more halogen atoms; with the proviso that if Z or Z1 is —SO2—Ar, then X or X1 is not a bond.
地址 Bagsvaerd DK