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US 9,260,503 B2Granted
Multi-substituted insulins
AssigneeNovo Nordisk A/S
InventorsThomas Hoeg-Jensen, Peter Madsen, Jane Spetzler, Tina Moeller Tagmose
Life of this patent
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Abstract
The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical comprising such an insulin derivative.
Claims15
A soluble insulin derivative or pharmaceutically acceptable salt thereof selected from the group consisting of
- A1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H desB27 desB30 human insulin,
- A1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H desB30 human insulin,
- A1Nα-hexadecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B1Nα-hexadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H desB27 desB30 human insulin,
- A1Nα-tetradecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B1Nα-tetradecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H desB27 desB30 human insulin,
- A1Nα-hexadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl B1Nα-hexadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H desB30 human insulin,
- B1N-octadecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B29Nε-octadecandioyl-γ-L-glutamyl-OEG-OEG A14E B25H desB30 human insulin,
- A1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl B29Nε-octadecandioyl-γ-L-glutamyl-OEG-OEG A14E B25H desB30 human insulin,
- B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl B29Nε-octadecandioyl-γ-L-glutamyl-OEG-OEG A14E B16H B25H desB30human insulin,
- B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-4-aminomethyl-benzyl A14E B25H B29Nε-octadecandioyl-γ-L-glutamyl-OEG-OEG desB30human insulin, and
- B1Nα-octadecandioyl-γ-L-glutamyl-OEG-OEG-aminomethyl-benzyl B29Nε-octadecandioyl-γ-L-glutamyl-OEG-OEG A14E B25H desB27 desB30 human insulin,
- wherein OEG is *—NH—(CH2)2O—(CH2)2O—CH2CO—*.
8 more elements
A soluble insulin derivative or a pharmaceutically acceptable salt thereof of general formula
- XZn-Ins-Z1mX1,
- wherein
- Ins represents an insulin comprising a B29 lysine or B29 arginine residue and/or a A22 lysine residue, X is a fatty diacid substitution, X1 is a fatty diacid substitution, Z is a linker between X and Ins, Z1 is a linker between Ins and X1, n is zero or 1, and m is zero or 1, and wherein at least one of Z and Z1 comprises OEG-OEG-aminomethyl-benzyl, wherein OEG is *—NH—(CH2)2O—(CH2)2O—CH2CO—*.
Dependencies are inferred from the claim text.