FIELD: medicine.
SUBSTANCE: group of inventions relates to biotechnology and medicine, namely to new acylated derivatives of human insulin analogues and use thereof for treating or preventing medical conditions relating to diabetes. Disclosed is an acylated human insulin analogue, representing [A22K, desB27, B29R, desB30] in relation to human insulin, which is derived by acylation of the epsilon-amino group of lysine residue in position A22 by a group of formula II [Acyl]-[linker]. Linker is an amino acid chain consisting of from 1 to 10 amino acid residues selected from -gGlu- and -OEG-, where gGlu is a gamma-glutamic acid residue; OEG is an 8-amino-3,6-dioxooctanoic acid residue. Said amino acid residues may be present in any order, and the amino acid chain comprises at least one gGlu residue. Acyl group is a residue of α,ω-dicarboxylic acid selected from 1,14-tetradecanedioic acid, 1,15-pentadecanedioic acid and 1,16-hexadecanedioic acid.
EFFECT: said acylated analog is short- and fast-acting, and it is used in pharmaceutical formulations without zinc for prandial insulin therapy.
16 cl, 21 dwg, 16 tbl, 45 ex
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Authors
Dates
2019-04-09—Published
2015-02-26—Filed