DOUBLE-ACYLATED GLP-1 DERIVATIVES Russian patent published in 2015 - IPC C07K14/605 A61K47/48 A61K38/26 A61P3/10 

Abstract RU 2559540 C2

FIELD: chemistry.

SUBSTANCE: invention relates to field of biotechnology, namely to derivatives of GPL-1 analogue, and can be used in medicine. Compound, possessing GLP-1 activity and representing derivative of GLP-1 analogue is synthesised, wherein analogue has first residue K37 in position, corresponding to position 37 GLP-1 (7-37) (SEQ ID No1), second residue K26 in position, corresponding to position 26 GLP-1 (7-37), as well as not more than four amino acid modifications in comparison with GLP-1 (7-37), including K37 and Q or R in position, corresponding to position 34 in GLP-1 (7-37). Derivative has prolonging grouping, bound via linker to each of epsilon-aminogroups K26 and K37, respectively, wherein prolonging grouping has formula of Compound 2a and linker contains Compound 6 and/or Compound 5.

EFFECT: invention makes it possible to obtain medication for peroral introduction, effective in treatment or prevention of diabetes mellitus and diseases, associated with diabetes mellitus, as well as capable of improving parameters of lipid metabolism and functioning of beta-cells and delay or prevent progression of diabetic disease.

12 cl, 58 ex

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RU 2 559 540 C2

Authors

Gehribehj Patrik Uill'Jam

Spetsler Jane

Kodra Janosh Tibor

Linderot Lars

Lau Esper

Zauehrberg Per

Dates

2015-08-10Published

2010-12-16Filed