DOUBLE ACYLATED GLP-1 DERIVATIVES Russian patent published in 2016 - IPC C07K14/605 A61K38/26 A61P3/10 

Abstract RU 2602601 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a derivative of GLP-1 analogue, where analogue comprises first residue K in position corresponding to position 27 in GLP-1 (7-37) (SEQ ID No. 1); second residue K in position corresponding to position 36 in GLP-1 (7-37), and maximum ten amino acid substitutions as compared to GLP-1 (7-37); where first residue K is designated as K27, and second residue K is designated as K36; where derivative contains two albumin-binding group attached to K27 and K36, respectively, through a linker, and albumin-binding group contains prolonging group selected among HOOC-(CH2)x-CO- and HOOC-C6H4-O-(CH2)y-CO-; where x is an integer within range of 6-16, and y is an integer within range of 3-17; where linker contains element of formula -NH-(CH2)2-(O-(CH2)2)k-O-(CH2)n-CO-, where k is an integer within range of 1-5 and n is an integer within range of 1-5; or pharmaceutically acceptable salt, amide or ester. Derivative of GLP-1 analogue is intended for treating and/or preventing sugar diabetes and related diseases.

EFFECT: said derivatives are suitable for oral administration.

13 cl, 4 tbl, 40 ex

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RU 2 602 601 C2

Authors

Vechorek Birgit

Spetsler Jane

Kruse Tomas

Linderot Lars

Kofed Jakob

Dates

2016-11-20Published

2012-04-12Filed