PHARMACEUTICAL STRUCTURES WITH INCREASED ALBUMIN BINDING AFFINITY Russian patent published in 2021 - IPC A61K47/00 A61K39/44 C07K19/00 

Abstract RU 2753880 C1

FIELD: biotechnology.

SUBSTANCE: invention relates to biotechnology and constitutes a linker unit containing a central base and 2 to 5 of first elements, wherein each of the first elements independently constitutes a derivative of C16-20 fatty acid or a derivative of C16-20 dicarboxylic fatty acid, and the central base comprises from 2 to 5 lysine (K) residues, wherein the ε-amino group of the K residue is acylated with one of the first elements; optionally, one or more fillers, wherein any two of the K residues directly follow each other or are separated by a filler; optionally, a terminal spacer, wherein the terminal spacers constitute an N-terminal spacer associated with the N-terminus of the first K residue or an C-terminal spacer associated with the C-terminus of the last K residue; and each of the fillers and terminal spacers independently comprises (1) from 1 to 12 amino acid residues different from the K residue, or (2) a pegylated amino acid with from 1 to 12 repeats of monomer units of ethylene glycol (EG); and a conjugating fragment linked with the terminal K residue, or, in the case of presence of a terminal spacer, the terminal amino acid residue of the terminal spacer by forming an amide bond therewith, wherein the conjugating fragment has a conjugating group selected from the group consisting of azide, alkyne, tetrazine, cyclooctene, and cyclooctyne group.

EFFECT: invention provides a possibility to obtain an effective linker.

15 cl, 19 dwg, 21 ex

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RU 2 753 880 C1

Authors

Chu, Hsing-Mao

Lin, Chien-Jen

Chang, Tse-Wen

Dates

2021-08-24Published

2018-09-19Filed