ANTITHROMBOTIC DUAL INHIBITORS CONTAINING BIOTIN LABEL Russian patent published in 2011 - IPC C07H15/08 A61K31/7042 A61P7/02 A61K47/48 C07H3/06 A61K31/702 

FIELD: chemistry.

SUBSTANCE: described is a novel compound of general formula (I): oligosaccharide-spacer-antagonist GpIIb/IIIa (1), where the oligosacharride is a negatively charged pentasaccharide residue of formula (B) (B), where R1 denotes OCH₃ or OSO₃ ^-. The charge is compensated for by positively charged counterions; the spacer is essentially a pharmacologically inactive binding residue having length of 10-35 atoms; the GpIIb/IIIa antagonist is a tirofiban residue (MK 383). The spacer includes a covalent bond with a biotin analogue of formula -(CH₂)₄-X-BT, where X=NH, N(1-4C)alkyl, -N-CH(CH₂OH)-CH₂-C(O)-NH-, -NH-CH(CH₃)-CH₂-C(O)-NH-, -NH-CH(COOH)-CH₂-C(O)-NH- or -NH-CH(CH₂COOH)-CH₂-C(O)-NH-, and BT is a label ; or pharmaceutically acceptable salt thereof.

EFFECT: compounds have antithrombotic activity and can be used to treat or prevent thrombotic diseases.

8 cl, 7 tbl, 21 ex