DOUBLE ANTITHROMBOTIC INHIBITORS CONTAINING BIOTIN RESIDUE Russian patent published in 2010 - IPC C07H15/26 C07H3/06 A61K31/706 A61K31/702 A61P7/02 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to antithrombotic compound of formula (I) (oligisaccaride-spacer-A(I)), where oligosaccharide is negatively charged pentasaccharide residue of formula given lower, where R⁵ - OCH₃ or OSO₃ ^-, charge is compensated by positively charged counterions, and where pentasaccharide residue is obtained from pentasaccharide which has AT-III mediated anti-Xa activity per se; spacer is, in fact, pharmacologically inactive movably bound residue, which has from 10 to 50 atoms long chain; A is residue of -CH[NH-SO₂-R¹] [CO-NR²-CH(4-benzamidin)-CO-NR³R⁴], where R¹ - 4-methoxy-2,3,6-trimethyphenyl; R² - H; NR³R⁴ is piperidinyl group or its pharmaceutically acceptable salt or derivative, where amino group of amidin residue is protected by hydroxyl or (1-6C) alcoxycarbonyl group; where spacer of formula I compound contains one covalent bond with biotin residue of formula -(CH₂)₄-NR-BT, where R - H or (1-4C)alkyl and BT is residue . Invention also relates to pharmaceutical composition based on formula I compounds for treatment or prevention of thrombosis or other connected with thrombin diseases.

EFFECT: elaboration of antithrombotic compound for treatment or prevention of thrombosis or other, connected with thrombin diseases.

6 cl, 3 tbl, 2 dwg, 3 ex