LOW MOLECULAR WEIGHT GLYCOSAMINOGLYCAN DERIVATIVE, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

摘要

Provided are a low-molecular-weight fucosylated glycosaminoglycan derivative (derivative of Low molecular weight Fucosylated Glycosaminoglycan, dLFG) having anticoagulant activity, a preparation method thereof, a pharmaceutical composition comprising dLFG or a pharmaceutically acceptable salt thereof, and the use of dLFG and pharmaceutical composition thereof in preparing medicine for treating thrombotic diseases.

主权项

1. A low-molecular-weight glycosaminoglycan derivative or a pharmaceutically acceptable salt thereof, wherein:
monosaccharide compositions of the low-molecular-weight glycosaminoglycan derivative comprise hexuronic acid, hexosamine, deoxyhexamethylose and the sulfate forms of those monosaccharides; wherein, the hexuronic acid is D-glucuronic acid and Δ4,5-hexuronic acid (4-deoxy-threo-hex-4-enepyranosyluronic acid), the hexosamine is acetylgalactosamine (2-N-acetylamino-2-deoxy-D-galactose) or a terminal reduction product thereof, the deoxyhexamethylose is L-fucose; based on molar ratio, the ratio of each monosaccharide and —OSO3− in the low-molecular-weight glycosaminoglycan derivative is hexuronic acid:hexosamine:deoxyhexamethylose:sulfate group=1:(1±0.3):(1±0.3):(3.0±1.0); in the hexuronic acid, based on molar ratio, the percentage of Δ4,5-hexuronic acid is not less than 2.5% of the total hexuronic acid; the low-molecular-weight glycosaminoglycan derivative has a weight average molecular weight (Mw) of 3 kD-20 kD; the low-molecular-weight glycosaminoglycan derivative has a polydispersity index of between 1.0 and 1.8.