GLYCOCONJUGATION PROCESS Russian patent published in 2018 - IPC C07H3/06 C07K1/107 A61K47/50 A61K39/09 

FIELD: medicine.

SUBSTANCE: invention relates to methods for preparing glycoconjugates suitable for use in medicine. Proposed are methods for the preparation of glycoconjugates having a molecular weight of 1,000 to 20,000 kDa, containing a bacterial capsular polysaccharide conjugated to a carrier protein, wherein said polysaccharide is covalently attached to said carrier protein, comprising the steps of: a) reacting a bacterial capsular polysaccharide, which is derived from S. pneumoniae and selected from capsular polysaccharides of Pn-serotype 3 (pneumococcal serotype 3), Pn-serotype 10A, Pn-serotype 12F and Pn-serotype 33F, with a stable nitroxyl radical compound and 0.1–10 molar equivalents of the oxidizing agent for selective oxidation of the primary hydroxyl groups to obtain an activated saccharide containing aldehyde groups; b) converting said activated bacterial capsular polysaccharide to an amino group of said carrier protein, selected from tetanus, diphtheria, pertussis toxin, Pseudomonas toxin, E. coli, Staphylococcus, Streptococcus or CRM197, at a ratio of saccharide: carrier/protein (wt/wt) from 0.2 to 4 under reductive amination conditions, wherein, after conjugation, the non-reacted aldehyde groups are converted back to primary alcohols and the glycoconjugate is purified. Also, provided is a glycoconjugate obtained by said methods from a capsular polysaccharide of Pn-serotype 12F, compositions comprising said glycoconjugate, and a method for preventing, treating or alleviating bacterial infections caused by serotype 12F S. pneumoniae, a method for inducing a protective immune response against S. pneumoniae infection by administering said composition to a subject.

EFFECT: provided are new effective methods for the preparation of glycoconjugates, new glycoconjugates and compositions based on them, effective for the treatment of infections caused by Streptococcus pneumoniae.

58 cl, 7 dwg, 5 tbl, 8 ex