发明名称 |
GLYCOCONJUGATION PROCESSES AND COMPOSITIONS |
摘要 |
The invention provides eTEC linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, immunogenic compositions comprising such glycoconjugates, and methods for the preparation and use of such glycoconjugates and immunogenic compositions. |
申请公布号 |
US2015216996(A1) |
申请公布日期 |
2015.08.06 |
申请号 |
US201314420822 |
申请日期 |
2013.08.12 |
申请人 |
PFIZER INC. |
发明人 |
Gu Jianxin;Kim Jin-hwan;Prasad A. Krishna;Yang Yu-ying |
分类号 |
A61K47/48;A61K45/06;A61K39/09 |
主分类号 |
A61K47/48 |
代理机构 |
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代理人 |
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主权项 |
1. A method of making a glycoconjugate comprising a saccharide conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, comprising the steps of:
a) reacting a saccharide with 1,1′-carbonyl-di-(1,2,4-triazole) (CDT) or 1,1′-carbonyldiimidazole (CDI), in an organic solvent to produce an activated saccharide; b) reacting the activated saccharide with cystamine or cysteamine or a salt thereof, to produce a thiolated saccharide; c) reacting the thiolated saccharide with a reducing agent to produce an activated thiolated saccharide comprising one or more free sulfhydryl residues; d) reacting the activated thiolated saccharide with an activated carrier protein comprising one or more α-haloacetamide groups, to produce a thiolated saccharide-carrier protein conjugate; and e) reacting the thiolated saccharide-carrier protein conjugate with (i) a first capping reagent capable of capping unconjugated α-haloacetamide groups of the activated carrier protein; and/or (ii) a second capping reagent capable of capping unconjugated free sulfhydryl residues; whereby an eTEC linked glycoconjugate is produced. |
地址 |
New York NY US |