发明名称 |
Methods for making saccharide-protein glycoconjugates |
摘要 |
The invention provides a process for the reductive amination of a carbonyl group at the reducing terminus of a polysaccharide, wherein the reductive amination is carried out at a pH between 4 and 5. The invention also provides a process for preparing a conjugate of a polysaccharide and a carrier molecule, comprising the steps of: (a) coupling the polysaccharide to a linker, to form a polysaccharide-linker compound in which the free terminus of the linker is an ester group; and (b) reacting the ester group with a primary amine group in the carrier molecule, to form a polysaccharide-linker-carrier molecule conjugate in which the linker is coupled to the carrier molecule via an amide linkage. The invention also provides a process for reducing contamination of a polysaccharide-linker compound with unreacted linker, comprising a step of precipitating unreacted linker under aqueous conditions at a pH of less than 5. |
申请公布号 |
US9358284(B2) |
申请公布日期 |
2016.06.07 |
申请号 |
US201214343351 |
申请日期 |
2012.09.14 |
申请人 |
GlaxoSmithKline Biologicals SA |
发明人 |
Saul Allan James;Micoli Francesca |
分类号 |
C07K14/34;C08B37/00;A61K39/02;A61K39/385;C07K16/12;C07K16/44;A61K47/48;A61K39/112;A61K39/095;A61K39/00 |
主分类号 |
C07K14/34 |
代理机构 |
Morrison & Foerster LLP |
代理人 |
Morrison & Foerster LLP |
主权项 |
1. A process for the reductive amination of a carbonyl group at the reducing terminus of a polysaccharide, comprising:
combining the polysaccharide with a primary amine group in the presence of a reducing agent,
wherein the polysaccharide comprises:
a core domain from a lipopolysaccharide of a Gram-negative bacterium; anda carbonyl group at the reducing terminus, and reacting the carbonyl group with the primary amine group by reductive amination,
wherein the reductive amination is carried out at a pH between 4 and 5. |
地址 |
Rixensart BE |