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Process and compositions clucoconjugacion
专利权人:
PFIZER INC.
发明人:
JIANXIN GU,JIN KIM,A. KRISHNA HWAN - PRASAD,YU-YING YANG
申请号:
ARP130102904
公开号:
AR092368A1
申请日:
2013.08.15
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Claim 1: a method to obtain a glucoconjugado, characterized in that it comprises a saccharide conjugated to a Carrier Protein through a Spacer (2 - (2-oxoethyl) thio) ethyl) carbamate (eTec), which comprises the following steps: a) reacting a saccharide with 1,1 - carbonyl - d I - (1,2,4 - triazole) (CDT) or 1.1 - carbonildiimidazol (CDI)In an organic Solvent to produce an activated saccharide; saccharide activated b) REACT with cystamine, cysteamine or a Salt thereof,To obtain a tiolado saccharide; saccharide tiolado c) REACT with a reducing Agent to obtain a tiolado activated saccharide comprising one or more free sulfhydryl residues; (d) REACT with a Protein Carrier tiolado activated saccharide comprising activated One or More groups of haloacetamida - to obtain a Conjugate of saccharide tiolado - Carrier Protein; and (e)React - Carrier Protein conjugate tiolado saccharide with (i) a First blocking Reagent capable of blocking Groups - non conjugated to the Carrier Protein haloacetamida activated; and / or (ii) a Second blocking Reagent capable of blocking free sulfhydryl residues not conju Charge; thus produces a glucoconjugado linked to etec.23: a glucoconjugado claim, characterized in that it comprises a bacterial capsular polysaccharide conjugated to a Carrier Protein through a Spacer eTec, where polysaccharide covalently binds in the carbamate Spacer ETEC through a Link, and the pro Carrier Protein binds covalently to the Spacer in ETEC through an amide Bond.Reivindicación 1: Un método para obtener un glucoconjugado caracterizado porque comprende un sacárido conjugado con una proteína portadora mediante un espaciador de (2-((2-oxoetil)tio)etil)carbamato (eTEC), que comprende las siguientes etapas: a) hacer reaccionar un sacárido con 1,1-carbonil-di-(1,2,4-triazol) (CDT) o 1,1-carbonildiimidazol (CDI), en un solvente orgánico para producir un sacárido activado; b) hacer reaccionar el sacárido activado con cistamina, cisteamina o una sal de estas, para obtener
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