[EN] IMMUNOCONJUGATE SYNTHESIS METHOD<br/>[FR] PROCÉDÉ DE SYNTHÈSE D'IMMUNOCONJUGUÉ
申请人:BOLT BIOTHERAPEUTICS INC
公开号:WO2018191746A1
公开(公告)日:2018-10-18
A method for producing an immunoconjugate, the method comprising combining one or more compounds of Formula I and an antibody of Formula II, wherein Formula II is an antibody with one or more lysine residues, in an aqueous solution buffered at a pH of about 7.5 to about 9 until at least 33 mol% of the one or more compounds of Formula I is conjugated to the antibody of Formula II to provide the immunoconjugate of Formula III, wherein Adj is an adjuvant, Z is –CH2–, –C(O)NH–, –C(O)O–, or –C(O)–, L is a linker, E is an ester, and r is the average number of adjuvants attached to the antibody and is a positive number up to about 8, in a first buffered aqueous solution.
一种制备免疫结合物的方法,所述方法包括将一种或多种I式化合物与II式抗体结合,其中II式抗体具有一种或多种赖氨酸残基,在pH约为7.5至9的缓冲水溶液中混合,直至至少33摩尔%的一种或多种I式化合物与II式抗体结合,以提供III式免疫结合物,其中Adj是一种佐剂,Z是-CH2-,-C(O)NH-,-C(O)O-或-C(O)-,L是一个连接物,E是一个酯,r是附着到抗体上的佐剂的平均数量,是一个正数,最多约为8,在第一个缓冲水溶液中。