MONOFUNCTIONAL BRANCHED POLYETHYLENEGLYCOL AND BIO-RELATED SUBSTANCE MODIFIED BY SAME
申请人:Xiamen Sinopeg Biotech Co., Ltd.
公开号:EP2947111A1
公开(公告)日:2015-11-25
Disclosed are a monofunctional branched polyethyleneglycol and a bio-related substance modified by same. The general formula of the monofunctional branched polyethyleneglycol is shown in Formula (1), and the general formula of the bio-related substance modified by the polyethyleneglycol is shown in Formula (2), wherein X1 and X2 are respectively an alkyl group with 1 to 20 carbon atoms; n1 and n2 are respectively an integer ranging from 1 to 1000; n3 is an integer ranging from 11 to 1000; L1 and L2 are respectively a linking group stably existing in illumination, enzyme, acidic, or alkaline conditions; p is 0 or 1, and q is 0 or 1; R1 is a hydrogen atom or an alkyl group with 1 to 20 carbon atoms; D is the bio-related substance; and Z is a linking group, through which a functional group capable of reacting with the bio-related substance is linked to a symmetric axis polyethyleneglycol main chain. The bio-related substance modified by the polyethyleneglycol maintains good biological activity, and has good solubility and long metabolic half-life in an organism.
本发明公开了一种单官能团支链聚乙二醇和由其改性的生物相关物质。单官能团支链聚乙二醇的通式如式(1)所示,由该聚乙二醇改性的生物相关物质的通式如式(2)所示,其中 X1 和 X2 分别为具有 1 至 20 个碳原子的烷基;n1 和 n2 分别为 1 至 1000 的整数;n3 为 11 至 1000 的整数;L1和L2分别为在光照、酶、酸性或碱性条件下稳定存在的连接基团;p为0或1,q为0或1;R1为氢原子或具有1至20个碳原子的烷基;D为生物相关物质;Z为连接基团,通过该连接基团,能够与生物相关物质反应的官能团被连接到对称轴聚乙二醇主链上。经聚乙二醇改性的生物相关物质可保持良好的生物活性,在生物体内具有良好的溶解性和较长的代谢半衰期。