Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof
申请人:XIAMEN SINOPEG BIOTECH CO., LTD.
公开号:US10434182B2
公开(公告)日:2019-10-08
Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups Ec form a highly symmetrical octavalent group CORE0; Lc connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n1 to n8 as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L0 to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.
本发明公开了一种八臂聚乙二醇(PEG)衍生物(式 I)、其生产方法及其改性生物相关物质。其中,一个四价基团 U 与四个三价基团 Ec 形成一个高度对称的八价基团 CORE0;Lc 将八价基团连接到八条具有多分散性或单分散性且聚合度为 n1 至 n8 的 PEG 链上;一条 PEG 链的末端与至少一个官能团 F 连接(k≥1);所述 PEG 链和 F 之间可以直接连接(g=0),也可以通过连接基团 L0 与末端支化基团 G 间接连接(g=1);后者提供了更多的反应位点,可以结合更多的药物分子,增加药物负载量。八臂聚乙二醇衍生物具有中心对称或近似中心对称结构,因此在大规模生产中可以更精确地控制分子量,产品的分子量分布也更窄。因此,改性生物相关物质的性能更均匀、更可控。
[EN] BIO-RELATED SUBSTANCE MODIFIED BY MULTIFUNCTIONALIZED POLYETHYLENE GLYCOL DERIVATIVE<br/>[FR] SUBSTANCE D'ORIGINE BIOLOGIQUE MODIFIÉE PAR UN DÉRIVÉ DU POLYÉTHYLÈNEGLYCOL MULTIFONCTIONNALISÉ<br/>[ZH] 一种多官能化聚乙二醇衍生物修饰的生物相关物质
EIGHT-ARM POLYETHYLENE GLYCOL DERIVATIVE, PRODUCTION METHOD THEREFOR, AND MODIFIEDBIO-RELATEDSUBSTANCETHEREOF
申请人:XIAMEN SINOPEG BIOTECH CO., LTD
公开号:US20180214561A1
公开(公告)日:2018-08-02
Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups E
c
form a highly symmetrical octavalent group CORE
0
; L
c
connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n
1
to n
8
as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L
0
to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.