Xiamen Sinopeg Biotech Co., Ltd.

Chun Zhou

Chao Liu

Wengui Weng

Ce Yan

Huihuang Su

Shaofeng Wu

Disclosed are a multifunctionalized polyethylene glycol derivative and a preparation method therefor. The derivative has an H-shaped structure as represented by formula (1) and comprises one linear core LPEG and four PEG branch chains, where n, n, n, and nrespectively are the degrees of polymerization of the branch chains, Uand Uare trivalent branching groups connecting the core LPEG to two of the PEG branch chains, Fand Fcontain a functional group or a protected form Rthereof and may or may not contain a branched group G, correspondingly, the number of Ris one or more, Fand Fare either identical or different, any one linking group in the molecule or any linking group formed with an adjacent heteroatom group can either remain stable or be degraded, and any one PEG segment in the molecule is discretely polydispersed or monodispersed. The multifunctional polyethylene glycol is flexible and diverse in terms of branch structures and the lengths of branching arms, has various parameters and performance indicators that are adjustable and easy to control, and has a broad applicability.

Multifunctionalized polyethylene glycol derivative and preparation method therefor

Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Eform a highly symmetric octavalent central structure COREtogether, Lconnects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n-nas the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k&#x2265;1), and said PEG chain and F can be directly connected (g=0) or connected with a divalent linking group Lconnected with a terminal branched group G (g=1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance. 

Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof

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 Eform a highly symmetrical octavalent group CORE; Lconnects the octavalent group to eight PEG chains having polydispersity or monodispersity and having nto nas the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k&#x2265;1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group Lto 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. 

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Xiamen, China

Chun Zhou