Multi-arm single molecular weight polyethylene glycol active derivative and application thereof
AssigneeJenkem Technology Co., Ltd. (Tianjin)
InventorsZhen Wei, Meina Lin, Xuan Zhao
Life of this patent
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Abstract
Being used for drug modification, the multi-arm single molecular weight polyethylene glycol active derivative provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the multi-arm single molecular weight polyethylene glycol active derivative provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.
Claims18
A multi-arm single molecular weight polyethylene glycol active derivative having the following structure:
- wherein A is a core structure, and is a polyol group selected from the group consisting of pentaerythritol, oligo-pentaerythritol, glycerol and oligoglycerol, or a glyceryl ether group thereof,
- X1 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)i—, —(CH2)iO—, —(CH2)iNHCO—, —(CH2)iCONH—, —(CH2)iOCO—, and —(CH2)iCOO—, and i is an integer from 1 to 10,
- R is a linking group selected from any one or a combination of two or more of the group consisting of —NHCO—, —CONH—, —OCO—, —COO—, and —O—,
- X2 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)j—, —(CH2)jO—, —(CH2)jCO—, —(CH2)jNH—, —(CH2)jNHCO—, —(CH2)jCONH—, —(CH2)jOCO— and —(CH2)jCOO—, and j is an integer from 0 to 10,
- PEG has the following structure:
- —(CH2CH2O)m—, m is an integer from 8 to 200, and
- F is the same or different —X3—Z type structure,
- X3 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)k—, —(CH2)kO—, —(CH2)kCO—, —(CH2)kNH—, —(CH2)kNHCO—, —(CH2)kCONH—, —(CH2)kNHCONH—, —(CH2)kOCO—, —(CH2)kCOO—, —(CH2)kOCOO— and —(CH2)kOCONH—, and k is an integer from 0 to 10,
- Z is an active terminal group selected from any one of the group consisting of —H and
- and
- n is an integer from 3 to 24.
Dependencies are inferred from the claim text.