Low molecular weight polyethylene glycol drug conjugates having improved drug biological activity
AssigneeJenkem Technology Co., Ltd. (Tianjin)
InventorsLihua Xu, Xuan Zhao, Zewang Feng, Jinliang Wang, Zhenguo Wang
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Abstract
Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.
Claims7
A drug-polyethylene glycol-drug conjugate of formula (I), the conjugate being formed by combining low molecular weight polyethylene glycol with two drug molecules,
- TA-X-PEG-X′-TA′ (I)
- Wherein:
- PEG is a polyethylene glycol residue having the following structure,
- n is an integer of 0-25;
- X, X′ are linking groups which may be identical or different, selected from a group consisting of
- i is an integer of 0-10;
- TA, TA′ are target compounds that may be identical or different, selected from a group consisting sumatriptan, dorzolamide, irinotecan, camptothecin, dasatinib, paclitaxel, docetaxel, Dccyclovirobuxinum D, diethyl stilbestrol, estradiol, prazosin, terazosin, metoclopramide, ursodesoxycholic acid, rapamycin, scopolamine, and procaine.
Dependencies are inferred from the claim text.