Y-type discrete polyethylene glycol derivative and preparation method thereof
AssigneeJenkem Technology Co., Ltd. (Beijing)
InventorsHui ZHU, Meina LIN, Xuan ZHAO
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Abstract
Disclosed is a Y-type discrete polyethylene glycol derivative as shown by Formula (I). The Y-type discrete polyethylene glycol derivative has the advantages of a determined molecular weight and number of segments in the chain, and can avoid the defects where the polyethylene glycol derivative itself is a mixture and the molecular weight is not homogeneous. The Y-type polyethylene glycol of the present invention can solve the problem of insufficient water solubility caused by an increase in the loading capacity when the discrete polyethylene glycol modifies an insoluble drug while increasing the drug loading capacity.
Claims20
A Y-type discrete polyethylene glycol derivative having the structure of formula (I):
- wherein:
- A1, A2, and A3 are the same or different Y—X—(CH2)n structures, wherein n is an integer from 0 to 12;
- X is a linking group selected from the group consisting of —(CH2)i—, —(CH2)iNH—, —(CH2)iOCOO—, —(CH2)iOCONH—, —(CH2)iNHCONH—, —OC(CH2)iCOO—, —(CH2)iCOO— and —(CH2)iCONH—, i is an integer from 0 to 10;
- Y is a reactive end group selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy, amino, aminomethyl, maleimido, carboxyl, sulfhydryl, succinimide carbonate, succinimide acetate, succinimide propionate, succinimide succinate, succinimide, dithiopyridinyl, propionic acid group, aldehyde group, thioester group, acryloxy, azido, glutaric acid group, hydrazide, alkynyl, p-nitrophenyl carbonate, isocyanato, o-dithiopyridinyl, silane, carboxymethyl, vinyl sulfone group and vitamin H;
- E1 is a discrete polyethylene glycol group with a structure of (CH2CH2O)j, j is an integer from 0 to 100;
- E2 is a discrete polyethylene glycol group with a structure of (CH2CH2O)k, k is an integer from 0 to 100;
- E3 is a discrete polyethylene glycol group with a structure of (CH2CH2O)l, l is an integer from 0 to 100;
- and
- r, s and t are independently selected from the group consisting of 0, 1, 2 or 3.
Dependencies are inferred from the claim text.