Pegylated Artesunate Derivative, Pharmaceutical Composition and Use Thereof

摘要

A pegylated artesunate derivative, a pharmaceutical composition and uses thereof, the pegylated artesunate derivative is represented by the general formula (I):;;The pegylated artesunate derivative has activity comparable to that of artesunate, increased water solubility and stability, and an extended half-life in vivo.

主权项

1. An artesunate-polyethylene glycol derivative as shown in Formula (I),wherein,
POLY represents a polyethylene glycol residue with a molecular weight of 200 to 100,000 Da; X represents amino or oxygen atom or methoxy; Y represents a compound with amino acid structure containing two amino groups and one carboxyl, wherein the carboxyl together with X of POLY form an amide bond or ester bond, while the multiple amino groups in the introduced distal end and the carboxyl of artesunate form amide bonds; n and m represents polymerization degree of Y, m and n independently are an integer of 0 to 12; r and s represents polymerization degree of artesunate; and when neither m nor n is 0, r and s separately are the double of n and m, and artesunate via carboxyl forms an amide bond with the multiple amino groups introduced by Y; when m is 0 and n is not 0, or m is not 0 and n is 0, r and s separately are the double of n and m, and artesunate via carboxyl forms amide bonds with the multiple amino groups introduced by Y, and X at the end where m is 0 or n is 0 is methoxy; or when both m and n are 0, both r and s are 1, artesunate via carboxyl forms an ester or an amide with X.