Water-soluble rapamycin derivatives
AssigneeZhejiang Hisun Pharmaceutical Co., Ltd.
InventorsHaibo Wang, Hongfu Kuang, Wei Zhang, Zhengjiang Cai, Tianmin Zhu, Xiaohe Zheng, Zhongwei Wu, Zhiqing Yang
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Abstract
The present invention relates to technical fields of organic chemistry and pharmaceutical chemistry, specifically to water-soluble rapamycin derivatives modified with glutathione. More specifically, the present invention discloses a compound of formula I and the preparation method thereof, wherein R1 and R2 are as defined in the description. The compound of formula I can be used in inducing immunosuppression and in the treatment of diseases such as transplant rejection and solid tumor, etc.
Claims27
A compound of formula I or a pharmaceutically acceptable salt thereof:
- wherein,
- R1 is H or R3;
- R2 is H or R4-R5;
- but R1 and R2 are not simultaneously H;
- R3 is R4-R5, —CH2CH2O—R4-R5,
- R4 is
- carbonyl C2-C6 alkenylene or carbonyl C2-C6 alkynylene;
- n is an integer less than or equal to 6;
- i.e., n is 1, 2, 3, 4, 5 or 6;
- m is an integer less than or equal to 6;
- i.e., m is 1, 2, 3, 4, 5 or 6;
- R5 is polypeptidyl group, preferably glutathionyl of formula II formed by dehydrogenating the mercapto group in glutathione:
- R6 is C1-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene.
Dependencies are inferred from the claim text.