Title:
CHOLINE CARBONATE PRODRUG, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/258035
Kind Code:
A1
Abstract:
Provided in the present invention are a choline carbonate prodrug, wherein the choline carbonate prodrug can be converted in vivo by plasma cholinesterase to release the choline carbonate prodrug of active compounds; a preparation method therefor; and the use thereof in treating tumors. Specifically, the present invention relates to a triptolide prodrug, a preparation method therefor and the use thereof in treating tumors. Experiments show that: the triptolide prodrug improves the solubility of triptolide and has good water solubility; the triptolide prodrug has low activity in vitro, and can be rapidly converted to triptolide in vivo by plasma cholinesterase, thereby exhibiting an anti-tumor effect; the triptolide prodrug significantly prolongs the survival time of a nude mouse model with an orthotopic pancreatic tumor, and effectively inhibits the tumor growth of a nude mouse model with a subcutaneous stomach tumor; and the triptolide prodrug has good safety. The triptolide prodrug of the present invention can be used in the treatment of various primary tumors and metastatic tumors, such as pancreatic cancer and gastric cancer.
Inventors:
LIU MIN (CN)
ZHANG ZHIYI (CN)
WANG RUIFENG (CN)
LU WEIYUE (CN)
XIE CAO (CN)
ZHANG ZHIYI (CN)
WANG RUIFENG (CN)
LU WEIYUE (CN)
XIE CAO (CN)
Application Number:
PCT/CN2022/098013
Publication Date:
December 15, 2022
Filing Date:
June 10, 2022
Export Citation:
Assignee:
UNIV FUDAN (CN)
International Classes:
C07D307/77; A61K9/107; A61P35/00; C07J73/00
Domestic Patent References:
| WO2017041701A1 | 2017-03-16 |
Foreign References:
| US7662976B2 | 2010-02-16 | |||
| US5663335A | 1997-09-02 | |||
| CN105263475A | 2016-01-20 | |||
| CN105263475A | 2016-01-20 | |||
| CN107708739A | 2018-02-16 |
Attorney, Agent or Firm:
INNOWISE INTELLECTUAL PROPERTY LAW OFFICE (CN)
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