专利名称 | LONG-ACTING RASAGILINE PRODRUG, PREPARATION METHOD AND USE THEREOF | ||
申请号 | WOCN18102494 | 申请日 | |
公开(公告)号 | WO2019037791A1 | 公开(公告)日 | 2018-08-27 |
申请(专利权)人 | 发明人 | ZHANG Jiancun; LI Deyao; ZHOU Yiqian; WU Yiwu | |
专利来源 | 国家知识产权局 | 转化方式 | |
摘要 |
Provided are a long-acting rasagiline prodrug and a preparation method and use thereof. The long-acting rasagiline prodrug has a structure of formula (I), wherein, T is selected from (II) or not present; R1 and R2 are each independently selected from hydrogen, deuterium, and methyl; W is selected from (CH2)n or does not exist, n is selected from an integer from 1 to 15; X is selected from (CH2)m or not present, m is selected from an integer from 1 to 10; Y is selected from -C(=O)NH-, -NHC(=O)- or not present; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane fatty chain, -R3a-C(=O)O-R3b, -R3a-OC(=O)-R3b, -R3a-C(=O)NH-R3b, -R3a-NHC(=O)-R3b, or -R3a-S(=O)1-2O-R3b and -R3a-OS(=O)1-2-R3b; The rasagiline prodrug provided has a high melting point and low solubility, and can form a drug depot in the body after being prepared into an injection and administered, thereby prolonging the release of the drug in the body and achieving a long-term treatment. |
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