发明名称 |
Camptothecin compound containing stable 7-membered lactone ring, preparation method and use |
摘要 |
Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.; |
申请公布号 |
US9115150(B2) |
申请公布日期 |
2015.08.25 |
申请号 |
US201214112583 |
申请日期 |
2012.04.13 |
申请人 |
EAST CHINA NORMAL UNIVERSITY;SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES;NANJING LUYESIKE PHARMACEUTICAL CO., LTD. |
发明人 |
Lv Wei;Yu Shanbao;Luo Yu;Chen Yi;Ding Jian |
分类号 |
C07D491/22 |
主分类号 |
C07D491/22 |
代理机构 |
Nixon & Vanderhye P.C. |
代理人 |
Nixon & Vanderhye P.C. |
主权项 |
1. A camptothecin compound with stable 7-membered lactone ring represented by formula I, and pharmaceutically acceptable salts thereof, wherein, R1 is acetyl or propionyl; R2 is H, C1˜C6 alkyl, C3˜C6 cycloalkyl, piperidyl or C1˜C6 alkyl substituted by amino; R3 is H, C1˜C3 alkyl, or C1˜C6 alkyl substituted by amino; R4 is H, hydroxyl, or C1˜C6 alkoxyl; R5 is H, or C1˜C6 alkoxyl; or, R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. |
地址 |
Shanghai CN |