Camptothecin compound containing stable 7-membered lactone ring, preparation method and use

US9115150B2 · kind B2 · utility

Assignees

• EAST CHINA NORMAL UNIVERSITY · CN
• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN
• NANJING LUYESIKE PHARMACEUTICAL CO., LTD. · CN

Inventors

• Wei Lv · Hoover, US
• Shanbao Yu · Shanghai, CN
• Yu Luo · New Taipei, TW
• Yi Chen · Shanghai, CN
• Jian Ding · Shanghai, CN

Key dates

• Filing date: Apr 13, 2012
• Grant date: Aug 25, 2015
• Expiry date: Apr 13, 2032

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.