Rapamycin derivative, and a preparation method, pharmaceutical composition and use thereof

US10160767B2 · kind B2 · utility

Assignee

• INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES · CN

Inventors

• Wu Zhong · Beijing, CN
• Song Li · Beijing, CN
• Shuang Cao · 安丰镇, CN
• Ruiyuan CAO · Beijing, CN
• Junhai Xiao · Beijing, CN
• Xinbo Zhou · Beijing, CN
• Xingzhou Li · Beijing, CN

Key dates

• Filing date: Jun 3, 2015
• Grant date: Dec 25, 2018
• Expiry date: Jun 3, 2035

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61L2300/426
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention pertains to the field of pharmaceutical chemicals, and relates to a rapamycin derivative of Formula I, and a preparation method, pharmaceutical composition and use thereof. The compounds of the present invention overcome the defects of rapamycin in terms of water solubility and metabolic properties, and some of the compounds have an in vitro anti-tumor activity superior to rapamycin, have less toxicity to normal cells than rapamycin, and have very good druggability.