Hydrophilic linkers and ligand-drug conjugates thereof

US10646585B2 · kind B2 · utility

Assignee

• HANGZHOU DAC BIOTECH CO., LTD. · CN

Inventors

• Sanxing Sun · Danbury, US
• Robert Yongxin Zhao · Lexington, US
• Xing-Ya Li · San Gabriel, US
• Huihui GUO · Hangzhou City, CN
• Junxiang JIA · Hangzhou City, CN
• Hongsheng Xie · Hangzhou City, CN
• Xiaomai ZHOU · Hangzhou City, CN
• Yuanyuan HUANG · Hangzhou City, CN
• Qingliang YANG · Hangzhou City, CN
• Xiaotao ZHUO · Hangzhou City, CN
• Hangbo YE · Hangzhou City, CN
• Shun GAI · Hangzhou City, CN
• Lan Qu · Hangzhou City, CN
• Wenjun LI · Hangzhou City, CN
• Chen-Huan Lin · Hangzhou City, CN

Key dates

• Filing date: Dec 19, 2018
• Grant date: May 12, 2020
• Expiry date: Dec 19, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K2317/73
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes a cell-binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.