Water-soluble taxane derivatives and uses thereof

US9650390B2 · kind B2 · utility

Assignee

• JIANGSU NHWALUOKANG PHARMACEUTICAL RESEARCH AND DEVELOPMENT CO., LTD. · CN

Inventors

• Qingeng Li · Chongqing, CN
• Tao Wang · Farmington, US
• Gang Chen · Sammamish, US
• Yuanzhong Wang · Shanghai, CN
• Wei Mao · Chengdu, CN
• Lingguo Zeng · Chongqing, CN
• Tong Wu · Västerås, SE
• Dahai Chen · Nanhu, CN

Key dates

• Filing date: Feb 16, 2015
• Grant date: May 16, 2017
• Expiry date: Feb 16, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention discloses a class of water soluble taxane derivatives, a method for treating tumor using the same, use thereof as anti-tumor drugs and use thereof in the preparation of anti-tumor drugs. The water soluble taxane derivatives have the general formula (I-1), (I-2) or (I-3): wherein, R1 is H or methyl; R2 is H, methyl or acetyl; R3 is phenyl or OC(CH3)3; X is H, C1-6 alkyl or F; Y is F or C1-6 alkyl substituted with one or more F; n is 1, 2, 3, 4, 5 or 6; W is NR4R5.A orR4 and R5 are each independently H, C1-6 alkyl optionally substituted with phenyl, or C3-6 cycloalkyl; m is 0, 1, 2 or 3; and A is a pharmaceutically acceptable acid.