Water-soluble propofol derivatives and uses thereof

US9643917B2 · kind B2 · utility

Assignee

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

Inventors

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

Key dates

• Filing date: Feb 16, 2015
• Grant date: May 9, 2017
• Expiry date: Feb 16, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W1 or W2; W1 is NR1R2.A orR1 and R2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W2 is COOM1/t or OPO3(M)2/t or PO3(M)2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M.