Water-soluble amino-acid ester derivative of propofol

A technology of amino acid esters and derivatives, which can be used in drug combinations, anesthetics, organic chemistry, etc., and can solve problems such as difficult to use, easy to grow bacteria, poor physical stability of emulsions, etc.
CN101880239AInactive Publication Date: 2010-11-10BEIJING MEIBEITA DRUG RES
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
BEIJING MEIBEITA DRUG RES
Publication Date
2010-11-10
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a water-soluble amino-acid ester derivative of propofol shown in a formula (I), nontoxic pharmaceutically-acceptable salts thereof, a pharmaceutical composition which contains the compound and is used as an active ingredient, and the application of the compound and the pharmaceutical composition as narcotic drugs, wherein R1 is an alkyl of H or C1-C3, and R2 is a lateral chain of L-amino acid of hydrogen, methyl, isopropyl, isobutyl, 2-methyl-propyl or benzyl, and the like.
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Description

technical field

[0001] The present invention relates to novel derivatives of amino acid esters of propofol and their non-toxic pharmaceutically acceptable salts, as well as pharmaceutical compositions containing these compounds as active ingredients, and the use of the compounds and pharmaceutical compositions as anesthetics . Background technique

[0002] Propofol (chemical name: 2,6-diisopropylphenol, also known as propofol), is a quick-acting, short-acting systemic intravenous anesthetic, with fast onset, fast and complete recovery, and no accumulation. It is widely used clinically for the induction and maintenance of general anesthesia. However, due to the poor water solubility of propofol, it can only be used clinically in the form of emulsion.

[0003]

[0004] Propofol

[0005] The emulsion of propofol has poor physical stability, which can easily cause pain at the injection site, easy to grow bacteria, and is not easy to be used together with other injection me...

Claims

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