Epothilone compounds, preparation method and use thereof
AssigneeLi Tang
InventorsLi Tang, Rongguo Qiu
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Abstract
Epothilone compounds represented by formula (I), their preparation methods and their use for preparing medicines are disclosed. The epothilone compounds are prepared by bioconversion and chemosynthesis or chemical modifications using epothilones or their derivatives as starting materials. Said epothilone compounds can be used to treat proliferative diseases.
Claims14
An epothilone compound represented by the following general formula (I):
- wherein,
- A-D is carbon-carbon double bond of the following formula (a) or epoxy group of the following formula (b),
- X is O;
- W is NR1R or W is OR′ provided that A-D is an epoxy group of formula (b), wherein R is selected from H, amino protective group, substituted or unsubstituted lower alkyl or unsaturated hydrocarbonyl;
- and R′ is selected from substituted or unsubstituted lower alkyl or unsaturated hydrocarbonyl;
- R1 is selected from OH, substituted or unsubstituted lower alkyl or unsaturated hydrocarbonyl, or forms cycloalkyl together with R;
- R2 is selected from H, substituted or unsubstituted lower alkyl or unsaturated hydrocarbonyl, or forms lower cycloalkyl with the methyl on C-4 position;
- R3 is selected from H, OH or NH2;
- R4 is methyl;
- or
- a pharmaceutically acceptable salt, hydrate, polymorph, optical isomer, racemate, diastereoisomer or enantiomer thereof.
An epothilone compound selected from the following compounds:
- or a pharmaceutically acceptable salt, hydrate, polymorph, optical isomer, racemate, diastereoisomer or enantiomer thereof.
A pharmaceutical composition comprising an epothilone compound selected from the following compounds, or a pharmaceutically acceptable salt, hydrate, polymorph, optical isomer, racemate, diastereoisomer or enantiomer thereof, and one or more pharmaceutical carriers and/or diluent:
Dependencies are inferred from the claim text.