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US 6,673,833 B2Granted
C7 heterosubstituted acetate taxanes
AssigneeFSU Research Foundation, Inc.
InventorRobert A. Holton
Life of this patent
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Abstract
Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
Claims79
A taxane having the formula:
- wherein
- R2 is acyloxy;
- R7 is heterosubstituted acetate;
- R9 is keto, hydroxy, or acyloxy;
- R10 is hydroxy;
- R14 is hydrido or hydroxy;
- X3 is substituted or unsubstituted alkyl, alkenyl, alkynyl or heterocyclo;
- X5 is —COX10, —COOX10, or —CONHX10;
- X10 is hydrocarbyl, substituted hydrocarbyl, or heterocyclo;
- and
- Ac is acetyl.
8 more elements
A taxane having the formula
- R7 is R7aCOO—;
- R10 is hydroxy;
- X3 is substituted or unsubstituted alkyl, alkenyl, alkynyl or heterocyclo;
- X5 is —COX10, —COOX10, or —CONHX10;
- X10 is hydrocarbyl, substituted hydrocarbyl, or heterocyclo;
- and
- R7a is heterosubstituted methyl, said heterosubstituted methyl moiety lacking a carbon atom which is in the beta position relative to the carbon of which R7a is a substituent.
4 more elements
Dependencies are inferred from the claim text.