12, 13-cyclopropane epothilone derivatives
First Claim
Patent Images
1. A compound of the formula wherein:
- B1 and B2 are selected from the group consisting of H, or OR6;
R1, R2, R3, and R4, are selected from H, lower alkyl;
R5 is selected from the group consisting of H, alkyl, substituted alkyl;
R8 is heterocyclo;
R9 is hydrogen or lower alkyl;
R6 is hydrogen or alkyl;
M is CR10R11;
R10 and R11 are selected from the group consisting of H, halogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R12C═
O, R13OC═
O, R14NHC═
O, hydroxy, O-alkyl or O-substituted alkyl, NR15R16;
R12, R13, R14, R15, R17, R18 and R19 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, acyl or substituted aryl;
R16 is selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R17C═
O, R18OC═
O, R19SO2, hydroxy, O-alkyl, or O-substituted alkyl;
and any salts, solvates or hydrates thereof.
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Abstract
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
60 Citations
22 Claims
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1. A compound of the formula
wherein: -
B1 and B2 are selected from the group consisting of H, or OR6;
R1, R2, R3, and R4, are selected from H, lower alkyl;
R5 is selected from the group consisting of H, alkyl, substituted alkyl;
R8 is heterocyclo;
R9 is hydrogen or lower alkyl;
R6 is hydrogen or alkyl;
M is CR10R11;
R10 and R11 are selected from the group consisting of H, halogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R12C═
O, R13OC═
O, R14NHC═
O, hydroxy, O-alkyl or O-substituted alkyl, NR15R16;
R12, R13, R14, R15, R17, R18 and R19 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, acyl or substituted aryl;
R16 is selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R17C═
O, R18OC═
O, R19SO2, hydroxy, O-alkyl, or O-substituted alkyl;
and any salts, solvates or hydrates thereof. - View Dependent Claims (2, 3, 4, 12, 13, 14, 15)
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-
5. A compound of the formulas
wherein: -
B1 and B2 are selected from the group consisting of H, or OR6;
R1, R2, R3, and R4 are selected from H, lower alkyl;
R5 is selected from the group consisting of H, alkyl, substituted alkyl;
R8 is heterocyclo;
R9 is hydrogen or lower alkyl;
R6 is hydrogen or alkyl;
M is CH2;
and any salts, solvates or hydrates thereof. - View Dependent Claims (16)
-
- 6. The compound of the formula:
- 7. The compound of the formula:
- 8. The compound of the formula:
- 9. The compound of the formula:
- 10. The compound of the formula:
- 11. The compound of the formula:
Specification