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US 2006/0040990 A1Published application
Epothilone derivatives, process for their production, and their pharmaceutical use
OwnerUlrich Klar, Werner Skuballa +3inventors
InventorsUlrich Klar, Werner Skuballa, Bernd Buchmann, Wolfgang Schwede, Michael Schirner
Life of this patent
Estimating the term…
Abstract
Disclosed are epothilone compounds of formula I, which are useful as pharmaceutical compounds for treating, for example, malignant tumors and chronic inflammatory diseases and are useful in anti-angiogenesis therapy.
Claims19
1-22. (canceled)
An epothilone compound of formula I,
- in which
- R4 means hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl,
- R5 means hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl,
- wherein, for R4 and R5, aryl is phenyl, wherein said phenyl is optionally substituted in one or more places by halogen, OH, O-alkyl, CO2H, CO2-alkyl, —NH2, —NO2, —N3, —CN, C1-C20 alkyl, C1-C20 acyl and/or C1-C20 acyloxy groups, and
- wherein, for R4 and R5, aralkyl is benzyl or phenylethyl, wherein said benzyl or phenylethyl is optionally substituted in one or more places by halogen, OH, O-alkyl, CO2H, CO2-alkyl, —NO2, —N3, —CN, C1-C20 alkyl, C1-C20 acyl and/or C1-C20 acyloxy groups,
- R6, R7 each mean a hydrogen atom, or together mean an additional bond to result in a double bond on the ring between their two positions or together mean an oxygen atom to provide an epoxide ring,
- R8 means a methyl group or hydrogen,
- and at the same time, R1a and R1b together stand for a trimethylene group, R2 stands for a phenyl or benzyl radical, and X stands for a 2-pyridyl, or
- at the same time R1a and R1b together stand for a trimethylene group, R2 stands for a methyl, ethyl or propyl group and X stands for a 2-pyridyl, or
- at the same time R1a and R1b in each case stand for a methyl group, R2 stands for a methyl, ethyl or propyl radical, and X stands for a 2-pyridyl,
- wherein the nitrogen atom and/or the sulfur atom in X can be present in oxidized form, and
- wherein, if R2 and R8 in each case mean a methyl radical, X can be only one 2-pyridyl radical that is optionally oxidized on the nitrogen atom,
- or a stereoisomer thereof.
10 more elements
A compound according to 23, in which X is 2-pyridyl that is oxidized on the nitrogen atom.
Dependencies are inferred from the claim text.