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US 7,001,916 B1Granted
Epothilon derivatives, method for the production and the use thereof as pharmaceuticals
AssigneeSchering Corporation
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.
Claims20
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-methyl-4-thiazolyl or 2-methyl-4-oxazolyl radical 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-methyl-4-thiazolyl or 2-methyl-4-oxazolyl radical 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-methyl-4-thiazolyl or 2-methyl-4-oxazolyl radical,
- wherein the nitrogen atom and/or the sulfur atom in X can be present in oxidized form, and
- wherein, R2 and R8 each are simultaneously not a methyl radical, or a stereoisomer thereof.
10 more elements
Dependencies are inferred from the claim text.