Epothilone derivatives and methods for making and using the same
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United States of America Patent
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-
Dec 3, 2002
Grant Date -
Dec 19, 2002
app pub date -
Apr 3, 2001
filing date -
Apr 3, 2001
priority date (Note) -
Granted
status (Latency Note)
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Abstract
The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula 1 are provided wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.5 are each independently hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl or alkylaryl; R.sup.4 is hydrogen, halogen, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 hydroxyalkyl, C.sub.1-C.sub.10 haloalkyl, aryl, --C(.dbd.O)R.sup.6, --C(.dbd.O)OR.sup.6, --NR.sup.6R.sup.7 where R.sup.6 and R.sup.7 are each independently hydrogen, C.sub.1-C.sub.10 aliphatic, aryl or alkylaryl; W is O, NR.sup.8 where R.sup.8 is hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl or alkylaryl; X is O, CH.sub.2 or a carbon-carbon double bond; Y is absent or a C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, or C.sub.2-C.sub.10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.
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