Taxane-based prodrugs

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United States of America Patent

PATENT NO 5824701
SERIAL NO

08794730

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Taxane-based compositions of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of aryls, substituted aryls, aralkyls, substituted aralkyls, alkyls and substituted alkyls; R.sub.2 is an aryl or substituted aryl, preferably phenyl; R.sub.3 is H, a C.sub.1-10 alkoxy, SiEt.sub.3 or ##STR2## Y is O or S; (n) is zero or a positive integer; X is oxygen, S, SO.sub.2 or NL, where L is selected from the group consisting of H, C.sub.1-8 alkyls, aryls and aralkyls; R.sub.4 is H or an aroyl of the formula: ##STR3## wherein Ar is an aromatic, substituted aromatic or heteroaromatic group; R.sub.5 is H, CH.sub.3 CO or a substituted acetic acid derivative; Z is H or OR.sub.6 where R.sub.6 is selected from the group consisting of H, C.sub.1-8 alkyls, C.sub.1-8 substituted alkyls, C.sub.1-8 aralkyls, substituted aryls, aralkyls, substituted aralkyls, C.sub.1-10 alkoxy, SiEt.sub.3, ##STR4## P is O or OH; R.sub.8 is one of H, S(CH.sub.3).sub.3, Si(C.sub.2 H.sub.5).sub.3, CH.sub.3 CO, or substituted acetic acid derivatives of the formula; ##STR5## where R.sub.10 is an alkyl, aryl, halogen, or hydrogen alkoxy or ##STR6## R.sub.9 is selected from the group consisting of substantially non-antigenic polymers, C.sub.1-12 alkyls, C.sub.1-12 substituted alkyls and bifunctional moieties such as alkyls or polymers containing a terminal group ##STR7## and one of R.sub.3, R.sub.6 and R.sub.8 is ##STR8## and methods of preparation and use of the compounds are also disclosed.

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Patent Owner(s)

Patent OwnerAddress
ENZON INC40 KINGSBRIDGE ROAD PISCATAWAY NJ 08854

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Greenwald, Richard B Somerset, NJ 79 5036
Pendri, Annapurna Matawan, NJ 54 2240

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