Taxol-7-carbazates

Details Taxol-7-carbazates Taxol-7-carbazates

1994-02-17

1996-08-20

Trinh, Ba Kim

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549510, 549511, 528421, A61K 31335, C07D30514

Patent

active

055479812

ABSTRACT:
Disclosed are 7-substituted taxoid derivatives, in particular taxol-7-carbazates which have improved water-solubility and/or enhanced therapeutic activity and methods of making the same. The preferred taxoid derivatives have the formula: ##STR1## wherein Z is H or ##STR2## Y=O or S; X=CH.sub.2 or O; n=zero or a positive integer, preferably one; with the proviso that when n=O, X=CH.sub.2 ; R=C.sub.1 -C.sub.4 alkyl, haloalkyl, carboxyalkyl, thioalkyl, sulfonylalkyl, phenyl, hydroxyphenyl, aminophenyl, carboxyphenyl, a polyalkyleneoxide homopolymer or water soluble polyalkyleneoxide containing copolymer, having a molecular weight of from about 1,000 to about 20,000; ##STR3## W=O, N--L, S or SO.sub.2 ; Ph is a phenyl group; L=H, C.sub.1 -C.sub.4 alkyl or phenyl; and R.sub.2 =C.sub.1-C.sub.4 alkyl, phenyl or a polyalkyleneoxide homopolymer or water soluble polyalkyleneoxide containing copolymer, having a molecular weight of from about 1,000 to about 20,000.

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