Benzoate derivatives of taxol

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United States of America Statutory Invention Reg

PATENT NO H1487
SERIAL NO

08128949

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl; R.sup.1 is hydrogen or a radical Z of the formula ##STR4## in which Q is --(CH.sub.2).sub.f --, optionally substituted with one to six same or different C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, or a carbon atom of said --(CH.sub.2).sub.f -- radical may also be a part of C.sub.3-6 cycloalkylidene; R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.3 and R.sup.4 taken together with the carbon atom to which they are attached form C.sub.3-6 cycloalkylidene; R.sup.5 is --OC(.dbd.O)R, --OP.dbd.O(OH).sub.2 or --CH.sub.2 OP.dbd.O(OH).sub.2, in which R is C.sub.1-6 alkyl; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or hydrogen, but when R.sup.5 is --OC(.dbd.O)R, one of R.sup.6, R.sup.7, R.sup.8 or R.sup.9 is --OP.dbd.O(OH).sub.2 ; f is 2 to 6; n is O, and m is 1 or 0 when R.sup.5 is --CH.sub.2 OP.dbd.O(OH).sub.2 ; and n is 1 or 0, and m is 1 when R.sup.5 is --OC(.dbd.O)R or --OP.dbd.O(OH).sub.2. Also provided by this invention are pharmaceutical formulations and a method for treating mammalian tumors with a compound of formula I.

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Patent Owner(s)

Patent OwnerAddress
BRISTOL-MYERS SQUIBB COMPANYPRINCETON NJ 08543

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Doyle, Terrence Killingworth, CT 2 112
Wong, Henry Durham, CT 78 1184

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