Patent IL-117760-A (IL)
Title: Taxoids, their preparation and pharmaceutical compositions containing them
IPC: C07D409/12
Filed: 1996-04-01
Abstract: Anti tumor compounds of the formula in which: R represents a substituted alkenyl radical containing 2 to 8 carbon atoms in an unbranched or branched chain, an unsubstituted or substituted alkynyl radical containing 2 to 8 carbon atoms in an unbranched or branched chain, an unsubstituted or substituted cycloalkyl radical containing 3 to 6 carbon atoms or an unsubstituted or substituted cycloalkenyl radical containing 3 to 6 carbon atoms, said substituted radicals being substituted with a halogen atom selected from fluorine, 2954 י' בכסלו התשס" ב - November 25, 2001 chlorine, bromine and iodine atoms or with an amino radical, an alkylamino radical in which the alkyl portion contains 1 to 4 carbon atoms, a dialkylamino radical in which each alkyl portion contains 1 to 4 carbon atoms or, with the nitrogen atom to which it is linked, forms a saturated 5- or 6-membered heterocyclic radical which may contain a second hetero atom selected from oxygen, sulphur and nitrogen atoms, wherein said heterocyclic radical is unsubstituted or substituted with an alkyl radical containing 1 to 4 carbon atoms, a phenyl radical or a phenylalkyl radical in which the alkyl portion contains 1 to 4 carbon atoms, a carboxyl radical, an alkoxycarbonyl radical in which the alkyl portion contains 1 to 4 carbon atoms, a cyano or carbamoyl radical, an N-alkylcarbamoyl radical in which the alkyl portion contains 1 to 4 carbon atoms, an N,N-dialkyl-carbamoyl radical in which each alkyl portion contains 1 to 4 carbon atoms or, with the nitrogen atom to which it is linked, forms a saturated 5- or 6-membered heterocyclic radical which may contain a second hetero atom selected from oxygen, sulphur and nitrogen atoms, wherein such heterocyclic radical is unsubstituted or substituted with an alkyl radical containing 1 to 4 carbon atoms, with a phenyl radical or a phenylalkyl radical in which the alkyl portion contains 1 to 4 carbon atoms; or a 5- or 6-membered aromatic heterocyclic radical containing an oxygen, sulphur or nitrogen atom as hetero atom, and Z represents hydrogen or a radical of formula: in which: R1 represents a benzoyl radical unsubstituted or substituted with one or more identical or different atoms or radicals selected from halogen, alkyl radicals containing 1 to 4 carbon atoms, alkoxy radicals containing 1 to 4 carbon atoms, and trifluoromethyl radicals, a thenoyl radical, a furoyl radical, or a radical R2-O-CO- in which: R2 represents an alkyl radical containing 1 to 8 carbon atoms, an alkenyl radical containing 2 to 8 carbon atoms, an alkynyl radical containing 3 to 8 carbon atoms, a cycloalkyl radical containing 3 to 6 carbon atoms, a cycloalkenyl radical containing 4 to 6 carbon atoms or bicycloalkyl radical containing 7 to 10 carbon atoms, these radicals being unsubstituted or substituted with one or more substituents selected from halogen, hydroxyl, alkoxy containing 1 to 4 carbon atoms, dialkylamino radicals in which each alkyl portion contains 1 to 4 carbon atoms, piperidino or morpholino radicals, 1-piperazinyl radicals 2955 י' בכסלו התשס" ב - November 25, 2001 unsubstituted or substituted at position 4 with an alkyl radical containing 1 to 4 carbon atoms or with a phenylalkyl radical in which the alkyl portion contains 1 to 4 carbon atoms, cycloalkyl radicals containing 3 to 6 carbon atoms, cycloalkenyl radicals containing 4 to 6 carbon atoms, phenyl radicals unsubstituted or substituted with one or more atoms or radicals selected from halogen atoms, alkyl radicals containing 1 to 4 carbon atoms, alkoxy radicals containing 1 to 4 carbon atoms, cyano radicals, carboxyl radicals and alkoxycarbonyl radicals in which the alkyl portion contains 1 to 4 carbon atoms, a phenyl or a- or b-naphthyl radical unsubstituted or substituted with one or more atoms or radicals selected from halogen atoms, alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, or a 5-