Patent IL-117636-A (IL)
Title: Taxoids, their preparation and pharmaceutical compositions containing them
IPC: A61K31/00
Filed: 1996-03-24
Abstract: A taxoid of the formula in which: Z represents a hydrogen atom or a radical of the formula in which: R1 represents a benzoyl radical optionally substituted by one or more identical or different atoms or radicals chosen from halogen, alkyl containing 1 to 4 carbon atoms, alkoxy containing 1 to 4 2202 י" ד באלול התשס" ד - August 31, 2004 carbon atoms, alkoxy containing 1 to 4 carbon atoms and trifluoromethyl, a thenoyl or 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, a a bicycloalkyl radical containing 7 to 10 carbon atoms, these radicals being optionally substituted by one or more substituents chosen from halogen, hydroxyl, alkoxy containing 1 to 4 carbon atoms, dialkylamino in which each alkyl portion contains 1 to 4 carbon atoms, piperidino, morpholino, 1-piperazinyl (optionally substituted at the 4-position by 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 containing 3 to 6 carbon atoms, cycloalkenyl containing 4 to 6 carbon atoms, phenyl (optionally substituted by one or more identical or different substituents chosen from halogen, alkyl containing 1 to 4 carbon atoms and alkoxy containing 1 to 4 carbon atoms), cyano, carboxyl and alkoxycarbonyl in which the alkyl portion contains 1 to 4 carbon atoms, a phenyl or a- or b-naphthyl radical optionally substituted by one or more identical or different substituents chosen from halogen, alkyl containing 1 to 4 carbon atoms and alkoxy containing 1 to 4 carbon atoms, or a 5-membered aromatic heterocycic radical, or a saturated heterocyclic radical containing 4 to 6 carbon atoms, optionally substituted by one or more alkyl radicals containing 1 to 4 carbon atoms, R3 represents an alkyl radical containing 1 to 8 carbon atoms, an alkenyl radical containing 2 to 8 carbon atoms, an alkynyl radical containing 2 to 8 carbon atoms, a cycloalkyl radical containing 3 to 6 carbon atoms, carbon atoms, a phenyl or b- or a-naphthyl radical optionally substituted by 2203 י" ד באלול התשס" ד - August 31, 2004 one or more identical or different substituents chosen from halogen, alkyl, alkenyl, alkyny, aryl, aralkyl, alkoxy, alkylthio, aryloxy, arylthio, hydroxyl, hydroxyalkyl, mercapto, formyl, acyl, acyamino, aroylamino, alkoxycarbonylamino, amino, alkylamino, dialkylamino, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, nitro and trifluoromethyl, or a 5-membered aromatic heterocycle containing one or more identical or different hetero atoms chosen from nitrogen, oxygen and sulphur atoms and optionally substituted by one or more identical or different substituents chosen from halogen, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxycarbonylamino, acyl, arylcarbonyl, cyano, carboxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl and alkoxycarbonyl, on the understanding that, in the substituents of the phenyl, a- or b-naphthyl and aromatic heterocyclic radicals, the alkyl radicals and the alkyl portions of other radicals contain 1 to 4 carbon atoms, and that the alkenyl and alkynyl radicals contain 2 to 8 carbon atoms, and that the aryl radicals are phenyl or a- or b-naphthyl radicals, R4 represents an unsubstituted alkoxy radical containing 1 to 6 carbon atoms, or an alkenyloxy radical containing 3 to 6 carbon atoms, an alkynyloxy radical containing 3 to 6 carbon atoms, a cycloalkyloxy radical containing 3 to 6 carbon atoms or a cycloalkenyloxy radical containing 4 to 6 carbon atoms, these radicals being optionally substituted by one or more halogen atoms or with an alkoxy radical containing 1 to 4 carbon atoms, an alkylthio radical containing 1 to 4 carb