Use of taxoid derivatives

Details Use of taxoid derivatives Use of taxoid derivatives

2000-01-13

2002-06-11

Goldberg, Jerome D. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

Reexamination Certificate

active

06403634

ABSTRACT:

The present invention relates to a new pharmaceutical form of taxoid derivatives. More precisely, it relates to the oral administration of a compound of general formula (I) or a pharmaceutically acceptable salt or solvent thereof:
in which:
Z represents a hydrogen atom or a radical of general formula:
 in which:
R
1
represents
a benzoyl radical optionally substituted with one or more identical or different atoms or radicals chosen from halogen atoms, alkyl radicals comprising 1 to 4 carbon atoms, alkoxy radicals comprising 1 to 4 carbon atoms, and trifluoromethyl radicals,
a thenoyl or furoyl radical,
a radical R
2
—O—CO— in which R
2
represents:
an alkyl radical comprising 1 to 8 carbon atoms,
an alkenyl radical comprising 2 to 8 carbon atoms,
an alkynyl radical comprising 3 to 8 carbon atoms,
a cycloalkyl radical comprising 3 to 6 carbon atoms,
a cycloalkenyl radical comprising 4 to 6 carbon atoms, or
a bicycloalkyl radical comprising 7 to 61 carbon atoms,
these radicals being optionally substituted with one or more identical or different substituents chosen from halogen atoms, hydroxyl radicals, alkoxy radicals comprising 1 to 4 carbon atoms, dialkylamino radicals in which each alkyl portion comprises 1 to 4 carbon atoms, piperidino or morpholino radicals, 1-piperazinyl radicals which are optionally substituted at position 4 with an alkyl radical comprising 1 to 4 carbon atoms or with a phenylalkyl radical in which the alkyl portion comprises 1 to 4 carbon atoms, cycloalkyl radicals comprising 3 to 6 carbon atoms, cycloalkenyl radicals comprising 4 to 6 carbon atoms, phenyl radicals which are optionally substituted with one or more identical or different atoms or radicals chosen from halogen atoms, alkyl radicals comprising 1 to 4 carbon atoms, and alkoxy radicals comprising 1 to 4 carbon atoms, cyano or carboxyl radicals, and alkoxycarbonyl radicals in which the alkyl portion comprises 1 to 4 carbon atoms,
a phenyl or &agr;- or &bgr;-naphthyl radical optionally substituted with one or more identical or different atoms or radicals chosen from halogen atoms, alkyl radicals comprising 1 to 4 carbon atoms and alkoxy radicals comprising 1 to 4 carbon atoms,
a 5-membered aromatic heterocyclic radical, preferably chosen from furyl and thienyl radicals, or
a saturated heterocyclic radical comprising 4 to 6 carbon atoms, and optionally substituted with one or more identical or different alkyl radicals comprising 1 to 4 carbon atoms;
R
3
represents
an unbranched or branched alkyl radical comprising 1 to 8 carbon atoms,
an unbranched or branched alkenyl radical comprising 2 to 8 carbon atoms,
an unbranched or branched alkynyl radical comprising 2 to 8 carbon atoms,
a cycloalkyl radical comprising 3 to 6 carbon atoms,
a phenyl or &agr;- or &bgr;-naphthyl radical optionally substituted with one or more identical or different atoms or radicals chosen from halogen atoms and alkyl, alkenyl, alkynyl, phenyl, &agr;- or &bgr;-naphthyl, aralkyl, alkoxy, alkylthio, aryloxy, arylthio, hydroxyl, hydroxyalkyl, mercapto, formyl, acyl, acylamino, aroylamino, alkoxycarbonylamino, amino, alkylamino, dialkylamino, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, nitro and trifluoromethyl radicals, it being understood that the alkyl radicals and alkyl portions of radicals comprise 1 to 4 carbon atoms, and the alkenyl and alkynyl radicals comprise 2 to 8 carbon atoms, or
a 5-membered aromatic heterocyclic radical comprising one or more identical or different hetero atoms chosen from nitrogen, oxygen and sulphur atoms, and optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, phenyl, &agr;- or &bgr;-naphthyl, alkoxy, aryloxy, amino, alkylamino, dialkylamino, acylamino, alkoxycarbonylamino, acyl, arylcarbonyl, cyano, carboxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl and alkoxycarbonyl radicals, it being understood that the alkyl radicals and alkyl portions of radicals comprise 1 to 4 carbon atoms, and the alkenyl and alkynyl radicals comprise 2 to 8 carbon atoms;
R
4
represents
an alkoxy radical comprising 1 to 6 carbon atoms in an unbranched or branched chain,
an alkenyloxy radical comprising,3 to 6 carbon atoms in an unbranched or branched chain,
an alkynyloxy radical comprising 3 to 6 carbon atoms in an unbranched or branched chain,
a cycloalkyloxy radical comprising 3 to 6 carbon atoms, or
a cycloalkenyloxy radical comprising 4 to 6 carbon atoms,
these radicals being optionally substituted with one or more identical or different halogen atoms or with an alkoxy radical comprising 1 to 4 carbon atoms, an alkylthio radical comprising 1 to 4 carbon atoms, a carboxyl radical, an alkyloxycarbonyl radical in which the alkyl portion comprises 1 to 4 carbon atoms, a cyano or carbamoyl radical, or an N-alkylcarbamoyl or N,N-dialkylcarbamoyl radical in which each alkyl portion comprises 1 to 4 carbon atoms or in which each alkyl portion forms, with the nitrogen atom to which it is attached, a saturated 5- or 6-membered heterocyclic radical optionally comprising a second hetero atom chosen from oxygen, sulphur and nitrogen atoms, and optionally substituted with an alkyl radical comprising 1 to 4 carbon atoms, a phenyl radical or a phenylalkyl radical in which the alkyl portion comprises 1 to 4 carbon atoms;
R
5
represents
an alkoxy radical comprising 1 to 6 carbon atoms in an unbranched or branched chain,
an alkenyloxy radical comprising 3 to 6 carbon atoms,
an alkynyloxy radical comprising 3 to 6 carbon atoms,
a cycloalkyloxy radical comprising 3 to 6 carbon atoms, or
a cycloalkenyloxy radical comprising 3 to 6 carbon atoms,
these radicals being optionally substituted with one or more identical or different halogen atoms or with an alkoxy radical comprising 1 to 4 carbon atoms, an alkylthio radical comprising 2 to 4 carbon atoms, a carboxyl radical, an alkyloxycarbonyl radical in which the alkyl portion comprises 1 to 4 carbon atoms, a cyano or carbamoyl radical, or an N-alkylcarbamoyl or N,N-dialkylcarbamoyl radical in which each alkyl portion comprises 1 to 4 carbon atoms or in which each alkyl portion forms, with the nitrogen atom to which it is attached, a saturated 5- or 6-membered heterocyclic radical optionally comprising a second hetero atom chosen from oxygen, sulphur and nitrogen atoms, and optionally substituted with an alkyl radical comprising 1 to 4 carbon atoms, a phenyl radical or a phenylalkyl radical in which the alkyl portion comprises 1 to 4 carbon atoms.
Preferably, R
3
is an aryl radical represented by a phenyl or &agr;- or &bgr;-naphthyl radical optionally substituted with one or more identical or different atoms or radicals chosen from fluorine, chlorine, bromine, and iodine atoms, and alkyl, alkenyl, alkynyl, phenyl, &agr;- or &bgr;-naphthyl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, hydroxyl, hydroxyalkyl, mercapto, formyl, acyl, acylamino, aroylamino, alkoxycarbonylamino, amino, alkylamino, dialkylamino, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, nitro and trifluoromethyl radicals, it being understood that the alkyl radicals and alkyl portions of the other radicals comprise 1 to 4 carbon atoms, and the alkenyl and alkynyl radicals comprise 2 to 8 carbon atoms.
Preferably, R
3
can also be a 5-membered aromatic heterocyclic radical comprising one or more identical or different hetero atoms chosen from nitrogen, oxygen and sulphur atoms, and optionally substituted with one or more identical or different substituents chosen from fluorine, chlorine, bromine, and iodine atoms, alkyl radicals comprising 1 to 4 carbon atoms, aryl radicals comprising 6 to 10 carbon atoms, alkoxy radicals comprising 1 to 4 carbon atoms, aryloxy radicals comprising 6 to 10 carbon atoms, amino radicals, alkylamino radicals comprising 1 to 4 carbon atoms, dialkylamino radicals in which each alkyl portion comprises 1 to 4 carbon atoms, acylamino radicals in which the acyl portion comprises 1 to 4carbon atoms, alkoxycarbonylamino radicals comprising 1 to 4 carbon atoms, a

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