Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-08-11
2002-02-12
Jones, Dwayne C. (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
06346543
ABSTRACT:
The present invention provides a new use of taxoid derivatives. More specifically, the present invention provides a method for treating abnormal cell proliferation in the brain of mammals, including humans, by administering a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof:
wherein:
Z represents a hydrogen atom or a radical of formula (II):
wherein:
R
1
represents:
a benzoyl radical which is unsubstituted or substituted with at least one identical or different atom or radical selected from halogen atoms and alkyl radicals containing from 1 to 4 carbon atoms, alkoxy radicals containing from 1 to 4 carbon atoms or trifluoromethyl radicals,
a thenoyl or furoyl radical, or
a radical R
2
—O—CO— in which R
2
represents:
an alkyl radical containing from 1 to 8 carbon atoms,
an alkenyl radical containing from 2 to 8 carbon atoms,
an alkynyl radical containing from 3 to 8 carbon atoms,
a cycloalkyl radical containing from 3 to 6 carbon atoms,
a cycloalkenyl radical containing from 4 to 6 carbon atoms, or
a bicycloalkyl radical containing from 7 to 10 carbon atoms,
these radicals being optionally substituted with one or more substituents selected from halogen atoms and hydroxyl radicals, alkoxy radicals containing from 1 to 4 carbon atoms, dialkylamino radicals in which each alkyl portion contains from 1 to 4 carbon atoms, piperidino or morpholino radicals, 1 -piperazinyl radicals, which radicals are unsubstituted or substituted at position 4 with an alkyl radical containing from 1 to 4 carbon atoms or with a phenylalkyl radical in which the alkyl portion contains from 1 to 4 carbon atoms, cycloalkyl radicals containing from 3 to 6 carbon atoms, cycloalkenyl radicals containing from 4 to 6 carbon atoms, phenyl radicals which are unsubstituted or substituted with at least one atom or radical selected from halogen atoms and alkyl radicals containing from 1 to 4 carbon atoms or alkoxy radicals containing from 1 to 4 carbon atoms, cyano or carboxyl radicals or alkoxycarbonyl radicals in which the alkyl portion contains from 1 to 4 carbon atoms,
a phenyl or &agr;- or &bgr;-naphthyl radical which is unsubstituted or substituted with at least one atom or radical selected from halogen atoms and alkyl radicals containing from 1 to 4 carbon atoms or alkoxy radicals containing from 1 to 4 carbon atoms,
a 5-membered aromatic heterocyclic radical preferably selected from furyl and thienyl radicals, or
a saturated heterocyclic radical containing from 4 to 6 carbon atoms, which is unsubstituted or substituted with at least one alkyl radical containing from 1 to 4 carbon atoms;
R
3
represents:
an unbranched or branched alkyl radical containing from 1 to 8 carbon atoms,
an unbranched or branched alkenyl radical containing from 2 to 8 carbon atoms,
an unbranched or branched alkynyl radical containing from 2 to 8 carbon atoms,
a cycloalkyl radical containing from 3 to 6 carbon atoms,
a phenyl or &agr;- or &bgr;-naphthyl radical which is unsubstituted or substituted with at least one atom or radical selected from halogen atoms and alkyl, alkenyl, alkynyl, aryl, 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,
or a 5-membered aromatic heterocycle containing one or more identical or different hetero atoms selected from nitrogen, oxygen and sulphur atoms, and which is unsubstituted or substituted with at least one identical or different substituent selected from halogen atoms and alkyl, aryl, amino, alkylamino, dialkylamino, alkoxycarbonylamino, acyl, arylcarbonyl, cyano, carboxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl and alkoxycarbonyl radicals,
with the provisos that, in the substituents of the phenyl, &agr;- or &bgr;-naphthyl and aromatic heterocyclic radicals, the alkyl radicals and the alkyl portions of the other radicals contain from 1 to 4 carbon atoms, and that the alkenyl and alkynyl radicals contain from 2 to 8 carbon atoms, and that the aryl radicals are phenyl or &agr;- or &bgr;-naphthyl radicals;
R
4
represents:
an alkoxy radical containing from 1 to 6 carbon atoms in an unbranched or branched chain,
an alkenyloxy radical containing from 3 to 6 carbon atoms in an unbranched or branched chain,
an alkynyloxy radical containing from 3 to 6 carbon atoms in an unbranched or branched chain,
a cycloalkyloxy radical containing from 3 to 6 carbon atoms, or
a cycloalkenyloxy radical containing from 4 to 6 carbon atoms,
these radicals being which is unsubstituted or substituted with at least one halogen atom or with an alkoxy radical containing from 1 to 4 carbon atoms, an alkylthio radical containing from 1 to 4 carbon atoms or a carboxyl radical, an alkyloxycarbonyl radical in which the alkyl portion contains from 1 to 4 carbon atoms, a cyano or carbamoyl radical or an N-alkylcarbamoyl or N,N-dialkylcarbamoyl radical in which each alkyl portion contains from 1 to 4 carbon atoms or, with the nitrogen atom to which it is linked, forms a saturated 5- or 6-membered heterocyclic radical containing or not containing a second hetero atom selected from oxygen, sulphur, and nitrogen atoms, which is unsubstituted or substituted with an alkyl radical containing from 1 to 4 carbon atoms or a phenyl radical or a phenylalkyl radical in which the alkyl portion contains from 1 to 4 carbon atoms; and
R
5
represents:
an alkoxy radical containing from 1 to 6 carbon atoms in an unbranched or branched chain,
an alkenyloxy radical containing from 3 to 6 carbon atoms,
an alkynyloxy radical containing from 3 to 6 carbon atoms,
a cycloalkyloxy radical containing from 3 to 6 carbon atoms or
a cycloalkenyloxy radical containing from 3 to 6 carbon atoms,
these radicals being which is unsubstituted or substituted with at least one halogen atom or with an alkoxy radical containing from 1 to 4 carbon atoms, an alkylthio radical containing from 2 to 4 carbon atoms or a carboxyl radical, an alkyloxycarbonyl radical in which the alkyl portion contains from 1 to 4 carbon atoms, a cyano or carbamoyl radical or an N-alkylcarbamoyl or N,N-dialkylcarbamoyl radical in which each alkyl portion contains from 1 to 4 carbon atoms or, with the nitrogen atom to which it is linked, forms a saturated 5- or 6-membered heterocyclic radical containing or not containing a second hetero atom selected from oxygen, sulphur, and nitrogen atoms, which is unsubstituted or substituted with an alkyl radical containing from 1 to 4 carbon atoms or a phenyl radical or a phenylalkyl radical in which the alkyl portion contains from 1 to 4 carbon atoms.
Both the foregoing general description and the following detailed description of the invention are exemplary and explanatory only and are not necessarily restrictive of the claimed invention.
Preferably, the aryl radicals which can be represented by R
3
are phenyl or &agr;- or &bgr;-naphthyl radicals which is unsubstituted or substituted with at least one atom or radical selected from halogen atoms (fluorine, chlorine, bromine, iodine) and alkyl, alkenyl, alkynyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, hydroxyl, hydroxyalkyl, mercapto, formyl, acyl, acylamino, aroylamino, alkoxycarbonylamino, amino, alkylamino, dialkylamino, carboxyl, alkoxycarbonyl, carbamoyl, dialkylcarbamoyl, cyano, nitro, and trifluoromethyl radicals, with the provisos that the alkyl radicals and the alkyl portions of the other radicals contain from 1 to 4 carbon atoms, that the alkenyl and alkynyl radicals contain from 2 to 8 carbon atoms, and that the aryl radicals are phenyl or &agr;- or &bgr;-naphthyl radicals.
Preferably, the heterocyclic radicals which can be represented by R
3
are 5-membered aromatic heterocyclic radicals containing one or more identical or different atoms selected from nitrogen, oxygen, and sulphur atoms, which is unsubstituted or substituted with at least one identical or different substituents selected from halogen atoms (fluo
Bissery Marie-Christine
Brealey Clive
Roberts Simon
Vrignaud Patricia
Aventis Pharma S.A.
Finnegan Henderson Farabow Garrett & Dunner LLP
Jones Dwayne C.
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