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Claims for Patent: 6,387,946

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Claims for Patent: 6,387,946

Title: Methods for treating pathological conditions of abnormal cell proliferation
Abstract:New taxoids of general formula (I): ##STR1## their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): ##STR2## display noteworthy antitumour and antileukaemic properties.
Inventor(s): Bouchard; Herve (Ivry-sur-Seine, FR), Bourzat; Jean-Dominique (Vincennes, FR), Commer.cedilla.on; Alain (Vitry-sur-Seine, FR)
Assignee: Aventis Pharma S.A. (Antony, FR)
Application Number:09/985,956
Patent Claims: 1. A method of treating at least one pathological condition associated with abnormal cell proliferation comprising administering to a patient in need thereof an effective amount of at least one compound, wherein said at least one compound is a taxoid of formula (I): ##STR23##

in which:

Z represents a hydrogen atom or a radical of formula (II): ##STR24##

in which:

R.sub.1 represents:

a benzoyl radical optionally substituted with one or more identical or different atoms or radicals selected from a halogen atom, an alkyl radical containing 1 to 4 carbon atoms, an alkoxy radical containing 1 to 4 carbon atoms, a trifluoromethyl radical, a thenoyl radical, a furoyl radical, or

a radical R.sub.2 --O--CO--, in which

R.sub.2 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 a bicycloalkyl radical containing 7 to 10 carbon atoms,

these radicals being optionally substituted with one or more substituents selected from a halogen atom, a hydroxyl radical, an alkoxy radical containing 1 to 4 carbon atoms, a dialkylamino radical in which each alkyl portion contains 1 to 4 carbon atoms, a piperidino radical, a morpholino radical, a 1-piperazinyl radical optionally 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, a cycloalkyl radical containing 3 to 6 carbon atoms, a cycloalkenyl radical containing 4 to 6 carbon atoms; a phenyl radical optionally substituted with one or more atoms or radicals selected from a halogen atom, an alkyl radical containing 1 to 4 carbon atoms and an alkoxy radical containing 1 to 4 carbon atoms, a cyano radical, a carboxyl radical, and a alkoxycarbonyl radical in which the alkyl portion contains 1 to 4 carbon atoms,

a phenyl or .alpha.- or .beta.-naphthyl radical optionally substituted with one or more atoms or radicals selected from a halogen atom; an alkyl radical containing 1 to 4 carbon atoms; and an alkoxy radical containing 1 to 4 carbon atoms,

a 5-membered aromatic heterocyclic radical, or

a saturated heterocyclic radical containing 4 to 6 carbon atoms, optionally substituted with one or more alkyl radicals containing 1 to 4 carbon atoms;

R.sub.3 represents:

an unbranched or branched alkyl radical containing 1 to 8 carbon atoms, an unbranched or branched alkenyl radical containing 2 to 8 carbon atoms, an unbranched or branched alkynyl radical containing 2 to 8 carbon atoms, a cycloalkyl radical containing 3 to 6 carbon atoms, a phenyl or .alpha.- or .beta.-naphthyl radical optionally substituted with one or more identical or different atoms or radicals selected from a halogen atom, 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 heteroatoms selected from nitrogen, oxygen and sulfur atoms and optionally substituted with one or more identical or different substituents selected from a halogen atom, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxycarbonylamino, acyl, arylcarbonyl, cyano, carboxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl and alkoxycarbonyl radicals,

with the proviso that, in the substituents of the phenyl, .alpha.- or .beta.-naphthyl and aromatic heterocyclic radicals in the definitions of R.sub.2 and R.sub.3, the alkyl radicals and the alkyl portions of the other radicals contain 1 to 4 carbon atoms, and the alkenyl and alkynyl radicals contain 2 to 8 carbon atoms, and the aryl radicals are phenyl or .alpha.- or .beta.-naphthyl radicals;

R.sub.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 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 optionally containing a second hetero atom selected from oxygen, sulfur, 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.sub.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 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 optionally containing a second heteroatom selected from an oxygen, sulfur, and nitrogen atom, 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.

2. The method of claim 1, wherein said abnormal cell proliferation is of malignant or nonmalignant cells.

3. The method of claim 1, wherein said abnormal cell proliferation is of cells of at least one tissue or organ.

4. The method of claim 3, wherein said organ is the ovary.

5. The method of claim 1, wherein said abnormal cell proliferation is of the ovary.

6. The method of claim 1, wherein said effective amount of said at least one compound comprises a dose from 0.01 to 200 mg/kg.

7. The method of any one of claims 1 to 6, wherein said administration is chosen from at least one of parenteral, intravenous, intraperitoneal, intramuscular and subcutaneous administration.

8. The method of claim 7, wherein said administration is at least one of intraperitoneal and intravenous administration.
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