4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase

Details 4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase 4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase

1998-07-23

1999-08-10

Richter, Johann

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548491, 548494, 548426, 548146, 5483351, 548469, 5483771, 549506, 546 22, 5462767, 560 24, 585400, 514 80, 514410, C07D20962, C07D20912, C07D27722, C07D30736

Patent

active

059360976

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to new products of general formula: ##STR2## to their preparation and to the pharmaceutical compositions which contain them.
In the general formula (I), R represents: --(CH.sub.2).sub.n Z in which an integer equal to 0 or 1 and n represents an integer equal to 0, 1 or 2, it being possible for the methylene radicals to be substituted by a carboxyl radical, an alkoxycarbonyl radical in which the alkyl part contains 1 to 4 carbon atoms, a carbamoyl radical, an alkylcarbamoyl radical in which the alkyl part contains 1 to 4 carbon atoms, a dialkylcarbamoyl radical in which each alkyl part contains 1 to 4 carbon atoms, an amino radical, an alkylamino radical containing 1 to 4 carbon atoms or a dialkylamino radical in which each alkyl part contains 1 to 4 carbon atoms and alkyl radical containing 1 to 3 carbon atoms, or atom or a straight or branched alkyl radical containing 1 to 6 carbon atoms and R.sub.6 represents a hydrogen atom or a straight or branched alkyl radical containing 1 to 6 carbon atoms optionally substituted by an amino, alkylamino containing 1 to 4 carbon atoms, dialkylamino in which each alkyl part contains 1 to 4 carbon atoms, hydroxyl, alkoxy containing 1 to 4 carbon atoms, mercapto, alkylthio containing 1 to 4 carbon atoms, alkyloxycarbonyl in which the alkyl part contains 1 to 4 carbon atoms, carboxyl, cyano, phenyl optionally substituted by one or a number of identical or different atoms or radicals chosen from halogen atoms and alkyl radicals containing 1 to 4 carbon atoms, alkoxy radicals containing 1 to 4 carbon atoms, dialkylamino radicals in which each alkyl part contains 1 to 4 carbon atoms, trifluoromethyl radicals or cyano radicals, 1- or 2-naphthyl, 2- or 3-furyl, 2- or 3-thienyl, 4- or 5-imidazolyl, 2-, 4- or 5-thiazolyl, 2-, 4- or 5-thiazolidinyl or 2-, 3- or 4-pyridyl radical or an indanyl or thiochromanyl radical or else R.sub.5 represents a hydrogen atom or a straight or branched alkyl radical containing 1 to 6 carbon atoms and R.sub.6 represents a hydroxyl radical, an amino radical or an alkyloxy radical containing 1 to 6 straight- or branched-chain carbon atoms optionally substituted by a phenyl radical, or a straight or branched alkyl radical containing 1 to 6 carbon atoms, or or branched alkyl radical containing 1 to 6 carbon atoms optionally substituted by an amino, carboxyl, alkyloxycarbonyl, in which the alkyl part contains 1 to 4 carbon atoms, hydroxyl, alkyloxy containing 1 to 4 carbon atoms, mercapto or alkylthio, containing 1 to 4 carbon atoms, radical, or else ##STR3## radical in which ##STR4## preferably represents a pyridinium radical, R.sub.1 and R.sub.2, which are identical or different, represent a hydrogen or halogen atom or an alkyl radical containing 1 to 4 carbon atoms, an alkyloxy radical containing 1 to 4 carbon atoms optionally substituted by a dialkylamino radical in which each alkyl part contains 1 to 4 carbon atoms or forms, with the nitrogen atom, a saturated heterocycle containing 5 or 6 carbon atoms, an alkylthio radical containing 1 to 4 carbon atoms or an alkyloxycarbonyl radical in which the alkyl part contains 1 to 4 carbon atoms, or else R.sub.1 and R.sub.2, situated in the ortho position with respect to one another, form a saturated or unsaturated heterocycle containing 1 or 2 heteroatoms chosen from nitrogen and oxygen, optionally substituted by a halogen atom or by an alkyl radical containing 1 to 4 carbon atoms or an alkyloxy radical containing 1 to 4 carbon atoms, or else R.sub.1 represents a hydrogen or halogen atom or an alkyl radical containing 1 to 4 carbon atoms, an alkyloxy radical containing 1 to 4 carbon atoms optionally substituted by a dialkylamino radical in which each alkyl part contains 1 to 4 carbon atoms, an alkylthio radical containing 1 to 4 carbon atoms or an alkyloycarbonyl radical in which the alkyl part contains 1 to 4 carbon atoms and R.sub.2 represents a thioalkyl radical containing 1 to 4 carbon atoms, it being understood that, in this case, the product of general formula (I) exists

REFERENCES:
patent: 4465688 (1984-08-01), Schroot et al.

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