Farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them

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United States of America Patent

PATENT NO 5861529
SERIAL NO

08750819

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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This invention relates to transferase inhibitors of the formula (I), their preparation, and pharmaceutical compositions containing them. ##STR1## In formula (I), R.sub.1 is Y--S--A.sub.1 --(Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl radical, an alkoxycarbonyl radical, or an R.sub.4 --S-- radical in which R.sub.4 is an alkyl radical containing 1 to 4 carbon atoms optionally substituted by a phenyl radical or a radical of the formula (II) ##STR2## in which A.sub.1 is an alkylene radical containing 1 to 4 carbon atoms optionally substituted at the position a in the grouping >C(X.sub.1)(Y.sub.1) with an amino, alkylamino, dialkylamino, alkanoylamino, or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or form, together with the carbon atom to which they are connected, a >C.dbd.O grouping; R'.sub.1 is hydrogen or methyl; R.sub.2 is an alkyl, alkenyl or an alkynyl radical containing 1 to 6 carbon atoms optionally substituted by a hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl, or alkylsulphonyl, wherein when R.sub.2 is an alkyl radical substituted by a hydroxyl radical, R.sub.2 can form a lactone with the carboxyl radical at the .alpha. position; R'.sub.2 is hydrogen or methyl; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical; and the radical ##STR3## is in position 5 or 6 of the naphthyl ring. These compounds have anti-cancer properties.

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Patent Owner(s)

Patent OwnerAddress
RHONE-POULENC RORER S A20 AVENUE RAYMOND ARON ANTONY CEDEX 92165

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Baudoin, Bernard Chaville, FR 10 140
Burns, Christopher Rosemont, PA 40 261
Commercon, Alain Vitry-sur-Seine, FR 54 987
Guitton, Jean-Dominique Paris, FR 13 850

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