Rhone-poulenc Rorer S.a.

Phone-poulenc Rorer Sa.

Christopher Burns

Alain Commercon

Bernard Baudoin

Jean-Dominique Guitton

Alain Le Brun

Alain Lebrun

Novel farnesyl transferase inhibitors of general formula (I), ##STR1## the preparation thereof and pharmaceutical compositions containing said inhibitors, are disclosed. In general formula (I), R.sub.1 is Y--S--A.sub.1 (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical or a radical R.sub.4 --S-- where R.sub.4 is a C.sub.1-4 alkyl radical optionally substituted by a phenyl radical or a radical of general formula (II) ##STR2## wherein A.sub.1, X, X.sub.1, Y.sub.1, R'.sub.1, R.sub.2, R'.sub.2 and R are defined as below, and A.sub.1 is a C.sub.1-4 alkylene radical optionally alpha-substituted in the &gt;C(X.sub.1)(Y.sub.1) grouping by an amino or alkylamino, dialkylamino, alkanoylamino or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, form a &gt;C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that when R.sub.2 is an alkyl radical substituted by a hydroxy radical, R.sub.2 can form a lactone with the .alpha.-carboxy radical; and R'.sub.2 is hydrogen or a C.sub.1-6 alkyl radical; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted pheny radical, with the proviso that radical (a) ##STR3## is in the 3 or 4 position of the naphthyl ring. The novel products have anticancer properties.

Farnesyl transferase inhibitors, preparation thereof and pharmaceuticals

Farnesyl transferase inhibitors, their preparation and the

Farnesyl transferase inhibitors, preparation thereof and pharmaceutical

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Rosemont, PA, United States of America

Christopher Burns