Novel farnesyl transferase inhibitors, preparation thereof and pharmaceutical compositions containing said inhibitors

摘要

Novel farnesyl transferase inhibitors of general formula (I), (I) the preparation thereof and pharmaceutical compositions containing said inhibitors, are disclosed. In general formula (I), R1 is Y-S-A1 (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical or a radical R4-S- where R4 is a C1-4 alkyl radical optionally substituted by a phenyl radical or a radical of general formula (II) (II) wherein A1, X, X1, Y1, R'1, R2, R'2 and R are defined as below, and A1 is a C1-4 alkylene radical optionally alpha-substituted in the >C(X1)(Y1) grouping by an amino or alkylamino, dialkylamino, alkanoylamino or alkoxycarbonylamino radical); X1 and Y1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, form a >C=O grouping; R'1 is hydrogen or a C1-6 alkyl radical; X is an oxygen or sulphur atom; R2 is a C1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that when R2 is an alkyl radical substituted by a hydroxy radical, R2 can form a lactone with the alpha -carboxy radical; and R'2 is hydrogen or a C1-6 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) (a) is in the 3 or 4 position of the naphthyl ring. The novel products have anticancer properties.