Farnesyl transferase inhibitors, preparation thereof and pharmac

Details Farnesyl transferase inhibitors, preparation thereof and pharmac Farnesyl transferase inhibitors, preparation thereof and pharmac

1998-01-09

1999-03-30

Barts, Samuel

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514502, 560 10, 562427, A61K 31235

Patent

active

058890530

ABSTRACT:
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 >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 >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.

REFERENCES:
patent: 5705686 (1998-01-01), Sebti et al.

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