NOVEL INHIBITORS OF FARNESYL TRANSFERASE, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH INHIBITORS

• Main Author: CLERC FRANCOIS-FREDERIC
• Format: Patent
• Language: English
• Published: 12.11.1997
• Edition: 6
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PCT No. PCT/FR96/00198 Sec. 371 Date Aug. 1, 1997 Sec. 102(e) Date Aug. 1, 1997 PCT Filed Feb. 7, 1996 PCT Pub. No. WO96/24611 PCT Pub. Date Aug. 15, 1996Novel farnesyl transferase inhibitors of general formula (I) (I) preparation thereof and pharmaceutical compositions containing same. 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 C1-6 alkyl radical optionally substituted by a phenyl radical, or a radical of general formula (II), (II) wherein A1, X1, Y1, R'2, R'2, X2, Y2, R3, R'3 and R are as defined below, and A1 is a C1-4 alkylene radical optionally alpha -substituted in the >C(X1) (Y1) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical); X1 and Y1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C=O grouping; R2 is a straight or branched C1-4 alkyl radical optionally substituted by a cyclohexyl radical; R'2 is hydrogen or alkyl; X2 and Y2 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C=O grouping; R3 is a C1-4 alkyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that, when R3 is an alkyl radical substituted by a hyroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that, when R3 is an alkyl radical substituted by a hydroxy radical, R3 may form a lactone with the alpha -carboxy radical; R'3 is hydrogen or alkyl; X is an oxygen or sulphur atom; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical. These novel products have anticancer properties.