Farnesyl transferase inhibitors, preparation thereof, and pharmaceutical compositions containing same

US5856439A · kind A · utility

Assignee

• RHONE-POULENC RORER S.A. · FR

Inventor

• Francois Clerc · Antony, FR

Key dates

• Filing date: Aug 1, 1997
• Grant date: Jan 5, 1999
• Expiry date: Aug 1, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. 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.1-6 alkyl radical optionally substituted by a phenyl radical, or a radical of general formula (II), ##STR2## wherein A.sub.1, X.sub.1, Y.sub.1, R'.sub.2, R'.sub.2, X.sub.2, Y.sub.2, R.sub.3, R'.sub.3 and R are as defined 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, alkylamino, 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, a >C.dbd.O grouping; R.sub.2 is a straight or branched C.sub.1-4 alkyl radical optionally substituted by a cyclohexyl radical; R'.sub.2 is hydrogen or alkyl; X.sub.2 and Y.sub.2 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C.dbd.O grouping; R.sub.3 is a C.sub.1-4 alkyl…