发明名称 Farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them
摘要 PCT No. PCT/FR95/00739 Sec. 371 Date Jun. 18, 1997 Sec. 102(e) Date Jun. 18, 1997 PCT Filed Jun. 7, 1995 PCT Pub. No. WO95/34535 PCT Pub. Date Dec. 21, 1995This invention relates to transferase inhibitors of the formula (I), their preparation, and pharmaceutical compositions containing them. <IMAGE> (I) In formula (I), R1 is Y-S-A1-(Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl radical, an alkoxycarbonyl radical, or an R4-S- radical in which R4 is an alkyl radical containing 1 to 4 carbon atoms optionally substituted by a phenyl radical or a radical of the formula (II) <IMAGE> (II) in which A1 is an alkylene radical containing 1 to 4 carbon atoms optionally substituted at the position a in the grouping >C(X1)(Y1) with an amino, alkylamino, dialkylamino, alkanoylamino, or alkoxycarbonylamino radical); X1 and Y1 are each a hydrogen atom or form, together with the carbon atom to which they are connected, a >C=O grouping; R'1 is hydrogen or methyl; R2 is an alkyl, alkenyl or an alkynyl radical containing 1 to 6 carbon atoms optionally substituted by a hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl, or alkylsulphonyl, wherein when R2 is an alkyl radical substituted by a hydroxyl radical, R2 can form a lactone with the carboxyl radical at the alpha position; R'2 is hydrogen or methyl; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical; and the radical <IMAGE> is in position 5 or 6 of the naphthyl ring. These compounds have anti-cancer properties.
申请公布号 US5861529(A) 申请公布日期 1999.01.19
申请号 US19970750819 申请日期 1997.06.18
申请人 RHONE-POULENC RORER S.A. 发明人 BAUDOIN, BERNARD;BURNS, CHRISTOPHER;COMMERCON, ALAIN;GUITTON, JEAN-DOMINIQUE
分类号 C07C323/25;C07C323/59;C07C323/60;(IPC1-7):C07C323/60;A01N37/12 主分类号 C07C323/25
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