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    • 4. 发明授权
    • 4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase
inhibitors
    • 4,9-乙 - 苯并(F)异吲哚衍生物作为法呢基转移酶抑制剂
    • US5936097A
    • 1999-08-10
    • US981840
    • 1998-07-23
    • Alain Commer.cedilla.onAlain Le BrunPatrick MaillietJean-Fran.cedilla.ois PeyronelFabienne Sounigo-ThompsonAlain TruchonMartine Zucco
    • Alain Commer.cedilla.onAlain Le BrunPatrick MaillietJean-Fran.cedilla.ois PeyronelFabienne Sounigo-ThompsonAlain TruchonMartine Zucco
    • C07D409/12A61K31/00A61K31/40A61K31/403A61K31/404A61K31/425A61K31/427A61P35/00A61P43/00C07D209/58C07D209/72C07D277/22C07D417/12C07F9/572C07D209/62C07D209/12C07D307/36
    • C07D209/72C07F9/5728
    • Novel products of formula (I): ##STR1## preparation thereof and pharmaceutical compositions containing said products are disclosed. In formula (I), R is a group of formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z, where X.sub.1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH.sub.2 groups being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR.sub.4, where R.sub.4 is alkyl, or CON(R.sub.5)(R.sub.6), where R.sub.5 hydrogen or alkyl and R.sub.6 is hydrogen or optionally substituted alkyl, or else R.sub.5 is hydrogen or alkyl and R.sub.6 is hydroxy, optionally substituted alkoxy or amino, or PO(OR.sub.7).sub.2, where R.sub.7 is hydrogen or alkyl; or a group --NH--CO--T where T is hydrogen or optionally substituted alkyl; or else a group (a); R.sub.1 and R.sub.2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R.sub.1 and R.sub.2 in the ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted hereoatoms, or R.sub.1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R.sub.2 is thioalkyl; R.sub.3 is hydrogen or halogen or alkyl alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or --NH--, --CO--,methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.
    • PCT No.PCT / FR96 / 01062 Sec。 371日期:1998年7月23日 102(e)1998年7月23日PCT PCT 1996年7月8日PCT公布。 出版物WO97 / 03050 日期1997年1月30日公开了式(I)的新产物:其制备方法和含有所述产物的药物组合物。 在式(I)中,R是式 - (CH2)m-X1-(CH2)nZ的基团,其中X1是简单键或O或S,n是0或1,n是0,1或2, CH 2基任选被羧基,烷氧基羰基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,氨基,烷基氨基或二烷基氨基取代,Z是羧基,COOR 4,其中R 4是烷基或CON(R 5)(R 6) R 6是氢或任选取代的烷基,或者R 5是氢或烷基,R 6是羟基,任选取代的烷氧基或氨基或PO(OR 7)2,其中R 7是氢或烷基; 或基团-NH-CO-T,其中T是氢或任选取代的烷基; 或者一组(a); R1和R2是氢或卤素或任选取代的烷氧基或烷基,或者邻位中的R1和R2形成含有1或2个任选取代的原子的杂环,或者R 1是氢或卤素或任选取代的烷氧基或烷基,R 2 是硫代烷基; R3是氢或卤素或烷基烯基,烷氧基,烷硫基,羧基或烷氧基羰基; X是O或S或-NH-,-CO-,亚甲基,亚乙基,亚烷基或1,1-环烷基; 并且Y是O或S.式(I)的新产物是具有显着的抗肿瘤和抗肿瘤性质的法呢基转移酶抑制剂。