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    • 33. 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。
    • 34. 发明授权
    • Complexes derived from platinum, their preparation and the
pharmaceutical compositions which contain them
    • 衍生自铂的复合物,其制备物和含有它们的药物组合物
    • US5225207A
    • 1993-07-06
    • US775410
    • 1991-10-15
    • Michel BarreauJean-Claude ChottardJean-Bernard Le PecoPatrick Mailliet
    • Michel BarreauJean-Claude ChottardJean-Bernard Le PecoPatrick Mailliet
    • C07F15/00
    • C07F15/0093
    • New complexes of general formula (I) in whichR.sub.1 and R.sub.2 together form a saturated or unsaturated polycyclic carbocyclic radical containing 7 to 12 carbon atoms, or a saturated or partially saturated mono-, bi- or tricyclic heterocyclic radical containing 5 to 11 chain members and a hetero-atom chosen from oxygen, sulphur or nitrogen, which latter atom can optionally be substituted by an alkoxycarbonyl radical, and,X.sub.1 and X.sub.2 represent chlorine atoms or together formeither a radical of structure: ##STR1## in which n is 0 to 2 and R.sub.6 and R.sub.7, which are identical or different, are hydrogen atoms or, when n=1, can be alkyl radicals or form, together with the carbon atom to which they are attached, a cyclobutyl radical,or a radical of structure: ##STR2## in which n, R.sub.6 and R.sub.7 are defined as above, or their salts where such exist, and their hydrates, their preparation and the pharmaceutical compositions which contain them. ##STR3##
    • 通式(I)的新络合物,其中R 1和R 2一起形成含有7至12个碳原子的饱和或不饱和多环碳环基团,或含有5至11个链成员的饱和或部分饱和的单,双或三环杂环基团 和选自氧,硫或氮的杂原子,其后一个原子可任选被烷氧基羰基取代,并且,X 1和X 2表示氯原子或一起形成结构式如下的基团:其中 n为0〜2,R6和R7为相同或不同的氢原子,n = 1时,可以为烷基,也可以与它们所连接的碳原子一起形成环丁基或 结构基团:其中n,R6和R7如上所定义,或其盐,如此存在,以及它们的水合物,它们的制备和含有它们的药物组合物。 (一)