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    • 3. 发明授权
    • Tumor retarding (1-benzyl-ethylenediamine)-platin (II)-complexes
    • 肿瘤抑制(1-苄基 - 乙二胺) - 铂(II) - 复合物
    • US4704464A
    • 1987-11-03
    • US831911
    • 1986-02-21
    • Henri BrunnerHelmut SchonenbergerManfred SchmidtUlrich HolzingerGerfried UngerJurgen Engel
    • Henri BrunnerHelmut SchonenbergerManfred SchmidtUlrich HolzingerGerfried UngerJurgen Engel
    • A61K31/28A61K31/555A61P35/00C07F15/00
    • C07F15/0093
    • There are described (1-benzylethylenediamine)-platin(II)-complexes of the general formula: ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a benzyl group, or a phenylethyl group, and B is a thienyl radical, an indolyl radical, an imidazolyl radical, or a phenyl radical substituted by the radicals R.sub.5, R.sub.6, an R.sub.7 which are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, phenoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, C.sub.1 -C.sub.6 -alkanesulfonyloxy, carboxy, C.sub.1 -C.sub.6 -carbalkoxy, cyano, aminocarboxyl, aminocarbonyl, which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkylcarbonyl, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, (C.sub.1 -C.sub.6 -alkyl).sub.3 N.sup.+, C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanoylamino, C.sub.1 -C.sub.6 -alkanesulfonylamino, C.sub.1 -C.sub.6 -alkyl-C.sub.1 -C.sub.6 -alkanesulfonylamino, aminosulfonyl, aminosulfonyl which contains one or two C.sub.1 -C.sub.6 -alkyl radicals, C.sub.1 -C.sub.6 -alkoxysulfonyl (--SO.sub.2 --O--C.sub.1 --C.sub.6 -alkyl), sulfo (--SO.sub.3 H) or C.sub.1 -C.sub.6 -alkanesulfonyl and two of these groups can be the methylenedioxy group and X is the equivalent of a physiologically compatible anion, as well as optionally their salts with physiologically compatible cations and anions and process of their production.
    • 描述了通式如下的(1-苯乙二胺) - 铂(II) - 复合物:其中基团R 1,R 2,R 3和R 4相同或不同,为氢,C 1 -C 6 - 烷基 ,苄基或苯基乙基,B是噻吩基,吲哚基,咪唑基或被基团R5,R6,R7相同或不同并且为氢的卤素取代的苯基,卤素 ,三卤代甲基,C 1 -C 6烷基,羟基,C 1 -C 6 - 烷氧基,苯氧基,苄氧基,C 1 -C 6 - 烷酰氧基,苯甲酰氧基,C 1 -C 6烷基磺酰氧基,羧基,C 1 -C 6烷氧基,氰基,氨基羰基,氨基羰基 含有一个或两个C 1 -C 6烷基,C 1 -C 6烷基羰基,硝基,氨基,C 1 -C 6烷基氨基,二-C 1 -C 6烷基氨基,(C 1 -C 6烷基)3 N +,C 1 -C 6烷酰基氨基, 含有一个或两个C 1 -C 6烷基的C 1 -C 6烷基-C 1 -C 6烷酰基氨基,C 1 -C 6烷基磺酰基氨基,C 1 -C 6烷基-C 1 -C 6烷基磺酰基氨基,氨基磺酰基,氨基磺酰基,C 1 -C 6烷氧基磺酰基 (-SO 2 -O-C 1 -C 6-a 烷基),磺基(-SO 3 H)或C 1 -C 6 - 烷基磺酰基,并且这些基团中的两个可以是亚甲二氧基,X是生理上相容的阴离子的当量,以及任选的与生理上相容的阳离子和阴离子的盐以及 他们的生产。
    • 6. 发明授权
    • Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes
    • 抗肿瘤剂(1,2-二苯基 - 乙二胺) - 铂(II) - 复合物
    • US4730068A
    • 1988-03-08
    • US831913
    • 1986-02-21
    • Helmut SchonenbergerErwin von AngererJohann KarlMargaretha JennerweinJurgen Engel
    • Helmut SchonenbergerErwin von AngererJohann KarlMargaretha JennerweinJurgen Engel
    • A61K31/28A61P35/00C07C45/29C07C45/51C07C45/56C07C47/575C07F15/00
    • C07F15/0093C07C45/298C07C45/515C07C45/562C07C47/575
    • There are disclosed antitumor active 1,2-diphenyl-ethylenediamine)-platinum(II)-complex of the general formula ##STR1## wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl and R.sub.2 is either (1) a halogen atom and the groups R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydrogen C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, or R.sub.2 is (2) a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group in the 4-position or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and if R.sub.2 is (2) then the groups R.sub.1 and R.sub.3 which are the same or differnt are in the 2 and 6 positions of the phenyl group and are halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, a C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alklanoyloxy group or a halo or C.sub.1 -C.sub.5 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, with the proviso that R.sub.1 can also be hydrogen and the groups R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy group or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and X is the equivalent of a physiologically compatible anion and process of their production.
    • 公开了具有通式“IMAGE”I的抗肿瘤活性的1,2-二苯基 - 乙二胺) - 铂(II) - 复合物,其中R 7是氢或C 1 -C 6 - 烷基,R 2是(1)卤素原子, 基团R 1,R 3,R 4,R 5和R 6相同或不同,为氢,卤素,三卤甲基,C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,或R 2为(2)羟基,C 1 -C 6 - 烷氧基,C 4 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧取代 C 2 -C 6 - 烷酰氧基,如果R 2为(2),则相同或不同的基团R 1和R 3为苯基的2和6位,为卤素,三卤代甲基,C 1 -C 6烷基,羟基, C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 5 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,条件是R 1也可以是氢,基团R 4,R 5和R 6是 相同或不同的 氢,卤素,三卤代甲基,C 1 -C 6 - 烷基,羟基,C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,X等同于 生理上相容的阴离子及其生产方法。