Tumor retarding (1-benzyl-ethylenediamine)-platin (II)-complexes
    1.
    发明授权
    Tumor retarding (1-benzyl-ethylenediamine)-platin (II)-complexes 失效
    肿瘤抑制(1-苄基 - 乙二胺) - 铂(II) - 复合物

    公开(公告)号:US4704464A

    公开(公告)日:1987-11-03

    申请号:US831911

    申请日:1986-02-21

    CPC分类号: C07F15/0093

    摘要: 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.

    摘要翻译: 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。

    Process for the treatment of humans suffering from undesired urotoxic
side effects caused by cytostatically active alkylating agents
    6.
    发明授权
    Process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents 失效
    用于治疗由细胞活性的活性烷化剂引起的不希望的尿毒性副作用的人的治疗方法

    公开(公告)号:US4220660A

    公开(公告)日:1980-09-02

    申请号:US967000

    申请日:1978-12-06

    申请人: Norbert Brock

    发明人: Norbert Brock

    CPC分类号: A61K31/675 A61K31/185

    摘要: The invention is related to a process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents administered to them against malign tumors, comprising administering a pharmacologically acceptable salt of a mercapto alkane sulfonic acid having the general formulaHS--alk--SO.sub.3 4to the human treated with the cytostatically active alkylating agent, in an amount ranging from 20% of the weight of the alkylating agent to the highest tolerated dosage of the salt of the mercapto alkane sulfonic acid, simultaneously or separately in combination with the alkylating agent.

    摘要翻译: 本发明涉及一种治疗患有由恶性肿瘤施用的细胞活性的烷化剂引起的不利的尿毒性副作用的人的方法,包括给予具有通式HS-alk的巯基烷烃磺酸的药学上可接受的盐 -SO34至用细胞活性的烷化剂处理的人,其量为烷基化剂重量的20%至巯基烷烃磺酸的盐的最高耐受剂量,同时或分开地与烷基化 代理商

    Process for the treatment of humans suffering from undesired urotoxic
side effects caused by cytostatically active alkylating agents
    7.
    发明授权
    Process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents 失效
    用于治疗由细胞活性的活性烷化剂引起的不希望的尿毒性副作用的人的治疗方法

    公开(公告)号:US4218471A

    公开(公告)日:1980-08-19

    申请号:US9625

    申请日:1979-02-06

    CPC分类号: A61K31/185 A61K31/675

    摘要: The invention is related to a process for the treatment of humans suffering from undesired urotoxic side effects caused by cytostatically active alkylating agents administered to them against malign tumors, comprising administering a pharmacologically acceptable salt of a dithiodi-(alkane sulfonic acid) having the general formula ##STR1## to the human treated with the cytostatically active alkylating agent, in an amount ranging from 20% of the weight of the alkylating agent to the highest tolerated dosage of the salt of the dithiodi-(alkane sulfonic acid), simultaneously or separately in combination with the alkylating agent.

    摘要翻译: 本发明涉及一种用于治疗患有由恶性肿瘤施用的细胞活性的烷化剂引起的不利的尿毒性副作用的人的方法,包括给予具有通式(II)的二硫代(烷烃磺酸)的药学上可接受的盐 对于用细胞活性活性烷化剂处理的人,其量为烷基化剂重量的20%至二硫代(烷烃磺酸)的盐的最高耐受剂量,同时或分开地 与烷基化剂组合。

    Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes
    8.
    发明授权
    Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes 失效
    抗肿瘤剂(1,2-二苯基 - 乙二胺) - 铂(II) - 复合物

    公开(公告)号:US4730068A

    公开(公告)日:1988-03-08

    申请号:US831913

    申请日:1986-02-21

    摘要: 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.

    摘要翻译: 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。