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    • 3. 发明授权
    • Compositions and methods to control abnormal cell growth
    • 控制异常细胞生长的组成和方法
    • US07943606B2
    • 2011-05-17
    • US12572793
    • 2009-10-02
    • Zoltan Kiss
    • Zoltan Kiss
    • A61K31/382C07D335/16
    • C07D335/08C07D335/16
    • A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. They can be used alone or in combination with other therapies to treat cancer and other cell proliferative diseases. Representative compounds of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide and N,N-diethyl-N-allyl-3-(2-methyl-9H-thioxanthen-9-ylidene)-propane-1-aminium bromide, were shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. These compounds had even greater effects on tumor volume, body weight, and survival when administered together with the human protein placental alkaline phosphatase.
    • 通常含有三烷基铵基团的一类化合物已被合成并被表征为抗癌化合物。 它们可以单独使用或与其他疗法组合用于治疗癌症和其他细胞增殖性疾病。 该类的代表性化合物是N,N-二乙基-N-甲基-2 - [(9-氧代-9H-噻吨-2-基)甲氧基]乙胺碘化物和N,N-二乙基-N-烯丙基-3-( 2-甲基-9H-噻吨-9-亚基) - 丙烷-1-氨基溴化物,显示在各种肿瘤模型中,以减少肿瘤体积,增强其他化学治疗剂(包括顺铂)的作用,减少化疗引起的体重下降, 并增加用有毒量的顺铂共同处理的动物的存活。 当与人类蛋白质胎盘碱性磷酸酶一起施用时,这些化合物对肿瘤体积,体重和存活率具有更大的影响。
    • 4. 发明申请
    • Use of one or more metal carriers to selectively kill mammalian cells
    • 使用一种或多种金属载体来选择性地杀死哺乳动物细胞
    • US20070010427A1
    • 2007-01-11
    • US11472763
    • 2006-06-22
    • Zoltan Kiss
    • Zoltan Kiss
    • A61K38/16
    • A61K38/16A61K33/24A61K33/30A61K47/547A61K47/665A61K47/6929B82Y5/00A61K2300/00
    • Compositions and methods for decreasing the viability of cells, particularly aberrant non-healthy cells, and most particularly cancer cells, are disclosed. The primary agent that causes cell death is a toxic metal atom or ion. Embodiments of the invention provide compositions and methods to ensure that the toxic metal is directed to the desired cell or tissue. In one embodiment, the metal is bound to a sulfur-rich peptide or protein carrier containing a targeting moiety. Such metal-protein complex is targeted to the selected cells or tissues to enrich the cell or tissue site with the metal-containing peptide or protein molecules followed by administering a dithiocarbonyl which carries the metal from the protein inside the cells to induce cell death.
    • 公开了用于降低细胞,特别是异常非健康细胞,特别是癌细胞活力的组合物和方法。 造成细胞死亡的主要原因是毒性金属原子或离子。 本发明的实施方案提供了确保有毒金属被引导到期望的细胞或组织的组合物和方法。 在一个实施方案中,金属与含有靶向部分的富含硫的肽或蛋白载体结合。 这样的金属蛋白复合物被靶向所选择的细胞或组织,以用含金属的肽或蛋白质分子富集细胞或组织部位,然后施用携带来自细胞内的蛋白质的金属的二硫代羰基以诱导细胞死亡。
    • 6. 发明申请
    • COMPOSITIONS AND METHODS TO CONTROL ABNORMAL CELL GROWTH
    • 组合物和控制异常细胞生长的方法
    • US20100022617A1
    • 2010-01-28
    • US12501895
    • 2009-07-13
    • Zoltan Kiss
    • Zoltan Kiss
    • A61K31/38A61K31/33
    • C07D335/08C07D335/16
    • A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. A representative of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide (CCDTHT) was shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. CCDTHT had even greater effects on tumor volume, body weight, and survival when administered to animals together with the human protein placental alkaline phosphatase. These trialkylammonium group-containing compounds and alkaline phosphatases, particularly in combination with each other and other therapies, may be used to treat cancer and other cell proliferative diseases.
    • 通常含有三烷基铵基团的一类化合物已被合成并被表征为抗癌化合物。 在各种肿瘤模型中显示了该类代表N,N-二乙基-N-甲基-2 - [(9-氧代-9H-噻吨-2-基)甲氧基]乙胺碘化物(CCDTHT)以减少肿瘤体积, 增强其他化学治疗剂(包括顺铂)的作用,减少化疗引起的体重减轻,并增加用有毒量的顺铂共同处理的动物的存活。 当与人类蛋白质胎盘碱性磷酸酶一起施用于动物时,CCDTHT对肿瘤体积,体重和存活有更大的影响。 这些含三烷基铵基的化合物和碱性磷酸酶,特别是彼此组合和其它疗法可用于治疗癌症和其它细胞增殖性疾病。
    • 9. 发明授权
    • Use of one or more metal carriers to selectively kill mammalian cells
    • 使用一种或多种金属载体来选择性地杀死哺乳动物细胞
    • US07655620B2
    • 2010-02-02
    • US11472763
    • 2006-06-22
    • Zoltan Kiss
    • Zoltan Kiss
    • A61K38/16C07C325/00
    • A61K38/16A61K33/24A61K33/30A61K47/547A61K47/665A61K47/6929B82Y5/00A61K2300/00
    • Compositions and methods for decreasing the viability of cells, particularly aberrant non-healthy cells, and most particularly cancer cells, are disclosed. The primary agent that causes cell death is a toxic metal atom or ion. Embodiments of the invention provide compositions and methods to ensure that the toxic metal is directed to the desired cell or tissue. In one embodiment, the metal is bound to a sulfur-rich peptide or protein carrier containing a targeting moiety. Such metal-protein complex is targeted to the selected cells or tissues to enrich the cell or tissue site with the metal-containing peptide or protein molecules followed by administering a dithiocarbonyl which carries the metal from the protein inside the cells to induce cell death.
    • 公开了用于降低细胞,特别是异常非健康细胞,特别是癌细胞活力的组合物和方法。 造成细胞死亡的主要原因是毒性金属原子或离子。 本发明的实施方案提供了确保有毒金属被引导到期望的细胞或组织的组合物和方法。 在一个实施方案中,金属与含有靶向部分的富含硫的肽或蛋白载体结合。 这样的金属蛋白复合物被靶向所选择的细胞或组织,以用含金属的肽或蛋白质分子富集细胞或组织部位,然后施用携带来自细胞内的蛋白质的金属的二硫代羰基以诱导细胞死亡。
    • 10. 发明申请
    • COMPOSITIONS AND METHODS TO CONTROL ABNORMAL CELL GROWTH
    • 组合物和控制异常细胞生长的方法
    • US20100048668A1
    • 2010-02-25
    • US12572793
    • 2009-10-02
    • Zoltan Kiss
    • Zoltan Kiss
    • A61K31/382C07D335/08C07D345/00A61K31/33
    • C07D335/08C07D335/16
    • A class of compounds commonly containing a trialkylammonium group have been synthesized and characterized as anticancer compounds. They can be used alone or in combination with other therapies to treat cancer and other cell proliferative diseases. Representative compounds of this class, N,N-diethyl-N-methyl-2-[(9-oxo-9H-thioxanthen-2-yl)methoxy]ethanaminium iodide and N,N-diethyl-N-allyl-3-(2-methyl-9H-thioxanthen-9-ylidene)-propane-1-aminium bromide, were shown in various tumor models to decrease tumor volume, enhance the effects of other chemotherapeutic agents including cisplatin, reduce chemotherapy-induced loss of body weight, and increase survival of animals co-treated with toxic amounts of cisplatin. These compounds had even greater effects on tumor volume, body weight, and survival when administered together with the human protein placental alkaline phosphatase.
    • 通常含有三烷基铵基团的一类化合物已被合成并被表征为抗癌化合物。 它们可以单独使用或与其他疗法组合用于治疗癌症和其他细胞增殖性疾病。 该类的代表性化合物是N,N-二乙基-N-甲基-2 - [(9-氧代-9H-噻吨-2-基)甲氧基]乙胺碘化物和N,N-二乙基-N-烯丙基-3-( 2-甲基-9H-噻吨-9-亚基) - 丙烷-1-氨基溴化物,显示在各种肿瘤模型中,以减少肿瘤体积,增强其他化学治疗剂(包括顺铂)的作用,减少化疗引起的体重下降, 并增加用有毒量的顺铂共同处理的动物的存活。 当与人类蛋白质胎盘碱性磷酸酶一起施用时,这些化合物对肿瘤体积,体重和存活率具有更大的影响。