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    • 6. 发明授权
    • Preparation method for perfluoroalkane sulfinate
    • 全氟烷基亚磺酸盐的制备方法
    • US09073828B2
    • 2015-07-07
    • US13574138
    • 2011-03-03
    • Takashi KashiwabaTsutomu NanmyoYoichi Takenaka
    • Takashi KashiwabaTsutomu NanmyoYoichi Takenaka
    • C07C313/04
    • C07C313/04
    • In a method for obtaining an alkali metal perfluoroalkanesulfinate by reacting a perfluoroalkanesulfonyl halide with a sulfur-containing reducing agent in the presence of water, a reaction liquid containing the alkali metal sulfinate obtained after the reaction is concentrated till a specific concentration, thereby inorganic salts, which are impurities in the solution, are precipitated and removed, and a filtrate after removing the inorganic salts is subjected to an operation such as concentration and drying, thereby obtaining the target alkali metal perfluorosulfinate with a high purity and a good operability. Furthermore, an organic solvent for extraction becomes unnecessary. Therefore, it is possible to greatly reduce wastes.
    • 在通过使全氟烷基磺酰卤与含硫还原剂在水的存在下反应来获得全氟烷基亚磺酸碱金属的方法中,将反应后得到的含有碱金属亚磺酸盐的反应液浓缩至特定浓度, 将溶液中的杂质析出除去,除去无机盐后的滤液进行浓缩干燥等操作,得到纯度高,操作性好的目标碱金属全氟亚磺酸酯。 此外,不需要用于萃取的有机溶剂。 因此,可以大大减少废物。
    • 10. 发明授权
    • Therapeutic compounds
    • 治疗化合物
    • US07030158B2
    • 2006-04-18
    • US10295139
    • 2002-11-15
    • Oleg StrelchenokJulian Aleksov
    • Oleg StrelchenokJulian Aleksov
    • C07C309/23C07C313/04A61K31/19A61K31/215
    • A61K31/185A61K31/337A61K45/06C07B2200/07C07B2200/09C07C309/18C07C313/04C07C2601/16A61K2300/00
    • A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.
    • 一组新化合物N-(全反式维甲酰基)-L-半胱氨酸,N-(13-顺 - 维甲酰基)-L-半胱氨酸,N-(全反式 - 维甲酰基)-L-半胱氨酸亚磺酸 ,N-(13-顺式 - 视黄酰基)-L-半胱氨酸亚磺酸,N-(全反式维甲酰基)-L-高半胱氨酸,N-(13-顺 - 维甲酰基)-L-高半胱氨酸和 这些化合物,包括它们的酯和酰胺的钠盐,显示出本身具有治疗效果,哪些化合物与细胞毒性化合物如多西紫杉醇,紫杉醇,多柔比星和米托蒽醌组合显示出协同效应。 这些化合物使得可以制备难溶性药物化合物的新制剂,并且本发明公开了制备这些化合物的水溶性制剂的方法,例如多西紫杉醇和紫杉醇,具有增强的药理活性,以及​​水溶性的制剂 药物以多柔比星和米托蒽醌为例,具有改善的疗效。