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    • 2. 发明授权
    • Conjugates of dithiocarbamates with pharmacologically active agents and uses therefor
    • 二硫代氨基甲酸酯与药理活性剂的结合物及其用途
    • US06407135B1
    • 2002-06-18
    • US09453608
    • 1999-12-03
    • Ching-San LaiTingmin Wang
    • Ching-San LaiTingmin Wang
    • C07D20704
    • C07C333/16
    • In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.
    • 根据本发明,提供了一氧化氮清除剂(例如二硫代氨基甲酸盐或“DC”)和药理活性剂(例如NSAID)的缀合物。 本发明共轭物提供了一类新的药理活性剂(例如抗炎剂),其由于通过改变如本文所述的药理学活性剂而赋予的保护作用,导致副作用的低得多的发生率。 此外,发明共轭物比未改性的药理活性剂更有效,因为与药理活性剂接触的细胞和组织被保护免受由于一氧化氮的共同产生而导致的一氧化氮过量产生的潜在的破坏性作用 除了游离的药理学活性剂之外,当发明结合物被切割时,清除剂(例如,二硫代氨基甲酸盐)。
    • 5. 发明授权
    • Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor
    • 二硫代氨基甲酸二硫化物与药理活性剂的结合物及其用途
    • US06274627B1
    • 2001-08-14
    • US09416619
    • 1999-10-12
    • Ching-San LaiVassil P. VassilevTingmin Wang
    • Ching-San LaiVassil P. VassilevTingmin Wang
    • A61K3116
    • A61K47/55
    • In accordance with the present invention, there are provided conjugates of physiologically compatible free radical scavengers (e.g., dithiocarbamate disulfides (DD)) and pharmacologically active agents (e.g., NSAIDS). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of free radical overproduction induced thereby as a result of the co-production of free radical scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.
    • 根据本发明,提供了生理上相容的自由基清除剂(例如二硫代氨基甲酸酯二硫化物(DD))和药理活性剂(例如NSAIDS)的缀合物。 本发明共轭物提供了一类新的药理活性剂(例如抗炎剂),其由于通过改变如本文所述的药理学活性剂而赋予的保护作用,导致副作用的低得多的发生率。 此外,发明共轭物比未改性的药理学活性剂更有效,因为与药理活性剂接触的细胞和组织被保护免受由此引起的自由基过度产生的潜在的破坏性作用,这是由于自由基的共同产生 除了游离的药理学活性剂之外,当发明结合物被切割时,清除剂(例如,二硫代氨基甲酸盐)。