PHENYLETHYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF MELANOMA
    7.
    发明申请
    PHENYLETHYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF MELANOMA 审中-公开
    苯乙烯衍生物及其在治疗梅毒中的应用

    公开(公告)号:WO02008174A1

    公开(公告)日:2002-01-31

    申请号:PCT/GB2001/003339

    申请日:2001-07-25

    摘要: Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, R is hydrogen or -COOR , R is hydrogen or C1-6 alkyl; R and R independently represent hydrogen and hydroxy, R is hydrogen, C1- 4 alkyl or halogen, X is -CHOH-, -CH2-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and -ODrug, -NHDrug and -N(Drug)2 each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells. The invention allows a greater amount of active agent to be used while reducing systemic side effects.

    摘要翻译: 提供了可用于治疗黑素瘤的新型单 - 和二羟基苯乙胺衍生物,其具有式(Ia,Ib或Ic)。 在上式中,R a是氢或-COOR b,R b是氢或C 1-6烷基; R e和R e独立地表示氢和羟基,R f是氢,C 1-4烷基或卤素,X是-CHOH-,-CH 2 - 氧或硫,m是0或1,W是 氧或硫,以及 - 药物,-NHDrug和-N(药物)2各自表示治疗活性剂的残基。 上述化合物是在由宿主黑素瘤细胞表达的酶代谢之前无活性的前药。 本发明允许使用更大量的活性剂,同时减少全身副作用。

    CONJUGATES OF DITHIOCARBAMATES WITH PHARMACOLOGICALLY ACTIVE AGENTS AND USES THEREFOR
    10.
    发明申请
    CONJUGATES OF DITHIOCARBAMATES WITH PHARMACOLOGICALLY ACTIVE AGENTS AND USES THEREFOR 审中-公开
    药理学活性药物与其用途的联合

    公开(公告)号:WO98055453A1

    公开(公告)日:1998-12-10

    申请号:PCT/US1998/010295

    申请日:1998-05-19

    CPC分类号: C07C333/16

    摘要: 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.

    摘要翻译: 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),其由于通过修饰如本文所述的药理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,发明偶联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作用 当发明结合物被切割时,除游离药理学活性剂外,清除剂(例如二硫代氨基甲酸盐)。