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22 条记录 (耗时 0.013 秒)

    CONJUGATES OF DITHIOCARBAMATES WITH PHARMACOLOGICALLY ACTIVE AGENTS AND USES THEREFOR
    3.
    发明公开
    CONJUGATES OF DITHIOCARBAMATES WITH PHARMACOLOGICALLY ACTIVE AGENTS AND USES THEREFOR 失效
    二硫代氨基甲缀合物活性药剂及其用途

    公开(公告)号：EP1001932A1

    公开(公告)日：2000-05-24

    申请号：EP98923563.5

    申请日：1998-05-19

    申请人： Medinox, Inc.

    发明人： LAI, Ching-San

    IPC分类号： C07C333/04 ,  C07C333/06 ,  C07C333/08 ,  C07D207/04 ,  C07D207/30 ,  A61K31/27 ,  A61K31/40

    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.

    COMBINATIONAL THERAPEUTIC METHODS EMPLOYING NITRIC OXIDE SCAVENGERS
    10.
    发明公开
    COMBINATIONAL THERAPEUTIC METHODS EMPLOYING NITRIC OXIDE SCAVENGERS 失效
    组合使用中医药STIKOXYDFÄNGERN

    公开(公告)号：EP0866695A1

    公开(公告)日：1998-09-30

    申请号：EP96939670.0

    申请日：1996-11-12

    申请人： Medinox, Inc.

    发明人： LAI, Ching-San

    IPC分类号： A61K38 ,  A61K31 ,  A61K39 ,  A61K45

    CPC分类号： A61K45/06

    摘要： In accordance with the present invention, there are provided combinational therapeutic methods for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .No synthase expression. In contrast to the inhibitory approach described in the prior art (i.e., wherein the function of the enzymes responsible for nitric oxide production is inhibited), the present invention employs a combination of inactivation (or inhibition) and scavenging approach whereby the stimulus of nitric oxide synthase expression is inactivated, or the production thereof is inhibited, and overproduced nitric oxide is bound in vivo to a suitable nitric oxide scavenger. The resulting complexes render the stimulus of nitric oxide synthase expression inactive (or inhibit the production thereof), and nitric oxide harmless. The resulting complexes are eventually excreted in the urine of the host. Further in accordance with the present invention, there are provided compositions and formulations useful for carrying out the above-described methods.