Conjugates of dithiocarbamates with pharmacologically active...

C - Chemistry – Metallurgy – 07 – C

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C07C 333/04 (2006.01) A61K 31/27 (2006.01) A61K 31/40 (2006.01) A61K 38/00 (2006.01) A61K 45/00 (2006.01) A61P 43/00 (2006.01) C07C 333/02 (2006.01) C07C 333/06 (2006.01) C07C 333/08 (2006.01) C07D 207/04 (2006.01) C07D 207/30 (2006.01)

Patent

CA 2292478

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.

L'invention concerne des conjugués d'accepteurs de monoxyde d'azote (dithiocarbamates ou "DC", par exemple) et des agents pharmacologiquement actifs (AINS, par exemple). Les conjugués de l'invention donnent une nouvelle catégorie d'agents pharmacologiquement actifs (agents anti-inflammatoires, par exemple) qui ont une incidence d'effets secondaires beaucoup moindre en raison de l'effet de protection produit par la modification de ces agents pharmacologiquement actifs. En outre, les conjugués de l'invention sont plus efficaces que les agents pharmacologiquement actifs puisse que des cellules ou des tissus placés au contact desdits agents sont protégés contre les effets potentiellement détériorants de la surproduction de monoxyde d'azote ainsi induite par la coproduction d'accepteurs de monoxyde d'azote (des dithiocarbamates, par exemple), à laquelle s'ajoute celle d'un agent libre pharmacologiquement actif lorsque le conjugué est clivé.

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