Fused imidazolium derivatives

Details Fused imidazolium derivatives Fused imidazolium derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/4184 (2006.01) A61K 31/4439 (2006.01) A61K 31/497 (2006.01) A61P 35/00 (2006.01) C07D 235/02 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2395717

This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof having the formula: Image The novel imidazolium derivatives fused with an aryl ring or heteroaryl ring, characterized in that the 1- and/or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of -OR a, -SR a, -prodrug-formed OH, -O-lower alkylene-OR a, -O-lower alkylene-O-lower alkylene-OR a, -O-lower alkylene-NR a R b, -O-lower alkylene-O-lower alkylene-NR a R b, -O-lower alkylene-NR c-lower alkylene-NR a R b, -OCO-NR a R b, -SOR a, -SO2R a, -SO2NR a R b, -NR a-SO2R b, -CO2H, -NR a R b, -NR c-lower alkylene-NR a R b, -N (-lower alkylene- NR a R b)2r, -RinD, -NO2, -CN, -halogen, -CO2R a, -COO-, -CONR a R b, -CONR a-O-R b, -NR a-COR b, -NR a-CO-NR b R c, -OCOR a and -CO-R a, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety.

L'invention concerne de nouveaux dérivés d'imidazolium fondus pouvant être utilisés comme médicaments, en particulier dans le traitement de cancers, ainsi que de nouveaux intermédiaires destinés à la préparation de ces dérivés. Les nouveaux dérivés d'imidazolium fondus avec des carbocycles ou des hétérocycles aromatiques et caractérisés par le fait qu'ils sont substitués en position 1 et/ou 3 avec alkyle portant -ORa, -SRa, ou autre substituant, présentent une excellente activité antitumorale et une faible toxicité, d'où leur utilité en tant que médicaments anticancéreux ayant de grandes marges de sécurité.

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