Patent ID: 6734203
Filing Date: 2004-05-11
Classification: A61K,A61P,C07C,C07D

Abstract:
A fused imidazolium derivative represented by the following general formula (I) (wherein symbols in the formula have the following meanings;R1 and R2: the same or different from each other and each represents -(lower alkyl having one or more substituents selected from group B), -(lower alkenyl having one or more substituents selected from group B), -(lower alkynyl having one or more substituents selected from group B), -RinD, -lower alkyl, -lower alkenyl or -lower alkynyl, with the proviso that at least one of R1 and R2 is -(lower alkyl having one or more substituents selected from group B), -(lower alkenyl having one or more substituents selected from group B), -(lower alkynyl having one or more substituents selected from group B), -(cycloalkyl having one or more substituents) or -(five- to seven-membered saturated heterocyclic ring which may have one or more substituents), group B: â€”ORa, â€”SRa, -prodrug-formed OH, â€”O-lower alkylene-ORa, â€”O-lower alkylene-O-lower alkylene-ORa, â€”O-lower alkylene-NRaRb, â€”O-lower alkylene-O-lower alkylene-NRaRb, â€”O-lower alkylene-NRc-lower alkylene-NRaRb, â€”OCOâ€”NRaRb, â€”SORa, â€”SO2Ra, â€”SO2NRaRb, â€”NRaâ€”SO2Rb, â€”NRaRb, â€”NRc-lower alkylene-NRaRb, â€”N(-lower alkylene-NRaRb)2, -RinD, â€”NO2, â€”CN, -halogen, â€”CO2Ra, â€”COOâˆ’, â€”CONRaRb, â€”CONRaâ€”Oâ€”Rb, â€”NRaâ€”CORb, â€”NRaâ€”COâ€”NRbRc, â€”OCORa and â€”COâ€”Ra, Ra, Rb and Rc: the same or different from one another and each represents â€”H, -lower alkyl, -lower alkylene-RinD or -RinD, RinD: -(five- to seven-membered saturated heterocyclic ring which may have one or more substituents), -(cycloalkyl which may have one or more substituents), -(cycloalkenyl which may have one or more substituents), -(aryl which may have one or more substituents) or -(heteroaryl which may have one or more substituents), R3: â€”H or -(lower alkyl which may have one or more substituents), or R2 and R3 may together form a lower alkylene having from 2 to 5 carbon atoms which may be interrupted with O, S or NR4 (R4: â€”H or -lower alkyl), ring A: aryl ring which may have one or more substituents or heteroaryl ring which may have one or more substituents, and Xâˆ’: counter anion, with the proviso that Xâˆ’ does not exist when the substituent â€”COOâˆ’ of the group B forms intramolecular salt with imidazolium cation, with the proviso that compounds having the following combinations of R1 and R2 are excluded: (1) one is -lower alkylene-(aryl which may have one or more substituents) and the other is â€”CH3, â€”(CH2)3CH3 or -phenyl, (2) one is -lower alkylene-CO-(aryl which may have one or more substituents) and the other is â€”CH2CH(CH3)2 or â€”(CH2)3CH3, or (3) R1 and R2 are both -benzyl, â€”(CH2)2OC2H5 or â€”(CH2)2Oâ€”COCH3.