Patent ID: 6686345
Filing Date: 2004-02-03
Classification: A61K,C07D

Abstract:
A chemical compound comprising an iminium ion of an aza-derivative having the structure:R4R3C&boxH;NR1R2 wherein R1 is â€”CH2Câ‰¡CH and R4 is â€”Câ‰¡Câ€”C6H5, â€”Câ‰¡Câ€”C6H4(CF3), â€”Câ‰¡Câ€”C6H4(OCH3), â€”Câ‰¡Câ€”C6H3(OCH3)2, â€”Câ‰¡Câ€”C6H2(OCH3)3, â€”Câ‰¡Câ€”C6H5(Si(CH3)), or â€”Câ‰¡Câ€”C6H5(Si(CH(CH3)2); wherein R2 is a substituted-ethynyl group having the structure â€”Câ‰¡Câ€”R5, a substituted-allenyl group having the structure â€”CR5&boxH;C&boxH;CR6R7, a substituted-propargyl group having the structure â€”CR5R6â€”Câ‰¡Câ€”R7, hydrogen, alkyl, phenyl, aryl, aryl (C1-C4) alkyl, or a heterocycle substituent; wherein in each instance R5, R6, and R7 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkyl carbonyl, alkoxy carbonyl, silyl, phenyl, aryl, aryl (C1-C4) alkyl, hydroxy alkyl, a substituted hydroxyalkyl, an alkyl carboxylic acid derivative, an alkenyl carboxylic acid derivative, a nucleic acid interactive compound, a phosphine oxide, a sulfoxide, a sulfone, a heterocycle substituent, a carbocyclic substituent, one or more aza-derivatives, or where R5, R6, and R7 can join with themselves or each other to form a 9-26 membered ring; and wherein R3 is â€”SR8, â€”NR8R9, or â€”CR8R9, wherein in each instance R8 and R9 are independently a hydrogen, alkyl, phenyl, aryl, aryl (C1-C4) alkyl, trifluoromethylsulfonyl, silyl, substituted-ethynyl, substituted-allenyl, substituted propargyl, a sugar, a C-glycoside, a nucleic acid interactive compound, or a heterocycle substituent; wherein R2 and R3 along with parent iminium combine to form a pyridinium ring; and wherein said compound is associated with a counter ion; or a pharmaceutical composition thereof.