Trifunctional agents useful as irreversible inhibitors of A1-adenosine receptors

摘要

Trifunctional agents useful as inhibitors of A1-Adenosine receptors may be formulated into pharmaceutical compositions. These agents are represented by formula (I): <IMAGE> +TR <IMAGE> wherein X is CH or N, R is an isothiocyanate group, an amino group or -NHCO2C(CH3)3 and R1 is hydrogen, carboxyl, lower alkoxycarbonyl, aminocarbonyl, <IMAGE> lower alkyl, optionally substituted with: -OH, -COOH, lower ester of COOH, carboxamide, NHCOCH3, NHCOCH2Br, halo, dimethylamino, triethylammonium, NHCONH2, SO2NH2, -SO3H, or a reporter group, particularly a spectroscopic reporter group such as a fluorescent dye, photoaffinity probe, or spin label probe, coupled through an amide, sulfonamide, amine or thiourea linkage, biotinylamino- (optionally containing an epsilon -aminocaproyl spacer chain or similar spacer chain) or; R1 is CONH-R2 or NHCSNH-R2, wherein R2 is lower alkyl, optionally substituted with: -OH, -COOH, lower ester of COOH, carboxamide, NHCOCH3, NHCOCH2Br, halo, dimethylamino, triethylammonium, NHCONH2, SO2NH2, -SO3H, or a reporter group, particularly a spectroscopic reporter group such as a fluorescent dye, photoaffinity probe, or spin label probe, coupled through an amide, sulfonamide, amine, or thiourea linkage, biotinylamino- (optionally containing an epsilon -aminocaproyl spacer chain or similar spacer chain).