To obtain a new compound useful as an antagonist to a bradykinin for treating inflammations or cardiovascular diseases in mammals, especially humans.
This compound is represented by formula I [A1 and A2 are each a halogen; R1 and R2 are each a 1-4C alkyl; R3 is a (substituted)phenyl or naphthyl; Y is a 5-10C azacycloalkyl, a 6-10C diazabicycloalkyl or the like; R4 is a (substituted) 1-8C alkyl, a (substituted)amino, a (substituted) 2-6C alkanoyl or the like], e.g. (-)-(4S)-dimethyl 4-(2,6-dichlorophenyl)-2-[4-(8-methyl-8- azabicyclo[3.2.1]oct-3-yl)-1-piperazinyl]carbonylmethyl-6-(S)- phenylsulfinylmethyl-1,4-dihydropyridine-3,5-dicarboxylate ditosylate. The objective compound is obtained by carrying out the coupling reaction of, e.g. a compound represented by formula II with a compound represented by the formula Y-R4 in a solvent such as tetrahydrofuran at -30 to 40°C for 10 min to 96 hr.
KAWAMURA MITSUHIRO
KATSURA GIYOKUTEI
