To obtain a sulfonamide derivative excellent in inhibitory action on blood platelet aggregation, useful as a therapeutic agent for circulatory system diseases such as myocardial infarction, pulmonary embolism, peripheral arterial obstruction, cerebral thrombosis and cerebral infarction.
This compound is shown by formula I (Ar is an aromatic hydrocarbon; A' is an alkylene; R1 and R2 are each H, an alkoxycarbonyl, a heterocyclic group or R1 and R2 form a heterocyclic group with N; R3 is H or an alkyl) or its salt such as 4-[2-(4-chlorobenzenesulfonyl)amino-5-(3-aminopyridin-2-yl) amino-phenoxy]butyric acid. The compound of formula I is obtained by reacting a compound of formula II (R3a is an alkyl) with a sulfonating reagent of the formula, ArSO2X (X is a halogen) in a solvent (e.g. dioxane) in the presence of a base (e.g. pyridine) at 0-50°C for several minutes to 12 hours. The dose of the active ingredient is 1-300mg/kg/day orally or parenterally as an ointment or an injection.
INOUE TSUTOMU
MURATA MITSUSHIGE
NAKANO HIROYUKI
UMEZAWA ISAO
YOKOTA SHIZUAKI
YOSHIKAWA HIROE
SASAKI TOMOMITSU
YAJIMA YUMI
NAKAMURA HIROSHI
WATABE TAKAFUMI
FUJI YAKUHIN KK