PURPOSE: To obtain a new indoloylguanidine derivative having Na+/H+ exchange transport system-inhibitory action, and effective for organ disorders due to hypertension, arrhythmia, cardiomegaly, diabetes, ischemia or ischemic reperfusion, cerebroischemic disorders, diseases involved in hyperplasia, etc.
CONSTITUTION: This new compound, an indoloylguanidine derivative (or a medicinally permissible acid-added salt thereof) is expressed by formula I [R1 is H, an alkyl, alkenyl, cycloalkyl, halogen, nitro, etc., or of formula II (A is O, etc.; R' is H or an alkyl; the ring is a 3 to 8-membered saturated heterocycle); R2 is H, an alkyl, cycloalkyl, OH, alkoxyl or aromatic group], e.g. 7-(2-aminoethoxy)-4-chloro-1-methyl-2-indoloylguanidine. The compound of formula I is obtained, for example, by reaction of guanidine with a reactive derivative from an indolecarboxylic acid of formula III (X is an eliminable group easily substituent by a nucleophilic reagent) in an inert solvent.
NAKANO KAZUHIRO
YAGI HIDEKI
OHASHI NAOHITO
KOJIMA ATSUYUKI
NOGUCHI TAKESHI
MIYAGISHI AKIRA
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