PURPOSE: To obtain a stimulant, containing a 2(1H)-quinolone-3-carboxylic acid derivative (salt) as an active ingredient and effective against alimentary diseases such as pyrosis, anorexia, epigastralgia or feeling of abdominal distension or regurgitant esophagitis, pseudoileus and constipation, etc.
CONSTITUTION: This stimulant contains a derivative (salt) of formula I (X is 0 or imino; R is H or a 1-6C alkyl), e.g., endo-N-(8-methyl-8-azabicyclo[3.2.1] oct-3-yl)-1-isopropyl-4-hydroxy-2-oxo-1,2-dihydro-3-quinoxalinecarboxamide as an active ingredient. The derivative (X is 0) is obtained by N-isopropylating isatonic acid anhydride of formula II, providing a compound of formula III, then reacting the resultant compound of formula III with malonic acid (derivative) in the presence of a base, affording a compound of formula IV and further reacting the prepared compound of formula IV (or its reactive derivative) with a tropine derivative of formula V.
SUZUKI MASATOSHI
ASANUMA HAJIME
YOKOMORI SADAKAZU
HATAYAMA KATSUO
ISOBE YOSHIHIKO
KIJIMA HARUKO
MURAMATSU MAKOTO
Next Patent: ANTAGONISTIC AGENT FOR CHOLECYSTOKININ-B/GASTRIN RECEPTOR