PURPOSE: To provide a new compd. having an anti-hyperalgesic effect and useful for the treatment for ache.
CONSTITUTION: This compd. is expressed by formula I, wherein X is oxy, thio, sulfinyl, methylene, etc.; Y is carbonyl, methylene; R1 is H, a halogen, trifluoromethyl, nitro, cyano, OH, 1 to 4C alkyl, etc.; m, n are 1 or 2; A1 is 1 to 4C alkylene, 3 to 4C alkenylene, etc.; Het is 5 or 6-member heteroaryl having up to two N, O, S heteroatoms; G is carboxy, 1H-tetrazol-5-yl, etc. The compd. is, for example, 5-(8-trifluoromethyl-10,11-dihydrodibenzo[b, f][1,4]oxyazepin-10-ylmethyl)thiophene-2-carboxylic acid. The compd. of formula I is obtd. by coupling a compd. expressed by formula II and a compd. expressed by formula III (Z is a group which can be removed), and if necessary, removing the protecting group, and then reducing.
JIYON OORUDOFUIIRUDO
Next Patent: PRODUCTION OF 4-SUBSTITUTED BENZYL-2-(N-SUBSTITUTED HEXAHYDROAZEPINYL)-1(2H)-PHTHALAZINONE DERIVATIV...