| 摘要 |
PROBLEM TO BE SOLVED: To reduce the intraocular pressure of mammals and treat especially glaucauma and ischemic retinopathy by administering a piperazinyl-heterocyclic compound. SOLUTION: A compound represented by formula I [Ar is benzisothiazolyl, quinolyl or the like; (n) is 1 or 2; X and Y, together with phenyl to which both are added, form quinolyl, 2-hydroxyquinolyl or the like], e.g. 6- 2-[4-(1-naphthyl) piperazinyl]ethyl}-benzoxazolone hydrochloride is administered. The compound represented by formula I is obtained by reacting a compound represented by formula II with a compound represented by formula III (Hal is fluoro, chloro or the like) in the presence of a weak base (e.g. triethylamine) preferably in a polar solvent at a refluxing temperature of the solvent or in the presence of a catalytic amount of sodium iodide and in the presence of a neutralizing agent for hydrogen chloride such as sodium carbonate. When the compound represented by formula I is used for a human patient to treat glaucoma or ischemic retinopathy, the daily dose thereof is preferably 0.025-20 mg.
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