BENZISOXAZOLE DERIVATIVES

摘要

of the Disclorure: Novel benzisoxazole compounds of the formula: wherein R1 and R2 are each hydrogen, C1-4 alkyl, C1-4 alkoxy, halogon or trifluoromethyl or, when taken together, they form C1-2 alkylenedioxy; Alk is C1-4 alkylene and A is a group of the formula: or (wherein R3 and R4 are each C1-4 alkyl, phenyl or phenyl substituted with C1-4 alkyl, C1-4 alkoxy or halogen, or when taken together with the adjacent nitrogen atom, they represent a hetorocyclic ring having 5 to 7 members wherein one nitrogen atom is included as the only hetero atom or having six members wherein one nitrogen atom and one oxygen atom are included as the only hetero atoms; and R5 is C1-4 alkyl, phenyl or phenyl substituted with C1-4 alkyl, C1-4 alkoxy or halogen and their non-toxic salts. The compounds can be produced by cyclization of the corresponding o-substituted nitrobenzenes of the formula: wherein Z is or (wherein R6 is C1-4 alkyl) and R1, R2, Alk and A are each as defined above. The compounds have a variety of pharmacological activities such as CNS depressing, muscle relaxing, vasodilating, bronchodilating, anti-asthmatic, spasmogenic, analgesic, anti-narcotic, antiarrhythmic, local anesthetic and anti-platelet aggregation activities. - ?