2-CYCLIC AMINO-2-(1,2-BENZISOXAZOL-3-YL)ACETIC ACID ESTER DERIVATIVES AND COMPOSITION CONTAINING THE SAME

摘要

2-Cyclic amino-2-[1,2-benzisoxazol-3-yl]acetic acid derivatives of the formula: …… (wherein R1 is hydrogen or a halogen atom, R2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the piperidine moiety is attached at its 3- or 4-position), and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia. The preferred compounds are …… and the 1-ethyl-1-methyl piperidinium iodide derivative thereof. …Compounds (I) may be made from Am-H and a 2-haloacetic acid derivative (whose synthesis is described). They can be selectively quaternised at the piperidine N-atom.