SOFT ANTICHOLINERGIC AGENTS EXHIBITING ANTI-SECRETORY ACTIVITY

摘要

The invention is concerned with novel pharmaceutically active compounds of the formula: (I) or (II) wherein: represents a tertiaxy amine: represents an unsaturated amine; R2, R3 and R4, which may be the same or different, each represents a hydrogen atom; a C1-C8 open chain alkyl group or cycloalkyl or cycloalkenyl group having up to 8 carbons; an alkoxyalkyl group having up to 8 carbon atoms; an acyloxyalkyl group having up to 8 carbon atoms; a C1-C8 haloalkyl group; a carboxyalkyl group having up to 8 carbon atoms; an alkenylphenyl group wherein the alkenyl portion contains up to 8 carbon atoms; an aryl group; a substituted aryl group whose substituent are selected from the group consisting of a halogen atom, an O-lower alkyl (C1-C4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; a -CH2OCOR1 qroup in which R1 is as defuned below; a -OH group; a halogen atom; a -OCOR1 group in which R1 is as defined below; or a -ONO2 group; with the proviso that at least two of the R2, R3 or R4 substitutients must be a substituent other than a hydrogen atom; with the further proviso that at least one of the R2, R3 and R4 substituents which is other than hydrogen must also be other than alkyl, alkoxyalkyl, acyloxyalkyl, haloalkyl, carboxyalkyl or halogen; and with the yet further proviso that R2, R3 and R4 taken together must contain at least 5 carbon atoms; or R2, R3 and R4, together with the .alpha.-carbon atom to which they are attached may form a fused polycarbocyclic ring or a polyheterocyclic ring; R1 represents any member defined by R2, R3 or R4 above; X represents -O- or -S-; and Y represents a halogen atom or any other organic or inorganic monovalent equivalent anion. The compounds of the invention are characterized as having excellent anticholinergic antisecretory activity, while exhibiting low toxicity following therapeutic application.