New spasmolytic gastrointestinal motility regulators - are quat. ((1S,5S)-6,6-di:methyl:bi:cyclo (3,1,1)-hept-2-yl)-substd. N-(2-ethoxy-ethyl) morpholinium cpds.

摘要

Quat. morpholinium cpds. of formula (I) are new. In (I), Z is C or R1, R2, R3 are H, halo, lower alkyl or lower alkoxy.--R4, R5 are lower alkyl and X(-) is derived from a hydrogen halide acid or a lower alkyl or aromatic sulphonic acid. Also claimed is a method for preparing (I) from the corresp. morpholino cpd. and a tri-substd. benzyl cpd. of formula (ii). (I) is e.g. N-(2-bromo-4,5-dimethoxybenzyl)- N-(2-(dimethyl-(2-((1S,2S,5S)- 6,6-dimethylbicyclo (3,1,1) hept-2-yl)-ethyl)-silyl) -ethoxy)-ethyl)-morpholinium bromide (Ia). USE/ADVANTAGE - As spasmolytic gastrointestinal motility regulators. (I) are esp. useful for calming spasms that occur in the colon and cause symptoms such as nausea, cramp etc. Unit dose is 10-200 mg. In an example, in in vitro tests on isolated guinea pig ileums, the EC(50) of (IA) against acetylcholine-induced contractions was 8.0 x 10 power (-6) mol/l.