New heterocyclyl-alkynyl N-(hetero)aryl (thio)carbamate cpds. - useful in treating Alzheimer's disease, senile dementia, cognitive disorders and glaucoma and to improve memory

摘要

Heterocyclyl-alkynyl -N-(hetero)aryl-(thio)carbamates (I) and their salts and quat. cpds. are new: R1 = Ph opt. substd. by 1` or more halo or CF3; pyridyl opt. substd. by 1 or more halo or thienyl opt. substd. by halo; R2 = H or Me; X = Y = O; or X = S and Y = O or S; n = 3.5. (I) are also acetylcholine esterase inhibitors. Quat. cpds. are esp. suitable for topical application e.g. to treat glaucoma. Single doses are 1-100 mg. USE/ADVANTAGE - (I) are selective muscarine M1 receptor agonists useful in treating Alzheimer's disease, senile dementia and cognitive disorders and in improving memory. (I) do not have the side effects, e.g. salivation, bronchoconstriction and bradycardia, associated with prior art cpds. such as (4-(N-(3-chlorophenyl)carbamoyloxy)-2-butynyl)trimethylammonium chloride (McN-A-343).