1,7-substituted heptyne-2-ones

Abstract From the Canadian patent

1,7- SUBSTITUTED HEPTYNE-2-ONES, ABSTRACT OF THE DISCLOSURE 1-phenyl-1-hydroxy or fluoro-hept-5-yn-2-ones substituted with a C1 to C7 alkyl, C3 to C6 cycloalkyl aryl, heteroaryl or, heterocycloalkyl group at the 1-position and an amino a, dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2one, 1-cyclohexyl-1-phenyl-1-hydroxy-7-methylaminohept-5-yn-2-one and1-cyclohexyl-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one. The compounds are highly specific M1-AChR antagonists with relatively prolonged duration of activity. They are particularly useful in the …