1,7-substituted heptyne-2-ones

Details 1,7-substituted heptyne-2-ones 1,7-substituted heptyne-2-ones

C - Chemistry, Metallurgy

07

C

167/207, 260/295

C07C 225/18 (2006.01) C07D 213/50 (2006.01) C07D 295/10 (2006.01) C07D 295/104 (2006.01)

Patent

CA 1329197

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-2- one, 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 treatment of neurogenic bladder disorders and may be administered orally or parenterally in conventional formulations containing optional conventional additives such as binders, surfactants, emulsifiers, flavorants, preservatives and the like.

540630

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