Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1989-11-16
1991-07-30
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514653, 514906, 514929, 514930, 514935, 564342, 564345, A61K 31135, C07C22518
Patent
active
050361074
ABSTRACT:
1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 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 which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.
The compounds are highly specific M.sub.1 -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.
REFERENCES:
patent: 2717895 (1955-09-01), Sprague et al.
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patent: 3176019 (1965-03-01), Campbell et al.
Burger, "Medicinal Chemistry", 3rd. Ed., Part I, p. 75 (1970).
The Merck Index, 10th Ed., p. 997, Section No. 6823 (1983).
Guzewska Maria E.
McPherson Daniel W.
Natalie, Jr. Kenneth J.
Rzeszotarski Waclaw J.
Spagnuolo Ciro J.
Gillis Theresa M.
Marion Merrell Dow Inc.
Raymond Richard L.
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