Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-01-25
1991-12-31
Shah, Mukund J.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
544337, 544405, 544406, 546 23, 546153, 546159, C07D21548, C07D40106
Patent
active
050774107
ABSTRACT:
The present invention relates to intermediate compounds to produce novel 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites.
The present invention is based on two characters. One is the selection of acyl substituents of 2,3-dihydro-4(1H)-quinolinone at 1-position, namely propionyl, t-butylcarbonyl, benzoyl, 2-bromobenzoyl, 4-chlorobenzoyl, 2-methylbenzoyl, 2-ethylbenzoyl, 2,3-dimethoxybenzoyl, 2,4-dichlorobenzoyl, 4-chloro-2-methyl benzoyl or 2-chloro-4-nitrobenzoyl. The other is the selection of substituents and positional specificity at 6- or 7-position, namely halogen atom, methoxy, trifluoromethyl or dimethylamino group.
1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives which are made from the intermediate compounds of the present invention have potent hypotensive, antioedematous and diuretic effect as well as an activity to remove ascites, and are extremely useful for the treatment of diseases and disorders mentioned above.
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Haga Akinori
Kato Kazuo
Mochida Ei
Tokunaga Hiroki
Uemura Akio
Bernhardt E.
Hodogaya Chemical Co. Ltd.
Mochida Pharmaceutical Co. Ltd.
Shah Mukund J.
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