Furobenzisoxazole derivatives

Details Furobenzisoxazole derivatives Furobenzisoxazole derivatives

1986-05-06

1988-12-13

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548241, 549 60, 549467, 549468, 514379, C07D49804, A61K 3142

Patent

active

047912090

ABSTRACT:
Novel furobenzisoxazole derivatives of the formula (I): ##STR1## (wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R.sub.5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a --CH.dbd.CH-- group), as well as intoxic salts thereof when R.sub.5 is a carboxyl group, and process for preparing the same are disclosed.
The derivatives of formula (I) and nontoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence ae useful as therapeutics for treating hyperuricemia, edema and hypertension.

REFERENCES:
patent: 4456612 (1984-06-01), Plattner et al.
patent: 4490384 (1984-12-01), Plattner et al.
patent: 4732906 (1988-03-01), Koga et al.
Plattner et al, "Substitutes 5,6-Dihydrofuro[3,2-f]-1,2-Benzisoxazole-6-Carboxylic Acids: High-Ceiling Diuretics with Uricosuric Activity", J. Med. Chem., 1984, 27, pp. 1016 to 1026.
Gregary M. Shutske et al., J. Med. Chem., 25, 36-44 (1982).

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