2,3-dihydrobenzofuran-5-sulfonamide derivatives

Details 2,3-dihydrobenzofuran-5-sulfonamide derivatives 2,3-dihydrobenzofuran-5-sulfonamide derivatives

C - Chemistry, Metallurgy

07

D

167/245, 260/361

C07D 307/78 (2006.01) A61K 31/34 (2006.01) C07D 307/79 (2006.01) C07D 307/80 (2006.01) C07D 307/85 (2006.01) C07D 307/88 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 1265800

ABSTRACT The present invention relates to 2,3-dihydrobenzofuran- 5-sulfonamide derivatives represented by the following formula: Image and the pharmaceutically acceptable salts thereof, wherein R1 and R2, each is identically or differently hydrogen, lower alkyl, 4- to 7-membered cycloalkyl, phenyl substituted by halo or alkoxy, unsubstituted phenyl, phenyl(lower alkyl), lower alkoxycarbonyl, or morpholinyl(lower alkyl); or NR1R2 represents lower alkyl substituted or unsubstituted pyrrolidine, piperidine, or morpholino, R3 is a group represented by COR4 or CH2R5, R4 is hydroxy or a group represented by OR6 or NR7R8, R5 is hydroxy, lower alkoxy, lower aliphatic acyloxy, or halogen, R6 is lower alkyl, phenyl, tolyl, xylyl, carboxymethyl or a lower alkyl ester thereof, hydroxymethyl or a lower aliphatic acylate thereof, or 1-phthalidyl, R7 and R8, each is identically or differently hydrogen or lower alkyl, and X and X', each is identically or differently hydrogen or halogen. The compounds are highly effective diuretic antihypertensives acting as loop diuretics with less adverse side-effects and can be adminstered orally at a daily dosage of 0.5-200 mg or parenterally of 0.02-50 mg.

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