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US 4,285,938 AGranted
7,8-Dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine derivatives
AssigneeSmithKline Corporation
InventorFrancis R. Pfeiffer
Life of this patent
Estimating the term…
Abstract
New 7,8-dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines having pharmaceutical activity together with new intermediates and methods of synthesis for preparing them. The lead compound is 6-chloro-7,8-dihydroxy-1-(p-sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzaz epine which has very potent renal dopaminergic activity.
Claims17
A compound of the formula:
- ##STR9## in which:
- R.sub.1 is hydrogen, lower alkyl of 1-4 carbons or allyl;
- R.sub.2 is hydrogen, halo or lower alkyl of 1-4 carbons;
- R.sub.3 is hydrogen, or when R.sub.2 is other than hydrogen, halo or lower alkyl of 1-4 carbons;
- and
- R.sub.4 and R.sub.5 are hydrogen or lower alkyl of 1-4 carbons;
- together with pharmaceutically acceptable acid addition salts thereof.
4 more elements
A compound of the formula:
- ##STR10## in which:
- R.sub.1 ' is allyl, lower alkyl of 1-4 carbons, trichloroacetyl, benzyloxycarbonyl, trifluoroacetyl or benzyl;
- R.sub.2 is hydrogen, halo or lower alkyl of 1-4 carbons;
- R.sub.3 is hydrogen or, when R.sub.2 is other than hydrogen, halo or lower alkyl of 1-4 carbons;
- R.sub.6 and R.sub.7 are lower alkyl of 1-4 carbons or, when taken together, methylene or ethylene;
- and
- R.sub.8 is --SO.sub.3 H, --SO.sub.2 Cl, --SO.sub.2 Br, --S--CH.sub.2 C.sub.6 H.sub.5 or ##STR11## together with acid addition salts thereof acceptable for use as chemical intermediates.
4 more elements
Dependencies are inferred from the claim text.