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US 3,953,476 AGranted
3-Amino-5-sulfonylbenzoic acids
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Life of this patent
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Abstract
Aminobenzoic acids of the structure ##SPC1## Having saluretic and diuretic properties are described. These compounds are prepared by amidation of a 2-halo analog thereof or by alkylation of the free amino compound.
Claims6
An aminobenzoic acid having the structure:
- ##SPC8##
- wherein Y is selected from the group consisting of (1) halo, (2) trifluoromethyl and (3) C.sub.1-3 alkyl;
- R is selected from the group consisting of (1) lower alkyl;
- (2) halo-lower alkyl, (3) phenyl-C.sub.1-3 alkyl, (4) (monosubstituted-phenyl)-C.sub.1-3 alkyl wherein the substituent is selected from lower alkyl, lower alkoxy and halo;
- R.sub.1 is selected from the group consisting of (1) phenyl-C.sub.1-3 alkyl, (2) (monosubstitutedphenyl)-C.sub.1-3 alkyl wherein the substituent is selected from halo, C.sub.1-3 alkyl and C.sub.1-3 alkoxy, (3) naphthyl-C.sub.1-3 alkyl, (4) furyl-C.sub.1-3 alkyl, (5) carboxyfuryl-C.sub.1-3 alkyl, (6) thienyl-C.sub.1-3 alkyl, (7) halo-C.sub.1-3 alkyl, (8) hydroxy-C.sub.1-3 alkyl, (9) di-C.sub.1-3 alkylamino-C.sub.1-3 alkyl, and (10) C.sub.3-6 cycloalkyl-C.sub.1-3 alkyl and R.sub.2 is selected from the group consisting of (1) hydroxy and its pharmaceutically acceptable salts, and (2) OR.sup.3 wherein R.sup.3 is C.sub.1-5 alkyl and di-C.sub.1-3 alkylamino-C.sub.1-3 alkyl.
2 more elements
Dependencies are inferred from the claim text.