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US 4,788,192 AGranted
2-Sulfamoylbenzo(b)thiophene derivatives pharmaceutical compositions and use
AssigneeMerck & Co., Inc.
InventorsKenneth L. Shepard, Samuel L. Graham
Life of this patent
Estimating the term…
Abstract
Novel 2-sulfamoylbenzo[b]thiopenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
Claims9
A compound of structural formula:
- ##STR40## or an ophthalmologically or pharmaceutically acceptable salt thereof, wherein:
- X is hydrogen, chloro, bromo or fluoro, C.sub.1-3 alkyl, hydroxy or C.sub.1-3 alkoxy;
- and
- R is:
- ##STR41## wherein R.sup.5 and R.sup.6 are independently:
- (a) hydrogen,
- (b) C.sub.1-18 alkyl, either straight or branched chain,
- (c) C.sub.3-6 cycloalkyl,
- (d) C.sub.3-6 cycloalkyl-C.sub.1-3 alkyl,
- (e) aryl-C.sub.1-3 alkyl wherein the aryl group is phenyl or naphthyl and is either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C.sub.1-3 alkyl or C.sub.1-3 alkoxy,
- (f) ##STR42## wherein R.sup.7 is (i) C.sub.1-18 alkyl, either straight or branched chain,
- (ii) aryl as previously defined, either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C.sub.1-3 alkyl, or C.sub.1-3 alkoxy,
- (iii) aryl-C.sub.1-3 alkyl wherein the aryl group is as previously defined and is either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C.sub.1-3 alkyl or C.sub.1-3 alkoxy,
- (iv) amino-C.sub.1-18 alkyl either straight or branched chain;
- or
- (g) R.sup.5 and R.sup.6 if lower alkyl, are joined together directly or through a heteroatom selected from O or N to form a 5 or 6-membered heterocycle selected from pyrrolidine, piperidine, morpholine, and piperazine.
13 more elements
Dependencies are inferred from the claim text.