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US 4,731,368 AGranted
Thienopyridine sulfonamides and their ophthalmological formulation
AssigneeMerck & Co., Inc.
InventorsJacob M. Hoffman, Jr., Kenneth L. Shepard
Life of this patent
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Abstract
Thienopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
Claims9
A compound of structural formula:
- ##STR11## or N-oxide, or an ophthalmologically acceptable salt thereof wherein ##STR12## is a pyrido, dihydropyrido or tetrahydropyrido group with the N at the 4-, 5-, 6- or 7-position;
- and
- R is
- (1) C.sub.1-5 alkyl, either straight chain, branched chain or cyclic,
- (2) hydroxy-C.sub.1-5 alkyl,
- (3) --OR.sup.1, wherein R.sup.1 is hydrogen, C.sub.1-3 alkyl, cyclopropyl, amino-C.sub.1-3 alkyl, C.sub.1-3 alkylamino-C.sub.1-3 alkyl, di(C.sub.1-3 alkyl)amino-C.sub.1-3 alkyl, hydroxy-C.sub.1-3 alkyl, or C.sub.2-4 alkanoyl,
- (4) ##STR13## alkyl, wherein n is 0, 1 or 2, (5) --N(R.sup.1).sub.2 wherein the R.sup.1 groups can be the same or different,
- (6) halo selected from the group consisting of chloro, bromo or fluoro,
- (7) hydrogen,
- (8) --NO.sub.2, or
- (9) oxo--;
- and if ##STR14## is dihydro- or tetrahydropyrido, the N can be substituted with R.sup.1 or CONH.sub.2.
9 more elements
Dependencies are inferred from the claim text.