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|Title:||Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use|
|Abstract:||Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.|
|Inventor(s):||Baldwin; John J. (Gwynedd Valley, PA), Ponticello; Gerald S. (Lansdale, PA), Christy; Marcia E. (Collegeville, PA)|
|Assignee:||Merck & Co., Inc. (Rahway, NJ)|
|Filing Date:||Jun 15, 1988|
|Claims:||1. A compound of structural formula: ##STR27## the individual diastereomers, the individual enantiomers or mixtures thereof, or a ophthalmologically acceptable salt thereof, wherein: |
X is --S--, --SO--, or --SO.sub.2 --;
Y is --S--,
m is 1;
(b) phenyl either unsubstituted or substituted with one or more of
(2) C.sub.1-3 alkoxy,
(3) R.sup.17 R.sup.18 N-C.sub.1-5 alkyl, wherein R.sup.17 and R.sup.18 are independently selected from:
(i) hydrogen or
(ii) C.sub.1-5 alkyl, or taken together with the nitrogen to which they are attached form a heterocycle selected from morpholine, piperidine, pyrrolidine, and piperazine,
(d) .dbd.O; or
(e) --NR.sup.17 R.sup.18
(d) NR.sup.17 R.sup.18
(e) --C.sub.1-5 alkyl
(f) R.sup.17 R.sup.18 N-C.sub.1-3 alkyl
(g) phenyl-C.sub.1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of
(2) C.sub.1-3 alkoxy, or
(a) hydrogen, or
(b) C.sub.1-5 alkyl;
R.sup.15 and R.sup.16 are alkyl groups joined together to form a spirocycle of 3-7 members.
2. An ophthalmological formulation for the treatment of ocular hypertension comprising an ophthalmologically acceptable carrier and an effective ocular antihypertensive amount of a compound of claim 1.
3. A method of treating elevated intraocular pressure comprising the administration to a patient in need of such treatment of an effective intraocular pressure lowering amount of the compound of claim 1.
4. A method of treating ocular hypertension comprising topical ocular administration to a patient in need of such treatment of an effective ocular antihypertensive amount of a compound of claim 1.