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US 5,175,284 AGranted
Tricyclic thienothiopyrans as pharmaceutical intermediates
AssigneeMerck & Co., Inc.
InventorsJohn J. Baldwin, Gerald S. Ponticello, Kenneth L. Shepard, Theresa M. Williams
Life of this patent
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Abstract
Intermediates are described for preparing conformationally constrained tricyclic thienothiopyran compounds that are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
Claims3
A compound of the formula:
- ##STR45## wherein R.sub.1 is H, unsubstituted or substituted lower alkyl, lower alkenyl, aryl or aralkyl wherein the aryl groups optionally are substituted;
- R.sub.2, R.sub.3, R.sub.5, R.sub.6 and R.sub.7 are independently H or alkyl or R.sub.2 and R.sub.3 together can be =0, R.sub.4 is H, lower alkyl, lower alkenyl or lower alkyl substituted by hydroxy, alkoxy, hydroxyalkoxy, lower alkenyloxy, alkoxyalkoxy, hydroxyalkoxyalkoxy, alkylamino, hydroxyalkylamino, alkoxyalkylamino, hydroxyalkoxyalkylamino, alkyl-S(O).sub.m -, hydroxyalkyl-S(O).sub.m -, alkoxyalkyl-S(O).sub.m -, hydroxyalkoxyalkyl-S(O).sub.m -, alkyl-S(O).sub.m -alkoxy, hydroxyalkylS(O).sub.m -alkoxy, alkyl-S(O).sub.m alkyl-S(O).sub.m and hydroxyalkyl-S(O).sub.m alkyl-S(O).sub.m ;
- and m and n are independently 0, 1, or 2.
Dependencies are inferred from the claim text.