US 5,308,842 AGranted

Tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds

AssigneeMerck & Co., Inc.

InventorsJohn J. Baldwin, Gerald S. Ponticello

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Abstract

Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith. The compounds are of general structure ##STR1##

Claims5

Dependent claims

A compound of structural formula:

##STR34## or an ophthalmologically acceptable salt thereof, wherein:
Y is --H or ##STR35## R is hydrogen or C.sub.1-3 alkyl;
R.sup.1 is
1) hydrogen,
2) C.sub.1-6 alkyl either unsubstituted or substituted with F, OH, C.sub.1-5 alkyl-S(O).sub.m, or C.sub.1-5 alkoxy;
3) C.sub.2-5 alkenyl;
4) phenyl or phenyl-C.sub.1-3 alkyl, where the phenyls are unsubstituted or substituted with C.sub.1-3 alkyl, C.sub.1, Br, F, CF.sub.3, OH or C.sub.1-3 alkoxy;
R.sup.2, R.sup.3 and R.sup.5 are independently hydrogen or C.sub.1-4 alkyl;
R.sup.6 is
(a) H,
(b) C.sub.1-4 alkyl,
(c) C.sub.2-4 alkenyl
(d) C.sub.1-4 alkyl substituted with
(1) hydroxy,
(2) C.sub.1-4 alkoxy,
(3) hydroxy-C.sub.1-4 alkoxy,
(4) C.sub.2-4 alkenyloxy,
(5) C.sub.1-4 -alkoxy-C.sub.1-4 alkoxy,
(6) hydroxy-C.sub.1-4 alkoxy-C.sub.1-4 -alkoxy,
(7) C.sub.1-4 alkylamino,
(8) di(C.sub.1-4 alkyl)amino,
(9) hydroxy-C.sub.1-4 alkylamino,
(10) C.sub.1-3 alkoxy-C.sub.1-4 alkylamino,
(11) hydroxy-C.sub.1-4 alkoxy-C.sub.1-4 alkylamino,
(12) C.sub.1-4 alkyl-S(O).sub.m -,
(13) hydroxy-C.sub.1-4 alkyl-S(O).sub.m,
(14) C.sub.1-4 alkoxy-C.sub.1-4 alkyl-S(O)m-,
(15) hydroxy-C.sub.1-4 alkoxy-C.sub.1-4 alkyl-S(O).sub.m -,
(16) C.sub.1-4 -alkyl-S(O).sub.m -C.sub.1-4 alkoxy,
(17) hydroxy-C.sub.1-4 -alkyl-S(O).sub.m -C.sub.1-4 alkoxy,
(18) C.sub.1-4 alkyl-S(O)m-C.sub.1-4 alkyl-S(O).sub.m,
(19) hydroxy-C.sub.1-4 alkyl-S(O)m-C.sub.1-4 alkyl-S(O)m or
(20) morpholino;
R.sup.7 and R.sup.8 are each hydrogen or together represent=O;
X is --S(O).sub.2 -- or --C(O)--;
m, is independently 0, 1 or 2;
and p is 0 or 1.

34 more elements

Dependencies are inferred from the claim text.

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Abstract