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US 5,314,898 AGranted
Aryl thiopyrano[4,3,2-cd]indoles as inhibitors of leukotriene biosynthesis
AssigneesMerck & Co., Inc., Merck Frosst Canada, Inc.
InventorsJohn Y. L. Chung, Robert A. Reamer, Yves Girard, Pierre Hamel
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Abstract
Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
Claims3
A compound of the formula:
- ##STR10## wherein:
- R.sup.2 is H, C.sub.1 -C.sub.7 lower alkyl, hydroxy, or C.sub.1 -C.sub.7 lower alkoxy, or two R.sup.2 groups on adjacent carbon atoms may be a bond;
- R.sup.3 is H or lower alkyl;
- m is 0 to 3;
- n is 0 to 3;
- R.sup.4 is [phenyl(R.sup.10)2]t;
- R.sup.10 is H, C.sub.1 -C.sub.7 lower alkyl, or halogen;
- t is 1 or 2;
- Y is a bond, O or S;
- Q is --CO.sub.2 H or --CONHS(O).sub.2 R.sup.12 ;
- R.sup.12 is C.sub.1 -C.sub.7 lower alkyl, R.sup.10 -phenyl, CF.sub.3, NH.sub.2 or N(C.sub.1 -C.sub.7 lower alkyl).sub.2 ;
- Z is CHR.sup.20, CHWR.sup.6, or CO;
- R.sup.6 is H or C.sub.1 -C.sub.7 lower alkyl;
- R.sup.20 is H or C.sub.1 -C.sub.7 lower alkyl;
- W is O, S, or NR.sup.6 ;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.