3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, a

Details 3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, a 3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, a

1984-10-09

1986-11-04

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514422, 514433, 546274, 548525, 549 54, A61K 3134, A61K 3138, C07D33364, C07D40112

Patent

active

046210911

ABSTRACT:
3-hydroxybenzo[b]thiophene-2-sulfide derivatives have been prepared by ring closure of an appropriately substituted 2--R.sup.1 SCH.sub.2 S-- benzoic acid ester in the presence of a strong base. These compounds have been found to be specific inhibitors of 5-lipoxygenase and thereby useful in the treatment of inflammation, pain and fever associated with inflammation, arthritic conditions, asthma, allergic disorders such as allergic rhinitis and chronic bronchitis, skin diseases like psoriasis and atopic exzema, cardiovascular or vascular disorders, and other leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.

REFERENCES:
patent: 3594478 (1971-07-01), Brandstrom et al.
Goodman et al, The Pharmaceutical Basis of Therapeutics, Sixth Ed., Macmillan Publ. Co., New York, NY 1980, pp. 28 and 33.

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