Abstract: Medicarpin derivatives and related pharmaceutical compositions and methods of treatment are disclosed. The compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, they are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: A water-soluble combination of sodium sulindac and an appropriate base, for example, tromethamine or sodium bicarbonate, has been found to exhibit unexpectedly improved onset of activity relative to conventional water-soluble formulations containing sodium sulindac.

Abstract: Tetrazolyl derivatives of .beta.-lactams are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: 2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.

Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.

Abstract: New substituted azetidinones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: 3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.

Abstract: Indene derivatives have been found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.

Abstract: 3',6-Diisopentenyl-2',4'-dihydroxy-5,7-dimethoxyisoflavan has been isolated from Glycyrrhiza uralensis Fisch. It has been found that this compound and other related compounds are potent stimulators of benzodiazepine receptors and thereby useful as effective anxiolytic agents. Furthermore, these compounds have been found to be potent antidotes of avermectin.

Abstract: Substituted cephalosporins are found to be potent elastase inhibitors and thereby useful antiinflammatory/antidegenerative agents.

Abstract: Racemic mixture of derivatives of 5-(1-methyl-5-methylthiopyrrol-2-oyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole -2-carboxylic acid and analogs were resolved into pure l- or d-isomers via concomitant isomerization and functional crystallization.

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.

Abstract: [(2-Hydroxy-5-alkoxyphenyl)methylthio]phenylmethanol and derivatives thereof were prepared from an appropriate 2-hydroxy-5-alkoxybenzaldehyde with a hydroxymethylthiophenol. These compounds were found to be potent anti-inflammatory agents.

Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

Abstract: Hydroxybenzylamino derivatives have been prepared from an appropriate hydroxybenzaldehyde and an amine followed by reduction. These compounds are found to be active topical anti-inflammatory agents.

Abstract: Substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs such as the substituted 6-hydroxy-2,3-dihydrobenzopyrans were prepared from an appropriately substituted (5-hydroxy-2,3-dihydrobenzofuran-6-yl) formaldehyde or analog thereof with an aryl amine followed by reduction. These compounds were found to be potent topical anti-inflammatory agents.

Abstract: Phenylthiomethyl-6-hydroxy-2,3-dihydrobenzopyran and analogs thereof were prepared from an appropriate (6-hydroxy-2,3-dihydro-benzopyran-7-yl) formaldehyde or analog thereof with a substituted thiophenol. These compounds were found to be potent anti-inflammatory agents.

Abstract: Substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

Abstract: 1-(Alkoxy or aroxy)carbonyloxyalkyl esters of diflunisal and related compounds are stable in aqueous medium and non-irritant to mucous membranes of mouth, throat, and stomach. Accordingly, they are useful Prodrugs of the analgesic and anti-inflammatory drug, diflunisal.