Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylen edioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyph eyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Abstract: This invention relates to a process for preparing epoxy esters, and intermediates prepared by this process, in particular, to a process which produces non-racemic epoxy esters which are of use as intermediates in the preparation of pharmaceutical compounds.

Abstract: A method of inhibiting the 5-lipoxygenase pathway in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a diaryl- substituted imidazole fused to a thiazole pyrrolidine, thiazide or piperidine ring to such animal.

Abstract: This invention relates to a process for preparing epoxy esters, and intermediates prepared by this process, in particular, to a process which produces non-racemic epoxy esters which are of use as intermediates in the preparation of pharmaceutical compounds.

Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.

Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.

Abstract: A new synthesis of auranofin comprising reacting 2,3,4,6-tetra-O-acetyl-.alpha.-D-glucopyranosyl bromide with a S-(triethylphosphineaurous)thiouronium salt.

Abstract: The compounds are 5/6-pyridyl-phenyl-2,3-dihydroimidazo[2,1-b]thiazoles which have utility as intermediates and/or as having antiarthritic activity. A preferred group of compounds is 5-(4-pyridyl)-6-(4-substituted phenyl)-2,3-dihydroimidazo[2,1-b]thiazoles which have significant anti-arthritic activity.

Abstract: The S-gold salt of 2,3,4,6-tetra-O-acetyl-1-thio-.beta.-D-glucopyranose reacts with triethylphosphine in an organic solvent to produce auranofin.

Abstract: A new synthesis of auranofin comprising reacting 2,3,4,6-tetra-O-acetyl-.alpha.-D-glucopyranosyl bromide with triethylphosphinegold(I) chloride and sodium or potassiumsulfide. Auranofin is an antiarthritic pharmaceutical compound. Auranofin is an orally active therapeutic agent which is useful in man as an antiarthritic.

Abstract: Auranofin is prepared by reacting 1-.beta.-D-thio-2,3,4,6-tetra-O-acetylglucose with a triethylphosphine gold mercaptide.

Abstract: Bis(triethylphosphine)gold salts are advantageous agents for preparing auranofin.

Abstract: Auranofin is prepared by direct O-acetylation of S-triethylphosphinegold 1-thio-.beta.-D-glucopyranoside.

Abstract: Auranofin and its congeners are prepared by the reaction of a S-substituted 2,3,4,6-tetra-O-acetyl-1-thio-.beta.-D-glucopyranose with a tertiary phosphine gold ester or sulfide.

Abstract: Auranofin and its congeners are prepared by reacting a bis(polyacetylsaccharide)disulfide with a tertiary phosphinegold mercaptide in a suitable organic solvent.

Abstract: A new series of lower alkyl sulfonyl esters of S-tri-lower-alkylphosphinegold 1-thio-.beta.-D-glucopyranosides has been prepared and found to have anti-arthritic activity and, in particular, are of use in treating rheumatoid arthritis.

Abstract: The compounds are trialkylphosphinegold(I)2,3,4,6-tetra-O-(N-loweralkylcarbamoyl)-1-thio-.be ta.-D-glucopyranosides which have antiarthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis.

Abstract: A new series of lower alkyl ethers of S-tri-lower-alkylphosphinegold 1-thio-.beta.-D-glucopyranoside has been prepared and found to have anti-arthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis.