Eli Lilly and Company

Edward R Lavagnino

Jack B Campbell

William A Day

Bryan B Molloy

David C Hunden

Bennie J Foster

Andrew J Pike

Charles J Paget, Jr

James Howard Wikel

Edward C Taylor

Robin D Cooper

Lawrence J McShane

James M Greene

Bernard J Graves

Paul Pranc

The present invention provides propanamines, substituted at the 3-position of the propanamine chain with a thio, sulfinyl or sulfonyl moiety, which are capable of selectively inhibiting the uptake of serotonin and norepinephrine.

Serotonin and norepinephrine uptake inhibitors

This invention provides for certain substituted 7H-benzimidazo[2,1-a]benz[de]isoquinoline-7-ones, formulations of the compounds, and a method for their use in suppressing the immune response in mammals.

Isoquinoline derivatives as immune regulants

7-(Thienothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.

Thienothienylglycyl cephalosporin derivatives

The present invention relates to a process for preparing aminonitropyridines comprising reacting an alkoxynitropyridine with ammonium acetate.

Process for the synthesis of intermediates in the preparation of

7-(2-Benzothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.

Benzothienylglycyl cephalosporin derivatives

This invention provides for a process of preparing certain trifluoromethyl substituted 7H-benzimidazo[2,1-a]benz[de]isoquinoline-7-ones.

Preparation of isoquinoline derivatives useful as immune regulants

9-Carbamoyl-9-(2-cyanoethyl)fluorenes are intermediates for synthesis of 9-aminoalkyl-9-carbamoyl-fluorenes, which are antiarrhythmic agents.

9-Carbamoyl-9-(2-cyanoethyl)fluorenes

1-Phenyl-3-(optionally substituted phenoxy)-propylamines, inhibitors of norepinephrine uptake.

1-Phenyl-3-(substituted phenoxy)propylamines

1-Hydroxy-3-substituted-tetrahydro and hexahydrodibenzo[b,d]pyrans having an amino group or amino derivative at the 9-position are useful as analgesics, anti-depressants, anti-anxiety agents, hypotensive agents, and intermediates. Pharmaceutical formulations containing such 9-amino derivatives are provided, as well as a method of treating hypertension.

9-Amino-dibenzopyrans

Trifluoromethylphenols are prepared by hydrogenation of the corresponding trifluoromethylbenzylethers.

Trifluoromethylphenyl benzyl ethers

Reaction of a 5-substituted resorcinol with a 1-alkoxy-4-(1-hydroxy-1-methylethyl)-1,4-cyclohexadiene in the presence of a suitable catalyst affords the corresponding dl-cis-1-hydroxy-3-substituted-6,6-dimethyl-6,6a,7,8,10,10a-hexahydro-9H-d ibenzo[b,d]pyran-9-one.

Process for preparing

N-2-(6-hydroxybenzothiazolyl)-N'-phenyl (or substituted-phenyl) ureas are prepared by reacting 2-amino-6-hydroxybenzothiazole with 1-2 moles of phenyl (or a substituted phenyl) isocyanate and then hydrolysing any 6-phenylcarbamoyloxy compound thus produced to the corresponding 6-hydroxy derivative.

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Indianapolis, IN, United States of America

Edward R Lavagnino