Abbott Laboratories Corporation

Thomas R Herrin

Hing L Sham

Daniel W Norbeck

Xiaoqi Chen

David A Betebenner

Gondi N Kumar

Dale J Kempf

Daniel A Dickman

Lawrence Kolaczkowski

Ketan M Patel

Arthur J Cooper

Eric J Stoner

Stephen L Condon

Patricia A Oliver

Steven M Hannick

Daniel J Plata

Jih-Hua Liu

Jieh-Heh J Tien

Peter J Stengel

Jacob J Plattner

Houston F Voss

John Scott Fairgrieve

Laman L Alani

Charles A Flentge

Soumojeet Ghosh

Jien-Heh J Tien

Dilip Kaul

John M Lipari

Alford M Thomas

Rong R Gao

Raymond Oslapas

A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Retroviral protease inhibiting compounds

The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding protein bindable to the ligand and the ligand analog-irreversible enzyme inhibitor conjugate and wherein the amount of ligand analog-irreversible enzyme inhibitor conjugate bound by the binding protein is related to the amount of ligand in the test sample, said binding protein inactivating the irreversible enzyme inhibitor when bound to the ligand analog portion of the conjugate; intermixing an enzyme which is irreversibly inhibited by the ligand analog-irreversible enzyme inhibitor conjugate unbound by the binding protein; and intermixing substrate to the enzyme and monitoring the enzyme substrate reaction. The invention also includes ligand analog-irreversible enzyme inhibitor conjugates useful as reagents in practicing the method. Methods and reagents of the present are particularly useful in determining drugs, hormones, and the like in biological fluids.

Ligand analog-irreversible enzyme inhibitor conjugates

Phenobarbital conjugates for use as enzyme inhibitors having the formula: ##STR1## wherein Z is a biologically compatible counter ion, n and m is an integer from 2 to 6 and R and R.sub.1 are each lower alkyl.

Phenobarbital enzyme inhibitors

Described is the use of .psi.-aglycone and other derivatives of ristocetin A as antibacterial agents.

Ristocetin .psi.-aglycone as an antibacterial agent

Ligand analog-irreversible enzyme inhibitor conjugates and methods for

A triglyceride carrying, in the .beta.-position, the anionic moiety of phosphonoacetic acid has been found to exhibit excellent activity against viral infections caused by a herpes virus.

Triglyceride ester of phosphonoacetic acid having antiviral activity

A method of treating herpes simplex infections in warm-blooded animals by administering to said animals a carboxylic ester of phosphonoacetic acid of the formula ##STR1## wherein R is a C.sub.3 -C.sub.8 alkyl, aralkyl, ##STR2## ADAMANTYL, OR GLYCERYL ESTERS OF THE FORMULA ##STR3## where R' is an alkyl of 2-20 carbon atoms, or its inorganic salts.

Carboxylic esters of phosphonoacetic acid

A competitive radioimmunoassay for the measurement of digoxin in a serum sample in which the non-radioactive digoxin competes with a constant amount of a radioactively labeled digoxin tyramine analog comprising 3-O-(4-Hydroxyphenethylcarbamoyl) digoxigenin for binding cites on a limited amount of digoxin antibody. The percentage of the radioactively labeled digoxin which is bound to the antibody is inversely proportional to the concentration of digoxin in the serum sample. The concentration of digoxin in the serum is determined by the comparison with standards containing measured amounts of unlabeled digoxin.

Radioimmunoassay for determining the digoxin content of a sample

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Waukegan, IL, United States of America

Thomas R Herrin