Merck + Co., Inc.

Steven M Pitzenberger

Harri G Ramjit

George D Hartman

Wasyl Halczenko

John J Baldwin

Suresh K Balani

Jiunn H Lin

Edgar H Ulm

Mark G Bock

Roger M Freidinger

Ben E Evans

Barry M Trost

David E McClure

Sandor L Varga

Richard W Ransom

Victor J Lotti

Michael S Schwartz

Keith M Witherup

Anthony Y Lu

William J Lumma

Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation product the compound 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone . This product is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Preparation of

A pyrroloquinoline compound of the following formula is disclosed: ##STR1## wherein H,

Pyrroloquinoline Bradykinin antagonist

Novel dipeptide isosteres are the biotransformed products after incubation with rat liver slices. They inhibit HIV protease, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Method of preparing HIV protease inhibitors

Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## are disclosed.

Prodrugs of antihypercholesterolemic compounds

A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4 H-i midazo[1,5a][1,4]benzodiazepine is a 1,2-dihydroxy derivative of the isopropyl moiety and is itself an anxiolytic agent of greater activity than its substrate.

7-chloro-5,6-di

A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4 H- imidazo[1,5a][1,4]benzodiazepine is a 2-hydroxy derivative of the isopropyl moiety and is itself an anxiolytic agent.

7-chloro-5,6-dihydro-3-(5-(2-hydroxy-isoprop

A process for the preparation of 1,4-dihydropyridine compounds, especially N-substituted 1,4-dihydropyridine compounds, is disclosed. The compounds are useful as cardiovascular agents and also as starting materials for the preparation of certain cyclized compounds which have properties as calcium entry blockers.

Process for 1,4-dihydropyridine compounds using a titanamine catalyst

Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.

Pharmaceutical compositions of specific substituted pyrimidines and methods of treatment of certain cardiovascular disorders are disclosed. Also disclosed are novel substituted acrylated pyrimidines which are useful as calcium channel blockers.

Substituted pyrimidines useful as calcium channel blockers

A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates is disclosed.

Process for preparing a benzodiazepinedione derivative

A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates are disclosed.

Growing community of inventors

Lansdale, PA, United States of America

Steven M Pitzenberger