Merck + Co., Inc.

Richard L Monaghan

Sheldon B Zimmerman

Otto D Hensens

Sagrario M Del Val

Michael A Goetz

Maria I Fernandez

Kenneth E Wilson

George E Albers-Schonberg

Alfred W Alberts

James E Flor

Louis Chaiet

Carl H Hoffman

Robert E Schwartz

George M Garrity

Robert A Giacobbe

Raymond S Chang

Vincent P Gullo

Maria B Lopez

Tony Y Lam

Tom G Holt

Cheryl Deriso

Deborah L Zink

Byron H Arison

Jerrold M Liesch

William Strohl

Janet C Onishi

Maria L Garcia

Gregory J Kaczorowski

George A Doss

Suzanne M Mandala

Prakash S Masurekar

Guy H Harris

Owen B McManus

James E Curotto

Eugene L Dulaney

John G MacConnell

August J Kempf

Jan S Tkacz

Sara A Currie

Richard K Jansson

Wesley L Shoop

Michael A Wallace

Joan A Lasota

Enrique Tejera

Pamela A McCormick

Yu-Lin Kong

Maria I Martin

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.

Maxi-k channel blockers, methods of use and process for making the same

An active avermectin analogue which can be produced by directed biosynthesis is described. The compound, named 26-R-Avermectin B.sub.1 a, is active in the Haemonchus egg to L3 assay and has the following structure: ##STR1##

Active avermectin analogue

A compound having the formula ##STR1## which is useful as an antifungal agent and for the treatment and control of several agricultural phytopathogens, including Phytophthora infestans, is disclosed.

Antifungal agent

Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.

Methods of achieving antitumor activity using 16-membered-macrolide-type

Cholesterol lowering compounds and compositions are formed from the photochemical treatment of the Zaragozic Acids followed by esterification. These compounds and compositions are active squalene synthetase inhibitors useful in the treatment of hypercholesterolemia.

Cholesterol lowering compounds

Methods of achieving antileukemia activity using

Compounds of Structural Formula (I) ##STR1## are produced by chemical modification of directed biosynthesis products. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.

Cholesterol lowering compounds produced by directed biosynthesis

A mixture of derivatives of 2-amino-3,4,5,14-tetrahydroxy-6-eicosenoic acid has been isolated from a culture medium after cultivation of microorganisms belonging to the genus Aspergillus. The compounds are useful as antifungal agents.

Process for producing antifungal fermentation products and compositions

Antifungal fermentation products and compositions thereof

A new antifungal agent which exhibits a moderately broad spectrum of activity towards filamentous fungi and also against Cryptococcus species of the yeast fungi, and which has been isolated from a solid stationary fermentation of an unidentified species of Fusarium is described.

Antifungal fermentation product

An antifungal agent produced by cultivation of Zalerion arboricola is a cyclic lipopeptide with very high activity against human pathogens and of very low mammalian toxicity. Its production and isolation are also described.

Process for antifungal fermentation product

A novel pyrrolidinol isolated from the fermentation of Aspergillus ochraceus and certain derivatives thereof are described. The compounds are broad spectrum antifungal agents.

Antifungal fermentation product and derivatives and compositions thereof

The process for the manufacture of the compound of the general structural formula ##STR1## which is a 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) synthase inhibitor and useful as an antihypercholesterolemic agent for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, and which is an antifungal agent is disclosed.

Process for the manufacture of an antifungal antihypercholesterolemic .beta

A process for preparing the compound having Formula I and several minor related compounds. ##STR1## The compound of Formula I and the several minor related compounds are antagonists of cholecystokinin (CCK). CCK antagonists are useful in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of animals, especially humans.

Process for the preparation of cholecystokinin antagonists

Process for the preparation of difficidin and derivative antibacterial compounds of the formula: ##STR1## where R.sub.a and R.sub.b are members independently selected from the group consisting of hydrogen; alkali metal and alkaline earth metal cations; ammonium; and substituted ammonium; and R.sup.1 is hydrogen or hydroxy.

Process for the preparation of difficidin and derivative antibacterials

Growing community of inventors

Somerset, NJ, United States of America

Richard L Monaghan