Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Sharp & Dohme De Espana Sa

Michael A Goetz

Sheo B Singh

Richard L Monaghan

Otto D Hensens

Gerald F Bills

Robert A Giacobbe

Anne W Dombrowski

Raymond S Chang

Sandra J Rattray

Jon David Polishook

Yu L Kong

Joyce A Greene

Siobhan Stevens-Miles

Gary K Darland

Christine Lange Cannova

Roger M Freidinger

Deborah L Zink

David Brian Olsen

Jerrold M Liesch

William Strohl

Fernando Pelaez

Edward S Inamine

Paul S Anderson

Maria L Garcia

Gregory J Kaczorowski

Douglas J Pettibone

Maria T Diez

Owen B McManus

Isabel Martin

Francisca Vicente

Jon D Polishook

Cheryl D Schwartz

Lawrence R Koupal

E Tracy Jones

Jan S Tkacz

David R Houck

Olga Genilloud

E Tracy Turner Jones

Leeyan Huang

Lucia Herranz

Gerard F Bills

Pamela A McCormick

Scott Knoble Smith

The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds. 

Extracts from kibdelos porangium as antibacterial agents

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

The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis.

Antiprotozoal cyclic tetrapeptides

Four triterpenes of Formula 1 (where '---' is either a single or double bond and R is H or acetate) are disclosed which are potent and selective immunosuppressive agents. These compounds have been isolated from Spachea correa root. ##STR1##

Triterpenes

Fermentation processes for the production of a compound of the Structural Formula I ##STR1## The compound of Structural Formula I has been shown to have endothelin antagonist activity and is therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure vasospasm, cerebral and cardia ischemia, myocardial infarction inflammatory diseases, Raynaud's disease, endotoxin shock and asthma.

Process for the production of a novel endothelin antagonist

Substituted hexahydrobenzopyran derivatives of the Formulae A, B, or C are useful as angiotensin II antagonists: ##STR1##

Substituted hexahydrobenzopyran derivatives as angiotensin II antagonists

Cyclic peptides are produced by the controlled aerobic fermentation of Streptomyces silvensis, ATTCC No. 53525 or ATCC No. 53526. These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and vasopressin and are thus useful in the treatment and prevention of disease states wherein vasopressin may be involved, for example congestive heart failure, hypertension, edema and hyponatremia.

Oxytocin and vasopressin antagonists

Products of Aspergillus alliaceus fermentation having cholecystokinin (CCK) antagonist activity, their preparation and use are disclosed.

Cholecystokinin antagonist compounds

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

The compound having Formula I and several minor related compounds are produced by the aerobic fermentation of Aspergillus alliaceus Thom and Church, ATCC No. 20655 or ATCC No. 20656. ##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.

Cholecystokinin antagonists

There is disclosed a macrolide isolated from the fermentation broth of a microorganism identified as MA-5285 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compound's structure is presented based upon analytical studies. The compound has insecticidal and antiparasitic activity.

Antiparasitic macrolide from a strain of Streptomyces hygroscopicus

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Fanwood, NJ, United States of America

Michael A Goetz