Merck + Co., Inc.

Jon David Polishook

Sheo B Singh

Deborah L Zink

Anne W Dombrowski

Gerald F Bills

Fernando Pelaez

Russell B Lingham

Keith C Silverman

Michael A Goetz

Guy H Harris

Sandra J Rattray

Joyce A Greene

Christine Lange Cannova

Gary K Darland

Janet C Onishi

Robert A Giacobbe

Ali Shafiee

John R Thompson

Suzanne M Mandala

Maria T Diez

Isabel Martin

James E Curotto

Rosemary A Thornton

Daria Jean Hazuda

Stanley L Streicher

Myra B Kurtz

Angeles Cabello

Maria S Meinz

Wendy H Clapp

Mark Rattray

Bruce W Burgess

Wendy H Clapp-Shapiro

Jeffrey C Hastings

Carmen Cascales

Marie Williams

Sarah J Driekorn

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

Natural products such as certain ermophilane sesquiterpenoids and derivatives thereof are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The fungal culture MF6254, Xylaria sp. (ATCC 74397) is also described and disclosed.

Ermophilane sesquiterpenoids as HIV intergrase inhibitors

There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.

Antifungal agent from sporomiella minimoides

Natural products such as equisetin and derivatives are described. These compounds are useful in the inhibition of HIV integrase.

In vitro HIV integrase inhibitors

The present invention is directed to non-peptide compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention also relates to the process for the preparation of a compound of this invention by cultivating a culture of Phoma sp. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Inhibitors of farnesyl-protein transferase

There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.

Antifungal agents

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Cranford, NJ, United States of America

Jon David Polishook