Merck + Co., Inc.

Fernando Pelaez

Gerald F Bills

Deborah L Zink

Maria T Diez

Francisca Vicente

Sheo B Singh

Robert A Giacobbe

Sandra A Morris

Jerrold M Liesch

Russell B Lingham

Keith C Silverman

John R Thompson

James E Curotto

Angela Basilio

Sarah J Dreikorn

Janet C Onishi

Robert E Schwartz

Mary N Omstead

Angeles Cabello

Rosalind G Jenkins

Otto D Hensens

Anne W Dombrowski

Isabel Martin

Jon David Polishook

Ana M Teran

Stanley L Streicher

Maria S Meinz

Manuel Sanchez

Bruce W Burgess

Isabella Martin

Seok H Lee

Leeyuan Huang

Ali Shafiee

Michael A Goetz

Suzanne M Mandala

Guy H Harris

Daria Hazuda

Yu L Kong

Gregory L Helms

Rosemary A Thornton

Hans E Huber

Wendy S Horn

Gino M Salituro

Wendy H Clapp

Bei B Zhang

Hiranthi Jayasuriya

Richard K Jansson

E Tracy Turner Jones

Denis R Patrick

Siobhan Stevens-Miles

Mark Rattray

Lucia Herranz

Gerard F Bills

Julian Gorrochategui

Royo Inmaculada

Barnali Pramanik

Teresa Diez

Carmen Cascales

Wendy H Clapp-Shapiro

M Dolores Vilella Amils

Marina Mojena Sanchez

Annie Z Zhao

Natural products such as certain chaetochromins 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.

HIV integrase inhibitors

Novel tetracyclic aromatic ketones are natural product compounds 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. Further, the novel fungal cultures MF6388 (ATCC 74478), Sterile Fungus, and MF6591 (ATCC 74477), Ascochyta sp. are also disclosed. Further, the cultures Sterile Fungus MF6388 (ATCC 74478) and Ascochyta sp. MF6591 (ATCC 74477) are also disclosed, as well as processes for making compounds of the present invention employing the cultures.

Indolylquinones are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients. Some of the indolylquinones are produced by fermentation of the novel fungus Pseudomassaria sp. ATCC 74411.

Indolylquinones as antidiabetic agents

A compound represented by the formula I is disclosed: ##STR1## or a pharmaceutically acceptable salt or hydrate thereof. The compound has inhibitory activity against the oncoprotein Raf. Also included are pharmaceutical compositions, methods of treating cancer, cultures of the producing fungal microorganism and methods of fermentative production of the compound.

Bis-aryl ethers, compositions containing such compounds and methods of

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

Antifungal agent from sporomiella minimoides

The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Inhibitors of farnesyl-protein transferase

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

Antifungal agents

Antifungal agent obtained from hormonema

Antifungal agent

There is disclosed a compound having the formula ##STR1## which is produced by the fungus, Arthrinium arundinis ATCC 74359, and exhibits antifungal activity.

Antifungal agent produced by arthrinium arundinis  ATCC 74359

The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer. The compounds of this invention have the following structure: ##STR1##

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.

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

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Madrid, Spain

Fernando Pelaez