Merck + Co., Inc.

Mary N Omstead

Gerald F Bills

Fernando Pelaez

George M Garrity

Maria T Diez

Deborah L Zink

Sheo B Singh

Russell B Lingham

Leeyuan Huang

Keith C Silverman

Louis Kaplan

Isabel Martin

Francis J Dumont

Kevin M Byrne

E Tracy Jones

Marvin D Schulman

Gino M Salituro

Teresa D Matas

Wendy H Clapp

Olga Genillourd

Isabel M Fernandez

Noel M Young

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. 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

This invention relates to a fungal microorganism Pseudodiplodia sp. (MF5767) isolated from bark discs of Hibiscus sp. and useful in a fermentation process to form compounds of formula (I): ##STR1## which are squalene synthetase inhibitors and thus useful as cholesterol lowering agents.

Process for forming cholesterol lowering compound using pseudodiplodia

Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors useful as cholesterol-lowering agents.

Directed biosynthesis of cholesterol lowering compounds

This invention relates to strains of the species Curvularia lunata isolated from tree bark and useful in a fermentation process to form compounds of formula (I): ##STR1##

Processes for preparing novel squalene synthetase inhibitors

Squalene synthetase inhibitors and processes therefrom

Described is a new process for producing the macrolide immunosuppressant, FK-506 under fermentation conditions utilizing the microorganism, Streptomyces sp., (Merck Culture Collection No. MA 6858) ATCC No. 55098. The immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Process for producing FK-506

Avermectin aglycones are glycosylated by fermentation in a medium of a non-producing mutant of Streptomyces avermitilis MA-6078. The glycosylation produces the monosaccharide and disaccharide derivatives while leaving the remainder of the molecule intact. The microorganism glycosylates with the .alpha.-L-oleandrose moiety.

Process for the glycosylation of avermectin agylcones

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Gladstone, NJ, United States of America

Mary N Omstead