Merck + Co., Inc.

Brian Heimbuch

Michel M Chartrain

Shieh-Shung T Chen

George M Garrity

Ali Shafiee

Barbara A Jackey

Deborah L Zink

Byron H Arison

Sheo B Singh

Thomas R Verhoeven

Paul J Reider

Guy H Harris

Colleen S Taylor

Chris H Senanayake

F Edward Roberts

Magda M Gagliardi

Ana M Teran

Christopher Roberge

Olga Genilloud

Neal C Connors

Jennifer Nielsen-Kahn

Michael G Sturr

Randolph L Greasham

Francis P Gailliot

Randall R Miller

Roger C Olewinski, Jr

Chanyong Lee

Barry C Buckland

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 are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Actinoplanes sp. MA7220 (ATCC 202188) is also disclosed, as well as processes for making compounds of the present invention employing the culture.

HIV integrase inhibitors

11-hydroxysordarin, biotransformation product of a fermentation with sordarin and Actinomyces spp., (Merck Culture Collection MA7235) ATCC No. 202103 is an antifungal agent. This compound may be useful in the treatment of diseases caused by fungal pathogens such as

11-hydroxysordarin and a process for producing it using actinomyces SSP

A method for preparing (1S)-amino-(2R)-indandiol substantially free of its stereoisomers is presented. The method comprises culturing indene with Rhodococcus sp. ATCC 55805, recovering the indandiol and subjecting the indandiol to chiral specific crystallization, treatment with strong acid and reverse ion pair extraction.

Conversion of indene to (1S)-amino-(2R)-indanol free of any steroisomer

A process is disclosed that bioconverts indene to (1S)-amino-(2R)-indanol substantially free of any of its stereoisomers, by the action of a strain of P. putida or Rhodococcus sp., followed by various chemical step(s), e.g., chiral specific crystallization, treatment with strong acid in the presence of acetonitrile.

Conversion of indene to (1S)-amino-(2R)-indanol free of any

Biotransformation products of a fermentation with culture MA7074 are potent HIV protease inhibitors. These products are useful in the prevention or treatment of infection by HIV and in 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.

Streptomyces sp. MA 7074 (ATCC 55605) used for microbial synthesis of

The present invention provides a process for the stereoselective reduction of phenylalkyl ketones to their corresponding (S)-hydroxy compounds. The process utilizes the novel microorganism Microbacterium MB 5614 to effectuate the chiral reduction. The present invention also provides said novel Microbacterium, which has been deposited with the ATCC and assigned the accession number ATCC 55557.

Microbial method

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North Brunswick, NJ, United States of America

Brian Heimbuch