Shaman Pharmaceuticals, Inc.

University of Michigan

Thien V Truong

Donald E Bierer

Jeffrey M Dener

Bernard Loev

Masato Koreeda

Michael S Tempesta

Wu Yang

Richard Hector

This invention pertains to a synthetic process for obtaining a unique phosphocholine derivative which has been isolated from the leaves of the plant Irbachia alata, identified to be 1,22-bis�2-(trimethylammonium)ethylphosphatyl! docosane is disclosed. Also disclosed is a synthetic process for obtaining a novel class of mono- and bis(phosphocholine) derivatives which are useful as antiinfective agents. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.

Process for the preparation of mono-  and bis(phosphocholine)

This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.

1,2-dithiin antiinfective agents

The present invention provides an improved procedure for the preparation of 3,6-disubstituted-1,2-dithiin derivatives, especially unsymmetrical 1,2-dithiins. In addition, the process offers significant process, scaleup, and safety advantages over the previously reported synthetic processes. The compounds synthesized by this new process and described herein are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Candida parapsilosis, Candida tropicalis, or Candida krusei.

Preparation of symmetrical and unsymmetrical

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Emeryville, CA, United States of America

Thien V Truong